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

Details

Stereochemistry ABSOLUTE
Molecular Formula C49H54N8O8
Molecular Weight 883.0037
Optical Activity UNSPECIFIED
Defined Stereocenters 6 / 6
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of VELPATASVIR

SMILES

CC(C)[C@@]([H])(C(=O)N1[C@@]([H])(C)CC[C@@]1([H])c2nc3ccc4cc5-c6ccc(cc6COc5cc4c3[nH]2)-c7cnc([C@]8([H])C[C@@]([H])(CN8C(=O)[C@@]([H])(c9ccccc9)N=C(O)OC)COC)[nH]7)N=C(O)OC

InChI

InChIKey=FHCUMDQMBHQXKK-CDIODLITSA-N
InChI=1S/C49H54N8O8/c1-26(2)41(54-48(60)63-5)47(59)57-27(3)12-17-38(57)45-51-36-16-14-30-20-35-33-15-13-31(19-32(33)25-65-40(35)21-34(30)43(36)53-45)37-22-50-44(52-37)39-18-28(24-62-4)23-56(39)46(58)42(55-49(61)64-6)29-10-8-7-9-11-29/h7-11,13-16,19-22,26-28,38-39,41-42H,12,17-18,23-25H2,1-6H3,(H,50,52)(H,51,53)(H,54,60)(H,55,61)/t27-,28-,38-,39-,41-,42+/m0/s1

HIDE SMILES / InChI

Molecular Formula C49H54N8O8
Molecular Weight 883.0037
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 6 / 6
E/Z Centers 0
Optical Activity UNSPECIFIED

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Epclusa

Approved Use

EPCLUSA is a fixed-dose combination of sofosbuvir, a hepatitis C virus (HCV) nucleotide analog NS5B polymerase inhibitor, and velpatasvir, an HCV NS5A inhibitor, and is indicated for the treatment of adult patients with chronic HCV genotype 1, 2, 3, 4, 5 or 6 infection.

Launch Date

1467072000000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
28.3 ng/mL
5 mg 1 times / day multiple, oral
dose: 5 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
411 ng/mL
50 mg 1 times / day multiple, oral
dose: 50 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
669 ng/mL
150 mg 1 times / day multiple, oral
dose: 150 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1200 ng/mL
450 mg 1 times / day multiple, oral
dose: 450 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
22.4 ng/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
371 ng/mL
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
398 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
608 ng/mL
150 mg single, oral
dose: 150 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
575 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
800 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: LOW-FAT
1120 ng/mL
450 mg single, oral
dose: 450 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
172 ng × h/mL
5 mg 1 times / day multiple, oral
dose: 5 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
3030 ng × h/mL
50 mg 1 times / day multiple, oral
dose: 50 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
4890 ng × h/mL
150 mg 1 times / day multiple, oral
dose: 150 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
9510 ng × h/mL
450 mg 1 times / day multiple, oral
dose: 450 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
159 ng × h/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
3020 ng × h/mL
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
3620 ng × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
4980 ng × h/mL
150 mg single, oral
dose: 150 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
5060 ng × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
7120 ng × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: LOW-FAT
9580 ng × h/mL
450 mg single, oral
dose: 450 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
13.7 h
5 mg 1 times / day multiple, oral
dose: 5 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
13 h
50 mg 1 times / day multiple, oral
dose: 50 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
15.2 h
150 mg 1 times / day multiple, oral
dose: 150 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
11.7 h
450 mg 1 times / day multiple, oral
dose: 450 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
11.2 h
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
13.6 h
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
14.2 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
16.2 h
150 mg single, oral
dose: 150 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
15.7 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
16.7 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: LOW-FAT
15 h
450 mg single, oral
dose: 450 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VELPATASVIR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
0.3%
unknown, unknown
VELPATASVIR plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
150 mg 1 times / day multiple, oral
Highest studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
unhealthy, 49 years (range: 28–63 years)
Health Status: unhealthy
Age Group: 49 years (range: 28–63 years)
Sex: M+F
Sources:
Disc. AE: Nausea...
Other AEs: Headache, Nausea...
AEs leading to
discontinuation/dose reduction:
Nausea (3.2%)
Other AEs:
Headache (12.9%)
Nausea (6.5%)
Vomiting (6.5%)
Cough (3.2%)
Hypertension (3.2%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Headache 12.9%
150 mg 1 times / day multiple, oral
Highest studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
unhealthy, 49 years (range: 28–63 years)
Health Status: unhealthy
Age Group: 49 years (range: 28–63 years)
Sex: M+F
Sources:
Cough 3.2%
150 mg 1 times / day multiple, oral
Highest studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
unhealthy, 49 years (range: 28–63 years)
Health Status: unhealthy
Age Group: 49 years (range: 28–63 years)
Sex: M+F
Sources:
Hypertension 3.2%
150 mg 1 times / day multiple, oral
Highest studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
unhealthy, 49 years (range: 28–63 years)
Health Status: unhealthy
Age Group: 49 years (range: 28–63 years)
Sex: M+F
Sources:
Nausea 3.2%
Disc. AE
150 mg 1 times / day multiple, oral
Highest studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
unhealthy, 49 years (range: 28–63 years)
Health Status: unhealthy
Age Group: 49 years (range: 28–63 years)
Sex: M+F
Sources:
Nausea 6.5%
150 mg 1 times / day multiple, oral
Highest studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
unhealthy, 49 years (range: 28–63 years)
Health Status: unhealthy
Age Group: 49 years (range: 28–63 years)
Sex: M+F
Sources:
Vomiting 6.5%
150 mg 1 times / day multiple, oral
Highest studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
unhealthy, 49 years (range: 28–63 years)
Health Status: unhealthy
Age Group: 49 years (range: 28–63 years)
Sex: M+F
Sources:
PubMed

