Pemetrexed 100mg/4ml solution for infusion vials
Prescription only
Requires a prescription from a doctor or prescriber
Pemetrexed is a chemotherapy drug that is manufactured and marketed by Eli Lilly and Company under the brand name Alimta.
Active ingredients:
Pemetrexed
No active safety alerts
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Source: MHRA Products DatabaseOGL 3.0
Updated 3 months ago(16 Jan 2026)Safety monitoring data
Yellow Card reports
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Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
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Suspected adverse reactions reported for Pemetrexed
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9 branded products available
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Pemetrexed 100mg/4ml concentrate for solution for infusion vials
Pemetrexed 100mg/4ml concentrate for solution for infusion vials
Pemetrexed 100mg/4ml concentrate for solution for infusion vials
Pemetrexed 100mg/4ml concentrate for solution for infusion vials
Pemetrexed 100mg/4ml concentrate for solution for infusion vials
Pemetrexed 100mg/4ml concentrate for solution for infusion vials
Discontinued
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Pemetrexed 700mg/100ml infusion bags
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Pemetrexed 750mg/100ml infusion bags
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Pemetrexed 800mg/100ml infusion bags
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Pemetrexed 900mg/100ml infusion bags
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Same therapeutic group
Similarity based on WHO Anatomical Therapeutic Chemical (ATC) classification and NHS BNF section grouping. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
Clinical guidelines and formulary information
British National Formulary
Pemetrexed
BNF
Drug monograph — bnf.nice.org.ukSource: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.
NICE clinical guidance(13)
Pemetrexed maintenance treatment for non-squamous non-small-cell lung cancer after pemetrexed and cisplatin (TA402)
TA402
Technology appraisal
Updated Aug 2016Pemetrexed for the treatment of malignant pleural mesothelioma (TA135)
TA135
Technology appraisal
Updated Jan 2008Pemetrexed for the treatment of non-small-cell lung cancer (TA124)
TA124
Technology appraisal
Updated Aug 2007Pemetrexed for the maintenance treatment of non-small-cell lung cancer (TA190)
TA190
Technology appraisal
Updated Aug 2017Pemetrexed for the first-line treatment of non-small-cell lung cancer (TA181)
TA181
Technology appraisal
Updated Sept 2009Pembrolizumab with pemetrexed and platinum chemotherapy for untreated, metastatic, non-squamous non-small-cell lung cancer (TA683)
TA683
Technology appraisal
Updated Mar 2021Pembrolizumab with pemetrexed and platinum-based chemotherapy for untreated unresectable advanced malignant pleural mesothelioma (terminated appraisal) (TA1125)
TA1125
Technology appraisal
Updated Jan 2026Osimertinib with pemetrexed and platinum-based chemotherapy for untreated EGFR mutation-positive advanced non-small-cell lung cancer (TA1060)
TA1060
Technology appraisal
Updated May 2025Atezolizumab in combination for treating metastatic non-squamous non-small-cell lung cancer (TA584)
TA584
Technology appraisal
Updated Jun 2019Erlotinib monotherapy for maintenance treatment of non-small-cell lung cancer (TA227)
TA227
Technology appraisal
Updated Jun 2011Selpercatinib for untreated RET fusion-positive advanced non-small-cell lung cancer (TA911)
TA911
Technology appraisal
Updated Jul 2023Entrectinib for treating ROS1-positive advanced non-small-cell lung cancer (TA643)
TA643
Technology appraisal
Updated Aug 2020Pralsetinib for treating RET fusion-positive advanced non-small-cell lung cancer (TA812)
TA812
Technology appraisal
Updated Aug 2022Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
Check stock at pharmacies and supply information
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Supply & product information
Official product databases and supply status monitoring
Pharmacy links redirect to the retailer's own search and do not represent real-time stock levels. emc (electronic medicines compendium) is operated by Datapharm Ltd. Shortage information sourced from NHS Specialist Pharmacy Service (SPS), sps.nhs.uk.
Codes for healthcare professionals and prescribing systems
Show details
These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
Browse tools
SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF codes from NHS Business Services Authority (NHSBSA). ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Show details
Searching UK clinical trials...
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
None known
Half-life
3.5 hours
Mechanism
Pemetrexed is an antifolate containing the pyrrolopyrimidine-based nucleus that…
Food interactions
2 warnings
Human targets
4 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
0.2 to 838 mg/m
The pharmacokinetics of pemetrexed when pemetrexed was administered as a single agent in doses ranging from 0.2…
Half-life
3.5 hours
The elimination half-life of pemetrexed is 3.5 hours in patients with normal renal function (creatinine clearance of 90 mL/min).
[L43807]
[L43807]
Protein binding
81%
In vitro studies indicated that pemetrexed is 81% bound to plasma proteins.
[L43807]
[L43807]
Volume of distribution
Pemetrexed has a steady-state volume of distribution of 16.1 liters.
[L43807]
[L43807]
Metabolism
Pemetrexed is not metabolized to an appreciable extent by the liver.
[L43807][A253987]
[L43807][A253987]
Elimination
70%
Pemetrexed is primarily eliminated in the urine, with 70% to 90% of the dose recovered unchanged within the first 24 hours following administration.…
Clearance
91.8 mL/min
The total systemic clearance of pemetrexed is 91.8 mL/min in patients with normal renal function (creatinine clearance of 90 mL/min).…
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Status:
Approved
Investigational
Small molecule
About this compound
Pemetrexed is a chemotherapy drug that is manufactured and marketed by Eli Lilly and Company under the brand name Alimta. It is indicated for use in combination with cisplatin for the treatment of patients with malignant pleural mesothelioma whose disease is either unresectable or who are otherwise not candidates for curative surgery. Its use in non-small cell lung cancer has also been investigated. Pemetrexed was first approved by the FDA in February 4, 2004.[A253907]
Properties:
View FDA drug labelsolid
Avg. mass: 427.41 Da
DrugBank indication
Pemetrexed is indicated for the treatment of the following conditions:
Non-squamous non-small cell lung cancer (NSCLC)
- in combination with [pembrolizumab] and platinum-based chemotherapy as initial treatment in metastatic disease where no EGFR or ALK genomic tumour aberrations exist [L40943]
- in combination with [cisplatin] as initial treatment for locally advanced or metastatic disease [L40943][L44883]
- as maintenance treatment for locally advanced or metastatic disease that has not progressed following four cycles of platinum-based chemotherapy [L40943][L44883]
- recurrent metastatic disease following prior chemotherapy [L40943]
- as monotherapy for the second-line treatment of patients with locally advanced or metastatic non-squamous non-small cell lung cancer [L44883]
Malignant pleural mesothelioma
- in combination with [cisplatin] for the initial treatment of patients with malignant pleural mesothelioma.
[L40943][L44883]
In the US, it is reserved for patients whose disease is unresectable or otherwise not candidates for curative surgery.
[L40943]
Non-squamous non-small cell lung cancer (NSCLC)
- in combination with [pembrolizumab] and platinum-based chemotherapy as initial treatment in metastatic disease where no EGFR or ALK genomic tumour aberrations exist [L40943]
- in combination with [cisplatin] as initial treatment for locally advanced or metastatic disease [L40943][L44883]
- as maintenance treatment for locally advanced or metastatic disease that has not progressed following four cycles of platinum-based chemotherapy [L40943][L44883]
- recurrent metastatic disease following prior chemotherapy [L40943]
- as monotherapy for the second-line treatment of patients with locally advanced or metastatic non-squamous non-small cell lung cancer [L44883]
Malignant pleural mesothelioma
- in combination with [cisplatin] for the initial treatment of patients with malignant pleural mesothelioma.
[L40943][L44883]
In the US, it is reserved for patients whose disease is unresectable or otherwise not candidates for curative surgery.
[L40943]
Also known as(82)
Pemetrexed
2.1.1.45
TS
TSase
AICAR transformylase/inosine monophosphate cyclohydrolase
ATIC
PURH
1.5.1.3
Dosage forms(97)
Powder (Intravenous)
Injection, powder, for solution (Intravenous) — 100 MG
Injection, powder, for solution (Intravenous) — 151.7 mg
Powder (Intravenous) — 100 mg/1vial
Solution (Parenteral) — 500 mg
Injection, powder, lyophilized, for solution (Intravenous) — 500 mg/vial
Solution (Intravenous) — 10 ml
Injection (Intravenous) — 100 mg
Molecular properties(19)
Drug interactions(1418)
Known interactions with other medications. Always consult a healthcare professional.
The risk or severity of adverse effects can be increased when Denosumab is combined with Pemetrexed.
Peginterferon alfa-2a
Unknown severity
The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Pemetrexed.
Interferon alfa-n1
Unknown severity
The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Pemetrexed.
Interferon alfa-n3
Unknown severity
The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Pemetrexed.
Interferon gamma-1b
Unknown severity
The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Pemetrexed.
Interferon alfa-2a
Unknown severity
The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Pemetrexed.
Aldesleukin
Unknown severity
The risk or severity of adverse effects can be increased when Aldesleukin is combined with Pemetrexed.
Gemtuzumab ozogamicin
Unknown severity
The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Pemetrexed.
Pegaspargase
Unknown severity
The risk or severity of adverse effects can be increased when Pegaspargase is combined with Pemetrexed.
Interferon beta-1b
Unknown severity
The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Pemetrexed.
Interferon alfacon-1
Unknown severity
The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Pemetrexed.
The risk or severity of adverse effects can be increased when Rituximab is combined with Pemetrexed.
Basiliximab
Unknown severity
The risk or severity of adverse effects can be increased when Basiliximab is combined with Pemetrexed.
The risk or severity of adverse effects can be increased when Muromonab is combined with Pemetrexed.
Ibritumomab tiuxetan
Unknown severity
The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Pemetrexed.
Tositumomab
Unknown severity
The risk or severity of adverse effects can be increased when Tositumomab is combined with Pemetrexed.
Alemtuzumab
Unknown severity
The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Pemetrexed.
The risk or severity of adverse effects can be increased when Alefacept is combined with Pemetrexed.
Efalizumab
Unknown severity
The risk or severity of adverse effects can be increased when Efalizumab is combined with Pemetrexed.
Antithymocyte immunoglobulin (rabbit)
Unknown severity
The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Pemetrexed.
Interferon alfa-2b
Unknown severity
The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Pemetrexed.
Daclizumab
Unknown severity
The risk or severity of adverse effects can be increased when Daclizumab is combined with Pemetrexed.
Phenylalanine
Unknown severity
The risk or severity of adverse effects can be increased when Phenylalanine is combined with Pemetrexed.
Flunisolide
Unknown severity
The risk or severity of adverse effects can be increased when Flunisolide is combined with Pemetrexed.
Bortezomib
Unknown severity
The risk or severity of adverse effects can be increased when Bortezomib is combined with Pemetrexed.
Cladribine
Moderate
Pemetrexed may increase the immunosuppressive activities of Cladribine.
Carmustine
Unknown severity
The risk or severity of adverse effects can be increased when Carmustine is combined with Pemetrexed.
The risk or severity of adverse effects can be increased when Amsacrine is combined with Pemetrexed.
The risk or severity of adverse effects can be increased when Bleomycin is combined with Pemetrexed.
Chlorambucil
Unknown severity
The risk or severity of adverse effects can be increased when Chlorambucil is combined with Pemetrexed.
Raltitrexed
Unknown severity
The risk or severity of adverse effects can be increased when Raltitrexed is combined with Pemetrexed.
The risk or severity of adverse effects can be increased when Mitomycin is combined with Pemetrexed.
Bexarotene
Unknown severity
The risk or severity of adverse effects can be increased when Bexarotene is combined with Pemetrexed.
The risk or severity of adverse effects can be increased when Vindesine is combined with Pemetrexed.
Floxuridine
Unknown severity
The risk or severity of adverse effects can be increased when Floxuridine is combined with Pemetrexed.
Tioguanine
Unknown severity
The risk or severity of adverse effects can be increased when Tioguanine is combined with Pemetrexed.
Vinorelbine
Unknown severity
The risk or severity of adverse effects can be increased when Vinorelbine is combined with Pemetrexed.
Dexrazoxane
Unknown severity
The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Pemetrexed.
Beclomethasone dipropionate
Unknown severity
The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Pemetrexed.
The risk or severity of adverse effects can be increased when Sorafenib is combined with Pemetrexed.
Streptozocin
Unknown severity
The risk or severity of adverse effects can be increased when Streptozocin is combined with Pemetrexed.
Trifluridine
Unknown severity
The risk or severity of adverse effects can be increased when Trifluridine is combined with Pemetrexed.
Gemcitabine
Unknown severity
The risk or severity of adverse effects can be increased when Gemcitabine is combined with Pemetrexed.
Betamethasone
Unknown severity
The risk or severity of adverse effects can be increased when Betamethasone is combined with Pemetrexed.
Teniposide
Unknown severity
The risk or severity of adverse effects can be increased when Teniposide is combined with Pemetrexed.
Epirubicin
Unknown severity
The risk or severity of adverse effects can be increased when Epirubicin is combined with Pemetrexed.
Chloramphenicol
Unknown severity
The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Pemetrexed.
Lenalidomide
Unknown severity
The risk or severity of adverse effects can be increased when Lenalidomide is combined with Pemetrexed.
