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

Details

Stereochemistry ACHIRAL
Molecular Formula C24H23N7O4
Molecular Weight 473.4839
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TEMSAVIR

SMILES

COC1=CN=C(N2C=NC(C)=N2)C3=C1C(=CN3)C(=O)C(=O)N4CCN(CC4)C(=O)C5=CC=CC=C5

InChI

InChIKey=QRPZBKAMSFHVRW-UHFFFAOYSA-N
InChI=1S/C24H23N7O4/c1-15-27-14-31(28-15)22-20-19(18(35-2)13-26-22)17(12-25-20)21(32)24(34)30-10-8-29(9-11-30)23(33)16-6-4-3-5-7-16/h3-7,12-14,25H,8-11H2,1-2H3

HIDE SMILES / InChI
Molecular Formula C24H23N7O4
Molecular Weight 473.4839
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/22547625 https://www.ncbi.nlm.nih.gov/pubmed/23774428

Temsavir (BMS-626529) is an attachment inhibitor (AI) in clinical development (administered as prodrug BMS-663068) that binds to HIV-1 gp120. Temsavir displays in vitro activity against HIV-1 envelopes with C-C chemokine receptor type 5 (CCR5-), C-X-C chemokine receptor type 4 (CXCR4), and dual tropism. It also is active against almost all HIV-1 subtypes tested except for subtype CRF01-AE and possibly group O. Temsavir can inhibit both CD4-induced and CD4-independent formation of the "open state" four-stranded gp120 bridging sheet, and the subsequent formation and exposure of the chemokine co-receptor binding site. This unique mechanism of action prevents the initial interaction of HIV-1 with the host CD4+ T cell, and subsequent HIV-1 binding and entry. Temsavir is administered as a phosphonooxymethyl ester prodrug (BMS-663068), which was developed to improve the solubility and dissolution of Temsavir. Temsavir is currently being investigated clinically through the use of the prodrug BMS-663068, and a Phase III study of BMS-663068 in HIV-1-infected treatment-experienced subjects is ongoing (NCT02362503).

Originator

Bristol-Myers Squibb
145
Curator's Comment: # Bristol-Myers Squibb

Approval Year

2020
742
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
Inhibitor
8297
 2.26 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Phase III
656
Unknown

