Elacestrant 345mg tablets
Prescription only
Requires a prescription from a doctor or prescriber
Tablet
345mg
Oral
Sex hormones and hormone antagonists in malignant disease
Active ingredients:
Elacestrant
No active safety alerts
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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.
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Clinical guidelines and formulary information
British National Formulary
Elacestrant
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(1)
Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
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Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
None known
Half-life
30 to 50 hours
Mechanism
Elacestrant is an oral selective estrogen receptor degrader (SERD) that binds to estrogen receptor-alpha (ERα).
Food interactions
1 warning
Human targets
1 target
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
345 mg
With the recommended dosage of 345 mg once daily, elacestrant has a steady-state Cmax of 119 ng/mL and an AUC0-24h of 2440 ng⋅h/mL.…
Half-life
30 to 50 hours
The elimination half-life of elacestrant is 30 to 50 hours.
[L44918]
[L44918]
Protein binding
99%
Elacestrant has a protein plasma binding higher than 99% and independent of concentration.
[L44918]
[L44918]
Volume of distribution
5800 L
Elacestrant has an apparent volume of distribution of 5800 L.
[L44918]
[L44918]
Metabolism
Elacestrant is metabolized in the liver, mainly by CYP3A4 and, to a lesser extent, by CYP2A6 and CYP2C9.
[L44918]
[L44918]
Elimination
82%
Elacestrant is mainly eliminated through feces and urine. Approximately 82% was recovered in feces (34% unchanged), and 7.5%…
Clearance
186 L/h
Elacestrant has an estimated clearance of 186 L/hr and a renal clearance of ≤ 0.14 L/hr.
[L44918]
[L44918]
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Status:
Approved
Investigational
Small molecule
About this compound
Elacestrant is a non-steroidal small molecule and an estrogen receptor (ER) antagonist.[A256838][L44918] In January 2023, it was approved by the FDA for the treatment of ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer.[L44918][L44948] It received a similar approval in the EU in September 2023.[L49334]
Elacestrant binds to estrogen receptor-alpha (ERα) and acts as a selective estrogen receptor degrader (SERD) thanks to its ability to block the transcriptional activity of the ER and promote its degradation.[A256828][A256863][L44948] Other types of endocrine therapy, such as selective estrogen receptor modulators (SERMs) and aromatase inhibitors (AIs), may lead to drug resistance over time; therefore, the use of a SERD represents a therapeutic approach for the treatment of endocrine-resistant breast cancers.[A256878] Unlike [fulvestrant], another FDA-approved SERD, elacestrant is orally bioavailable.[A256833]
Elacestrant binds to estrogen receptor-alpha (ERα) and acts as a selective estrogen receptor degrader (SERD) thanks to its ability to block the transcriptional activity of the ER and promote its degradation.[A256828][A256863][L44948] Other types of endocrine therapy, such as selective estrogen receptor modulators (SERMs) and aromatase inhibitors (AIs), may lead to drug resistance over time; therefore, the use of a SERD represents a therapeutic approach for the treatment of endocrine-resistant breast cancers.[A256878] Unlike [fulvestrant], another FDA-approved SERD, elacestrant is orally bioavailable.[A256833]
Properties:
solid
Avg. mass: 458.65 Da
DrugBank indication
Elacestrant is indicated for the treatment of postmenopausal women or adult men with ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer with disease progression following at least one line of endocrine therapy.
[L44918]
Elacestrant is indicated for the same in the EU, with an additional requirement that patients trial a CDK 4/6 inhibitor as a prior line of therapy.
[L49329]
[L44918]
Elacestrant is indicated for the same in the EU, with an additional requirement that patients trial a CDK 4/6 inhibitor as a prior line of therapy.
