Resmetirom 60mg tablets
Prescription only
Requires a prescription from a doctor or prescriber
Tablet
60mg
Oral
Resmetirom is a thyroid hormone receptor-beta (THR-beta) agonist.
Active ingredients:
Resmetirom
No active safety alerts
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Safety monitoring data
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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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EudraVigilance data is published by the European Medicines Agency (EMA). A suspected adverse reaction is not necessarily caused by the medicine.
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1 products
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View all licensed products for Resmetirom on the MHRA register
Possibly available on the UK market
Rezdiffra 60mg tablets
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Similarity is based on WHO Anatomical Therapeutic Chemical (ATC) classification and on a factual NHS dm+d therapeutic-grouping code prefix. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
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Codes for healthcare professionals and prescribing systems
These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
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SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
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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
4.5 hours
Mechanism
Thyroid hormones, such as FT4 and free triiodothyronine (FT3), are key regulators of lipid metabolism in the liver.
Food interactions
1 warning
Human targets
1 target
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
80 mg
The median Tmax is approximately four hours following multiple daily doses of resmetirom 80 mg or 100 mg.
[L50331]
Concomitant…
[L50331]
Concomitant…
Half-life
4.5 hours
The median terminal plasma half-life is 4.5 hours.
[L50331]
[L50331]
Protein binding
99%
Resmetirom is greater than 99% protein-bound.
[L50331]
[L50331]
Volume of distribution
227%
Resmetirom apparent volume of distribution (Vd/F) at steady-state is 68 (227%) L.
[L50331]
[L50331]
Metabolism
8. MG
Resmetirom is metabolized by CYP2C8. MGL-3623 is a major metabolite with a 28-times lower potency for THR-β than resmetirom.…
Elimination
100 mg
Following oral administration of a 100 mg radio-labeled dose of resmetirom, approximately 67% of the total radioactive dose was recovered in…
Clearance
56.3%
The steady state apparent clearance (CL/F) is 17.5 (56.3%) L/h.
[L50331]
[L50331]
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Status:
Approved
Investigational
Small molecule
About this compound
Resmetirom is a thyroid hormone receptor-beta (THR-beta) agonist. On March 14, 2024, it was approved by the FDA as the first treatment of liver fibrosis due to noncirrhotic non-alcoholic steatohepatitis (NASH), which is a form of non-alcoholic fatty liver disease (NAFLD).[L50336]
Thyroid hormones directly regulate lipid metabolism in the liver; thus, impaired thyroid function, such as low serum thyroid hormone levels, is often observed in NAFLD.[A263461] Resmetirom works to reduce liver fat by stimulating fatty acid degradation and oxidation.[L50336]
Thyroid hormones directly regulate lipid metabolism in the liver; thus, impaired thyroid function, such as low serum thyroid hormone levels, is often observed in NAFLD.[A263461] Resmetirom works to reduce liver fat by stimulating fatty acid degradation and oxidation.[L50336]
Properties:
solid
Avg. mass: 435.22 Da
DrugBank indication
Resmetirom is indicated in conjunction with diet and exercise for the treatment of adults with noncirrhotic nonalcoholic steatohepatitis (NASH) with moderate to advanced liver fibrosis (consistent with stages F2 to F3 fibrosis). Its use should be avoided in patients with decompensated cirrhosis.
[L50331]
This indication is approved under accelerated approval based on the improvement of NASH and fibrosis. Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trials.
[L50331]
[L50331]
This indication is approved under accelerated approval based on the improvement of NASH and fibrosis. Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trials.
[L50331]
Also known as(84)
1,2,4-Triazine-6-carbonitrile, 2-[3,5-dichloro-4-[[1,6-dihydro-5-(1-methylethyl)-6-oxo-3-pyridazinyl]oxy]phenyl]-2,3,4,5-tetrahydro-3,5-dioxo-
2-[3,5-Dichloro-4-[[1,6-dihydro-5-(1-methylethyl)-6-oxo-3-pyridazinyl]oxy]phenyl]-2,3,4,5-tetrahydro-3,5-dioxo-1,2,4-triazine-6-carbonitrile
Resmetirom
c-erbA-2
c-erbA-beta
ERBA2
NR1A2
Nuclear receptor subfamily 1 group A member 2
Molecular properties(19)
Drug interactions(317)
Known interactions with other medicines. Always consult a healthcare professional.
