Identification

Name
Telaprevir
Accession Number
DB05521
Type
Small Molecule
Groups
Approved, Withdrawn
Description

Telaprevir 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, and affecting 72% of all chronic HCV patients [7]. Treatment options for chronic Hepatitis C have advanced significantly since 2011, with the development of Direct Acting Antivirals (DAAs) such as Telaprevir. Telaprevir is an inhibitor of NS3/4A, a serine protease enzyme, encoded by HCV genotype 1 [Label]. These enzymes are essential for viral replication and serve to cleave the virally encoded polyprotein into mature proteins like NS4A, NS4B, NS5A and NS5B. The barrier for develoment of resistance to NS3/4A inhibitors is lower than that of NS5B inhibitors, another class of DAAs [6]. Subtitutions at amino acid positions 155, 156, or 168 are known to confer resistance. The substitutions of the enzyme's catalytic triad consisting of H58, D82, and S139 are also likely to alter the affinity of the drug for NS3/4A or the activity of the enzyme itself. Despite this disadvantage Telaprevir is still effective against HCV when paired with Ribavirin, Peginterferon alfa-2a, and Peginterferon alfa-2b.

Telaprevir, Ribavirin, Peginterferon alfa-2a, and Peginterferon alfa-2b were used with the intent to cure, or achieve a sustained virologic response (SVR), after 12 weeks of daily administration of the combination therapy followed by 12 or 36 weeks of therapy with Ribavirin, Peginterferon alfa-2a, and Peginterferon alfa-2b. SVR and eradication of HCV infection is 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 [5].

Telaprevir was available as a fixed dose product (tradename Incivek) used for the treatment of chronic Hepatitis C. Approved in May 2011 by the FDA, Incivek was indicated for the treatment of HCV genotype 1 in combination with Ribavirin, Peginterferon alfa-2a, and Peginterferon alfa-2b [Label]. Incivek has since been withdrawn from the market.

Structure
Thumb
Synonyms
  • (1S,3AR,6as)-(2S)-2-cyclohexyl-N-(pyrazinylcarbonyl)glycyl-3-methyl-L-valyl-N-((1S)-1-((cyclopropylamino)oxoacetyl)butyl)octahydrocyclopenta(c)pyrrole-1-carboxamide
External IDs
AIDS-213006 / AIDS213006 / LY 570310 / LY-570310 / MP 424 / MP-424 / VRT 111950 / VRT-111950 / VRT111950 / VX 950 / VX-950
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
IncivekTablet375 mgOralVertex Pharmaceuticals Incorporated2011-10-032015-04-21Canada
IncivekTablet, film coated375 mg/1OralVertex Pharmaceuticals Incorporated2011-05-232014-10-16Us
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
IncivoTelaprevir (375 mg)Tablet, film coatedOralJanssen Cilag International Nv2011-09-192016-10-06Eu
IncivoTelaprevir (375 mg)Tablet, film coatedOralJanssen Cilag International Nv2011-09-192016-10-06Eu
International/Other Brands
Incivek
Categories
UNII
655M5O3W0U
CAS number
402957-28-2
Weight
Average: 679.8493
Monoisotopic: 679.405732463
Chemical Formula
C36H53N7O6
InChI Key
BBAWEDCPNXPBQM-GDEBMMAJSA-N
InChI
InChI=1S/C36H53N7O6/c1-5-10-25(29(44)34(48)39-23-15-16-23)40-33(47)28-24-14-9-13-22(24)20-43(28)35(49)30(36(2,3)4)42-32(46)27(21-11-7-6-8-12-21)41-31(45)26-19-37-17-18-38-26/h17-19,21-25,27-28,30H,5-16,20H2,1-4H3,(H,39,48)(H,40,47)(H,41,45)(H,42,46)/t22-,24-,25-,27-,28-,30+/m0/s1
IUPAC Name
(3S)-3-{[(1S,3aR,6aS)-2-[(2S)-2-[(2S)-2-cyclohexyl-2-(pyrazin-2-ylformamido)acetamido]-3,3-dimethylbutanoyl]-octahydrocyclopenta[c]pyrrol-1-yl]formamido}-N-cyclopropyl-2-oxohexanamide
SMILES
[H][C@@]12CCC[C@]1([H])[C@H](N(C2)C(=O)[C@@H](NC(=O)[C@@H](NC(=O)C1=NC=CN=C1)C1CCCCC1)C(C)(C)C)C(=O)N[C@@H](CCC)C(=O)C(=O)NC1CC1

