fostemsavir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antivirals 5401 864953-29-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fostemsavir
  • fostemsavir tromethamine
  • BMS-663068
  • GSK3684934
  • rukobia
  • BMS-663068-03
  • GSK-3684934A
  • BMS-626529
  • BMS 626529
Fostemsavir is a prodrug without significant biochemical or antiviral activity that is hydrolyzed to the active moiety, temsavir, which is an HIV-1 attachment inhibitor. Temsavir binds directly to the gp120 subunit within the HIV-1 envelope glycoprotein gp160 and selectively inhibits the interaction between the virus and cellular CD4 receptors, thereby preventing attachment. Additionally, temsavir can inhibit gp120-dependent post-attachment steps required for viral entry into host cells.
  • Molecular weight: 583.50
  • Formula: C25H26N7O8P
  • CLOGP: -1.04
  • LIPINSKI: 2
  • HAC: 15
  • HDO: 2
  • TPSA: 182.21
  • ALOGS: -3.13
  • ROTB: 8

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
1.20 g O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Feb. 4, 2021 EMA ViiV HEALTHCARE B.V.
July 2, 2020 FDA ViiV Healthcare Company

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Virologic failure 25.34 19.76 3 3 3463 64495263

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J05AX29 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Other antivirals
MeSH PA D019380 Anti-HIV Agents
MeSH PA D000890 Anti-Infective Agents
MeSH PA D044966 Anti-Retroviral Agents
MeSH PA D000998 Antiviral Agents
MeSH PA D023581 HIV Fusion Inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Human immunodeficiency virus I infection indication 40780007
Drug induction of cytochrome p450 CYP3A enzyme contraindication 423236002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 600MG BASE RUKOBIA VIIV HLTHCARE N212950 July 2, 2020 RX TABLET, EXTENDED RELEASE ORAL July 2, 2025 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 4.66 CHEMBL
Envelope glycoprotein gp160 Viral envelope protein INHIBITOR Kd 9.08 SCIENTIFIC LITERATURE DRUG LABEL
Envelope glycoprotein gp160 [Cleaved into: Surface protein gp120 Unclassified Kd 9.08 CHEMBL

External reference:

IDSource
D10707 KEGG_DRUG
97IQ273H4L UNII
C4519220 UMLSCUI
CHEMBL3301594 ChEMBL_ID
11319217 PUBCHEM_CID
DB11796 DRUGBANK_ID
CHEMBL3301598 ChEMBL_ID
CHEMBL3301620 ChEMBL_ID
C584152 MESH_SUPPLEMENTAL_RECORD_UI
11100 IUPHAR_LIGAND_ID
2380373 RXNORM
336206 MMSL
38617 MMSL
d09591 MMSL
890266008 SNOMEDCT_US
890270000 SNOMEDCT_US
4039527 VANDF
11317439 PUBCHEM_CID
C3712177 UMLSCUI
018436 NDDF
018437 NDDF
C576364 MESH_SUPPLEMENTAL_RECORD_UI
10292 INN_ID
864953-39-9 SECONDARY_CAS_RN

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Rukobia HUMAN PRESCRIPTION DRUG LABEL 1 49702-250 TABLET, FILM COATED, EXTENDED RELEASE 600 mg ORAL NDA 27 sections