Altretamine
Unknown severity
The risk or severity of adverse effects can be increased when Altretamine is combined with Pemetrexed.
Zidovudine
Moderate
Zidovudine may decrease the excretion rate of Pemetrexed which could result in a higher serum level.
Showing 50 of 1418 interactions
Food & lifestyle interactions
Advice
Administer folic acid supplement. Folic acid supplement of 400 to 1000 mcg daily should be given 7 days before treatment with pemetrexed and continued until 21 days after discontinuation of pemetrexed to reduce the risk of hematologic and gastrointestinal toxicities.
Advice
Administer vitamin supplements. Administration of vitamin B12 intramuscular supplement one week before treatment with pemetrexed and every three cycles will reduce the risk of hematological and gastrointestinal toxicities.
How it works
Mechanism of action
Pemetrexed is an antifolate containing the pyrrolopyrimidine-based nucleus that exerts its antineoplastic activity by disrupting folate-dependent metabolic processes essential for cell replication. In vitro studies have shown that pemetrexed inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), all folate-dependent enzymes involved in the de novo biosynthesis of thymidine and purine nucleotides. Pemetrexed is transported into cells by both the reduced folate carrier and membrane folate binding protein transport systems. Once in the cell, pemetrexed is converted to polyglutamate forms by the enzyme folylpolyglutamate synthetase. The polyglutamate forms are retained in cells and are inhibitors of TS and GARFT. Polyglutamation is a time- and concentration-dependent process that occurs in tumor cells and, to a lesser extent, in normal tissues. Polyglutamated metabolites have an increased intracellular half-life resulting in prolonged drug action in malignant cells.[A973][A974][A975][A976][A253907][L40943]
Pharmacodynamics
Pemetrexed inhibited the in vitro growth of mesothelioma cell lines (MSTO-211H, NCI-H2052) and showed synergistic
effects when combined with cisplatin. Based on population pharmacodynamic analyses, the depth of the absolute neutrophil counts (ANC) nadir correlates with systemic exposure to pemetrexed and supplementation with folic acid and vitamin B12. There is no cumulative effect of pemetrexed exposure on ANC nadir over multiple treatment cycles.[L40943]
effects when combined with cisplatin. Based on population pharmacodynamic analyses, the depth of the absolute neutrophil counts (ANC) nadir correlates with systemic exposure to pemetrexed and supplementation with folic acid and vitamin B12. There is no cumulative effect of pemetrexed exposure on ANC nadir over multiple treatment cycles.[L40943]
Pharmacokinetics
How the body processes this drug — absorption, distribution, metabolism, and elimination
Absorption
The pharmacokinetics of pemetrexed when pemetrexed was administered as a single agent in doses ranging from 0.2 to 838 mg/m2 infused over a 10-minute period have been evaluated in 426 cancer patients with a variety of solid tumors. Pemetrexed total systemic exposure (AUC) and maximum plasma concentration (Cmax) increased proportionally with the increase in dose. The pharmacokinetics of pemetrexed did not change over multiple treatment cycles.
[L43807]
[L43807]
Half-life
The elimination half-life of pemetrexed is 3.5 hours in patients with normal renal function (creatinine clearance of 90 mL/min).
[L43807]
[L43807]
Protein binding
In vitro studies indicated that pemetrexed is 81% bound to plasma proteins.
[L43807]
[L43807]
Volume of distribution
Pemetrexed has a steady-state volume of distribution of 16.1 liters.
[L43807]
[L43807]
Metabolism
Pemetrexed is not metabolized to an appreciable extent by the liver.
[L43807][A253987]
[L43807][A253987]
Route of elimination
Pemetrexed is primarily eliminated in the urine, with 70% to 90% of the dose recovered unchanged within the first 24 hours following administration. In vitro studies indicated that pemetrexed is a substrate of OAT3 (organic anion transporter 3), a transporter that is involved in the active secretion of pemetrexed.
[L43807]
[L43807]
Clearance
The total systemic clearance of pemetrexed is 91.8 mL/min in patients with normal renal function (creatinine clearance of 90 mL/min). As renal function decreases, the clearance of pemetrexed decreases, and exposure (AUC) of pemetrexed increases.
[L43807]
[L43807]
Drug targets(4)
Proteins and enzymes this drug interacts with in the body
Thymidylate synthase
TYMS
inhibitor
Specific functionfolic acid binding
Cellular location
Nucleus
General function & pharmacology
Catalyzes the reductive methylation of 2'-deoxyuridine 5'-monophosphate (dUMP) to thymidine 5'-monophosphate (dTMP), using the cosubstrate, 5,10- methylenetetrahydrofolate (CH2H4folate) as a 1-carbon donor and reductant and contributes to the de novo mitochondrial thymidylate biosynthesis pathway
Bifunctional purine biosynthesis protein ATIC
ATIC
inhibitor
Specific functioncadherin binding
Cellular location
Cytoplasm, cytosol
General function & pharmacology
Bifunctional enzyme that catalyzes the last two steps of purine biosynthesis .
PMID:11948179 PMID:14756554
Acts as a transformylase that incorporates a formyl group to the AMP analog AICAR (5-amino-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide) to produce the intermediate formyl-AICAR (FAICAR) .
PMID:10985775 PMID:11948179 PMID:9378707
Can use both 10-formyldihydrofolate and 10-formyltetrahydrofolate as the formyl donor in this reaction .
PMID:10985775
Also catalyzes the cyclization of FAICAR to inosine monophosphate (IMP) .
PMID:11948179 PMID:14756554
Is able to convert thio-AICAR to 6-mercaptopurine ribonucleotide, an inhibitor of purine biosynthesis used in the treatment of human leukemias .
PMID:10985775
Promotes insulin receptor/INSR autophosphorylation and is involved in INSR internalization PMID:25687571
PMID:11948179 PMID:14756554
Acts as a transformylase that incorporates a formyl group to the AMP analog AICAR (5-amino-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide) to produce the intermediate formyl-AICAR (FAICAR) .
PMID:10985775 PMID:11948179 PMID:9378707
Can use both 10-formyldihydrofolate and 10-formyltetrahydrofolate as the formyl donor in this reaction .
PMID:10985775
Also catalyzes the cyclization of FAICAR to inosine monophosphate (IMP) .
PMID:11948179 PMID:14756554
Is able to convert thio-AICAR to 6-mercaptopurine ribonucleotide, an inhibitor of purine biosynthesis used in the treatment of human leukemias .
PMID:10985775
Promotes insulin receptor/INSR autophosphorylation and is involved in INSR internalization PMID:25687571
Dihydrofolate reductase
DHFR
inhibitor
Specific functiondihydrofolate reductase activity
Cellular location
Mitochondrion
General function & pharmacology
Key enzyme in folate metabolism. Contributes to the de novo mitochondrial thymidylate biosynthesis pathway. Catalyzes an essential reaction for de novo glycine and purine synthesis, and for DNA precursor synthesis.
