U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C36H53N7O6
Molecular Weight 679.8507
Optical Activity UNSPECIFIED
Defined Stereocenters 6 / 6
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TELAPREVIR

SMILES

CCC[C@@]([H])(C(=O)C(=O)NC1CC1)N=C([C@]2([H])[C@@]3([H])CCC[C@@]3([H])CN2C(=O)[C@]([H])(C(C)(C)C)N=C([C@]([H])(C4CCCCC4)N=C(c5cnccn5)O)O)O

InChI

InChIKey=BBAWEDCPNXPBQM-GDEBMMAJSA-N
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

HIDE SMILES / InChI

Molecular Formula C36H53N7O6
Molecular Weight 679.8507
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 6 / 6
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: description was created based on several sources, including http://www.millionpharma.com/telaprevir.php; https://www.jnj.com/media-center/press-releases/incivo-telaprevir-approved-in-europe-offering-higher-cure-rates-for-genotype-1-chronic-hepatitis-c-compared-to-standard-treatment

Telaprevir (marketed under the brand names Incivek and Incivo) is a direct-acting antiviralagent against the hepatitis C virus (HCV). It is a hepatitis C virus NS3/4A protease inhibitor indicated for the treatment of genotype 1 chronic hepatitis C (CHC) in adult patients with compensated liver disease, including cirrhosis, who are treatment-naïve or who have been previously treated with interferon-based treatment, including prior null responders, partial responders, and relapsers in combination with peginterferon alfa and ribavirin. Telaprevir is not used as a monotherapy. It is necessary for the proteolytic cleavage of the HCV encoded polyprotein into mature forms of the NS4A, NS4B, NS5A and NS5B proteins and essential for viral replication. It belongs to the chemical class of alpha-ketoamids and binds to NS3/4A in a covalent but reversible manner.

Originator

Curator's Comment:: The Janssen Companies have the right to commercialize telaprevir in Europe, Latin America, the Middle East, Africa, India, Australia and New Zealand under the commercial name INCIVO®; Vertex has the right to commercialize telaprevir in North America under the name INCIVEK™ (approved by US FDA in May 2011 and by Health Canada in August 2011 for genotype-1 chronic hepatitis C with compensated liver disease); Mitsubishi Tanabe Pharma has the right to commercialize telaprevir in Japan and certain Far Eastern countries. # Tibotec (Janssen Pharmaceutical Companies) in collaboration with Vertex and Mitsubishi Tanabe Pharma

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
10.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
INCIVEK

Approved Use

Indicated, in combination with peginterferon alfa and ribavirin, for the treatment of genotype 1 chronic hepatitis C (CHC) in adult patients with compensated liver disease, including cirrhosis, who are treatment-naïve or who have been previously treated with interferon-based treatment, including prior null responders, partial responders, and relapsers. Incivek must not be used as monotherapy and must only be used in combination with peginterferon alfa and ribavirin.

Launch Date

1.30610876E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1940 ng/mL
750 mg 3 times / day steady-state, oral
dose: 750 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
VRT-127394 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
511 ng/mL
750 mg single, oral
dose: 750 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VRT-127394 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
3090 ng/mL
750 mg 3 times / day steady-state, oral
dose: 750 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TELAPREVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
1740.84 ng/mL
750 mg single, oral
dose: 750 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TELAPREVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
3232.22 ng/mL
1500 mg single, oral
dose: 1500 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TELAPREVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
539.79 ng/mL
375 mg single, oral
dose: 375 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TELAPREVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
13274.77 ng × h/mL
750 mg 3 times / day steady-state, oral
dose: 750 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
VRT-127394 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
5203 ng × h/mL
750 mg single, oral
dose: 750 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VRT-127394 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
19809.27 ng × h/mL
750 mg 3 times / day steady-state, oral
dose: 750 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TELAPREVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
11749.1 ng × h/mL
750 mg single, oral
dose: 750 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TELAPREVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
24250.23 ng × h/mL
1500 mg single, oral
dose: 1500 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TELAPREVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
3146.52 ng × h/mL
375 mg single, oral
dose: 375 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TELAPREVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
4.77 h
750 mg single, oral
dose: 750 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VRT-127394 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
3.96 h
750 mg single, oral
dose: 750 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TELAPREVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
6.49 h
1500 mg single, oral
dose: 1500 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TELAPREVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
3.23 h
375 mg single, oral
dose: 375 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TELAPREVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
32.5%
375 mg single, oral
dose: 375 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TELAPREVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
Doses