Mifepristone
Moderate
The serum concentration of Resmetirom can be increased when it is combined with Mifepristone.
The metabolism of Phenytoin can be decreased when combined with Resmetirom.
Secobarbital
Moderate
The metabolism of Resmetirom can be increased when combined with Secobarbital.
The metabolism of Resmetirom can be increased when combined with Rifampin.
Troglitazone
Moderate
The serum concentration of Resmetirom can be increased when it is combined with Troglitazone.
Bexarotene
Moderate
The metabolism of Resmetirom can be decreased when combined with Bexarotene.
The metabolism of Resmetirom can be decreased when combined with Diltiazem.
Trimethoprim
Moderate
The metabolism of Resmetirom can be decreased when combined with Trimethoprim.
Levothyroxine
Moderate
The metabolism of Resmetirom can be decreased when combined with Levothyroxine.
Loratadine
Moderate
The metabolism of Resmetirom can be decreased when combined with Loratadine.
The serum concentration of Resmetirom can be increased when it is combined with Quinine.
The metabolism of Resmetirom can be decreased when combined with Ritonavir.
The metabolism of Resmetirom can be decreased when combined with Medroxyprogesterone acetate.
Nicardipine
Moderate
The serum concentration of Resmetirom can be increased when it is combined with Nicardipine.
The metabolism of Resmetirom can be decreased when combined with Efavirenz.
The metabolism of Resmetirom can be decreased when combined with Tamoxifen.
Ketoconazole
Moderate
The serum concentration of Resmetirom can be increased when it is combined with Ketoconazole.
Irbesartan
Moderate
The metabolism of Resmetirom can be decreased when combined with Irbesartan.
Oxybutynin
Moderate
The metabolism of Resmetirom can be decreased when combined with Oxybutynin.
Fluvastatin
Moderate
The serum concentration of Resmetirom can be increased when it is combined with Fluvastatin.
Pioglitazone
Moderate
The metabolism of Resmetirom can be decreased when combined with Pioglitazone.
Saquinavir
Moderate
The serum concentration of Resmetirom can be increased when it is combined with Saquinavir.
The serum concentration of Resmetirom can be increased when it is combined with Genistein.
Topiroxostat
Moderate
The metabolism of Resmetirom can be decreased when combined with Topiroxostat.
Abiraterone
Moderate
The metabolism of Resmetirom can be decreased when combined with Abiraterone.
Eltrombopag
Moderate
The serum concentration of Resmetirom can be increased when it is combined with Eltrombopag.
Teriflunomide
Moderate
The serum concentration of Resmetirom can be increased when it is combined with Teriflunomide.
Enzalutamide
Moderate
The metabolism of Resmetirom can be decreased when combined with Enzalutamide.
Pirtobrutinib
Moderate
The metabolism of Resmetirom can be decreased when combined with Pirtobrutinib.
The metabolism of Resmetirom can be decreased when combined with Erlotinib.
Fluticasone propionate
Moderate
The metabolism of Resmetirom can be decreased when combined with Fluticasone propionate.
Clopidogrel
Moderate
The metabolism of Resmetirom can be decreased when combined with Clopidogrel.
Candesartan cilexetil
Moderate
The metabolism of Resmetirom can be decreased when combined with Candesartan cilexetil.
Salmeterol
Moderate
The metabolism of Resmetirom can be decreased when combined with Salmeterol.
Felodipine
Moderate
The metabolism of Resmetirom can be decreased when combined with Felodipine.
Gemfibrozil
Moderate
The metabolism of Resmetirom can be decreased when combined with Gemfibrozil.
Dabrafenib
Moderate
The metabolism of Resmetirom can be decreased when combined with Dabrafenib.
Fluticasone
Moderate
The metabolism of Resmetirom can be decreased when combined with Fluticasone.
Mometasone furoate
Moderate
The metabolism of Resmetirom can be decreased when combined with Mometasone furoate.
Cholic Acid
Moderate
The serum concentration of Resmetirom can be increased when it is combined with Cholic Acid.