[L49329]
Also known as(72)
(2R)-2-(2-(ethyl-((4-(2-(ethylamino)ethyl)phenyl)methyl)amino)-4-methoxy-phenyl)tetralin-6-ol
(6R)-6-(2-(ethyl((4-(2- (ethylamino)ethyl)phenyl)methyl)amino)-4-methoxyphenyl)- 5,6,7,8-tetrahydronaphthalen-2-ol
2-naphthalenol, 6-(2-(ethyl((4-(2-(ethylamino)ethyl)phenyl)methyl)amino)-4-methoxyphenyl)-5,6,7,8-tetrahydro-, (6R)-
Elacestrant
ER
ER-alpha
ESR
Estradiol receptor
Dosage forms(4)
Tablet, film coated (Oral) — 345 mg/1
Tablet, film coated (Oral) — 345 mg
Tablet, film coated (Oral) — 86 mg/1
Tablet, film coated (Oral) — 86 mg
Molecular properties(19)
Drug interactions(357)
Known interactions with other medications. Always consult a healthcare professional.
Darbepoetin alfa
Unknown severity
The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Elacestrant.
Erythropoietin
Unknown severity
The risk or severity of Thrombosis can be increased when Erythropoietin is combined with Elacestrant.
Peginesatide
Unknown severity
The risk or severity of Thrombosis can be increased when Peginesatide is combined with Elacestrant.
Methoxy polyethylene glycol-epoetin beta
Unknown severity
The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Elacestrant.
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Lidocaine.
Ropivacaine
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Ropivacaine.
Bupivacaine
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Bupivacaine.
Cinchocaine
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Cinchocaine.
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Dyclonine.
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Procaine.
Prilocaine
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Prilocaine.
Proparacaine
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Proparacaine.
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Meloxicam.
Oxybuprocaine
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Oxybuprocaine.
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Cocaine.
Mepivacaine
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Mepivacaine.
Levobupivacaine
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Levobupivacaine.
Diphenhydramine
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Diphenhydramine.
Benzocaine
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Benzocaine.
Chloroprocaine
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Chloroprocaine.
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Phenol.
Tetrodotoxin
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Tetrodotoxin.
Benzyl alcohol
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Benzyl alcohol.
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Capsaicin.
Etidocaine
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Etidocaine.
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Articaine.
Tetracaine
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Tetracaine.
Propoxycaine
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Propoxycaine.
Pramocaine
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Pramocaine.
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Butamben.
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Butacaine.
Oxethazaine
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Oxetacaine.
Ethyl chloride
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Ethyl chloride.
Butanilicaine
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Butanilicaine.
Metabutethamine
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Metabutethamine.
Quinisocaine
Unknown severity
The risk or severity of methemoglobinemia can be increased when Elacestrant is combined with Quinisocaine.
Cyclosporine
Unknown severity
The serum concentration of Elacestrant can be increased when it is combined with Cyclosporine.
Fluvoxamine
Unknown severity
The serum concentration of Elacestrant can be increased when it is combined with Fluvoxamine.
Fluconazole
Unknown severity
The serum concentration of Elacestrant can be increased when it is combined with Fluconazole.
Erythromycin
Unknown severity
The serum concentration of Elacestrant can be increased when it is combined with Erythromycin.
Ziprasidone
Unknown severity
The serum concentration of Elacestrant can be increased when it is combined with Ziprasidone.
Isradipine
Unknown severity
The serum concentration of Elacestrant can be increased when it is combined with Isradipine.
The serum concentration of Elacestrant can be increased when it is combined with Diltiazem.
The serum concentration of Elacestrant can be increased when it is combined with Clozapine.
Haloperidol
Unknown severity
The serum concentration of Elacestrant can be increased when it is combined with Haloperidol.
Ciprofloxacin
Unknown severity
The serum concentration of Elacestrant can be increased when it is combined with Ciprofloxacin.
Voriconazole
Unknown severity
The serum concentration of Elacestrant can be increased when it is combined with Voriconazole.
Nicardipine
Unknown severity
The serum concentration of Elacestrant can be increased when it is combined with Nicardipine.
The serum concentration of Elacestrant can be increased when it is combined with Verapamil.
Aprepitant
Unknown severity
The serum concentration of Elacestrant can be increased when it is combined with Aprepitant.
Showing 50 of 357 interactions
Food & lifestyle interactions
Take With Food
Take with food. Take with food to reduce nausea and vomiting.
Toxicity & overdose
Toxicity information regarding elacestrant is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as dyslipidemia and gastrointestinal disorders.
[L44918]
Symptomatic and supportive measures are recommended. The carcinogenicity of elacestrant has not been evaluated.
Elacestrant did not show mutagenicity in the in vitro Ames assay and was negative for clastogenicity in in vitro chromosome aberration assays and the in vivo rat bone marrow micronucleus assay.
[L44918]
Fertility studies with elacestrant in animals have not been performed. Rats and cynomolgus monkeys presented adverse reactions in female reproductive organs including atrophy of the vagina, cervix, and uterus and follicular cysts in the ovary after receiving repeated doses of elacestrant. Male rats presented decreased cellularity of Leydig cells and degeneration/atrophy of the seminiferous epithelium in the testis.
[L44918]
[L44918]
Symptomatic and supportive measures are recommended. The carcinogenicity of elacestrant has not been evaluated.
Elacestrant did not show mutagenicity in the in vitro Ames assay and was negative for clastogenicity in in vitro chromosome aberration assays and the in vivo rat bone marrow micronucleus assay.
[L44918]
Fertility studies with elacestrant in animals have not been performed. Rats and cynomolgus monkeys presented adverse reactions in female reproductive organs including atrophy of the vagina, cervix, and uterus and follicular cysts in the ovary after receiving repeated doses of elacestrant. Male rats presented decreased cellularity of Leydig cells and degeneration/atrophy of the seminiferous epithelium in the testis.
[L44918]
How it works
Mechanism of action
Elacestrant is an oral selective estrogen receptor degrader (SERD) that binds to estrogen receptor-alpha (ERα).[A256833][A256838][L44918] Breast tumors that express ERα depend on estrogen-mediated growth signaling; therefore, endocrine therapies that target the estrogen receptor (ER) are commonly used in the treatment of this type of cancer. SERDs are a type of endocrine therapy that antagonizes the transcriptional activity of the ER and promotes its degradation.[A256828]
In ER-positive (ER+) HER2-negative (HER2-) breast cancer cells, elacestrant inhibits 17β-estradiol-mediated cell proliferation and induces ERα degradation through the proteasomal pathway.[L44918] Elacestrant also slows ER nuclear translocation and promotes ER turnover, disrupting downstream signaling.[A256828] Elacestrant has in vitro and in vivo anti-tumor activity in ER+ HER2- breast cancer models resistant to fulvestrant and cyclin-dependent kinase 4/6 inhibitors, as well as cancer models with estrogen receptor 1 gene (ESR1) mutations.[A256843][A256848][L44918]
In ER-positive (ER+) HER2-negative (HER2-) breast cancer cells, elacestrant inhibits 17β-estradiol-mediated cell proliferation and induces ERα degradation through the proteasomal pathway.[L44918] Elacestrant also slows ER nuclear translocation and promotes ER turnover, disrupting downstream signaling.[A256828] Elacestrant has in vitro and in vivo anti-tumor activity in ER+ HER2- breast cancer models resistant to fulvestrant and cyclin-dependent kinase 4/6 inhibitors, as well as cancer models with estrogen receptor 1 gene (ESR1) mutations.[A256843][A256848][L44918]
Pharmacodynamics
The exposure-response relationships and pharmacodynamics time course of elacestrant have not been fully characterized. At the approved recommended dose, the use of elacestrant does not lead to QTc interval increases higher than 20 msec. Hypercholesterolemia and hypertriglyceridemia have occurred in patients taking elacestrant, and administering this drug to pregnant women may cause fetal harm.[L44918] Unlike other selective estrogen receptor modulators and degraders, elacestrant is capable of crossing the blood-brain barrier.[A256863]
Pharmacokinetics
How the body processes this drug — absorption, distribution, metabolism, and elimination
Absorption
With the recommended dosage of 345 mg once daily, elacestrant has a steady-state Cmax of 119 ng/mL and an AUC0-24h of 2440 ng⋅h/mL. The Cmax and AUC of elacestrant increase more than dose-proportional between 43 mg and 862 mg once daily (0.125 to 2.5 times the approved recommended dosage). By day 6, elacestrant reaches steady-state and has a 2-fold mean accumulation ratio based on AUC0-24h.