Binds its own mRNA and that of DHFR2
Binds its own mRNA and that of DHFR2
Trifunctional purine biosynthetic protein adenosine-3
GART
inhibitor
Specific functionATP binding
General function & pharmacology
Trifunctional enzyme that catalyzes three distinct reactions as part of the 'de novo' inosine monophosphate biosynthetic pathway
Metabolizing enzymes(2)
Enzymes involved in drug metabolism — important for understanding drug interactions
Enzyme activity key
substrate
inhibitor
inducer
SLC29A1Equilibrative nucleoside transporter 1
inducer
DCKDeoxycytidine kinase
inducer
Transporters(7)
Proteins that transport this drug across cell membranes
Organic anion transporter 3
SLC22A8
substrate
Specific functionorganic anion transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Functions as an organic anion/dicarboxylate exchanger that couples organic anion uptake indirectly to the sodium gradient .
PMID:14586168 PMID:15644426 PMID:15846473 PMID:16455804 PMID:31553721
Transports organic anions such as estrone 3-sulfate (E1S) and urate in exchange for dicarboxylates such as glutarate or ketoglutarate (2-oxoglutarate) .
PMID:14586168 PMID:15846473 PMID:15864504 PMID:22108572 PMID:23832370
Plays an important role in the excretion of endogenous and exogenous organic anions, especially from the kidney and the brain .
PMID:11306713 PMID:14586168 PMID:15846473
E1S transport is pH- and chloride-dependent and may also involve E1S/cGMP exchange .
PMID:26377792
Responsible for the transport of prostaglandin E2 (PGE2) and prostaglandin F2(alpha) (PGF2(alpha)) in the basolateral side of the renal tubule .
PMID:11907186
Involved in the transport of neuroactive tryptophan metabolites kynurenate and xanthurenate .
PMID:22108572 PMID:23832370
Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins .
PMID:28534121
May be involved in the basolateral transport of steviol, a metabolite of the popular sugar substitute stevioside .
PMID:15644426
May participate in the detoxification/ renal excretion of drugs and xenobiotics, such as the histamine H(2)-receptor antagonists fexofenadine and cimetidine, the antibiotic benzylpenicillin (PCG), the anionic herbicide 2,4-dichloro-phenoxyacetate (2,4-D), the diagnostic agent p-aminohippurate (PAH), the antiviral acyclovir (ACV), and the mycotoxin ochratoxin (OTA), by transporting these exogenous organic anions across the cell membrane in exchange for dicarboxylates such as 2-oxoglutarate .
PMID:11669456 PMID:15846473 PMID:16455804
Contributes to the renal uptake of potent uremic toxins (indoxyl sulfate (IS), indole acetate (IA), hippurate/N-benzoylglycine (HA) and 3-carboxy-4-methyl-5-propyl-2-furanpropionate (CMPF)), pravastatin, PCG, E1S and dehydroepiandrosterone sulfate (DHEAS), and is partly involved in the renal uptake of temocaprilat (an angiotensin-converting enzyme (ACE) inhibitor) .
PMID:14675047
May contribute to the release of cortisol in the adrenals .
PMID:15864504
Involved in one of the detoxification systems on the choroid plexus (CP), removes substrates such as E1S or taurocholate (TC), PCG, 2,4-D and PAH, from the cerebrospinal fluid (CSF) to the blood for eventual excretion in urine and bile (By similarity). Also contributes to the uptake of several other organic compounds such as the prostanoids prostaglandin E(2) and prostaglandin F(2-alpha), L-carnitine, and the therapeutic drugs allopurinol, 6-mercaptopurine (6-MP) and 5-fluorouracil (5-FU) (By similarity). Mediates the transport of PAH, PCG, and the statins pravastatin and pitavastatin, from the cerebrum into the blood circulation across the blood-brain barrier (BBB).
In summary, plays a role in the efflux of drugs and xenobiotics, helping reduce their undesired toxicological effects on the body (By similarity)
PMID:14586168 PMID:15644426 PMID:15846473 PMID:16455804 PMID:31553721
Transports organic anions such as estrone 3-sulfate (E1S) and urate in exchange for dicarboxylates such as glutarate or ketoglutarate (2-oxoglutarate) .
PMID:14586168 PMID:15846473 PMID:15864504 PMID:22108572 PMID:23832370
Plays an important role in the excretion of endogenous and exogenous organic anions, especially from the kidney and the brain .
PMID:11306713 PMID:14586168 PMID:15846473
E1S transport is pH- and chloride-dependent and may also involve E1S/cGMP exchange .
PMID:26377792
Responsible for the transport of prostaglandin E2 (PGE2) and prostaglandin F2(alpha) (PGF2(alpha)) in the basolateral side of the renal tubule .
PMID:11907186
Involved in the transport of neuroactive tryptophan metabolites kynurenate and xanthurenate .
PMID:22108572 PMID:23832370
Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins .
PMID:28534121
May be involved in the basolateral transport of steviol, a metabolite of the popular sugar substitute stevioside .
PMID:15644426
May participate in the detoxification/ renal excretion of drugs and xenobiotics, such as the histamine H(2)-receptor antagonists fexofenadine and cimetidine, the antibiotic benzylpenicillin (PCG), the anionic herbicide 2,4-dichloro-phenoxyacetate (2,4-D), the diagnostic agent p-aminohippurate (PAH), the antiviral acyclovir (ACV), and the mycotoxin ochratoxin (OTA), by transporting these exogenous organic anions across the cell membrane in exchange for dicarboxylates such as 2-oxoglutarate .
PMID:11669456 PMID:15846473 PMID:16455804
Contributes to the renal uptake of potent uremic toxins (indoxyl sulfate (IS), indole acetate (IA), hippurate/N-benzoylglycine (HA) and 3-carboxy-4-methyl-5-propyl-2-furanpropionate (CMPF)), pravastatin, PCG, E1S and dehydroepiandrosterone sulfate (DHEAS), and is partly involved in the renal uptake of temocaprilat (an angiotensin-converting enzyme (ACE) inhibitor) .
PMID:14675047
May contribute to the release of cortisol in the adrenals .
PMID:15864504
Involved in one of the detoxification systems on the choroid plexus (CP), removes substrates such as E1S or taurocholate (TC), PCG, 2,4-D and PAH, from the cerebrospinal fluid (CSF) to the blood for eventual excretion in urine and bile (By similarity). Also contributes to the uptake of several other organic compounds such as the prostanoids prostaglandin E(2) and prostaglandin F(2-alpha), L-carnitine, and the therapeutic drugs allopurinol, 6-mercaptopurine (6-MP) and 5-fluorouracil (5-FU) (By similarity). Mediates the transport of PAH, PCG, and the statins pravastatin and pitavastatin, from the cerebrum into the blood circulation across the blood-brain barrier (BBB).
In summary, plays a role in the efflux of drugs and xenobiotics, helping reduce their undesired toxicological effects on the body (By similarity)
Reduced folate transporter
SLC19A1
substrate
Specific function2',3'-cyclic GMP-AMP binding
Cellular location
Cell membrane
General function & pharmacology
Antiporter that mediates the import of reduced folates or a subset of cyclic dinucleotides, driven by the export of organic anions .
PMID:10787414 PMID:15337749 PMID:16115875 PMID:22554803 PMID:31126740 PMID:31511694 PMID:32276275 PMID:36071163 PMID:36265513 PMID:36575193 PMID:7826387 PMID:9041240
Acts as an importer of immunoreactive cyclic dinucleotides, such as cyclic GMP-AMP (2'-3'-cGAMP), an immune messenger produced in response to DNA virus in the cytosol, and its linkage isomer 3'-3'-cGAMP, thus playing a role in triggering larger immune responses .
PMID:31126740 PMID:31511694 PMID:36745868
Mechanistically, acts as a secondary active transporter, which exports intracellular organic anions down their concentration gradients to facilitate the uptake of its substrates .
PMID:22554803 PMID:31126740 PMID:31511694
Has high affinity for N5-methyltetrahydrofolate, the predominant circulating form of folate .
PMID:10787414 PMID:14609557 PMID:22554803 PMID:36071163 PMID:36265513 PMID:36575193
Also mediates the import of antifolate drug methotrexate .
PMID:22554803 PMID:36071163 PMID:7615551 PMID:7641195 PMID:9767079
5-amino-4-imidazolecarboxamide riboside (AICAR), when phosphorylated to AICAR monophosphate, can serve as an organic anion for antiporter activity PMID:22554803
PMID:10787414 PMID:15337749 PMID:16115875 PMID:22554803 PMID:31126740 PMID:31511694 PMID:32276275 PMID:36071163 PMID:36265513 PMID:36575193 PMID:7826387 PMID:9041240
Acts as an importer of immunoreactive cyclic dinucleotides, such as cyclic GMP-AMP (2'-3'-cGAMP), an immune messenger produced in response to DNA virus in the cytosol, and its linkage isomer 3'-3'-cGAMP, thus playing a role in triggering larger immune responses .
PMID:31126740 PMID:31511694 PMID:36745868
Mechanistically, acts as a secondary active transporter, which exports intracellular organic anions down their concentration gradients to facilitate the uptake of its substrates .
PMID:22554803 PMID:31126740 PMID:31511694
Has high affinity for N5-methyltetrahydrofolate, the predominant circulating form of folate .
PMID:10787414 PMID:14609557 PMID:22554803 PMID:36071163 PMID:36265513 PMID:36575193
Also mediates the import of antifolate drug methotrexate .
PMID:22554803 PMID:36071163 PMID:7615551 PMID:7641195 PMID:9767079
5-amino-4-imidazolecarboxamide riboside (AICAR), when phosphorylated to AICAR monophosphate, can serve as an organic anion for antiporter activity PMID:22554803
Proton-coupled folate transporter
SLC46A1
substrate
Specific functionfolic acid binding
Cellular location
Cell membrane
General function & pharmacology
Proton-coupled folate symporter that mediates folate absorption using an H(+) gradient as a driving force .
PMID:17129779 PMID:17446347 PMID:17475902 PMID:19389703 PMID:19762432 PMID:25504888 PMID:29344585 PMID:30858177 PMID:31494288 PMID:31792273 PMID:32893190 PMID:34619546
Involved in the intestinal absorption of folates at the brush-border membrane of the proximal jejunum, and the transport from blood to cerebrospinal fluid across the choroid plexus .
PMID:17129779 PMID:17446347 PMID:17475902 PMID:19389703 PMID:25504888 PMID:29344585 PMID:30858177 PMID:31494288 PMID:32893190
Functions at acidic pH via alternate outward- and inward-open conformation states .
PMID:32893190 PMID:34040256
Protonation of residues in the outward open state primes the protein for transport .
PMID:34040256
Binding of folate promotes breaking of salt bridge network and subsequent closure of the extracellular gate, leading to the inward-open state and release of protons and folate .
PMID:34040256
Also able to transport antifolate drugs, such as methotrexate and pemetrexed, which are established treatments for cancer and autoimmune diseases .
PMID:18524888 PMID:19762432 PMID:22345511 PMID:25608532 PMID:28802835 PMID:29326243 PMID:34040256 PMID:34619546
Involved in FOLR1-mediated endocytosis by serving as a route of export of folates from acidified endosomes .
PMID:19074442
Also acts as a lower-affinity, pH-independent heme carrier protein and constitutes the main importer of heme in the intestine .
PMID:17156779
Imports heme in the retina and retinal pigment epithelium, in neurons of the hippocampus, in hepatocytes and in the renal epithelial cells .
PMID:32621820
Hence, participates in the trafficking of heme and increases intracellular iron content PMID:32621820
PMID:17129779 PMID:17446347 PMID:17475902 PMID:19389703 PMID:19762432 PMID:25504888 PMID:29344585 PMID:30858177 PMID:31494288 PMID:31792273 PMID:32893190 PMID:34619546
Involved in the intestinal absorption of folates at the brush-border membrane of the proximal jejunum, and the transport from blood to cerebrospinal fluid across the choroid plexus .
PMID:17129779 PMID:17446347 PMID:17475902 PMID:19389703 PMID:25504888 PMID:29344585 PMID:30858177 PMID:31494288 PMID:32893190
Functions at acidic pH via alternate outward- and inward-open conformation states .
PMID:32893190 PMID:34040256
Protonation of residues in the outward open state primes the protein for transport .
PMID:34040256
Binding of folate promotes breaking of salt bridge network and subsequent closure of the extracellular gate, leading to the inward-open state and release of protons and folate .
PMID:34040256
Also able to transport antifolate drugs, such as methotrexate and pemetrexed, which are established treatments for cancer and autoimmune diseases .
PMID:18524888 PMID:19762432 PMID:22345511 PMID:25608532 PMID:28802835 PMID:29326243 PMID:34040256 PMID:34619546
Involved in FOLR1-mediated endocytosis by serving as a route of export of folates from acidified endosomes .
PMID:19074442
Also acts as a lower-affinity, pH-independent heme carrier protein and constitutes the main importer of heme in the intestine .
PMID:17156779
Imports heme in the retina and retinal pigment epithelium, in neurons of the hippocampus, in hepatocytes and in the renal epithelial cells .
PMID:32621820
Hence, participates in the trafficking of heme and increases intracellular iron content PMID:32621820
Broad substrate specificity ATP-binding cassette transporter ABCG2
ABCG2
Specific functionABC-type xenobiotic transporter activity
Cellular location
Cell membrane
General function & pharmacology
Broad substrate specificity ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes a wide variety of physiological compounds, dietary toxins and xenobiotics from cells .
PMID:11306452 PMID:12958161 PMID:19506252 PMID:20705604 PMID:28554189 PMID:30405239 PMID:31003562
Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme .
PMID:20705604 PMID:23189181
Also mediates the efflux of sphingosine-1-P from cells .
PMID:20110355
Acts as a urate exporter functioning in both renal and extrarenal urate excretion .
PMID:19506252 PMID:20368174 PMID:22132962 PMID:31003562 PMID:36749388
In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates .
PMID:12682043 PMID:28554189 PMID:30405239
Mediates the secretion of the riboflavin and biotin vitamins into milk (By similarity). Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity).
Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux .
PMID:11306452 PMID:12477054 PMID:15670731 PMID:18056989 PMID:31254042
In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity).
In inflammatory macrophages, exports itaconate from the cytosol to the extracellular compartment and limits the activation of TFEB-dependent lysosome biogenesis involved in antibacterial innate immune response
PMID:11306452 PMID:12958161 PMID:19506252 PMID:20705604 PMID:28554189 PMID:30405239 PMID:31003562
Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme .
PMID:20705604 PMID:23189181
Also mediates the efflux of sphingosine-1-P from cells .
PMID:20110355
Acts as a urate exporter functioning in both renal and extrarenal urate excretion .
PMID:19506252 PMID:20368174 PMID:22132962 PMID:31003562 PMID:36749388
In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates .
PMID:12682043 PMID:28554189 PMID:30405239
Mediates the secretion of the riboflavin and biotin vitamins into milk (By similarity). Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity).
Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux .
PMID:11306452 PMID:12477054 PMID:15670731 PMID:18056989 PMID:31254042
In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity).
In inflammatory macrophages, exports itaconate from the cytosol to the extracellular compartment and limits the activation of TFEB-dependent lysosome biogenesis involved in antibacterial innate immune response
ATP-binding cassette sub-family C member 5
ABCC5
Specific functionABC-type xenobiotic transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes physiological compounds, and xenobiotics from cells. Mediates ATP-dependent transport of endogenous metabolites such as cAMP and cGMP, folic acid and N-lactoyl-amino acids (in vitro) .
PMID:10893247 PMID:12637526 PMID:12695538 PMID:15899835 PMID:17229149 PMID:25964343
Also acts as a general glutamate conjugate and analog transporter that can limit the brain levels of endogenous metabolites, drugs, and toxins .
PMID:26515061
Confers resistance to the antiviral agent PMEA .
PMID:12695538
Able to transport several anticancer drugs including methotrexate, and nucleotide analogs in vitro, however it does with low affinity, thus the exact role of ABCC5 in mediating resistance still needs to be elucidated .
PMID:10840050 PMID:12435799 PMID:12695538 PMID:15899835
Acts as a heme transporter required for the translocation of cytosolic heme to the secretory pathway .
PMID:24836561
May play a role in energy metabolism by regulating the glucagon-like peptide 1 (GLP-1) secretion from enteroendocrine cells (By similarity)
PMID:10893247 PMID:12637526 PMID:12695538 PMID:15899835 PMID:17229149 PMID:25964343
Also acts as a general glutamate conjugate and analog transporter that can limit the brain levels of endogenous metabolites, drugs, and toxins .
PMID:26515061
Confers resistance to the antiviral agent PMEA .
PMID:12695538
Able to transport several anticancer drugs including methotrexate, and nucleotide analogs in vitro, however it does with low affinity, thus the exact role of ABCC5 in mediating resistance still needs to be elucidated .
PMID:10840050 PMID:12435799 PMID:12695538 PMID:15899835
Acts as a heme transporter required for the translocation of cytosolic heme to the secretory pathway .
PMID:24836561
May play a role in energy metabolism by regulating the glucagon-like peptide 1 (GLP-1) secretion from enteroendocrine cells (By similarity)
Solute carrier family 22 member 6
SLC22A6
substrate
Specific functionalpha-ketoglutarate transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Secondary active transporter that functions as a Na(+)-independent organic anion (OA)/dicarboxylate antiporter where the uptake of one molecule of OA into the cell is coupled with an efflux of one molecule of intracellular dicarboxylate such as 2-oxoglutarate or glutarate .
PMID:11669456 PMID:11907186 PMID:14675047 PMID:22108572 PMID:23832370 PMID:28534121 PMID:9950961
Mediates the uptake of OA across the basolateral side of proximal tubule epithelial cells, thereby contributing to the renal elimination of endogenous OA from the systemic circulation into the urine .
PMID:9887087
Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins .
PMID:28534121
Transports prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) and may contribute to their renal excretion .
PMID:11907186
Also mediates the uptake of cyclic nucleotides such as cAMP and cGMP .
PMID:26377792
Involved in the transport of neuroactive tryptophan metabolites kynurenate (KYNA) and xanthurenate (XA) and may contribute to their secretion from the brain .
PMID:22108572 PMID:23832370
May transport glutamate .
PMID:26377792
Also involved in the disposition of uremic toxins and potentially toxic xenobiotics by the renal organic anion secretory pathway, helping reduce their undesired toxicological effects on the body .
PMID:11669456 PMID:14675047
Uremic toxins include the indoxyl sulfate (IS), hippurate/N-benzoylglycine (HA), indole acetate (IA), 3-carboxy-4- methyl-5-propyl-2-furanpropionate (CMPF) and urate .
PMID:14675047 PMID:26377792
Xenobiotics include the mycotoxin ochratoxin (OTA) .
PMID:11669456
May also contribute to the transport of organic compounds in testes across the blood-testis-barrier PMID:35307651
PMID:11669456 PMID:11907186 PMID:14675047 PMID:22108572 PMID:23832370 PMID:28534121 PMID:9950961
Mediates the uptake of OA across the basolateral side of proximal tubule epithelial cells, thereby contributing to the renal elimination of endogenous OA from the systemic circulation into the urine .
PMID:9887087
Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins .
PMID:28534121
Transports prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) and may contribute to their renal excretion .
PMID:11907186
Also mediates the uptake of cyclic nucleotides such as cAMP and cGMP .
PMID:26377792
Involved in the transport of neuroactive tryptophan metabolites kynurenate (KYNA) and xanthurenate (XA) and may contribute to their secretion from the brain .
PMID:22108572 PMID:23832370
May transport glutamate .