Taurocholic acid
Moderate
The serum concentration of Resmetirom can be increased when it is combined with Taurocholic acid.
Apalutamide
Moderate
The serum concentration of Resmetirom can be decreased when it is combined with Apalutamide.
Cyclosporine
Moderate
The serum concentration of Resmetirom can be increased when it is combined with Cyclosporine.
The serum concentration of Resmetirom can be increased when it is combined with Valsartan.
Erythromycin
Moderate
The serum concentration of Resmetirom can be increased when it is combined with Erythromycin.
Sildenafil
Moderate
The serum concentration of Resmetirom can be increased when it is combined with Sildenafil.
The serum concentration of Resmetirom can be increased when it is combined with Reserpine.
Pantoprazole
Moderate
The serum concentration of Resmetirom can be increased when it is combined with Pantoprazole.
Nelfinavir
Moderate
The serum concentration of Resmetirom can be increased when it is combined with Nelfinavir.
The serum concentration of Resmetirom can be increased when it is combined with Indinavir.
Showing 50 of 317 interactions
Food & lifestyle interactions
Advice
Take with or without food. A high fat meal may reduce Cmax and AUC delay Tmax, but not to a clinically significant extent.
Toxicity & overdose
There is no information regarding the acute toxicity and overdosage of resmetirom.
How it works
Mechanism of action
Thyroid hormones, such as FT4 and free triiodothyronine (FT3), are key regulators of lipid metabolism in the liver.[A263451] Thyroid hormone receptor-beta (THR-β) is the major form of the thyroid hormone receptor in the liver,[A263456] and stimulation of this receptor reduces intrahepatic triglycerides.[L50331]
Many patients with non-alcoholic fatty liver disease (NAFLD) present with impaired thyroid function, such as hypothyroidism, rendering it a significant risk factor for NAFLD.[A263451][A263456][A263461] Hypothyroidism has also been linked to dysregulated adipose tissue lipolysis and increased free fatty acid release from the adipose to the liver, promoting hepatic insulin resistance.[A263451] Increased circulating levels of proinflammatory adipokines, which contribute to hepatic inflammation and fibrosis, may also be observed.[A263451]
Resmetirom is a partial agonist of THR-β [L50331] that promotes lipophagy and hepatic fatty acid β-oxidation, thereby reducing liver fat.[A263461] It is approximately 28 times more selective than FT3 for THR-β versus thyroid hormone receptor-alpha (THR-α), which is mainly expressed in the heart and bones.[A263471]
Many patients with non-alcoholic fatty liver disease (NAFLD) present with impaired thyroid function, such as hypothyroidism, rendering it a significant risk factor for NAFLD.[A263451][A263456][A263461] Hypothyroidism has also been linked to dysregulated adipose tissue lipolysis and increased free fatty acid release from the adipose to the liver, promoting hepatic insulin resistance.[A263451] Increased circulating levels of proinflammatory adipokines, which contribute to hepatic inflammation and fibrosis, may also be observed.[A263451]
Resmetirom is a partial agonist of THR-β [L50331] that promotes lipophagy and hepatic fatty acid β-oxidation, thereby reducing liver fat.[A263461] It is approximately 28 times more selective than FT3 for THR-β versus thyroid hormone receptor-alpha (THR-α), which is mainly expressed in the heart and bones.[A263471]
Pharmacodynamics
Resmetirom is a partial agonist of the thyroid hormone receptor-beta (THR-β). Resmetirom produced 83.8% of the maximum response compared to triiodothyronine (T3), with an EC50 of 0.21 µM in an in vitro functional assay for THR-β activation. The same functional assay for thyroid hormone receptor-alpha (THR-α) agonism showed 48.6% efficacy for resmetirom relative to T3, with an EC50 of 3.74 µM.[L50331]
Resmetirom decreases liver fat content and the concentrations of free thyroxine (FT4), which is a prohormone.[L50331] Although it is inconclusive, there have been some reports in the literature suggesting that resmetirom may convert thyroxine (T4) to triiodothyronine (T3).[A263461] It increases the concentrations of sex hormone-binding globulin.[L50331]
Resmetirom decreases liver fat content and the concentrations of free thyroxine (FT4), which is a prohormone.[L50331] Although it is inconclusive, there have been some reports in the literature suggesting that resmetirom may convert thyroxine (T4) to triiodothyronine (T3).[A263461] It increases the concentrations of sex hormone-binding globulin.[L50331]
Pharmacokinetics
How the body processes this drug — absorption, distribution, metabolism, and elimination
Absorption
The median Tmax is approximately four hours following multiple daily doses of resmetirom 80 mg or 100 mg.
