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Details

Stereochemistry ACHIRAL
Molecular Formula C25H26N7O8P
Molecular Weight 583.4908
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of FOSTEMSAVIR

SMILES

Cc1ncn(-c2c3c(c(cn3COP(=O)(O)O)C(=O)C(=O)N4CCN(CC4)C(=O)c5ccccc5)c(cn2)OC)n1

InChI

InChIKey=SWMDAPWAQQTBOG-UHFFFAOYSA-N
InChI=1S/C25H26N7O8P/c1-16-27-14-32(28-16)23-21-20(19(39-2)12-26-23)18(13-31(21)15-40-41(36,37)38)22(33)25(35)30-10-8-29(9-11-30)24(34)17-6-4-3-5-7-17/h3-7,12-14H,8-11,15H2,1-2H3,(H2,36,37,38)

HIDE SMILES / InChI
Fostemsavir (BMS-663068) is an investigational attachment inhibitor with a unique mechanism of action. It is a prodrug of temsavir, which binds to HIV envelope glycoprotein 120 (gp120), thereby preventing viral attachment to the host CD4 cell surface receptor. In the absence of effective binding of HIV gp120 with the host CD4 receptor, HIV does not enter the host cell. Because fostemsavir has a novel mechanism of action, the drug should have full activity against HIV strains that have developed resistance to other classes of antiretroviral medications. In a phase 2b study of treatment-experienced individuals, fostemsavir appeared to be well tolerated. Phase 3 studies are ongoing.

Originator

Curator's Comment:: # Bristol-Myers Squibb

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1770 ng/mL
600 mg 2 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: other antiretroviral drugs
TEMSAVIR plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
3.39 μg/mL
1200 mg 2 times / day multiple, oral
dose: 1200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEMSAVIR plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: FED
2.55 ug/mL
1200 mg single, oral
dose: 1200 mg
route of administration: oral
experiment type: single
co-administered:
TEMSAVIR plasma
Homo sapiens
3.18 ug/mL
1200 mg 1 times / 12 hours multiple, oral
dose: 1200 mg
route of administration: oral
experiment type: multiple
co-administered:
TEMSAVIR plasma
Homo sapiens
3.38999999999999 ug/mL
1200 mg 1 times / 12 hours multiple, oral
dose: 1200 mg
route of administration: oral
experiment type: multiple
co-administered:
TEMSAVIR plasma
Homo sapiens
3.61 ug/mL
1200 mg 1 times / 12 hours multiple, oral
dose: 1200 mg
route of administration: oral
experiment type: multiple
co-administered:
TEMSAVIR plasma
Homo sapiens
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
12900 ng × h/mL
600 mg 2 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: other antiretroviral drugs
TEMSAVIR plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
42.6 μg × h/mL
1200 mg 2 times / day multiple, oral
dose: 1200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
TEMSAVIR plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: FED
13.8 ug*h/mL
1200 mg single, oral
dose: 1200 mg
route of administration: oral
experiment type: single
co-administered:
TEMSAVIR plasma
Homo sapiens
19.5 ug*h/mL
1200 mg 1 times / 12 hours multiple, oral
dose: 1200 mg
route of administration: oral
experiment type: multiple
co-administered:
TEMSAVIR plasma
Homo sapiens
22.5 ug*h/mL
1200 mg 1 times / 12 hours multiple, oral
dose: 1200 mg
route of administration: oral
experiment type: multiple
co-administered:
TEMSAVIR plasma
Homo sapiens
42.6 ug*h/mL
1200 mg 1 times / 12 hours multiple, oral
dose: 1200 mg
route of administration: oral
experiment type: multiple
co-administered:
TEMSAVIR plasma
Homo sapiens
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
11 h
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEMSAVIR plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
26.9%
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TEMSAVIR plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Disc. AE: Immune reconstitution inflammatory syndrome...
Other AEs: Nausea, Diarrhea...
AEs leading to
discontinuation/dose reduction:
Immune reconstitution inflammatory syndrome (grade 3, 3%)
Other AEs:
Nausea (grade 1-4, 10%)
Diarrhea (grade 1-4, 4%)
Headache (grade 1-4, 4%)
Abdominal pain (grade 1-4, 3%)
Dyspepsia (grade 1-4, 3%)
Fatigue (grade 1-4, 3%)
Rash (grade 1-4, 3%)
Sleep disturbance (grade 1-4, 3%)
Immune reconstitution inflammatory syndrome (grade 1-4, 2%)
Somnolence (grade 1-4, 2%)
Vomiting (grade 1-4, 2%)
ALT increased (grade 3-4, 5%)
AST increased (grade 3-4, 4%)
Direct bilirubin increased (grade 3, 7%)
Bilirubin increased (grade 3-4, 3%)
Creatinine increased (grade 3-4, 19%)
Creatine kinase increased (grade 3-4, 2%)
Hemoglobin decreased (grade 3-4, 6%)
Hyperglycemia (grade 3-4, 4%)
Lipase increased (grade 3-4, 5%)
Neutrophils reduced (grade 3-4, 4%)
Blood triglycerides increased (grade 3-4, 5%)
Sources:
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
healthy, 18-49 years
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Sources:
Other AEs: Scleral icterus, Abdominal pain...
Other AEs:
Scleral icterus (27.8%)
Abdominal pain (11.1%)
Headache (13.9%)
Dizziness (5.6%)
Nausea (8.3%)
Musculoskeletal chest pain (2.8%)
Sources:
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
healthy, 18-49 years
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Sources:
Other AEs: Headache...
Other AEs:
Headache (5.6%)
Sources:
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
healthy, 18-49 years
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Sources:
Other AEs: Scleral icterus, Abdominal pain...
Other AEs:
Scleral icterus (5.6%)
Abdominal pain (5.6%)
Nausea (5.6%)
Sources:
1050 mg 2 times / day steady, oral
Studied dose
Dose: 1050 mg, 2 times / day
Route: oral
Route: steady
Dose: 1050 mg, 2 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Other AEs: Headache...
Other AEs:
Headache (grade 1, 14%)
Sources:
1200 mg 1 times / day steady, oral
Studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Disc. AE: Disseminated tuberculosis, Back pain...
AEs leading to
discontinuation/dose reduction:
Disseminated tuberculosis (2%)
Back pain (2%)
Sources:
400 mg 2 times / day steady, oral
Studied dose
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Disc. AE: Ischaemia...
AEs leading to
discontinuation/dose reduction:
Ischaemia (2%)
Sources:
800 mg 2 times / day steady, oral
Studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: steady
Dose: 800 mg, 2 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Disc. AE: Bone tuberculosis, Acute renal failure...
AEs leading to
discontinuation/dose reduction:
Bone tuberculosis (2%)
Acute renal failure (2%)
Sources:
2400 mg 2 times / day steady, oral
Highest studied dose
Dose: 2400 mg, 2 times / day
Route: oral
Route: steady
Dose: 2400 mg, 2 times / day
Sources:
healthy
Health Status: healthy
Sources:
Other AEs: QT interval prolonged...
Other AEs:
QT interval prolonged
Sources:
AEs