Approved Use

Unknown
Primary
Phase III
656
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1770 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
600 mg 2 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: other antiretroviral drugs
other antiretroviral drugs
 TEMSAVIR plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
3.39 μg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/22896665/
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
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01009814
1200 mg single, oral
dose: 1200 mg
route of administration: oral
experiment type: single
co-administered:
TEMSAVIR plasma
Homo sapiens
3.18 ug/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01009814
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
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01009814
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
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01009814
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
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
600 mg 2 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: other antiretroviral drugs
other antiretroviral drugs
 TEMSAVIR plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
42.6 μg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/22896665/
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
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01009814
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
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01009814
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
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01009814
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
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01009814
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
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Co-administed with::
ritonavir(100 mg; oral; 1/day)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
healthy, 18-49 years
n = 18
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Population Size: 18
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
Other AEs: Scleral icterus, Abdominal pain...
Other AEs:
Scleral icterus (5.6%)
Abdominal pain (5.6%)
Nausea (5.6%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Co-administed with::
atazanavir(300 mg; oral; 1/day)
ritonavir(100 mg; oral; 1/day)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
healthy, 18-49 years
n = 36
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Population Size: 36
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
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:
https://pubmed.ncbi.nlm.nih.gov/25870057/
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:
https://pubmed.ncbi.nlm.nih.gov/25870057/
healthy, 18-49 years
n = 36
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Population Size: 36
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
Other AEs: Headache...
Other AEs:
Headache (5.6%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
1050 mg 2 times / day steady, oral (mean)
Studied dose
Dose: 1050 mg, 2 times / day
Route: oral
Route: steady
Dose: 1050 mg, 2 times / day
Co-administed with::
raltegravir and tenofovir disoproxil fumarate
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
unhealthy, adults
n = 200
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: adults
Sex: M+F
Population Size: 200
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
Other AEs: Headache...
Other AEs:
Headache (grade 1, 14%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
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
Co-administed with::
raltegravir and tenofovir disoproxil fumarate
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
unhealthy, adults
n = 50
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: adults
Sex: M+F
Population Size: 50
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
Disc. AE: Disseminated tuberculosis, Back pain...
AEs leading to
discontinuation/dose reduction:
Disseminated tuberculosis (2%)
Back pain (2%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
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
Co-administed with::
raltegravir and tenofovir disoproxil fumarate
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
unhealthy, adults
n = 50
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: adults
Sex: M+F
Population Size: 50
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
Disc. AE: Ischaemia...
AEs leading to
discontinuation/dose reduction:
Ischaemia (2%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
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
Co-administed with::
raltegravir and tenofovir disoproxil fumarate
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
unhealthy, adults
n = 49
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: adults
Sex: M+F
Population Size: 49
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
Disc. AE: Bone tuberculosis, Acute renal failure...
AEs leading to
discontinuation/dose reduction:
Bone tuberculosis (2%)
Acute renal failure (2%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
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:
https://www.fda.gov/media/140641/download
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
https://www.fda.gov/media/140641/download
Other AEs: QT interval prolonged...
Other AEs:
QT interval prolonged
Sources:
https://www.fda.gov/media/140641/download
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
optimized background therapy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
unhealthy, 17-43 years
n = 271
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: 17-43 years
Sex: M+F
Population Size: 271