Pharmacology

Indication

Telaprevir, when used in combination with Ribavirin, Peginterferon alfa-2a, and Peginterferon alfa-2b is indicated for use in the treatment of chronic HCV genotype 1 infection in adults [Label].

Pharmacodynamics

Telaprevir is classified as a direct-acting antiviral (DAA) and prevents viral replication in HCV genotype 1 [Label].

Mechanism of action

Telaprevir is a NS3/4a protease inhibitor used to inhibit viral HCV replication [Label]. NS3/4a protease is an integral part of viral replication and mediates the cleavage the virally encoded polyprotein to mature proteins (NS4A, NS4B, NS5A and NS5B) [Label]. Telaprevir inhibits NS3/4A with an IC50 of 10nM.

TargetActionsOrganism
ANS3/4A protein
inhibitor
Hepatitis C virus
USolute carrier organic anion transporter family member 1B1
inhibitor
Human
USolute carrier organic anion transporter family member 2B1
inhibitor
Human
Absorption

Telaprevir reaches peak plasma concentration 4-5hours after administration [Label]. Absolute bioavailability has not been determined. When taken with a normal fat meal (21g of fat), exposure increases by 235% compared to fasting conditions. With low (3.6g of fat) and high fat (56g of fat) meals, exposure increased 117% and 330% respectively.

Volume of distribution

The estimated apparent volume of distribution for Telapravir is 252 litres with an inter-individual variability of 72% [Label].

Protein binding

Telapravir is 59-76% bound to human plasma proteins following a single dose [Label]. It binds to both human serum albumin and α1-acid glycoprotein.

Metabolism

Telaprevir is extensively metabolized via hydrolysis, oxidation, and reduction. The major metabolites of Telaprevir are pyrazinoic acid, a metabolite that underwent reduction at the α-ketoamide bond, and the R-diastereomer of telaprevir which is 30-fold less active than the parent compound were found to be the predominant metabolites. The primary enzyme involved in the metabolism of Telaprevir is CYP3A4. Some metabolism is performed by aldo-keto reductases and other reductases.

Route of elimination

Telaprevir is mainly eliminated in the feces (82%) with a smaller amount eliminated via expiration (9%) and very little in the urine (1%) [Label]. 31.9% and 18.8% of drug in the feces was present as the parent compound and R-diastereomer of the parent compound respectively.

Half life

Telaprevir has a half-life of elimination of 4.0-4.7 hours after a single dose and an effective half life of 9-11 hours at steady state [Label].

Clearance

Telaprevir has an estimated aparent total body clearance of 32.4 liters per hour with an interindividual variability of 27.2% [Label].

Toxicity

Serious skin reactions, including Stevens Johnson Syndrome, Drug Reaction with Eosinophilia and Systemic Symptoms, and Toxic Epidermal Necrolysis, have been reported in patients treated with telaprevir combination treatment. Use of Ribavirin, Peginterferon alfa-2a, Peginterferon alfa-2b and Telaprevir is associated with a further increase in anemia frequency than in Ribavirin, Peginterferon alfa-2a, and Peginterferon alfa-2b without telaprevir.

Affected organisms
  • Hepatitis C Virus
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
16-BromoepiandrosteroneThe serum concentration of Telaprevir can be decreased when it is combined with 16-Bromoepiandrosterone.
19-norandrostenedioneThe serum concentration of Telaprevir can be decreased when it is combined with 19-norandrostenedione.
5-androstenedioneThe serum concentration of Telaprevir can be decreased when it is combined with 5-androstenedione.
AbacavirThe serum concentration of Abacavir can be decreased when it is combined with Telaprevir.
AbemaciclibThe risk or severity of adverse effects can be increased when Telaprevir is combined with Abemaciclib.
AbirateroneThe metabolism of Abiraterone can be decreased when combined with Telaprevir.
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Telaprevir.
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Telaprevir.
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Telaprevir.
AcetazolamideThe metabolism of Telaprevir can be decreased when combined with Acetazolamide.
Food Interactions
  • St. John's wort is a CYP3A4 inducer which will decrease levels of telaprevir.

References

Synthesis Reference

Znabet A, Polak MM, Janssen E, de Kanter FJ, Turner NJ, Orru RV, Ruijter E. A highly efficient synthesis of telaprevir by strategic use of biocatalysis and multicomponent reactions. Chem Commun (Camb). 2010 Nov 14;46(42):7918-20. Epub 2010 Sep 20.