The tmax of elacestrant goes from 1 to 4 hr, and its oral bioavailability is approximately 10%. Compared to a fasted state, the Cmax and AUC of elacestrant (345 mg) were 42% and 22% higher, respectively, when administered with a high-fat meal (800 to 1000 calories, 50% fat).
[L44918]
The tmax of elacestrant goes from 1 to 4 hr, and its oral bioavailability is approximately 10%. Compared to a fasted state, the Cmax and AUC of elacestrant (345 mg) were 42% and 22% higher, respectively, when administered with a high-fat meal (800 to 1000 calories, 50% fat).
[L44918]
Half-life
The elimination half-life of elacestrant is 30 to 50 hours.
[L44918]
[L44918]
Protein binding
Elacestrant has a protein plasma binding higher than 99% and independent of concentration.
[L44918]
[L44918]
Volume of distribution
Elacestrant has an apparent volume of distribution of 5800 L.
[L44918]
[L44918]
Metabolism
Elacestrant is metabolized in the liver, mainly by CYP3A4 and, to a lesser extent, by CYP2A6 and CYP2C9.
[L44918]
[L44918]
Route of elimination
Elacestrant is mainly eliminated through feces and urine. Approximately 82% was recovered in feces (34% unchanged), and 7.5% was recovered in urine (< 1% unchanged) following a single radiolabeled oral dose of 345 mg.
[L44918]
[L44918]
Clearance
Elacestrant has an estimated clearance of 186 L/hr and a renal clearance of ≤ 0.14 L/hr.
[L44918]
[L44918]
Drug targets(1)
Proteins and enzymes this drug interacts with in the body
Estrogen receptor
ESR1
antagonist
Specific function14-3-3 protein binding
Cellular location
Nucleus
General function & pharmacology
Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription factors, such as AP-1/c-Jun, c-Fos, ATF-2, Sp1 and Sp3, to mediate ERE-independent signaling.
Ligand binding induces a conformational change allowing subsequent or combinatorial association with multiprotein coactivator complexes through LXXLL motifs of their respective components. Mutual transrepression occurs between the estrogen receptor (ER) and NF-kappa-B in a cell-type specific manner. Decreases NF-kappa-B DNA-binding activity and inhibits NF-kappa-B-mediated transcription from the IL6 promoter and displace RELA/p65 and associated coregulators from the promoter.
Recruited to the NF-kappa-B response element of the CCL2 and IL8 promoters and can displace CREBBP. Present with NF-kappa-B components RELA/p65 and NFKB1/p50 on ERE sequences. Can also act synergistically with NF-kappa-B to activate transcription involving respective recruitment adjacent response elements; the function involves CREBBP.
Can activate the transcriptional activity of TFF1. Also mediates membrane-initiated estrogen signaling involving various kinase cascades. Essential for MTA1-mediated transcriptional regulation of BRCA1 and BCAS3 .
PMID:17922032
Maintains neuronal survival in response to ischemic reperfusion injury when in the presence of circulating estradiol (17-beta-estradiol/E2) (By similarity)
Ligand binding induces a conformational change allowing subsequent or combinatorial association with multiprotein coactivator complexes through LXXLL motifs of their respective components. Mutual transrepression occurs between the estrogen receptor (ER) and NF-kappa-B in a cell-type specific manner. Decreases NF-kappa-B DNA-binding activity and inhibits NF-kappa-B-mediated transcription from the IL6 promoter and displace RELA/p65 and associated coregulators from the promoter.