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf
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
Co-administed with::
ritonavir(100 mg; oral; 1/day)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
healthy, 18-49 years
n = 18
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Population Size: 18
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
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
Co-administed with::
ritonavir(100 mg; oral; 1/day)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
healthy, 18-49 years
n = 18
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Population Size: 18
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
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
Co-administed with::
ritonavir(100 mg; oral; 1/day)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
healthy, 18-49 years
n = 18
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Population Size: 18
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
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
Co-administed with::
atazanavir(300 mg; oral; 1/day)
ritonavir(100 mg; oral; 1/day)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
healthy, 18-49 years
n = 36
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Population Size: 36
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
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
Co-administed with::
atazanavir(300 mg; oral; 1/day)
ritonavir(100 mg; oral; 1/day)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
healthy, 18-49 years
n = 36
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Population Size: 36
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
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
Co-administed with::
atazanavir(300 mg; oral; 1/day)
ritonavir(100 mg; oral; 1/day)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
healthy, 18-49 years
n = 36
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Population Size: 36
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
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
Co-administed with::
atazanavir(300 mg; oral; 1/day)
ritonavir(100 mg; oral; 1/day)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
healthy, 18-49 years
n = 36
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Population Size: 36
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
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
Co-administed with::
atazanavir(300 mg; oral; 1/day)
ritonavir(100 mg; oral; 1/day)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
healthy, 18-49 years
n = 36
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Population Size: 36
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
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
Co-administed with::
atazanavir(300 mg; oral; 1/day)
ritonavir(100 mg; oral; 1/day)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
healthy, 18-49 years
n = 36
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Population Size: 36
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
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:
https://pubmed.ncbi.nlm.nih.gov/25870057/
healthy, 18-49 years
n = 36
Health Status: healthy
Age Group: 18-49 years
Sex: M+F
Population Size: 36
Sources:
https://pubmed.ncbi.nlm.nih.gov/25870057/
Headache grade 1, 14%
1050 mg 2 times / day steady, oral (mean)
Studied dose
Dose: 1050 mg, 2 times / day
Route: oral
Route: steady
Dose: 1050 mg, 2 times / day
Co-administed with::
raltegravir and tenofovir disoproxil fumarate
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
unhealthy, adults
n = 200
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: adults
Sex: M+F
Population Size: 200
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
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
Co-administed with::
raltegravir and tenofovir disoproxil fumarate
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
unhealthy, adults
n = 50
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: adults
Sex: M+F
Population Size: 50
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
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
Co-administed with::
raltegravir and tenofovir disoproxil fumarate
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
unhealthy, adults
n = 50
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: adults
Sex: M+F
Population Size: 50
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
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
Co-administed with::
raltegravir and tenofovir disoproxil fumarate
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
unhealthy, adults
n = 50
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: adults
Sex: M+F
Population Size: 50
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
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
Co-administed with::
raltegravir and tenofovir disoproxil fumarate
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
unhealthy, adults
n = 49
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: adults
Sex: M+F
Population Size: 49
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
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
Co-administed with::
raltegravir and tenofovir disoproxil fumarate
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
unhealthy, adults
n = 49
Health Status: unhealthy
Condition: HIV-1 infection
Age Group: adults
Sex: M+F
Population Size: 49
Sources:
https://pubmed.ncbi.nlm.nih.gov/26423650/
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:
https://www.fda.gov/media/140641/download
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
https://www.fda.gov/media/140641/download
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
1587