PubMed

TitleDatePubMed
Sofosbuvir/Velpatasvir: A Review in Chronic Hepatitis C.
2016 Oct
Preclinical Pharmacokinetics and First-in-Human Pharmacokinetics, Safety, and Tolerability of Velpatasvir, a Pangenotypic Hepatitis C Virus NS5A Inhibitor, in Healthy Subjects.
2017 May
Patents

Sample Use Guides

Recommended dosage: One tablet (400 mg of sofosbuvir and
Route of Administration: Oral
Velpatasvir had mean EC50
Substance Class Chemical
Created
by admin
on Sat Jun 26 13:35:18 UTC 2021
Edited
by admin
on Sat Jun 26 13:35:18 UTC 2021
Record UNII
KCU0C7RS7Z
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
VELPATASVIR
INN   USAN   WHO-DD  
USAN   INN  
Official Name English
VELPATASVIR [MI]
Common Name English
VELPATASVIR [INN]
Common Name English
VELPATASVIR [WHO-DD]
Common Name English
EPCLUSA COMPONENT VELPATASVIR
Brand Name English
VELPATASVIR COMPONENT OF EPCLUSA
Brand Name English
VELPATASVIR [USAN]
Common Name English
VOSEVI COMPONENT VELPATASVIR
Common Name English
VELPATASVIR COMPONENT OF VOSEVI
Common Name English
VELPATASVIR [ORANGE BOOK]
Common Name English
GS-5816
Code English
Classification Tree Code System Code
FDA ORPHAN DRUG 554816
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
NCI_THESAURUS C281
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
WHO-ATC J05AP56
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
NDF-RT N0000191256
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
NCI_THESAURUS C783
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
WHO-ATC J05AP55
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
Code System Code Type Description
LACTMED
Velpatasvir
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
PRIMARY
NDF-RT
N0000190107
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
PRIMARY Organic Anion Transporting Polypeptide 1B1 Inhibitors [MoA]
DRUG CENTRAL
5154
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
PRIMARY
FDA UNII
KCU0C7RS7Z
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
PRIMARY
NDF-RT
N0000190108
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
PRIMARY Organic Anion Transporting Polypeptide 1B3 Inhibitors [MoA]
CAS
1377049-84-7
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
PRIMARY
ChEMBL
CHEMBL3545062
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
PRIMARY
NDF-RT
N0000190113
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
PRIMARY Breast Cancer Resistance Protein Inhibitors [MoA]
RXCUI
1799206
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
PRIMARY
NDF-RT
N0000190109
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
PRIMARY Organic Anion Transporting Polypeptide 2B1 Inhibitors [MoA]
NDF-RT
N0000185503
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
PRIMARY P-Glycoprotein Inhibitors [MoA]
MERCK INDEX
M11941
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
PRIMARY
PUBCHEM
67683363
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
PRIMARY
NCI_THESAURUS
C152851
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
PRIMARY
INN
9960
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
PRIMARY
DRUG BANK
DB11613
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
PRIMARY
EVMPD
SUB180213
Created by admin on Sat Jun 26 13:35:18 UTC 2021 , Edited by admin on Sat Jun 26 13:35:18 UTC 2021
PRIMARY
Related Record Type Details
TRANSPORTER -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
BINDER->LIGAND
BINDING
TRANSPORTER -> INHIBITOR
IC50
TRANSPORTER -> INHIBITOR
IC50
METABOLIC ENZYME -> SUBSTRATE
TRANSPORTER -> INHIBITOR
inhibit 30% at 10 ?M
IC50
TRANSPORTER -> INHIBITOR
IC50
TRANSPORTER -> SUBSTRATE
TRANSPORTER -> INHIBITOR
IC50
METABOLIC ENZYME -> SUBSTRATE
EXCRETED UNCHANGED
AMOUNT EXCRETED
FECAL
TRANSPORTER -> SUBSTRATE
IC50
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Blood-to-plasma ratio PHARMACOKINETIC
Tmax PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC