Elbasvir (original) (raw)
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Description
A medication used to treat hepatitis C infections.
Description
A medication used to treat hepatitis C infections.
DrugBank ID
DB11574
Type
Small Molecule
US Approved
YES
Other Approved
YES
Therapeutic Categories
Mechanism of Action
Summary
Elbasvir is an antiviral and NS5A inhibitor used to treat hepatitis C infections.
Brand Names
Zepatier
Generic Name
Elbasvir
DrugBank Accession Number
DB11574
Background
Elbasvir is a direct-acting antiviral medication used as part of combination therapy to treat chronic hepatitis C, an infectious liver disease caused by infection with hepatitis C virus (HCV). HCV is a single-stranded RNA virus that is categorized into nine distinct genotypes, with genotype 1 being the most common in the United States, affecting 72% of all chronic HCV patients.6 Treatment options for chronic hepatitis C have advanced significantly since 2011, with the development of direct-acting antivirals (DAAs) such as elbasvir. Elbasvir is an inhibitor of NS5A, a protein essential for viral replication and virion assembly.Synthesis The barrier to the development of resistance to NS5A inhibitors is lower than that of NS5B inhibitors, another class of DAAs.3 Substitutions at amino acid positions 28, 30, 31, or 93 are known to confer resistance to elbasvir.7 Despite this disadvantage elbasvir is still effective against HCV, particularly when paired with grazoprevir.
Elbasvir is available as a fixed-dose combination product with grazoprevir (tradename: Zepatier) used for the treatment of chronic hepatitis C. Approved in January 2016 by the FDA, Zepatier is indicated for the treatment of HCV genotypes 1 and 4 with or without ribavirin depending on the presence of resistance-associated amino acid substitutions in the NS5A protein and previous treatment failure with ribavirin, peginterferon alfa-2a, peginterferon alfa-2b, or other NS3/4A inhibitors like boceprevir, simeprevir, or telaprevir.7 Elbasvir and grazoprevir are used with or without ribavirin with the intent to cure, or achieve a sustained virologic response (SVR), and have been shown to achieve a SVR between 94% and 97% for genotype 1 and 97% and 100% for genotype 4 after 12 weeks of treatment.6. SVR and eradication of HCV infection are associated with significant long-term health benefits including reduced liver-related damage, improved quality of life, reduced incidence of hepatocellular carcinoma, and reduced all-cause mortality.4
In a computational target-based drug repurposing investigation published in April 2020, elbasvir was predicted to bind stably and preferentially to three proteins necessary for viral replication of SARS-CoV-2, the human coronavirus responsible for the COVID-19 pandemic.5 While these results are suggestive of antiviral efficacy, follow-up clinical trials are required to validate elbasvir as a potential therapy against SARS-CoV-2.
Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 882.035
Monoisotopic: 881.422445147
Chemical Formula
C49H55N9O7
Synonyms
- Elbasvir
- MK 8742
- MK-8742
- MK8742
Indication
Elbasvir, when used in combination with grazoprevir as the combination product Zepatier, is indicated for use with or without ribavirin for the treatment of chronic HCV genotypes 1 or 4 infection in adults.7
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Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics
Elbasvir is classified as a direct-acting antiviral (DAA) and prevents viral replication in HCV genotypes 1a, 1b, and 4.7
Mechanism of action
Elbasvir is an inhibitor of the HCV non-structural protein 5A. While the precise role of this protein is unknown, it is essential to viral replication and virion assembly.Synthesis Potential modes of action of NS5A inhibitors like elbasvir include blocking signaling interactions, redistribution of NS5A from the endoplasmic reticulum to the surface of lipid droplets, and modification of the HCV replication complex.3
Computational target-based in silico research suggests that elbasvir may carry activity at several proteins required for replication of SARS-CoV-2 - namely RNA-dependent RNA polymerase, helicase, and papain-like proteinase - although specific activity has yet to be affirmed by follow-up clinical studies.5
| Target | Actions | Organism |
|---|---|---|
| ANonstructural protein 5A | inhibitor | Hepatitis C Virus |
Absorption
Elbasvir reaches peak plasma concentration 3-6 hours after administration7 and has an absolute bioavailability of 32%. When co-administered with food, the peak concentration of elbasvir increases 1.5-fold, but this increase in exposure is not likely to be clinically relevant.