inducer
781
substrate
1037

inhibitor
1767
substrate
1217

inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
OATP1B1
788

OATP1B3
706

CYP
111

UGT
35

BCRP
699

MATE2
263

CYP1A2
1524

CYP2B6
810

CYP2C8
911

CYP2C19
1478

CYP2A6
707

UGT1A1
204

UGT1A4
77

UGT1A9
116

UGT1A6
108

UGT2B7
146

P-gp
1461

OAT1
599

OAT3
642

MATE1
306

MRP2
383

NTCP
34

OCT2
647

BSEP
402

OCT1
512
CYP3A
191

P-gp
1537

BCRP
561

esterase
72

UGT
192

CYP1A1
349

CYP1A2
1054

CYP2A6
543

CYP1B1
92

CYP2B6
664

CYP2C8
693

CYP2C19
991

FMO3
67

CYP4A11
119

CYP2E1
667

CYP3A5
395
CYP1A2
701

CYP2B6
547
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
OAT1
603
 no [IC50 110 uM]
temsavir
5
OCT1
543
 no [IC50 32.8 uM]
temsavir
5
UGT1A6
141
 no [IC50 >10 uM]
temsavir
5
UGT1A9
121
 no [IC50 >10 uM]
temsavir
5
UGT2B7
157
 no [IC50 >10 uM]
UGT2B7
157
 no [IC50 >10 uM]
temsavir
5
OCT2
648
 no [IC50 >100 uM]
temsavir
5
UGT1A1
254
 no [IC50 >100 uM]
UGT1A1
254
 no [IC50 >100 uM]
temsavir
5
UGT1A4
80
 no [IC50 >100 uM]
UGT1A4
80
 no [IC50 >100 uM]
temsavir
5
UGT1A6
141
 no [IC50 >100 uM]
UGT1A9
121
 no [IC50 >100 uM]
BCRP
773
 no [IC50 >250 uM]
P-gp
1650
 no [IC50 >250 uM]
CYP1A2
1692
 no [IC50 >40 uM]
temsavir
5
CYP2A6
739
 no [IC50 >40 uM]
temsavir
5
CYP2B6
1001
 no [IC50 >40 uM]
temsavir
5
CYP2C19
1553
 no [IC50 >40 uM]
temsavir
5
CYP2C8
965
 no [IC50 >40 uM]
temsavir
5
CYP2C9
1819
 no [IC50 >40 uM]
temsavir
5
CYP2D6
1891
 no [IC50 >40 uM]
temsavir
5
CYP3A4
1925
 no [IC50 >40 uM]
temsavir
5
BSEP
403
 no [IC50 >50 uM]
temsavir
5
MRP2
475
 no [IC50 >50 uM]
temsavir
5
NTCP
35
 no [IC50 >50 uM]
temsavir
5
OAT3
644
 no [IC50 >50 uM]
temsavir
5
P-gp
1650
 no [Inhibition 25 uM]
temsavir
5
CYP
147
 no
temsavir
5
CYP1A2
1692
 no
temsavir
5
CYP2B6
1001
 no
temsavir
5
CYP3A4
1925
 no
temsavir
5
UGT
59
 no
temsavir
5
MATE2
263
 yes [IC50 12.2 uM]
temsavir
5
MATE1
308
 yes [IC50 18.5 uM]
temsavir
5
BCRP
773
 yes
temsavir
5
OATP1B1
803
 yes
temsavir
5
OATP1B3
715
 yes
temsavir
5
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
UGT
192
 minor
temsavir
5
CYP1A1
349
 no
temsavir
5
CYP1A2
1054
 no
temsavir
5
CYP1B1
92
 no
temsavir
5
CYP2A6
543
 no
temsavir
5
CYP2B6
664
 no
temsavir
5
CYP2C19
991
 no
temsavir
5
CYP2C8
693
 no
temsavir
5
CYP2C9
1037
 no
temsavir
5
CYP2D6
1217
 no
temsavir
5
CYP2E1
667
 no
temsavir
5
CYP3A5
395
 no
temsavir
5
CYP4A11
119
 no
temsavir
5
FMO3
67
 no
temsavir
5
BCRP
561
 yes
temsavir
5
P-gp
1537
 yes
temsavir
5
esterase
72
 yes
temsavir
5
CYP3A
191
 yes
temsavir
5
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