Recruited to the NF-kappa-B response element of the CCL2 and IL8 promoters and can displace CREBBP. Present with NF-kappa-B components RELA/p65 and NFKB1/p50 on ERE sequences. Can also act synergistically with NF-kappa-B to activate transcription involving respective recruitment adjacent response elements; the function involves CREBBP.
Can activate the transcriptional activity of TFF1. Also mediates membrane-initiated estrogen signaling involving various kinase cascades. Essential for MTA1-mediated transcriptional regulation of BRCA1 and BCAS3 .
PMID:17922032
Maintains neuronal survival in response to ischemic reperfusion injury when in the presence of circulating estradiol (17-beta-estradiol/E2) (By similarity)
Metabolizing enzymes(3)
Enzymes involved in drug metabolism — important for understanding drug interactions
Enzyme activity key
substrate
inhibitor
inducer
CYP3A4Cytochrome P450 3A4
substrate
CYP2A6Cytochrome P450 2A6
substrate
CYP2C9Cytochrome P450 2C9
substrate
Transporters(3)
Proteins that transport this drug across cell membranes
Solute carrier organic anion transporter family member 2B1
SLCO2B1
substrate
Specific functionbile acid transmembrane transporter activity
Cellular location
Cell membrane
General function & pharmacology
Mediates the Na(+)-independent transport of steroid sulfate conjugates and other specific organic anions .
PMID:10873595 PMID:11159893 PMID:11932330 PMID:12724351 PMID:14610227 PMID:16908597 PMID:18501590 PMID:20507927 PMID:22201122 PMID:23531488 PMID:25132355 PMID:26383540 PMID:27576593 PMID:28408210 PMID:29871943 PMID:34628357
Responsible for the transport of estrone 3-sulfate (E1S) through the basal membrane of syncytiotrophoblast, highlighting a potential role in the placental absorption of fetal-derived sulfated steroids including the steroid hormone precursor dehydroepiandrosterone sulfate (DHEA-S) .
PMID:11932330 PMID:12409283
Also facilitates the uptake of sulfated steroids at the basal/sinusoidal membrane of hepatocytes, therefore accounting for the major part of organic anions clearance of liver .
PMID:11159893
Mediates the intestinal uptake of sulfated steroids .
PMID:12724351 PMID:28408210
Mediates the uptake of the neurosteroids DHEA-S and pregnenolone sulfate (PregS) into the endothelial cells of the blood-brain barrier as the first step to enter the brain .
PMID:16908597 PMID:25132355
Also plays a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons .
PMID:25132355
May act as a heme transporter that promotes cellular iron availability via heme oxygenase/HMOX2 and independently of TFRC .
PMID:35714613
Also transports heme by-product coproporphyrin III (CPIII), and may be involved in their hepatic disposition .
PMID:26383540
Mediates the uptake of other substrates such as prostaglandins D2 (PGD2), E1 (PGE1) and E2 (PGE2), taurocholate, L-thyroxine, leukotriene C4 and thromboxane B2 (PubMed:10873595, PubMed:14610227, PubMed:19129463, PubMed:29871943, Ref.25). May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable). Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:14610227 PMID:19129463 PMID:22201122
The exact transport mechanism has not been yet deciphered but most likely involves an anion exchange, coupling the cellular uptake of organic substrate with the efflux of an anionic compound .
PMID:19129463 PMID:20507927 PMID:26277985
Hydrogencarbonate/HCO3(-) acts as a probable counteranion that exchanges for organic anions .
PMID:19129463
Cytoplasmic glutamate may also act as counteranion in the placenta .
PMID:26277985
An inwardly directed proton gradient has also been proposed as the driving force of E1S uptake with a (H(+):E1S) stoichiometry of (1:1) PMID:20507927
PMID:10873595 PMID:11159893 PMID:11932330 PMID:12724351 PMID:14610227 PMID:16908597 PMID:18501590 PMID:20507927 PMID:22201122 PMID:23531488 PMID:25132355 PMID:26383540 PMID:27576593 PMID:28408210 PMID:29871943 PMID:34628357
Responsible for the transport of estrone 3-sulfate (E1S) through the basal membrane of syncytiotrophoblast, highlighting a potential role in the placental absorption of fetal-derived sulfated steroids including the steroid hormone precursor dehydroepiandrosterone sulfate (DHEA-S) .