Volume of distribution
Elbasvir has an estimated apparent volume of distribution of 680 liters.7 It is thought to distribute into most tissues including the liver.
Protein binding
Elbasvir is more than 99.9% bound to plasma proteins.7 It binds both human serum albumin and α1-acid glycoprotein.
Metabolism
Elbasvir is partially eliminated by oxidative metabolism meditated by CYP3A.7 No circulating metabolites of elbasvir have been detected in human plasma.
Route of elimination
Elbasvir is mainly eliminated in the feces (90%) with very little eliminated in the urine (<1%).7
Half-life
The geometric mean apparent terminal half-life for elbasvir is 24 hours in HCV-infected subjects.7
Clearance
The clearance of elbasvir has not been determined.7
Adverse Effects
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Toxicity
The most commonly reported adverse reactions of all intensity (greater than or equal to 5% in placebo-controlled trials) were fatigue, headache, and nausea.7
Pathways
Not Available
Not Available
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
| Drug | Interaction |
|---|---|
| Integrate drug-drug interactions in your software | |
| Abametapir | The serum concentration of Elbasvir can be increased when it is combined with Abametapir. |
| Abatacept | The metabolism of Elbasvir can be increased when combined with Abatacept. |
| Abemaciclib | Elbasvir may decrease the excretion rate of Abemaciclib which could result in a higher serum level. |
| Abrocitinib | The serum concentration of Elbasvir can be increased when it is combined with Abrocitinib. |
| Acalabrutinib | The metabolism of Elbasvir can be decreased when combined with Acalabrutinib. |
Food Interactions
- Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of elbasvir. Co-administration of Elbasvir with St. John's Wort is contraindicated.
- Exercise caution with grapefruit products. Grapefruit inhibits CYP3A, which may increase the serum levels of elbasvir, a CYP3A substrate.
- Take at the same time every day.
- Take with or without food.
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Mixture Products
ATC Codes
J05AP54 — Elbasvir and grazoprevir
- J05AP — Antivirals for treatment of HCV infections
- J05A — DIRECT ACTING ANTIVIRALS
- J05 — ANTIVIRALS FOR SYSTEMIC USE
- J — ANTIINFECTIVES FOR SYSTEMIC USE J05AP10 — Elbasvir
- J05AP — Antivirals for treatment of HCV infections
- J05A — DIRECT ACTING ANTIVIRALS
- J05 — ANTIVIRALS FOR SYSTEMIC USE
- J — ANTIINFECTIVES FOR SYSTEMIC USE
Drug Categories
- Antiinfectives for Systemic Use
- Antiviral Agents
- Antivirals for Systemic Use
- Antivirals for treatment of HCV infections
- BCRP/ABCG2 Inhibitors
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Inhibitors
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 CYP3A7 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Direct Acting Antivirals
- Experimental Unapproved Treatments for COVID-19
- Hepatitis C Virus NS5A Inhibitor
- Heterocyclic Compounds, Fused-Ring
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- Treatments for Hepatitis C
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as valine and derivatives. These are compounds containing valine or a derivative thereof resulting from reaction of valine at the amino group or the carboxy group, or from the replacement of any hydrogen of glycine by a heteroatom.