[L50331]
Concomitant food administration resulted in a 33% decrease in Cmax, an 11% decrease in AUC, and a delay in median Tmax by about two hours compared to an under-fasted condition.
[L50331]
[L50331]
Concomitant food administration resulted in a 33% decrease in Cmax, an 11% decrease in AUC, and a delay in median Tmax by about two hours compared to an under-fasted condition.
[L50331]
Half-life
The median terminal plasma half-life is 4.5 hours.
[L50331]
[L50331]
Protein binding
Resmetirom is greater than 99% protein-bound.
[L50331]
[L50331]
Volume of distribution
Resmetirom apparent volume of distribution (Vd/F) at steady-state is 68 (227%) L.
[L50331]
[L50331]
Metabolism
Resmetirom is metabolized by CYP2C8. MGL-3623 is a major metabolite with a 28-times lower potency for THR-β than resmetirom. MGL-3623 represents 33% to 51% of resmetirom AUC at steady-state following administration of 100 mg once daily.
[L50331]
[L50331]
Route of elimination
Following oral administration of a 100 mg radio-labeled dose of resmetirom, approximately 67% of the total radioactive dose was recovered in the feces, mostly as metabolites and 24% of the total radioactive dose was recovered in the urine. Unchanged labeled resmetirom was not detected in feces and accounted for 1% of the dose recovered in urine. A metabolite MGL-3623 accounted for 3.3% and 16% of the dose recovered in feces and urine, respectively.
Oxalic acid metabolite was observed in plasma but not in urine.
[L50331]
Oxalic acid metabolite was observed in plasma but not in urine.
[L50331]
Clearance
The steady state apparent clearance (CL/F) is 17.5 (56.3%) L/h.
[L50331]
[L50331]
Drug targets(1)
Proteins and enzymes this drug interacts with in the body
Thyroid hormone receptor beta
THRB
partial agonist
Specific functionchromatin DNA binding
Cellular location
Nucleus
General function & pharmacology
Nuclear hormone receptor that can act as a repressor or activator of transcription. High affinity receptor for thyroid hormones, including triiodothyronine and thyroxine
Metabolizing enzymes(3)
Enzymes involved in drug metabolism — important for understanding drug interactions
Enzyme activity key
substrate
inhibitor
inducer
CYP2C8Cytochrome P450 2C8
substrate
inhibitor
UGT1A4UDP-glucuronosyltransferase 1A4
inhibitor
UGT1A9UDP-glucuronosyltransferase 1A9
inhibitor
Transporters(5)
Proteins that transport this drug across cell membranes
Solute carrier organic anion transporter family member 1B1
SLCO1B1
substrate
inhibitor
Specific functionbile acid transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Mediates the Na(+)-independent uptake of organic anions .
PMID:10358072 PMID:15159445 PMID:17412826
Shows broad substrate specificity, can transport both organic anions such as bile acid taurocholate (cholyltaurine) and conjugated steroids (dehydroepiandrosterone 3-sulfate, 17-beta-glucuronosyl estradiol, and estrone 3-sulfate), as well as eicosanoids (prostaglandin E2, thromboxane B2, leukotriene C4, and leukotriene E4), and thyroid hormones (T4/L-thyroxine, and T3/3,3',5'-triiodo-L-thyronine) .
PMID:10358072 PMID:10601278 PMID:10873595 PMID:11159893 PMID:12196548 PMID:12568656 PMID:15159445 PMID:15970799 PMID:16627748 PMID:17412826 PMID:19129463 PMID:26979622
Can take up bilirubin glucuronides from plasma into the liver, contributing to the detoxification-enhancing liver-blood shuttling loop .
PMID:22232210
Involved in the clearance of endogenous and exogenous substrates from the liver .