PMID:11932330 PMID:12409283
Also facilitates the uptake of sulfated steroids at the basal/sinusoidal membrane of hepatocytes, therefore accounting for the major part of organic anions clearance of liver .
PMID:11159893
Mediates the intestinal uptake of sulfated steroids .
PMID:12724351 PMID:28408210
Mediates the uptake of the neurosteroids DHEA-S and pregnenolone sulfate (PregS) into the endothelial cells of the blood-brain barrier as the first step to enter the brain .
PMID:16908597 PMID:25132355
Also plays a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons .
PMID:25132355
May act as a heme transporter that promotes cellular iron availability via heme oxygenase/HMOX2 and independently of TFRC .
PMID:35714613
Also transports heme by-product coproporphyrin III (CPIII), and may be involved in their hepatic disposition .
PMID:26383540
Mediates the uptake of other substrates such as prostaglandins D2 (PGD2), E1 (PGE1) and E2 (PGE2), taurocholate, L-thyroxine, leukotriene C4 and thromboxane B2 (PubMed:10873595, PubMed:14610227, PubMed:19129463, PubMed:29871943, Ref.25). May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable). Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:14610227 PMID:19129463 PMID:22201122
The exact transport mechanism has not been yet deciphered but most likely involves an anion exchange, coupling the cellular uptake of organic substrate with the efflux of an anionic compound .
PMID:19129463 PMID:20507927 PMID:26277985
Hydrogencarbonate/HCO3(-) acts as a probable counteranion that exchanges for organic anions .
PMID:19129463
Cytoplasmic glutamate may also act as counteranion in the placenta .
PMID:26277985
An inwardly directed proton gradient has also been proposed as the driving force of E1S uptake with a (H(+):E1S) stoichiometry of (1:1) PMID:20507927
ATP-dependent translocase ABCB1
ABCB1
inhibitor
Specific functionABC-type xenobiotic transporter activity
Cellular location
Cell membrane
General function & pharmacology
Translocates drugs and phospholipids across the membrane .
PMID:2897240 PMID:35970996 PMID:8898203 PMID:9038218 PMID:35507548
Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins .
PMID:8898203
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells PMID:2897240 PMID:35970996 PMID:9038218
PMID:2897240 PMID:35970996 PMID:8898203 PMID:9038218 PMID:35507548
Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins .
PMID:8898203
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells PMID:2897240 PMID:35970996 PMID:9038218
Broad substrate specificity ATP-binding cassette transporter ABCG2
ABCG2
inhibitor
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
Scientific references(7)
Lloyd M.R., Wander S.A., Hamilton E., Razavi P., Bardia A.
Next-generation selective estrogen receptor degraders and other novel endocrine therapies for management of metastatic hormone receptor-positive breast cancer: current and emerging role.
Therapeutics Advanced Medicine Oncology
2022 Jul 3014:17588359221113694. doi: 10.1177/17588359221113694. eCollection 2022
Garner F., Shomali M., Paquin D., Lyttle C.R., Hattersley G.
RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models.
Anticancer Drugs
2015 Oct26(9):948-56. doi: 10.1097/CAD.0000000000000271
Bihani T., Patel H.K., Arlt H., Tao N., Jiang H., Brown J.L., Purandare D.M., Hattersley G., Garner F.
Elacestrant (RAD1901), a Selective Estrogen Receptor Degrader (SERD), Has Antitumor Activity in Multiple ER(+) Breast Cancer Patient-derived Xenograft Models.
Clinical Cancer Research
2017 Aug 1523(16):4793-4804. doi: 10.1158/1078-0432.CCR-16-2561. Epub 2017 May 4
Patel H.K., Tao N., Lee K.M., Huerta M., Arlt H., Mullarkey T., Troy S., Arteaga C.L., Bihani T.