Doses

DosePopulationAdverse events​
750 mg 3 times / day multiple, oral
Recommended
Dose: 750 mg, 3 times / day
Route: oral
Route: multiple
Dose: 750 mg, 3 times / day
Co-administed with::
peginterferon alfa
ribavirin
Sources:
unhealthy, 58 years
n = 1
Health Status: unhealthy
Condition: chronic hepatitis C virus
Age Group: 58 years
Sex: F
Population Size: 1
Sources:
Disc. AE: DRESS syndrome...
AEs leading to
discontinuation/dose reduction:
DRESS syndrome (1 patient)
Sources:
1875 mg 3 times / day multiple, oral
Highest studied dose
Dose: 1875 mg, 3 times / day
Route: oral
Route: multiple
Dose: 1875 mg, 3 times / day
Sources:
healthy, adult
Other AEs: Nausea, Headache...
Other AEs:
Nausea
Headache
Diarrhea
Decreased appetite
Dysgeusia
Vomiting
Sources:
750 mg 3 times / day multiple, oral
Recommended
Dose: 750 mg, 3 times / day
Route: oral
Route: multiple
Dose: 750 mg, 3 times / day
Co-administed with::
peginterferon alfa
ribavirin
Sources: Page: p. 68
unhealthy, adult
n = 1797
Health Status: unhealthy
Age Group: adult
Population Size: 1797
Sources: Page: p. 68
Disc. AE: Anemia, Skin disorder...
AEs leading to
discontinuation/dose reduction:
Anemia (22%)
Skin disorder (20%)
Fatigue (6%)
Nausea (4%)
Vomiting (4%)
Sources: Page: p. 68
AEs

AEs

AESignificanceDosePopulation
DRESS syndrome 1 patient
Disc. AE
750 mg 3 times / day multiple, oral
Recommended
Dose: 750 mg, 3 times / day
Route: oral
Route: multiple
Dose: 750 mg, 3 times / day
Co-administed with::
peginterferon alfa
ribavirin
Sources:
unhealthy, 58 years
n = 1
Health Status: unhealthy
Condition: chronic hepatitis C virus
Age Group: 58 years
Sex: F
Population Size: 1
Sources:
Decreased appetite
1875 mg 3 times / day multiple, oral
Highest studied dose
Dose: 1875 mg, 3 times / day
Route: oral
Route: multiple
Dose: 1875 mg, 3 times / day
Sources:
healthy, adult
Diarrhea
1875 mg 3 times / day multiple, oral
Highest studied dose
Dose: 1875 mg, 3 times / day
Route: oral
Route: multiple
Dose: 1875 mg, 3 times / day
Sources:
healthy, adult
Dysgeusia
1875 mg 3 times / day multiple, oral
Highest studied dose
Dose: 1875 mg, 3 times / day
Route: oral
Route: multiple
Dose: 1875 mg, 3 times / day
Sources:
healthy, adult
Headache
1875 mg 3 times / day multiple, oral
Highest studied dose
Dose: 1875 mg, 3 times / day
Route: oral
Route: multiple
Dose: 1875 mg, 3 times / day
Sources:
healthy, adult
Nausea
1875 mg 3 times / day multiple, oral
Highest studied dose
Dose: 1875 mg, 3 times / day
Route: oral
Route: multiple
Dose: 1875 mg, 3 times / day
Sources:
healthy, adult
Vomiting
1875 mg 3 times / day multiple, oral
Highest studied dose
Dose: 1875 mg, 3 times / day
Route: oral
Route: multiple
Dose: 1875 mg, 3 times / day
Sources:
healthy, adult
Skin disorder 20%
Disc. AE
750 mg 3 times / day multiple, oral
Recommended
Dose: 750 mg, 3 times / day
Route: oral
Route: multiple
Dose: 750 mg, 3 times / day
Co-administed with::
peginterferon alfa
ribavirin
Sources: Page: p. 68
unhealthy, adult
n = 1797
Health Status: unhealthy
Age Group: adult
Population Size: 1797
Sources: Page: p. 68
Anemia 22%
Disc. AE
750 mg 3 times / day multiple, oral
Recommended
Dose: 750 mg, 3 times / day
Route: oral
Route: multiple
Dose: 750 mg, 3 times / day
Co-administed with::
peginterferon alfa
ribavirin
Sources: Page: p. 68
unhealthy, adult
n = 1797
Health Status: unhealthy
Age Group: adult
Population Size: 1797
Sources: Page: p. 68
Nausea 4%
Disc. AE
750 mg 3 times / day multiple, oral
Recommended
Dose: 750 mg, 3 times / day
Route: oral
Route: multiple
Dose: 750 mg, 3 times / day
Co-administed with::
peginterferon alfa
ribavirin
Sources: Page: p. 68
unhealthy, adult
n = 1797
Health Status: unhealthy
Age Group: adult
Population Size: 1797
Sources: Page: p. 68
Vomiting 4%
Disc. AE
750 mg 3 times / day multiple, oral
Recommended
Dose: 750 mg, 3 times / day
Route: oral
Route: multiple
Dose: 750 mg, 3 times / day
Co-administed with::
peginterferon alfa
ribavirin
Sources: Page: p. 68
unhealthy, adult
n = 1797
Health Status: unhealthy
Age Group: adult
Population Size: 1797
Sources: Page: p. 68
Fatigue 6%
Disc. AE
750 mg 3 times / day multiple, oral
Recommended
Dose: 750 mg, 3 times / day
Route: oral
Route: multiple
Dose: 750 mg, 3 times / day
Co-administed with::
peginterferon alfa
ribavirin
Sources: Page: p. 68
unhealthy, adult
n = 1797
Health Status: unhealthy
Age Group: adult
Population Size: 1797
Sources: Page: p. 68
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
likely
no
no
yes (co-administration study)
Comment: telaprevir caused a nearly 2-fold increase in exposure (Cmax, AUClast) to digoxin. Clearance of digoxin was decreased by 46% in the presence of telaprevir
Page: 50.0
unlikely
unlikely
unlikely
weak [IC50 >100 uM]
weak [IC50 >100 uM]
weak [IC50 >100 uM]
weak [IC50 >100 uM]
weak [IC50 >100 uM]
weak [IC50 >100 uM]
weak [IC50 >100 uM]
weak [IC50 >100 uM]
yes [IC50 2.8 uM]
weak (co-administration study)
Comment: 21 days of dosing with Modicon (0.5 mg NE + 0.035 mg EE) and telaprevir resulted in a decrease in EE plasma concentrations: Mean EE Cmax, Cmin, and AUCss were decreased by 26%, 32%, and 27%, respectively. Telaprevir also decreased NE exposure: mean NE Cmax, Cmin, and AUCss were decreased by 16%, 7%, and 10%, respectively
Page: 81.0
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
yes (co-administration study)
Comment: mean telaprevir AUCinf and mean AUC0-24h values were approximately 67% higher and mean telaprevir Cmax values were approximately 29% higher in subjects receiving telaprevir+ketoconazole; rifampin causes a significant increase in CYP3A4 metabolism resulting in a greater than 10-fold decrease in telaprevir AUClast exposure and 7-fold decrease in Cmax; Lopinavir/ritonavir (CYP3A4/P-gp inhibitors) significantly lowers telaprevir exposure (54% decrease in AUCτ and 55% decrease in Cmax) and could result in subtherapeutic concentrations of telaprevir
Page: 48.0
no
no
no
no
no
yes
yes (co-administration study)
Comment: Lopinavir/ritonavir (CYP3A4/P-gp inhibitors) significantly lowers telaprevir exposure (54% decrease in AUCτ and 55% decrease in Cmax) and could result in subtherapeutic concentrations of telaprevir
Page: 49.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Non-HIV antivirals - a review of the recent patent literature.
2002 Aug
In vitro resistance studies of hepatitis C virus serine protease inhibitors, VX-950 and BILN 2061: structural analysis indicates different resistance mechanisms.
2004 Apr 23
P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors.
2004 Oct 4
Discovery of small-molecule inhibitors of HCV NS3-4A protease as potential therapeutic agents against HCV infection.
2005
In vitro studies of cross-resistance mutations against two hepatitis C virus serine protease inhibitors, VX-950 and BILN 2061.
2005 Nov 4
Potent inhibitors of the hepatitis C virus NS3 protease: use of a novel P2 cyclopentane-derived template.
2006 Aug 1
VX-950, a novel hepatitis C virus (HCV) NS3-4A protease inhibitor, exhibits potent antiviral activities in HCv replicon cells.
2006 May
Inhibitors of hepatitis C virus NS3.4A protease. Effect of P4 capping groups on inhibitory potency and pharmacokinetics.
2007 Jun 15
Preclinical characteristics of the hepatitis C virus NS3/4A protease inhibitor ITMN-191 (R7227).
2008 Dec
Hepatitis C protease and polymerase inhibitors in development.
2008 Jun
The hepatitis C virus replicon presents a higher barrier to resistance to nucleoside analogs than to nonnucleoside polymerase or protease inhibitors.
2008 May
Inhibitors of hepatitis C virus NS3/4A: alpha-ketoamide based macrocyclic inhibitors.
2009 Apr 15
In vitro and in vivo isotope effects with hepatitis C protease inhibitors: enhanced plasma exposure of deuterated telaprevir versus telaprevir in rats.
2009 Dec 24
Substituted imidazopyridines as potent inhibitors of HCV replication.
2009 May
Synthesis of potent antitumor and antiviral benzofuran derivatives.
2009 May 1
Advances in the development of macrocyclic inhibitors of hepatitis C virus NS3-4A protease.
2010
Activity of aminocandin (IP960; HMR3270) compared with amphotericin B, itraconazole, caspofungin and micafungin in neutropenic murine models of disseminated infection caused by itraconazole-susceptible and -resistant strains of Aspergillus fumigatus.
2010 Feb
A cell protection screen reveals potent inhibitors of multiple stages of the hepatitis C virus life cycle.
2010 Feb 23
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
2010 Jan
The hepatitis C virus (HCV) NS4B RNA binding inhibitor clemizole is highly synergistic with HCV protease inhibitors.
2010 Jul 1
Improved P2 phenylglycine-based hepatitis C virus NS3 protease inhibitors with alkenylic prime-side substituents.
2010 Jul 15
Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
2010 Nov
Selective irreversible inhibition of a protease by targeting a noncatalytic cysteine.
2011 Jan
Elimination of hepatitis C virus by short term NS3-4A and NS5B inhibitor combination therapy in human hepatocyte chimeric mice.
2011 May
Estimation of inhibitory quotient using a comparative equilibrium dialysis assay for prediction of viral response to hepatitis C virus inhibitors.
2011 May
Differential efficacy of protease inhibitors against HCV genotypes 2a, 3a, 5a, and 6a NS3/4A protease recombinant viruses.
2011 Sep
Telaprevir: pharmacokinetics and drug interactions.
2012
Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants.
2012 Apr 12
Telaprevir: an oral protease inhibitor for hepatitis C virus infection.
2012 Jan 1
Telaprevir for the treatment of hepatitis C.
2012 Mar
Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
2013 Dec 1
Resistance studies of a dithiazol analogue, DBPR110, as a potential hepatitis C virus NS5A inhibitor in replicon systems.
2013 Feb
Myriberine A, a new alkaloid with an unprecedented heteropentacyclic skeleton from Myrioneuron faberi.
2013 Feb 1
In vitro efficacy of approved and experimental antivirals against novel genotype 3 hepatitis C virus subgenomic replicons.
2013 Nov
Synthesis and antiviral activity of a novel class of (5-oxazolyl)phenyl amines.
2013 Nov
Restoration of the activated Rig-I pathway in hepatitis C virus (HCV) replicon cells by HCV protease, polymerase, and NS5A inhibitors in vitro at clinically relevant concentrations.
2013 Sep
Inhibition of hepatitis C virus replication by GS-6620, a potent C-nucleoside monophosphate prodrug.
2014
Preclinical characterization of the novel hepatitis C virus NS3 protease inhibitor GS-9451.
2014
Highly efficient infectious cell culture of three hepatitis C virus genotype 2b strains and sensitivity to lead protease, nonstructural protein 5A, and polymerase inhibitors.
2014 Feb
Rhabdomyolysis in a hepatitis C virus infected patient treated with telaprevir and simvastatin.
2014 Jul-Aug
Hepatitis C virus: Virology, diagnosis and treatment.
2015 Jun 8
Systems pharmacological analysis of drugs inducing stevens-johnson syndrome and toxic epidermal necrolysis.
2015 May 18
Patents