AEs

AESignificanceDosePopulation
Nausea grade 1-4, 10%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Immune reconstitution inflammatory syndrome grade 1-4, 2%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Somnolence grade 1-4, 2%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Vomiting grade 1-4, 2%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Abdominal pain grade 1-4, 3%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Dyspepsia grade 1-4, 3%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Fatigue grade 1-4, 3%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Rash grade 1-4, 3%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Sleep disturbance grade 1-4, 3%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Diarrhea grade 1-4, 4%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Headache grade 1-4, 4%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Immune reconstitution inflammatory syndrome grade 3, 3%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Direct bilirubin increased grade 3, 7%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Creatinine increased grade 3-4, 19%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Creatine kinase increased grade 3-4, 2%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Bilirubin increased grade 3-4, 3%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
AST increased grade 3-4, 4%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Hyperglycemia grade 3-4, 4%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Neutrophils reduced grade 3-4, 4%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
ALT increased grade 3-4, 5%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Blood triglycerides increased grade 3-4, 5%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Lipase increased grade 3-4, 5%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Hemoglobin decreased grade 3-4, 6%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 17-43 years
Health Status: unhealthy
Age Group: 17-43 years
Sex: M+F
Sources:
Abdominal pain 11.1%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
healthy, 18-49 years
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Sources:
Headache 13.9%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
healthy, 18-49 years
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Sources:
Musculoskeletal chest pain 2.8%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
healthy, 18-49 years
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Sources:
Scleral icterus 27.8%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
healthy, 18-49 years
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Sources:
Dizziness 5.6%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
healthy, 18-49 years
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Sources:
Nausea 8.3%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
healthy, 18-49 years
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Sources:
Headache 5.6%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
healthy, 18-49 years
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Sources:
Abdominal pain 5.6%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
healthy, 18-49 years
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Sources:
Nausea 5.6%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
healthy, 18-49 years
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Sources:
Scleral icterus 5.6%
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
healthy, 18-49 years
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Sources:
Headache grade 1, 14%
1050 mg 2 times / day steady, oral
Studied dose
Dose: 1050 mg, 2 times / day
Route: oral
Route: steady
Dose: 1050 mg, 2 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Back pain 2%
Disc. AE
1200 mg 1 times / day steady, oral
Studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Disseminated tuberculosis 2%
Disc. AE
1200 mg 1 times / day steady, oral
Studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Ischaemia 2%
Disc. AE
400 mg 2 times / day steady, oral
Studied dose
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Acute renal failure 2%
Disc. AE
800 mg 2 times / day steady, oral
Studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: steady
Dose: 800 mg, 2 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Bone tuberculosis 2%
Disc. AE
800 mg 2 times / day steady, oral
Studied dose
Dose: 800 mg, 2 times / day
Route: oral
Route: steady
Dose: 800 mg, 2 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
QT interval prolonged
2400 mg 2 times / day steady, oral
Highest studied dose
Dose: 2400 mg, 2 times / day
Route: oral
Route: steady
Dose: 2400 mg, 2 times / day
Sources:
healthy
Health Status: healthy
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 110 uM]
no [IC50 32.8 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >250 uM]
no [IC50 >250 uM]
no [IC50 >40 uM]
no [IC50 >40 uM]
no [IC50 >40 uM]
no [IC50 >40 uM]
no [IC50 >40 uM]
no [IC50 >40 uM]
no [IC50 >40 uM]
no [IC50 >40 uM]
no [IC50 >50 uM]
no [IC50 >50 uM]
no [IC50 >50 uM]
no [IC50 >50 uM]
no [Inhibition 25 uM]
no
no
no
no
no
yes [IC50 12.2 uM]
yes [IC50 18.5 uM]
yes
yes
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
minor
no
no
no
no
no
no
no
no
no
no
no
no
no
yes
yes
yes
yes
yes (co-administration study)
Comment: coadministration of fostemsavir with rifampin significantly decreases temsavir plasma concentrations, reduced temsavir AUC by 80%; coadministration of fostemsavir with drugs that are strong CYP3A inducers result in decreased concentrations of temsavir.
Page: 35, 111, 112, 113
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Safety and efficacy of the HIV-1 attachment inhibitor prodrug fostemsavir in antiretroviral-experienced subjects: week 48 analysis of AI438011, a Phase IIb, randomized controlled trial.
2017
[What can new substances offer?]
2017 Jun
Patents