PMID:26377792
Also involved in the disposition of uremic toxins and potentially toxic xenobiotics by the renal organic anion secretory pathway, helping reduce their undesired toxicological effects on the body .
PMID:11669456 PMID:14675047
Uremic toxins include the indoxyl sulfate (IS), hippurate/N-benzoylglycine (HA), indole acetate (IA), 3-carboxy-4- methyl-5-propyl-2-furanpropionate (CMPF) and urate .
PMID:14675047 PMID:26377792
Xenobiotics include the mycotoxin ochratoxin (OTA) .
PMID:11669456
May also contribute to the transport of organic compounds in testes across the blood-testis-barrier PMID:35307651
Solute carrier family 22 member 11
SLC22A11
substrate
Specific functionorganic anion transmembrane transporter activity
Cellular location
Cell membrane
General function & pharmacology
Antiporter that mediates the transport of conjugated steroids and other specific organic anions at the basal membrane of syncytiotrophoblast and at the apical membrane of proximal tubule epithelial cells, in exchange for anionic compounds .
PMID:10660625 PMID:11907186 PMID:15037815 PMID:15102942 PMID:15291761 PMID:15576633 PMID:17229912 PMID:18501590 PMID:26277985 PMID:28027879
May be responsible for placental absorption of fetal-derived steroid sulfates such as estrone sulfate (E1S) and the steroid hormone precursor dehydroepiandrosterone sulfate (DHEA-S), as well as clearing waste products and xenobiotics from the fetus .
PMID:12409283
Maybe also be involved in placental urate homeostasis .
PMID:17229912
Facilitates the renal reabsorption of organic anions such as urate and derived steroid sulfates .
PMID:15037815 PMID:17229912
Organic anion glutarate acts as conteranion for E1S renal uptake .
PMID:15037815 PMID:17229912
Possible transport mode may also include DHEA-S/E1S exchange .
PMID:28027879
Also interacts with inorganic anions such as chloride and hydroxyl ions, therefore possible transport modes may include E1S/Cl(-), E1S/OH(-), urate/Cl(-) and urate/OH(-) .
PMID:17229912
Also mediates the transport of prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) and may be involved in their renal excretion .
PMID:11907186
Also able to uptake anionic drugs, diuretics, bile salts and ochratoxin A .
PMID:10660625 PMID:26277985
Mediates the unidirectional efflux of glutamate and aspartate .
PMID:28027879
Glutamate efflux down its transmembrane gradient may drive SLC22A11/OAT4-mediated placental uptake of E1S PMID:26277985
PMID:10660625 PMID:11907186 PMID:15037815 PMID:15102942 PMID:15291761 PMID:15576633 PMID:17229912 PMID:18501590 PMID:26277985 PMID:28027879
May be responsible for placental absorption of fetal-derived steroid sulfates such as estrone sulfate (E1S) and the steroid hormone precursor dehydroepiandrosterone sulfate (DHEA-S), as well as clearing waste products and xenobiotics from the fetus .
PMID:12409283
Maybe also be involved in placental urate homeostasis .
PMID:17229912
Facilitates the renal reabsorption of organic anions such as urate and derived steroid sulfates .
PMID:15037815 PMID:17229912
Organic anion glutarate acts as conteranion for E1S renal uptake .
PMID:15037815 PMID:17229912
Possible transport mode may also include DHEA-S/E1S exchange .
PMID:28027879
Also interacts with inorganic anions such as chloride and hydroxyl ions, therefore possible transport modes may include E1S/Cl(-), E1S/OH(-), urate/Cl(-) and urate/OH(-) .
PMID:17229912
Also mediates the transport of prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) and may be involved in their renal excretion .
PMID:11907186
Also able to uptake anionic drugs, diuretics, bile salts and ochratoxin A .
PMID:10660625 PMID:26277985
Mediates the unidirectional efflux of glutamate and aspartate .
PMID:28027879
Glutamate efflux down its transmembrane gradient may drive SLC22A11/OAT4-mediated placental uptake of E1S PMID:26277985
Carriers(1)
Proteins that carry this drug through the body
Albumin
ALB
binder
Specific functionantioxidant activity
Cellular location
Secreted
General function & pharmacology
Binds water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs (Probable). Its main function is the regulation of the colloidal osmotic pressure of blood (Probable). Major zinc transporter in plasma, typically binds about 80% of all plasma zinc .
PMID:19021548
Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity).
Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity).
Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli .
PMID:6234017
Does not prevent iron uptake by the bacterial siderophore aerobactin PMID:6234017
PMID:19021548
Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity).
Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity).
Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli .
PMID:6234017
Does not prevent iron uptake by the bacterial siderophore aerobactin PMID:6234017
Scientific references(10)
Rollins K.D., Lindley C.
Pemetrexed: A multitargeted antifolate.
Clinical Therapeutics
200527(9):1343-1382. doi: 10.1016/j.clinthera.2005.09.010
Lansiaux A., Lokiec F.
P53, A Target Antigen For Immunotherapy in Ovarian Cancer - From Preclinic to Clinic.
International Journal of Gynecological Cancer
200313:44. doi: 10.1136/ijgc-00009577-200303001-00153
Fuld A.D., Dragnev K.H., Rigas J.R.
Pemetrexed in advanced non-small-cell lung cancer.
Expert Opinion on Pharmacotherapy
2010 Jun11(8):1387-402. doi: 10.1517/14656566.2010.482560
Adjei A.A.
Pemetrexed (Alimta<sup>®</sup>): a novel multitargeted antifolate agent.
Expert Review of Anticancer Therapy
20033(2):145-156. doi: 10.1586/14737140.3.2.145
Hazarika M., White R.M., Johnson J.R., Pazdur R.
FDA drug approval summaries: pemetrexed (Alimta).
Oncologist
20049(5):482-8. doi: 10.1634/theoncologist.9-5-482
Sehouli J., Alvarez A.M., Manouchehrpour S., Ghatage P., Szczylik C., Zimmermann A., Bauknecht T., Look K.Y., Oskay-Oezcelik G.
A phase II trial of pemetrexed in combination with carboplatin in patients with recurrent ovarian or primary peritoneal cancer.
Gynecology Oncology
2012 Feb124(2):205-9. doi: 10.1016/j.ygyno.2011.09.007. Epub 2011 Nov 1
Gbolahan O.B., Porter R.F., Salter J.T., Yiannoutsos C., Burns M., Chiorean E.G., Loehrer PJ Sr
A Phase II Study of Pemetrexed in Patients with Recurrent Thymoma and Thymic Carcinoma.
Journal Thorac Oncology
2018 Dec13(12):1940-1948. doi: 10.1016/j.jtho.2018.07.094. Epub 2018 Aug 16
Choi Y.J., Lee S.H., Lee J.L., Ahn J.H., Lee K.H., You D., Hong B., Hong J.H., Ahn H.
Phase II study of pemetrexed in combination with cisplatin in patients with advanced urothelial cancer: the PECULIAR study (KCSG 10-17).
British Journal Cancer
2015 Jan 20112(2):260-5. doi: 10.1038/bjc.2014.591. Epub 2014 Nov 27
He Y., Wang J., Xie S., Xue Q.
Efficacy of Bevacizumab Combined with Pemetrexed in the Treatment of Recurrent and Metastatic Cervical Cancer.
Front Surgery
2022 May 169:908101. doi: 10.3389/fsurg.2022.908101. eCollection 2022
Sorensen J.B.
Pharmacokinetic evaluation of pemetrexed.
Expert Opinion Drug Metabolism Toxicology
2011 Jul7(7):919-28. doi: 10.1517/17425255.2011.587411. Epub 2011 May 21
ATC classification(1 code)
ATC L01BA04
Affected organisms(1)
Humans and other mammals
Salt forms(5)
Pemetrexed disodium(DBSALT000846)
Pemetrexed disodium hemipentahydrate(DBSALT001782)
Pemetrexed disodium heptahydrate(DBSALT001641)
Pemetrexed ditromethamine(DBSALT003140)
Pemetrexed monohydrate(DBSALT002627)
Experimental properties(1)
Commercial products(175)
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Show
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Pemetrexed
Additional database identifiers
Drugs Product Database (DPD)
13326
ChemSpider
393879
BindingDB
18796
PDB
LYA
ZINC
ZINC000001540998
HUGO Gene Nomenclature Committee (HGNC)
HGNC:12441
GenAtlas
TYMS
GeneCards
TYMS
GenBank Gene Database
X02308
GenBank Protein Database
37479
Guide to Pharmacology
2642
UniProt Accession
TYSY_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:794
GenAtlas
ATIC
GeneCards
ATIC
GenBank Gene Database
U37436
GenBank Protein Database
1263196
UniProt Accession
PUR9_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2861
GenAtlas
DHFR
GeneCards
DHFR
GenBank Gene Database
J00140
GenBank Protein Database
182724
Guide to Pharmacology
2603
UniProt Accession
DYR_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:4163
GenAtlas
GART
GeneCards
GART
GenBank Gene Database
X54199
GenBank Protein Database
31642
UniProt Accession
PUR2_HUMAN
GenBank Gene Database
J04230
GenBank Protein Database
7537304
UniProt Accession
TYSY_CANAL
HUGO Gene Nomenclature Committee (HGNC)
HGNC:11003
GenAtlas
SLC29A1
GeneCards
SLC29A1
GenBank Gene Database
U81375
GenBank Protein Database
1845345
Guide to Pharmacology
1117
UniProt Accession
S29A1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2704
GenAtlas
DCK
GeneCards
DCK
GenBank Gene Database
M60527
UniProt Accession
DCK_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:399
GenAtlas
ALB
GeneCards
ALB
GenBank Gene Database
V00494
GenBank Protein Database
28590
UniProt Accession
ALBU_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10972
GeneCards
SLC22A8
GenBank Gene Database
AF097491
GenBank Protein Database
4378059
Guide to Pharmacology
1027
UniProt Accession
S22A8_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10937
GeneCards
SLC19A1
Guide to Pharmacology
1014
UniProt Accession
S19A1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:30521
GenAtlas
SLC46A1
GeneCards
SLC46A1
GenBank Gene Database
AK054669
GenBank Protein Database
16549261
Guide to Pharmacology
1213
UniProt Accession
PCFT_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:74
GenAtlas
ABCG2
GeneCards
ABCG2
GenBank Gene Database
AF103796
GenBank Protein Database
4185796
Guide to Pharmacology
792
UniProt Accession
ABCG2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:56
GeneCards
ABCC5
GenBank Gene Database
AF104942
GenBank Protein Database
4140698
Guide to Pharmacology
783
UniProt Accession
MRP5_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10970
GenAtlas
hROAT1
GeneCards
SLC22A6
GenBank Gene Database
AF057039
GenBank Protein Database
3831566
Guide to Pharmacology
1025
UniProt Accession
S22A6_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:18120
GenAtlas
SLC22A11
GeneCards
SLC22A11
GenBank Gene Database
AB026116
GenBank Protein Database
7707622
Guide to Pharmacology
1030
UniProt Accession
S22AB_HUMAN
International reference pricing
3 formulations
Reference pricing from DrugBank. Prices are indicative and may not reflect current UK costs.
From $606.72/vial
To $3154.94/vial
Alimta 100 mg vial
$606.72/vial
Alimta 500 mg vial
$3033.60/vial
Alimta 500 mg Solution Vial
$3154.94/vial
Source: DrugBank. Used under CC BY-NC 4.0 academic licence for non-commercial purposes.
Patent information
4 active patents, 5 expired
11793813
United States
Approved 24 Oct 2023 · Expires 19 Feb 2036
9y 10m
12115164
United States
Approved 19 Feb 2016 · Expires 19 Feb 2036
9y 10m
9604990
United States
Approved 28 Mar 2017 · Expires 28 Oct 2035
9y 7m
11147817
United States
Approved 19 Oct 2021 · Expires 26 Mar 2035
8y 11m
Approved 10 Aug 2010 · Expires 24 May 2022
Expired
Source: DrugBank · CC BY-NC 4.0. Patent data sourced from national patent offices. Expiry dates may not reflect extensions, regulatory exclusivity periods, or legal challenges.
DrugBank citations
If you use DrugBank data in your research, please cite the following publications:
Knox C., Wilson M., Klinger C.M., et al
DrugBank 6.
0: the DrugBank Knowledgebase for 2024
Nucleic Acids Res. 2024 Jan 552(D1):D1265-D1275
Wishart D.S., Feunang Y.D., Guo A.C., et al
DrugBank 5.
0: a major update to the DrugBank database for 2018
Nucleic Acids Res. 2017 Nov 846(D1):D1074-D1082
Show earlier publications
Law V., Knox C., Djoumbou Y., et al
DrugBank 4.
0: shedding new light on drug metabolism
Nucleic Acids Res. 2014 Jan 142(1):D1091-7
Knox C., Law V., Jewison T., et al
DrugBank 3.
0: a comprehensive resource for 'omics' research on drugs
Nucleic Acids Res. 2011 Jan39(Database issue):D1035-41
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a knowledgebase for drugs, drug actions and drug targets.
Nucleic Acids Research
2008 Jan36(Database issue):D901-6
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a comprehensive resource for in silico drug discovery and exploration.
Nucleic Acids Research
2006 Jan 134(Database issue):D668-72
Source: go.drugbank.comCC BY-NC 4.0
Updated 27 days ago(8 Mar 2026)