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
temsavir
5
Sourcing

Sourcing

Vendor/AggregatorIDURL
001 Chemical
DY575616
https://www.001chemical.com/chem/864953-29-7
1PlusChem LLC
1P00FCG8
https://www.1pchem.com/search?query=1P00FCG8
AA Blocks
AA00GTZ5
https://www.aablocks.com/goods/Goods/detail?id=AA00GTZ5
AChemBlock
L13964
http://www.achemblock.com/catalogsearch/result/?q=L13964
AK Scientific
3501AH
https://aksci.com/item_detail.php?cat=3501AH
AK Scientific, Inc. (AKSCI)
3502AH
http://www.aksci.com/item_detail.php?cat=3502AH
Acadechem
ACDS-0781672
http://acadechemical.com/product/229218
Achemtek
0102-013953
http://www.achemtek.com/864953-29-7
Adooq BioScience
A15025
https://www.adooq.com/bms-663068.html
Ambinter
Amb22396014
http://www.ambinter.com/reference/22396014
Angene
AGN-PC-0TXRVI
http://www.angenechemical.com/productshow/AGN-PC-0TXRVI.html
Angene
AGN-PC-0WCXR0
http://www.angenechemical.com/productshow/AGN-PC-0WCXR0.html
ApexBio Technology
A3253
https://www.apexbt.com/catalogsearch/result/?q=A3253
AstaTech
43242
http://astatechinc.com/CPSResult.php?CRNO=43242
Aurora Fine Chemicals LLC
A24.141.513
http://online.aurorafinechemicals.com/info?ID=A24.141.513
Aurum Pharmatech LLC
W-5998
http://www.Aurumpharmatech.com/Product/ProductDetails/W_5998
BOC Sciences
864953-29-7
https://www.bocsci.com/bms-663068-cas-864953-29-7-item-84-463659.html
BioChemPartner
BCP13226
http://www.biochempartner.com/864953-29-7-BCP13226
BioCrick
BCC1428
http://www.biocrick.com/BMS-663068-BCC1428.html
Boerchem
BC600763
http://www.boerchem.com/?product_43597.html
Cayman Chemical
18413
http://www.caymanchem.com/app/template/Product.vm/catalog/18413
Chem Scene
CS-1059
http://www.chemscene.com/864953-29-7.html
Chem Scene
CS-0938
http://www.chemscene.com/goproductList/searchProductList?productObj=CS-0938
ChemShuttle
155599
https://www.chemshuttle.com/catalogsearch/result/?q=155599
Chemspace
CSSB00137314448
https://chem-space.com/CSSB00137314448
DC Chemicals
DC8163
http://www.dcchemicals.com/product_show-Fostemsavir_BMS_663068_.html
Debye Scientific
DA-35014
https://www.debyesci.com/index.php?id=product&ext[cno]=DA-35014
Excenen
EX-A2034
http://www.excenen.com/searchresultlist.php?id=EX-A2034
Excenen
EX-A1973
https://www.excenen.com/searchresultlist.php?id=864953-29-7
Hairui
FOXF012
http://www.hairuichem.com/en/product/864953-29-7.html
Hairui
FOXF01210
http://www.hairuichem.com/en/product/search.do?q=FOXF01210
KeyOrganics
AS-35292
http://www.keyorganicsinc.com/bionet/catalogsearch/result?q=AS-35292
MedChem Express
HY-15440A
https://www.medchemexpress.com/BMS-663068.html
MedChem Express
HY-15440
https://www.medchemexpress.com/search.html?q=HY-15440&ft=&fa=&fp=
MolPort
MolPort-039-137-511
https://www.molport.com/shop/molecule-link/MolPort-039-137-511
MolPort
MolPort-046-703-070
https://www.molport.com/shop/molecule-link/MolPort-046-703-070
Molcore
MC575616
https://www.molcore.com/product/864953-29-7
MuseChem
I005194
https://www.musechem.com/product/I005194.html
Selleck Chemicals
S7220
http://www.selleckchem.com/products/bms-663068.html
ShangHai Biochempartner
BCP09613
http://www.biochempartner.com/search_BCP09613
Smolecule
S528400
http://www.smolecule.com/products/s528400
Synblock Inc
SB11250
http://www.synblock.com/product/864953-29-7.html
THE BioTek
bt-268684
https://www.thebiotek.com/product/inhibitors/bt-268684
THE BioTek
bt-342630
https://www.thebiotek.com/product/others/bt-342630
THE BioTek
bt-464747
https://www.thebiotek.com/product/others/bt-464747
Toronto Research Chemicals
D449298
https://www.trc-canada.com/product-detail/?CatNum=D449298
Toronto Research Chemicals
T017900
https://www.trc-canada.com/product-detail/?CatNum=T017900
eMolecules
44811344
https://orderbb.emolecules.com/search/#?query=44811344
mcule
MCULE-6503554438
https://mcule.com/MCULE-6503554438/
PubMed

PubMed

TitleDatePubMed
In vitro antiviral characteristics of HIV-1 attachment inhibitor BMS-626529, the active component of the prodrug BMS-663068.
2012 Jul
Safety and efficacy of the HIV-1 attachment inhibitor prodrug BMS-663068 in treatment-experienced individuals: 24 week results of AI438011, a phase 2b, randomised controlled trial.
2015 Oct
Model-Based Phase 3 Dose Selection for HIV-1 Attachment Inhibitor Prodrug BMS-663068 in HIV-1-Infected Patients: Population Pharmacokinetics/Pharmacodynamics of the Active Moiety, BMS-626529.
2016 May
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
Current Status of the Pharmacokinetics and Pharmacodynamics of HIV-1 Entry Inhibitors and HIV Therapy.
2017 Oct 16
Patents

Patents

20050209246
6
20070155702
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Sample Use Guides

In Vivo Use Guide
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
In Vitro Use Guide
Curator's Comment: Temsavir (BMS-626529) had half-maximal effective concentration (EC(50)) values of <10 nM against the vast majority of HIV-1 viral isolates; however, susceptibility varied by >6 log(10), with half-maximal effective concentration values in the low pM range against the most susceptible viruses.
BMS-626529 (an active moiety of BMS-663068) exhibits an average EC50 against LAI of 0.7 +/-0.4 nM.
Substance Class Chemical
Created
by admin
on Sat Dec 16 17:22:00 GMT 2023
Edited
by admin
on Sat Dec 16 17:22:00 GMT 2023
Record UNII
4B6J53W8N3
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
TEMSAVIR
INN   USAN   WHO-DD  
INN   USAN  
Official Name English
1,2-ETHANEDIONE, 1-(4-BENZOYL-1-PIPERAZINYL)-2-(4-METHOXY-7-(3-METHYL-1H-1,2,4-TRIAZOL-1-YL)-1H-PYRROLO(2,3-C)PYRIDIN-3-YL)-
Systematic Name English
temsavir [INN]
Common Name English
TEMSAVIR [USAN]
Common Name English
BMS-626529
Code English
Temsavir [WHO-DD]
Common Name English
TEMSAVIR [MI]
Common Name English
PIPERAZINE, 1-BENZOYL-4-((4-METHOXY-7-(3-METHYL-1H-1,2,4-TRIAZOL-1-YL)-1H-PYRROLO(2,3-C)PYRIDIN-3-YL)OXOACETYL)-
Systematic Name English
Classification Tree Code System Code
NCI_THESAURUS C1660
Created by admin on Sat Dec 16 17:22:02 GMT 2023 , Edited by admin on Sat Dec 16 17:22:02 GMT 2023
Code System Code Type Description
ChEMBL
CHEMBL3301620
Created by admin on Sat Dec 16 17:22:02 GMT 2023 , Edited by admin on Sat Dec 16 17:22:02 GMT 2023
PRIMARY
CAS
701213-36-7
Created by admin on Sat Dec 16 17:22:02 GMT 2023 , Edited by admin on Sat Dec 16 17:22:02 GMT 2023
PRIMARY
MERCK INDEX
m12225
Created by admin on Sat Dec 16 17:22:02 GMT 2023 , Edited by admin on Sat Dec 16 17:22:02 GMT 2023
PRIMARY
FDA UNII
4B6J53W8N3
Created by admin on Sat Dec 16 17:22:02 GMT 2023 , Edited by admin on Sat Dec 16 17:22:02 GMT 2023
PRIMARY
EPA CompTox
DTXSID20462146
Created by admin on Sat Dec 16 17:22:02 GMT 2023 , Edited by admin on Sat Dec 16 17:22:02 GMT 2023
PRIMARY
USAN
ZZ-57
Created by admin on Sat Dec 16 17:22:02 GMT 2023 , Edited by admin on Sat Dec 16 17:22:02 GMT 2023
PRIMARY
PUBCHEM
11317439
Created by admin on Sat Dec 16 17:22:02 GMT 2023 , Edited by admin on Sat Dec 16 17:22:02 GMT 2023
PRIMARY
NCI_THESAURUS
C152553
Created by admin on Sat Dec 16 17:22:02 GMT 2023 , Edited by admin on Sat Dec 16 17:22:02 GMT 2023
PRIMARY
INN
9941
Created by admin on Sat Dec 16 17:22:02 GMT 2023 , Edited by admin on Sat Dec 16 17:22:02 GMT 2023
PRIMARY
DRUG BANK
DB14675
Created by admin on Sat Dec 16 17:22:02 GMT 2023 , Edited by admin on Sat Dec 16 17:22:02 GMT 2023
PRIMARY
SMS_ID
300000034446
Created by admin on Sat Dec 16 17:22:02 GMT 2023 , Edited by admin on Sat Dec 16 17:22:02 GMT 2023
PRIMARY
Related Record Type Details
ATP-BINDING CASSETTE SUB-FAMILY G MEMBER 2
TRANSPORTER -> SUBSTRATE
Drugs that induce or inhibit CYP3A, P-gp, and BCRP may affect temsavir plasma concentrations.
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
Drugs that induce or inhibit CYP3A, P-gp, and BCRP may affect temsavir plasma concentrations.
Structure of TEMSAVIR
EXCRETED UNCHANGED
FECAL
Structure of TEMSAVIR
EXCRETED UNCHANGED
URINE
OATP-8
TRANSPORTER -> INHIBITOR
HUMAN IMMUNODEFICIENCY VIRUS TYPE 1
TARGET ORGANISM->INHIBITOR
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> SUBSTRATE
Drugs that induce or inhibit CYP3A, P-gp, and BCRP may affect temsavir plasma concentrations.
OATP1B1
TRANSPORTER -> INHIBITOR
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
Related Record Type Details
Structure of FOSTEMSAVIR
PRODRUG -> METABOLITE ACTIVE
Related Record Type Details
Structure of TEMSAVIR
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Blood-to-plasma ratio PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC ORAL ADMINISTRATION

Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC ORAL ADMINISTRATION

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