Kingdom
Super Class
Class
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
Alternative Parents
Alpha amino acid amides / Indoles / N-acylpyrrolidines / Benzene and substituted derivatives / Tertiary carboxylic acid amides / Pyrroles / Heteroaromatic compounds / Imidazoles / Methylcarbamates / Organic carbonic acids and derivatives / Oxacyclic compounds / Azacyclic compounds / Carbonyl compounds / Hydrocarbon derivatives / Organopnictogen compounds / Organic oxides / Organonitrogen compounds show 7 more
Substituents
Alpha-amino acid amide / Aromatic heteropolycyclic compound / Azacycle / Azole / Benzenoid / Carbamic acid ester / Carbonic acid derivative / Carbonyl group / Carboxamide group / Heteroaromatic compound / Hydrocarbon derivative / Imidazole / Indole / Indole or derivatives / Methylcarbamate / Monocyclic benzene moiety / N-acylpyrrolidine / Organic nitrogen compound / Organic oxide / Organic oxygen compound / Organoheterocyclic compound / Organonitrogen compound / Organooxygen compound / Organopnictogen compound / Oxacycle / Pyrrole / Pyrrolidine / Tertiary carboxylic acid amide / Valine or derivatives show 19 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available
Affected organisms
- Hepatitis C Virus
- SARS-CoV-2
UNII
CAS number
1370468-36-2
InChI Key
BVAZQCUMNICBAQ-PZHYSIFUSA-N
InChI
InChI=1S/C49H55N9O7/c1-27(2)41(54-48(61)63-5)45(59)56-20-10-14-37(56)43-50-25-34(52-43)30-17-19-36-32(22-30)23-39-33-18-16-31(24-40(33)65-47(58(36)39)29-12-8-7-9-13-29)35-26-51-44(53-35)38-15-11-21-57(38)46(60)42(28(3)4)55-49(62)64-6/h7-9,12-13,16-19,22-28,37-38,41-42,47H,10-11,14-15,20-21H2,1-6H3,(H,50,52)(H,51,53)(H,54,61)(H,55,62)/t37-,38-,41-,42-,47-/m0/s1
IUPAC Name
methyl N-[(2S)-1-[(2S)-2-{5-[(9S)-14-{2-[(2S)-1-[(2S)-2-[(methoxycarbonyl)amino]-3-methylbutanoyl]pyrrolidin-2-yl]-1H-imidazol-5-yl}-9-phenyl-8-oxa-10-azatetracyclo[8.7.0.0^{2,7}.0^{11,16}]heptadeca-1(17),2(7),3,5,11(16),12,14-heptaen-5-yl]-1H-imidazol-2-yl}pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]carbamate
SMILES
[H][C@]1(CCCN1C(=O)[C@@H](NC(=O)OC)C(C)C)C1=NC=C(N1)C1=CC2=C(C=C1)N1[C@@H](OC3=C(C=CC(=C3)C3=CN=C(N3)[C@]3([H])CCCN3C(=O)[C@@H](NC(=O)OC)C(C)C)C1=C2)C1=CC=CC=C1
Synthesis Reference
Coburn CA, Meinke PT, Chang W, Fandozzi CM, Graham DJ, Hu B, Huang Q, Kargman S, Kozlowski J, Liu R, McCauley JA, Nomeir AA, Soll RM, Vacca JP, Wang D, Wu H, Zhong B, Olsen DB, Ludmerer SW: Discovery of MK-8742: an HCV NS5A inhibitor with broad genotype activity. ChemMedChem. 2013 Dec;8(12):1930-40. doi: 10.1002/cmdc.201300343. Epub 2013 Oct 14.
General References
- Bell AM, Wagner JL, Barber KE, Stover KR: Elbasvir/Grazoprevir: A Review of the Latest Agent in the Fight against Hepatitis C. Int J Hepatol. 2016;2016:3852126. doi: 10.1155/2016/3852126. Epub 2016 Jun 15. [Article]
- Coburn CA, Meinke PT, Chang W, Fandozzi CM, Graham DJ, Hu B, Huang Q, Kargman S, Kozlowski J, Liu R, McCauley JA, Nomeir AA, Soll RM, Vacca JP, Wang D, Wu H, Zhong B, Olsen DB, Ludmerer SW: Discovery of MK-8742: an HCV NS5A inhibitor with broad genotype activity. ChemMedChem. 2013 Dec;8(12):1930-40. doi: 10.1002/cmdc.201300343. Epub 2013 Oct 14. [Article]
- Bagaglio S, Uberti-Foppa C, Morsica G: Resistance Mechanisms in Hepatitis C Virus: implications for Direct-Acting Antiviral Use. Drugs. 2017 May 12. doi: 10.1007/s40265-017-0753-x. [Article]
- Myers RP, Shah H, Burak KW, Cooper C, Feld JJ: An update on the management of chronic hepatitis C: 2015 Consensus guidelines from the Canadian Association for the Study of the Liver. Can J Gastroenterol Hepatol. 2015 Jan-Feb;29(1):19-34. Epub 2015 Jan 13. [Article]
- Balasubramaniam M, Reis RS: Computational Target-Based Drug Repurposing of Elbasvir, an Antiviral Drug Predicted to Bind Multiple SARS-CoV-2 Proteins ChemRxiv. [Article]
- American Association for the Study of Liver Diseases; Infectious Diseases Society of America. HCV guidance. http://hcvguidelines.org. Accessed June 12, 2017. [Link]
- Zepatier FDA label [Link]
External Links
KEGG Drug
PubChem Compound
PubChem Substance
ChemSpider
RxNav
ChEBI
ChEMBL
ZINC
PharmGKB
RxList
Wikipedia
FDA label
Clinical Trials
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Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
| Form | Route | Strength |
|---|---|---|
| Tablet | Oral | |
| Tablet, film coated | Oral | |
| Tablet, coated | Oral | |
| Tablet, film coated | Oral | 50.00 mg |
Prices
Not Available
Patents
| Patent Number | Pediatric Extension | Approved | Expires (estimated) | Region |
|---|---|---|---|---|
| US8871759 | No | 2014-10-28 | 2031-05-04 |  |
| US7973040 | No | 2011-07-05 | 2029-07-24 | |
State
Solid
Experimental Properties
Not Available
Predicted Properties
| Property | Value | Source |
|---|---|---|
| Water Solubility | 0.00457 mg/mL | ALOGPS |
| logP | 5.6 | ALOGPS |
| logP | 6.14 | Chemaxon |
| logS | -5.3 | ALOGPS |
| pKa (Strongest Acidic) | 11.11 | Chemaxon |
| pKa (Strongest Basic) | 6.06 | Chemaxon |
| Physiological Charge | 0 | Chemaxon |
| Hydrogen Acceptor Count | 7 | Chemaxon |
| Hydrogen Donor Count | 4 | Chemaxon |
| Polar Surface Area | 188.8 Å2 | Chemaxon |
| Rotatable Bond Count | 13 | Chemaxon |
| Refractivity | 241.52 m3·mol-1 | Chemaxon |
| Polarizability | 100.15 Å3 | Chemaxon |
| Number of Rings | 9 | Chemaxon |
| Bioavailability | 0 | Chemaxon |
| Rule of Five | No | Chemaxon |
| Ghose Filter | No | Chemaxon |
| Veber's Rule | No | Chemaxon |
| MDDR-like Rule | Yes | Chemaxon |
Predicted ADMET Features
Not Available
Mass Spec (NIST)
Not Available
Spectra
| Spectrum | Spectrum Type | Splash Key |
|---|---|---|
| Predicted MS/MS Spectrum - 10V, Positive (Annotated) | Predicted LC-MS/MS | splash10-02mi-0000011690-4da344c0e5b0bf196559 |
| Predicted MS/MS Spectrum - 10V, Negative (Annotated) | Predicted LC-MS/MS | splash10-03ka-3100000950-441892d5ebab8b7b8f0e |
| Predicted MS/MS Spectrum - 20V, Positive (Annotated) | Predicted LC-MS/MS | splash10-0096-0000004890-5f26e40eeaad4c5aadf0 |
| Predicted MS/MS Spectrum - 20V, Negative (Annotated) | Predicted LC-MS/MS | splash10-0296-2000000930-ce410f76833a5d89b395 |
| Predicted MS/MS Spectrum - 40V, Negative (Annotated) | Predicted LC-MS/MS | splash10-008a-6000029780-5762f27669b594190784 |
| Predicted MS/MS Spectrum - 40V, Positive (Annotated) | Predicted LC-MS/MS | splash10-0kh9-9300000210-27ea8a5243612b85a602 |
Chromatographic Properties
Collision Cross Sections (CCS)
| Adduct | CCS Value (Å2) | Source type | Source |
|---|---|---|---|
| [M-H]- | 296.62204 | predicted | DeepCCS 1.0 (2019) |
| [M+H]+ | 298.34573 | predicted | DeepCCS 1.0 (2019) |
| [M+Na]+ | 304.6747 | predicted | DeepCCS 1.0 (2019) |
Targets
Enzymes
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
A cytochrome P450 monooxygenase involved in the metabolism of sterols, steroid hormones, retinoids and fatty acids (PubMed:10681376, PubMed:11093772, PubMed:11555828, PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:19965576, PubMed:20702771, PubMed:21490593, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:21490593, PubMed:21576599, PubMed:2732228). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2, as well as D-ring hydroxylated E1 and E2 at the C-16 position (PubMed:11555828, PubMed:12865317, PubMed:14559847). Plays a role in the metabolism of androgens, particularly in oxidative deactivation of testosterone (PubMed:15373842, PubMed:15764715, PubMed:22773874, PubMed:2732228). Metabolizes testosterone to less biologically active 2beta- and 6beta-hydroxytestosterones (PubMed:15373842, PubMed:15764715, PubMed:2732228). Contributes to the formation of hydroxycholesterols (oxysterols), particularly A-ring hydroxylated cholesterol at the C-4beta position, and side chain hydroxylated cholesterol at the C-25 position, likely contributing to cholesterol degradation and bile acid biosynthesis (PubMed:21576599). Catalyzes bisallylic hydroxylation of polyunsaturated fatty acids (PUFA) (PubMed:9435160). Catalyzes the epoxidation of double bonds of PUFA with a preference for the last double bond (PubMed:19965576). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:20702771). Plays a role in the metabolism of retinoids. Displays high catalytic activity for oxidation of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes atRA toward 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Responsible for oxidative metabolism of xenobiotics. Acts as a 2-exo-monooxygenase for plant lipid 1,8-cineole (eucalyptol) (PubMed:11159812). Metabolizes the majority of the administered drugs. Catalyzes sulfoxidation of the anthelmintics albendazole and fenbendazole (PubMed:10759686). Hydroxylates antimalarial drug quinine (PubMed:8968357). Acts as a 1,4-cineole 2-exo-monooxygenase (PubMed:11695850). Also involved in vitamin D catabolism and calcium homeostasis. Catalyzes the inactivation of the active hormone calcitriol (1-alpha,25-dihydroxyvitamin D(3)) (PubMed:29461981)
Specific Function
1,8-cineole 2-exo-monooxygenase activity
Gene Name
CYP3A4
Uniprot ID
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
- Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins (PubMed:10681376, PubMed:11093772, PubMed:12865317, PubMed:2732228). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:10681376, PubMed:11093772, PubMed:12865317, PubMed:2732228). Exhibits high catalytic activity for the formation of catechol estrogens from 17beta-estradiol (E2) and estrone (E1), namely 2-hydroxy E1 and E2 (PubMed:12865317). Catalyzes 6beta-hydroxylation of the steroid hormones testosterone, progesterone, and androstenedione (PubMed:2732228). Catalyzes the oxidative conversion of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes all trans-retinoic acid (atRA) to 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Also involved in the oxidative metabolism of xenobiotics, including calcium channel blocking drug nifedipine and immunosuppressive drug cyclosporine (PubMed:2732228)
Specific Function
aromatase activity
Gene Name
CYP3A5
Uniprot ID
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
- Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins during embryogenesis (PubMed:11093772, PubMed:12865317, PubMed:14559847, PubMed:17178770, PubMed:9555064). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:11093772, PubMed:12865317, PubMed:14559847, PubMed:17178770, PubMed:9555064). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes 3beta-hydroxyandrost-5-en-17-one (dehydroepiandrosterone, DHEA), a precursor in the biosynthesis of androgen and estrogen steroid hormones (PubMed:17178770, PubMed:9555064). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1), particularly D-ring hydroxylated estrone at the C16-alpha position (PubMed:12865317, PubMed:14559847). Mainly hydroxylates all trans-retinoic acid (atRA) to 4-hydroxyretinoate and may play a role in atRA clearance during fetal development (PubMed:11093772). Also involved in the oxidative metabolism of xenobiotics including anticonvulsants (PubMed:9555064)
Specific Function
all-trans retinoic acid 18-hydroxylase activity
Gene Name
CYP3A7
Uniprot ID
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57469.95 Da
References
- Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Exhibits low testosterone 6-beta-hydroxylase activity
Specific Function
aromatase activity
Gene Name
CYP3A43
Uniprot ID
Uniprot Name
Cytochrome P450 3A43
Molecular Weight
57669.21 Da
Transporters
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Inhibitor
General Function
Translocates drugs and phospholipids across the membrane (PubMed:2897240, PubMed:35970996, PubMed:8898203, PubMed:9038218). 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 (PubMed:8898203). Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells (PubMed:2897240, PubMed:35970996, PubMed:9038218)
Specific Function
ABC-type xenobiotic transporter activity
Gene Name
ABCB1
Uniprot ID
Uniprot Name
ATP-dependent translocase ABCB1
Molecular Weight
141477.255 Da
Drug created at April 07, 2016 16:37 / Updated at April 01, 2022 19:23