Sample Use Guides

A phase 2b trial enrolled treatment-experienced adults with HIV infection and randomized study subjects to one of four doses of fostemsavir (400 mg twice daily, 800 mg twice daily, 600 mg once daily, or 1200 mg once daily).
Route of Administration: Oral
BMS-626529 (an active moiety of BMS-663068) exhibits an average EC50 against LAI of 0.7 +/-0.4 nM.
Name Type Language
FOSTEMSAVIR
INN   USAN   WHO-DD  
USAN   INN  
Official Name English
FOSTEMSAVIR [INN]
Common Name English
BMS-663068
Code English
(3-((4-BENZOYLPIPERAZIN-1-YL)-OXOACETYL)-4-METHOXY- 7-(3-METHYL-1H-1,2,4-TRIAZOL-1-YL)-1H-PYRROLO(2,3-C)PYRIDIN- 1-YL)METHYL DIHYDROGEN PHOSPHATE
Systematic Name English
FOSTEMSAVIR [USAN]
Common Name English
PIPERAZINE, 1-BENZOYL-4-((4-METHOXY-7-(3-METHYL-1H-1,2,4-TRIAZOL-1-YL)-1-((PHOSPHONOOXY)METHYL)-1H-PYRROLO(2,3-C)PYRIDIN-3-YL)OXOACETYL)-
Systematic Name English
FOSTEMSAVIR [WHO-DD]
Common Name English
BMS-663068 FREE ACID
Common Name English
Code System Code Type Description
PUBCHEM
11319217
Created by admin on Sat Jun 26 02:58:56 UTC 2021 , Edited by admin on Sat Jun 26 02:58:56 UTC 2021
PRIMARY
RXCUI
2380373
Created by admin on Sat Jun 26 02:58:56 UTC 2021 , Edited by admin on Sat Jun 26 02:58:56 UTC 2021
PRIMARY
DRUG BANK
DB11796
Created by admin on Sat Jun 26 02:58:56 UTC 2021 , Edited by admin on Sat Jun 26 02:58:56 UTC 2021
PRIMARY
ChEMBL
CHEMBL3301594
Created by admin on Sat Jun 26 02:58:56 UTC 2021 , Edited by admin on Sat Jun 26 02:58:56 UTC 2021
PRIMARY
INN
10292
Created by admin on Sat Jun 26 02:58:56 UTC 2021 , Edited by admin on Sat Jun 26 02:58:56 UTC 2021
PRIMARY
FDA UNII
97IQ273H4L
Created by admin on Sat Jun 26 02:58:56 UTC 2021 , Edited by admin on Sat Jun 26 02:58:56 UTC 2021
PRIMARY
CAS
864953-29-7
Created by admin on Sat Jun 26 02:58:56 UTC 2021 , Edited by admin on Sat Jun 26 02:58:56 UTC 2021
PRIMARY
EPA CompTox
864953-29-7
Created by admin on Sat Jun 26 02:58:56 UTC 2021 , Edited by admin on Sat Jun 26 02:58:56 UTC 2021
PRIMARY
NCI_THESAURUS
C175066
Created by admin on Sat Jun 26 02:58:56 UTC 2021 , Edited by admin on Sat Jun 26 02:58:56 UTC 2021
PRIMARY