General References
  1. Kim JJ, Culley CM, Mohammad RA: Telaprevir: an oral protease inhibitor for hepatitis C virus infection. Am J Health Syst Pharm. 2012 Jan 1;69(1):19-33. doi: 10.2146/ajhp110123. [PubMed:22180548]
  2. Liu-Young G, Kozal MJ: Hepatitis C protease and polymerase inhibitors in development. AIDS Patient Care STDS. 2008 Jun;22(6):449-57. doi: 10.1089/apc.2007.0199. [PubMed:18479202]
  3. Forestier N, Zeuzem S: Telaprevir for the treatment of hepatitis C. Expert Opin Pharmacother. 2012 Mar;13(4):593-606. doi: 10.1517/14656566.2012.660524. Epub 2012 Feb 15. [PubMed:22332992]
  4. Garg V, Kauffman RS, Beaumont M, van Heeswijk RP: Telaprevir: pharmacokinetics and drug interactions. Antivir Ther. 2012;17(7):1211-21. doi: 10.3851/IMP2356. Epub 2012 Sep 7. [PubMed:22954756]
  5. 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. [PubMed:25585348]
  6. 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. [PubMed:28497432]
  7. American Association for the Study of Liver Diseases; Infectious Diseases Society of America. HCV guidance. http://hcvguidelines.org. Accessed June 12, 2017. [Link]
External Links
Human Metabolome Database
HMDB0015616
KEGG Drug
D09012
PubChem Compound
3010818
PubChem Substance
175427024
ChemSpider
2279948
BindingDB
50326056
ChEBI
68595
ChEMBL
CHEMBL231813
PharmGKB
PA165958354
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Telaprevir
ATC Codes
J05AE11 — Telaprevir
FDA label
Download (508 KB)
MSDS
Download (88.2 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableChronic Hepatitis C Virus (HCV) Infection1
1CompletedNot AvailableChronic Hepatitis C Virus (HCV) Infection / Hemophilia1
1CompletedNot AvailableHepatitis C Viral Infection3
1CompletedBasic ScienceChronic Hepatitis C Virus (HCV) Infection1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedBasic ScienceHepatic Insufficiency1
1CompletedBasic ScienceHepatitis C Viral Infection1
1CompletedBasic SciencePharmacokinetic Assessments in Healthy Volunteers1
1CompletedOtherHuman Immunodeficiency Virus (HIV) Infections1
1CompletedOtherThrombocytopenias1
1CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / Hepatitis C Viral Infection1
1CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / Human Immunodeficiency Virus (HIV) Infections1
1CompletedTreatmentHealthy Participants2
1CompletedTreatmentHepatic Impairment1
1CompletedTreatmentHepatitis C Viral Infection2
1CompletedTreatmentHepatitis C Viral Infection / Human Immunodeficiency Virus (HIV)1
1CompletedTreatmentHepatitis C Viral Infection / Human Immunodeficiency Virus (HIV) / Telaprevir1
1CompletedTreatmentHepatitis C Viral Infection / Kidney Diseases1
1CompletedTreatmentHepatitis C Viral Infection / Opioid-Related Disorders1
1, 2TerminatedTreatmentHepatitis C Viral Infection1
2CompletedNot AvailableHepatitis C Viral Infection1
2CompletedTreatmentChronic Hepatitis C Virus2
2CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection7
2CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / Human Immunodeficiency Virus (HIV) Infections1
2CompletedTreatmentHepatitis C Viral Infection5
2CompletedTreatmentThrombocytopenias1
2TerminatedNot AvailableDepression / Hepatitis C Infection1
2TerminatedTreatmentChronic Hepatitis C Virus (HCV) Infection1
2TerminatedTreatmentHepatitis C Infection1
2TerminatedTreatmentHepatitis C Viral Infection1
2Unknown StatusTreatmentChronic Hepatitis C Virus (HCV) Infection1
2, 3WithdrawnTreatmentHepatitis C Viral Infection1
3CompletedHealth Services ResearchHuman Immunodeficiency Virus (HIV)1
3CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection12
3CompletedTreatmentGenotype 1 Chronic Hepatitis C1
3CompletedTreatmentGenotype 1 Chronic Hepatitis C / Treatment Naive1
3CompletedTreatmentHepatitis C Viral Infection6
3CompletedTreatmentHepatitis C Virus (HCV)1
3CompletedTreatmentHepatitis C Virus Infection1
3TerminatedTreatmentChronic Hepatitis C Virus (HCV) Infection1
3TerminatedTreatmentHepatitis C Viral Infection1
3TerminatedTreatmentInfection NOS1
3WithdrawnTreatmentChronic Hepatitis C Virus (HCV) Infection1
4TerminatedTreatmentHepatitis C Viral Infection2
4Unknown StatusTreatmentHepatitis C Viral Infection1
4WithdrawnPreventionHepatitis C Viral Infection1
4WithdrawnTreatmentHepatitis C Viral Infection1
Not AvailableCompletedNot AvailableHepatitis C Viral Infection1
Not AvailableCompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / Hepatitis C Viral Infection / Liver Cirrhosis1
Not AvailableRecruitingNot AvailableChronic Hepatitis C Virus (HCV) Infection1
Not AvailableRecruitingNot AvailableChronic Hepatitis C Virus (HCV) Infection / Human Immunodeficiency Virus (HIV)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
TabletOral375 mg
Tablet, film coatedOral375 mg/1
Tablet, film coatedOral375 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US8431615No2008-05-302028-05-30Us
US8529882No2001-08-312021-08-31Us
US7820671No2005-02-252025-02-25Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubility0.0047 mg/mLFDA Label
Predicted Properties
PropertyValueSource
Water Solubility0.0355 mg/mLALOGPS
logP2.56ALOGPS
logP2.58ChemAxon
logS-4.3ALOGPS
pKa (Strongest Acidic)11.86ChemAxon
pKa (Strongest Basic)-0.69ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area179.56 Å2ChemAxon
Rotatable Bond Count14ChemAxon
Refractivity180.04 m3·mol-1ChemAxon
Polarizability74.37 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9547
Blood Brain Barrier-0.9659
Caco-2 permeable-0.7982
P-glycoprotein substrateSubstrate0.8567
P-glycoprotein inhibitor IInhibitor0.9355
P-glycoprotein inhibitor IIInhibitor0.8879
Renal organic cation transporterNon-inhibitor0.8919
CYP450 2C9 substrateNon-substrate0.8245
CYP450 2D6 substrateNon-substrate0.6612
CYP450 3A4 substrateSubstrate0.7632
CYP450 1A2 substrateNon-inhibitor0.6961
CYP450 2C9 inhibitorInhibitor0.5969
CYP450 2D6 inhibitorNon-inhibitor0.7431
CYP450 2C19 inhibitorInhibitor0.5866
CYP450 3A4 inhibitorInhibitor0.8926
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8476
Ames testNon AMES toxic0.7536
CarcinogenicityNon-carcinogens0.8622
BiodegradationNot ready biodegradable0.9954
Rat acute toxicity2.6980 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9894
hERG inhibition (predictor II)Inhibitor0.6931
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as hybrid peptides. These are compounds containing at least two different types of amino acids (alpha, beta, gamma, delta) linked to each other through a peptide bond.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Peptidomimetics
Sub Class
Hybrid peptides
Direct Parent
Hybrid peptides
Alternative Parents
Valine and derivatives / N-acyl-alpha amino acids and derivatives / Alpha amino acid amides / Pyrazinecarboxamides / 2-heteroaryl carboxamides / N-acylpyrrolidines / Pyrrolidinecarboxamides / N-acyl amines / Tertiary carboxylic acid amides / Heteroaromatic compounds
show 7 more
Substituents
Hybrid peptide / Valine or derivatives / N-acyl-alpha amino acid or derivatives / Alpha-amino acid amide / N-substituted-alpha-amino acid / Alpha-amino acid or derivatives / Pyrazine carboxylic acid or derivatives / Pyrazinecarboxamide / 2-heteroaryl carboxamide / N-acylpyrrolidine
show 24 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
oligopeptide, pyrazines, cyclopropanes, cyclopentapyrrole (CHEBI:68595)

Targets

Kind
Protein
Organism
Hepatitis C virus
Pharmacological action
Yes
Actions
Inhibitor
General Function
Serine-type peptidase activity
Specific Function
Not Available
Gene Name
NS3/4A
Uniprot ID
B0B3C9
Uniprot Name
Genome polyprotein
Molecular Weight
72789.28 Da
References
  1. Liu-Young G, Kozal MJ: Hepatitis C protease and polymerase inhibitors in development. AIDS Patient Care STDS. 2008 Jun;22(6):449-57. doi: 10.1089/apc.2007.0199. [PubMed:18479202]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
Gene Name
SLCO2B1
Uniprot ID
O94956
Uniprot Name
Solute carrier organic anion transporter family member 2B1
Molecular Weight
76709.98 Da

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Kim JJ, Culley CM, Mohammad RA: Telaprevir: an oral protease inhibitor for hepatitis C virus infection. Am J Health Syst Pharm. 2012 Jan 1;69(1):19-33. doi: 10.2146/ajhp110123. [PubMed:22180548]
  2. Kiang TK, Wilby KJ, Ensom MH: Telaprevir: clinical pharmacokinetics, pharmacodynamics, and drug-drug interactions. Clin Pharmacokinet. 2013 Jul;52(7):487-510. doi: 10.1007/s40262-013-0053-x. [PubMed:23553423]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Flockhart Table - Indiana University [Link]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Garg V, Kauffman RS, Beaumont M, van Heeswijk RP: Telaprevir: pharmacokinetics and drug interactions. Antivir Ther. 2012;17(7):1211-21. doi: 10.3851/IMP2356. Epub 2012 Sep 7. [PubMed:22954756]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Not Available
Specific Function
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
Gene Name
ORM1
Uniprot ID
P02763
Uniprot Name
Alpha-1-acid glycoprotein 1
Molecular Weight
23511.38 Da
References
  1. Garg V, Kauffman RS, Beaumont M, van Heeswijk RP: Telaprevir: pharmacokinetics and drug interactions. Antivir Ther. 2012;17(7):1211-21. doi: 10.3851/IMP2356. Epub 2012 Sep 7. [PubMed:22954756]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Kiang TK, Wilby KJ, Ensom MH: Telaprevir: clinical pharmacokinetics, pharmacodynamics, and drug-drug interactions. Clin Pharmacokinet. 2013 Jul;52(7):487-510. doi: 10.1007/s40262-013-0053-x. [PubMed:23553423]

Drug created on November 18, 2007 11:25 / Updated on October 01, 2018 14:01