Sample Use Guides

1125 mg taken twice daily (10-14 hours apart) with food (not low fat). Incivek must be administered with both peginterferon alfa and ribavirin for all patients for 12 weeks, followed by a response-guided regimen of either 12 or 36 additional weeks of peginterferon alfa and ribavirin depending on viral response and prior response status.
Route of Administration: Oral
Telaprevir demonstrated excellent antiviral activity both in genotype 1b HCV replicon cells with the IC50 of 354 nM and in human fetal hepatocytes infected with genotype 1a HCV-positive patient sera (IC50 = 280 nM).
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:44:42 UTC 2021
Edited
by admin
on Fri Jun 25 21:44:42 UTC 2021
Record UNII
655M5O3W0U
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
TELAPREVIR
DASH   INN   JAN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
VRT-111950
Code English
VX-950
Code English
TELAPREVIR [JAN]
Common Name English
LY 570310
Code English
INCIVO
Brand Name English
VRT 111950
Code English
TELAPREVIR [INN]
Common Name English
(1S,3AR,6AS)-2-((2S)-2-(((2S)-CYCLOHEXYL((PYRAZINYLCARBONYL)AMINO)ACETYL)AMINO)-3,3-DIMETHYLBUTANOYL)-N-((1S)-1-((CYCLOPROPYLAMINO)OXOACETYL)BUTYL) OCTAHYDROCYCLOPENTA(C)PYRROLE-1-CARBOXAMIDE
Common Name English
TELAPREVIR [ORANGE BOOK]
Common Name English
TELAPREVIR [USAN]
Common Name English
LY-570310
Code English
MP 424
Code English
INCIVEK
Brand Name English
TELAPREVIR [VANDF]
Common Name English
CYCLOPENTA(C)PYRROLE-1-CARBOXAMIDE, (2S)-2-CYCLOHEXYL-N-(PYRAZINYLCARBONYL)GLYCYL-3-METHYL-L-VALYL-N-((1S)-1-((CYCLOPROPYLAMINO)OXOACETYL)BUTYL)OCTAHYDRO-, (1S,3AR,6AS)-
Common Name English
VX 950
Code English
TELAPREVIR [WHO-DD]
Common Name English
MP-424
Code English
TELAPREVIR [MI]
Common Name English
TELAPREVIR [MART.]
Common Name English
Classification Tree Code System Code
WHO-VATC QJ05AE11
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
EMA ASSESSMENT REPORTS INCIVO (AUTHORIZED: HEPATITIS C, CHRONIC)
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
NDF-RT N0000182639
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
NCI_THESAURUS C783
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
LIVERTOX 926
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
NCI_THESAURUS C281
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
WHO-ATC J05AP02
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
WHO-ATC J05AE11
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
Code System Code Type Description
FDA UNII
655M5O3W0U
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY
HSDB
8125
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY
CAS
402957-28-2
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY
MESH
C486464
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY
NDF-RT
N0000190114
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY Cytochrome P450 3A Inhibitors [MoA]
NDF-RT
N0000190109
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY Organic Anion Transporting Polypeptide 2B1 Inhibitors [MoA]
EVMPD
SUB31651
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY
NDF-RT
N0000182638
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY HCV NS3/4A Protease Inhibitors [MoA]
DRUG BANK
DB05521
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY
DRUG CENTRAL
4173
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY
INN
8686
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY
NCI_THESAURUS
C81603
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY
EPA CompTox
402957-28-2
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY
PUBCHEM
3010818
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY
LACTMED
Telaprevir
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY
RXCUI
1102261
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY RxNorm
NDF-RT
N0000185503
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY P-Glycoprotein Inhibitors [MoA]
NDF-RT
N0000190107
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY Organic Anion Transporting Polypeptide 1B1 Inhibitors [MoA]
MERCK INDEX
M10526
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY Merck Index
ChEMBL
CHEMBL231813
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY
WIKIPEDIA
TELAPREVIR
Created by admin on Fri Jun 25 21:44:42 UTC 2021 , Edited by admin on Fri Jun 25 21:44:42 UTC 2021
PRIMARY
Related Record Type Details
METABOLIC ENZYME -> SUBSTRATE
MAJOR
TRANSPORTER -> SUBSTRATE
EXCRETED UNCHANGED
FECAL
BINDER->LIGAND
The protein binding is concentration dependent and decreases with increasing telaprevir concentrations at all concentrations of human serum albumin (HSA) and ?-1-acid glycoprotein (AAG). In addition, protein binding of telaprevir is affected by the concentration of HSA and AAG.
BINDING
Related Record Type Details
METABOLITE INACTIVE -> PARENT
METABOLITE LESS ACTIVE -> PARENT
Approximately 30-fold less potent than telaprevir.
MAJOR
PLASMA
METABOLITE -> PARENT
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC single dose

Volume of Distribution PHARMACOKINETIC