PMID:10358072 PMID:10601278
Transports coproporphyrin I and III, by-products of heme synthesis, and may be involved in their hepatic disposition .
PMID:26383540
May contribute to regulate the transport of organic compounds in testes across the blood-testis-barrier (Probable). Can transport HMG-CoA reductase inhibitors (also known as statins), such as pravastatin and pitavastatin, a clinically important class of hypolipidemic drugs .
PMID:10601278 PMID:15159445 PMID:15970799
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drug methotrexate .
PMID:23243220
May also transport antihypertension agents, such as the angiotensin-converting enzyme (ACE) inhibitor prodrug enalapril, and the highly selective angiotensin II AT1-receptor antagonist valsartan, in the liver .
PMID:16624871 PMID:16627748
Shows a pH-sensitive substrate specificity towards prostaglandin E2 and T4 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:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions PMID:19129463
PMID:10358072 PMID:15159445 PMID:17412826
Shows broad substrate specificity, can transport both organic anions such as bile acid taurocholate (cholyltaurine) and conjugated steroids (dehydroepiandrosterone 3-sulfate, 17-beta-glucuronosyl estradiol, and estrone 3-sulfate), as well as eicosanoids (prostaglandin E2, thromboxane B2, leukotriene C4, and leukotriene E4), and thyroid hormones (T4/L-thyroxine, and T3/3,3',5'-triiodo-L-thyronine) .
PMID:10358072 PMID:10601278 PMID:10873595 PMID:11159893 PMID:12196548 PMID:12568656 PMID:15159445 PMID:15970799 PMID:16627748 PMID:17412826 PMID:19129463 PMID:26979622
Can take up bilirubin glucuronides from plasma into the liver, contributing to the detoxification-enhancing liver-blood shuttling loop .
PMID:22232210
Involved in the clearance of endogenous and exogenous substrates from the liver .
PMID:10358072 PMID:10601278
Transports coproporphyrin I and III, by-products of heme synthesis, and may be involved in their hepatic disposition .
PMID:26383540
May contribute to regulate the transport of organic compounds in testes across the blood-testis-barrier (Probable). Can transport HMG-CoA reductase inhibitors (also known as statins), such as pravastatin and pitavastatin, a clinically important class of hypolipidemic drugs .
PMID:10601278 PMID:15159445 PMID:15970799
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drug methotrexate .
PMID:23243220
May also transport antihypertension agents, such as the angiotensin-converting enzyme (ACE) inhibitor prodrug enalapril, and the highly selective angiotensin II AT1-receptor antagonist valsartan, in the liver .
PMID:16624871 PMID:16627748
Shows a pH-sensitive substrate specificity towards prostaglandin E2 and T4 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:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions PMID:19129463
Solute carrier organic anion transporter family member 1B3
SLCO1B3
substrate
inhibitor
Specific functionbile acid transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Mediates the Na(+)-independent uptake of organic anions .
PMID:10779507 PMID:15159445 PMID:17412826
Shows broad substrate specificity, can transport both organic anions such as bile acid taurocholate (cholyltaurine) and conjugated steroids (17-beta-glucuronosyl estradiol, dehydroepiandrosterone sulfate (DHEAS), and estrone 3-sulfate), as well as eicosanoid leukotriene C4, prostaglandin E2 and L-thyroxine (T4) .
PMID:10779507 PMID:11159893 PMID:12568656 PMID:15159445 PMID:17412826 PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions .
PMID:19129463
Shows a pH-sensitive substrate specificity towards sulfated steroids, taurocholate and T4 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:19129463
Involved in the clearance of bile acids and organic anions from the liver .
PMID:22232210
Can take up bilirubin glucuronides from plasma into the liver, contributing to the detoxification-enhancing liver-blood shuttling loop .
PMID:22232210
Transports coproporphyrin I and III, by-products of heme synthesis, and may be involved in their hepatic disposition .
PMID:26383540
May contribute to regulate the transport of organic compounds in testes across the blood-testis-barrier (Probable). Can transport HMG-CoA reductase inhibitors (also known as statins) such as pitavastatin, a clinically important class of hypolipidemic drugs .