Elacestrant (RAD1901) exhibits anti-tumor activity in multiple ER+ breast cancer models resistant to CDK4/6 inhibitors.
Breast Cancer Research
2019 Dec 1821(1):146. doi: 10.1186/s13058-019-1230-0
Bidard F.C., Kaklamani V.G., Neven P., Streich G., Montero A.J., Forget F., Mouret-Reynier M.A., Sohn J.H., Taylor D., Harnden K.K., Khong H., Kocsis J., Dalenc F., Dillon P.M., Babu S., Waters S., Deleu I., Garcia Saenz J.A., Bria E., Cazzaniga M., Lu J., Aftimos P., Cortes J., Liu S., Tonini G., Laurent D., Habboubi N., Conlan M.G., Bardia A.
Elacestrant (oral selective estrogen receptor degrader) Versus Standard Endocrine Therapy for Estrogen Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Advanced Breast Cancer: Results From the Randomized Phase III EMERALD Trial.
Journal of Clinical Oncology
2022 Oct 140(28):3246-3256. doi: 10.1200/JCO.22.00338. Epub 2022 May 18
Chinnasamy K., Saravanan M., Poomani K.
Investigation of binding mechanism and downregulation of elacestrant for wild and L536S mutant estrogen receptor-alpha through molecular dynamics simulation and binding free energy analysis.
Journal Computational Chemistry
2020 Jan 1541(2):97-109. doi: 10.1002/jcc.26076. Epub 2019 Oct 10
Lu Y., Liu W.
Selective Estrogen Receptor Degraders (SERDs): A Promising Strategy for Estrogen Receptor Positive Endocrine-Resistant Breast Cancer.
Journal of Medicinal Chemistry
2020 Dec 2463(24):15094-15114. doi: 10.1021/acs.jmedchem.0c00913. Epub 2020 Nov 2
ATC classification(1 code)
ATC L02BA04
Affected organisms(1)
Humans and other mammals
International brands(1)
Protein Data Bank entries(1)
Commercial products(4)
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)
Elacestrant
Additional database identifiers
ChemSpider
57583807
BindingDB
349630
PDB
I0V
HUGO Gene Nomenclature Committee (HGNC)
HGNC:3467
GenAtlas
ESR1
GeneCards
ESR1
GenBank Gene Database
X03635
GenBank Protein Database
31234
Guide to Pharmacology
620
UniProt Accession
ESR1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2637
GenAtlas
CYP3A4
GeneCards
CYP3A4
GenBank Gene Database
M18907
Guide to Pharmacology
1337
UniProt Accession
CP3A4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2610
GenAtlas
CYP2A6
GeneCards
CYP2A6
GenBank Gene Database
X13897
Guide to Pharmacology
1321
UniProt Accession
CP2A6_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2623
GenAtlas
CYP2C9
GeneCards
CYP2C9
GenBank Gene Database
AY341248
Guide to Pharmacology
1326
UniProt Accession
CP2C9_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10962
GenAtlas
SLCO2B1
GeneCards
SLCO2B1
GenBank Gene Database
AB026256
GenBank Protein Database
5006263
Guide to Pharmacology
1224
UniProt Accession
SO2B1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:40
GenAtlas
ABCB1
GeneCards
ABCB1
GenBank Gene Database
M14758
GenBank Protein Database
307180
Guide to Pharmacology
768
UniProt Accession
MDR1_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
Patent information
7 active patents, 1 expired
10745343
United States
Approved 18 Aug 2020 · Expires 5 Jan 2038
11y 9m
10385008
United States
Approved 20 Aug 2019 · Expires 5 Jan 2038
11y 9m
11819480
United States
Approved 21 Nov 2023 · Expires 29 Nov 2036
10y 8m
10071066
United States
Approved 11 Sept 2018 · Expires 10 Oct 2034
8y 6m
10420734
United States
Approved 24 Sept 2019 · Expires 10 Oct 2034
8y 6m
The earliest active patent expires August 2026. Generic versions may become available after this date.
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 about 1 month ago(4 Mar 2026)