PMID:15159445
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel .
PMID:23243220
May also transport antihypertension agents, such as the angiotensin-converting enzyme (ACE) inhibitor prodrug enalapril, and the highly selective angiotensin II AT1-receptor antagonist valsartan, in the liver PMID:16624871 PMID:16627748
PMID:10779507 PMID:15159445 PMID:17412826
Shows broad substrate specificity, can transport both organic anions such as bile acid taurocholate (cholyltaurine) and conjugated steroids (17-beta-glucuronosyl estradiol, dehydroepiandrosterone sulfate (DHEAS), and estrone 3-sulfate), as well as eicosanoid leukotriene C4, prostaglandin E2 and L-thyroxine (T4) .
PMID:10779507 PMID:11159893 PMID:12568656 PMID:15159445 PMID:17412826 PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions .
PMID:19129463
Shows a pH-sensitive substrate specificity towards sulfated steroids, taurocholate and T4 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:19129463
Involved in the clearance of bile acids and organic anions from the liver .
PMID:22232210
Can take up bilirubin glucuronides from plasma into the liver, contributing to the detoxification-enhancing liver-blood shuttling loop .
PMID:22232210
Transports coproporphyrin I and III, by-products of heme synthesis, and may be involved in their hepatic disposition .
PMID:26383540
May contribute to regulate the transport of organic compounds in testes across the blood-testis-barrier (Probable). Can transport HMG-CoA reductase inhibitors (also known as statins) such as pitavastatin, a clinically important class of hypolipidemic drugs .
PMID:15159445
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel .
PMID:23243220
May also transport antihypertension agents, such as the angiotensin-converting enzyme (ACE) inhibitor prodrug enalapril, and the highly selective angiotensin II AT1-receptor antagonist valsartan, in the liver PMID:16624871 PMID:16627748
Broad substrate specificity ATP-binding cassette transporter ABCG2
ABCG2
substrate
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
Organic anion transporter 3
SLC22A8
inhibitor
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)
Bile salt export pump
ABCB11
inhibitor
Specific functionABC-type bile acid transporter activity
Cellular location
Apical cell membrane
General function & pharmacology
Catalyzes the transport of the major hydrophobic bile salts, such as taurine and glycine-conjugated cholic acid across the canalicular membrane of hepatocytes in an ATP-dependent manner, therefore participates in hepatic bile acid homeostasis and consequently to lipid homeostasis through regulation of biliary lipid secretion in a bile salts dependent manner .
PMID:15791618 PMID:16332456 PMID:18985798 PMID:19228692 PMID:20010382 PMID:20398791 PMID:22262466 PMID:24711118 PMID:29507376 PMID:32203132
Transports taurine-conjugated bile salts more rapidly than glycine-conjugated bile salts .
PMID:16332456
Also transports non-bile acid compounds, such as pravastatin and fexofenadine in an ATP-dependent manner and may be involved in their biliary excretion PMID:15901796 PMID:18245269
PMID:15791618 PMID:16332456 PMID:18985798 PMID:19228692 PMID:20010382 PMID:20398791 PMID:22262466 PMID:24711118 PMID:29507376 PMID:32203132
Transports taurine-conjugated bile salts more rapidly than glycine-conjugated bile salts .
PMID:16332456
Also transports non-bile acid compounds, such as pravastatin and fexofenadine in an ATP-dependent manner and may be involved in their biliary excretion PMID:15901796 PMID:18245269
Scientific references(4)
Hatziagelaki E., Paschou S.A., Schon M., Psaltopoulou T., Roden M.
NAFLD and thyroid function: pathophysiological and therapeutic considerations.
Trends Endocrinol Metabolism
2022 Nov33(11):755-768. doi: 10.1016/j.tem.2022.08.001. Epub 2022 Sep 26
Li L., Song Y., Shi Y., Sun L.
Thyroid Hormone Receptor-beta Agonists in NAFLD Therapy: Possibilities and Challenges.
Journal Clinical Endocrinol Metabolism
2023 Jun 16108(7):1602-1613. doi: 10.1210/clinem/dgad072
Karim G., Bansal M.B.
Resmetirom: An Orally Administered, Smallmolecule, Liver-directed, beta-selective THR Agonist for the Treatment of Non-alcoholic Fatty Liver Disease and Non-alcoholic Steatohepatitis.
touchREV Endocrinol
2023 May19(1):60-70. doi: 10.17925/EE.2023.19.1.60. Epub 2023 May 1
Harrison S.A., Bashir M.R., Guy C.D., Zhou R., Moylan C.A., Frias J.P., Alkhouri N., Bansal M.B., Baum S., Neuschwander-Tetri B.A., Taub R., Moussa S.E.
Resmetirom (MGL-3196) for the treatment of non-alcoholic steatohepatitis: a multicentre, randomised, double-blind, placebo-controlled, phase 2 trial.
The Lancet
2019 Nov 30394(10213):2012-2024. doi: 10.1016/S0140-6736(19)32517-6. Epub 2019 Nov 11
Affected organisms(1)
Humans and other mammals
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)
Resmetirom
Additional database identifiers
ChemSpider
13112637
BindingDB
50012905
ZINC
ZINC000034842512
HUGO Gene Nomenclature Committee (HGNC)
HGNC:11799
GenAtlas
THRB
GeneCards
THRB
GenBank Gene Database
X04707
GenBank Protein Database
31207
Guide to Pharmacology
589
UniProt Accession
THB_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2622
GenAtlas
CYP2C8
GeneCards
CYP2C8
GenBank Gene Database
M17397
Guide to Pharmacology
1325
UniProt Accession
CP2C8_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:12536
GeneCards
UGT1A4
GenBank Gene Database
M57951
GenBank Protein Database
184475
UniProt Accession
UD14_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:12541
GeneCards
UGT1A9
GenBank Gene Database
S55985
GenBank Protein Database
7690346
UniProt Accession
UD19_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10959
GenAtlas
SLCO1B1
GeneCards
SLCO1B1
GenBank Gene Database
AF060500
GenBank Protein Database
5051630
Guide to Pharmacology
1220
UniProt Accession
SO1B1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10961
GeneCards
SLCO1B3
GenBank Gene Database
AJ251506
GenBank Protein Database
9187497
Guide to Pharmacology
1221
UniProt Accession
SO1B3_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: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:42
GenAtlas
ABCB11
GeneCards
ABCB11
GenBank Gene Database
AF091582
GenBank Protein Database
3873243
Guide to Pharmacology
778
UniProt Accession
ABCBB_HUMAN
DrugBank citations
If you use DrugBank data in your research, please cite:
- DrugBank 6.02024Recommended citationKnox C., Wilson M., Klinger C.M., et alDrugBank 6.0: the DrugBank Knowledgebase for 2024Nucleic Acids Res. 2024 Jan 552(D1):D1265-D1275
- DrugBank 5.02018Wishart D.S., Feunang Y.D., Guo A.C., et alDrugBank 5.0: a major update to the DrugBank database for 2018Nucleic Acids Res. 2017 Nov 846(D1):D1074-D1082
- DrugBank 4.02014Law V., Knox C., Djoumbou Y., et alDrugBank 4.0: shedding new light on drug metabolismNucleic Acids Res. 2014 Jan 142(1):D1091-7
- DrugBank 3.02011Knox C., Law V., Jewison T., et alDrugBank 3.0: a comprehensive resource for 'omics' research on drugsNucleic Acids Res. 2011 Jan39(Database issue):D1035-41
- DrugBank 2.02008Wishart D.S., Knox C., Guo A.C., et alDrugBank: a knowledgebase for drugs, drug actions and drug targets.Nucleic Acids Research2008 Jan36(Database issue):D901-6
- DrugBank 1.02006Wishart D.S., Knox C., Guo A.C., et alDrugBank: a comprehensive resource for in silico drug discovery and exploration.Nucleic Acids Research2006 Jan 134(Database issue):D668-72
Source: go.drugbank.comCC BY-NC 4.0
Updated 4 Mar 2026Structured knowledge from the free knowledge base
drugbank match (98%)
Linked open data from Wikidata (Q27288071), a free and open knowledge base operated by the Wikimedia Foundation. Data is available under the Creative Commons CC0 1.0 Public Domain Dedication.