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

Stem definitionDrug idCAS RN
antivirals 5274 1611493-60-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • bictegravir
  • bictegravir sodium
  • GS-9883
  • GS-9883-01
Bictegravir inhibits the strand transfer activity of HIV-1 integrase (integrase strand transfer inhibitor; INSTI), an HIV-1 encoded enzyme that is required for viral replication. Inhibition of integrase prevents the integration of linear HIV-1 DNA into host genomic DNA, blocking the formation of the HIV-1 provirus and propagation of the virus.
  • Molecular weight: 449.39
  • Formula: C21H18F3N3O5
  • CLOGP: 0.02
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 2
  • TPSA: 99.18
  • ALOGS: -3.92
  • ROTB: 3
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
S (Water solubility) 0.10 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
June 21, 2018 EMA Gilead Sciences International Limited
Feb. 7, 2018 FDA GILEAD SCIENCES INC
March 26, 2019 PMDA Gilead Sciences K.K.

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J05AR20 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Human immunodeficiency virus infection indication 86406008 DOID:526




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.24 acidic
pKa2 12.47 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 30MG BASE;120MG;EQ 15MG BASE BIKTARVY GILEAD SCIENCES INC N210251 Oct. 7, 2021 RX TABLET ORAL 8754065 Aug. 15, 2032 TREATMENT OF HIV INFECTION
EQ 30MG BASE;120MG;EQ 15MG BASE BIKTARVY GILEAD SCIENCES INC N210251 Oct. 7, 2021 RX TABLET ORAL 9296769 Aug. 15, 2032 TREATMENT OF HIV INFECTION
EQ 50MG BASE;200MG;EQ 25MG BASE BIKTARVY GILEAD SCIENCES INC N210251 Feb. 7, 2018 RX TABLET ORAL 8754065 Aug. 15, 2032 TREATMENT OF HIV INFECTION
EQ 50MG BASE;200MG;EQ 25MG BASE BIKTARVY GILEAD SCIENCES INC N210251 Feb. 7, 2018 RX TABLET ORAL 9296769 Aug. 15, 2032 TREATMENT OF HIV INFECTION
EQ 30MG BASE;120MG;EQ 15MG BASE BIKTARVY GILEAD SCIENCES INC N210251 Oct. 7, 2021 RX TABLET ORAL 10385067 June 19, 2035 TREATMENT OF HIV INFECTION
EQ 50MG BASE;200MG;EQ 25MG BASE BIKTARVY GILEAD SCIENCES INC N210251 Feb. 7, 2018 RX TABLET ORAL 10385067 June 19, 2035 TREATMENT OF HIV INFECTION

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 30MG BASE;120MG;EQ 15MG BASE BIKTARVY GILEAD SCIENCES INC N210251 Oct. 7, 2021 RX TABLET ORAL Feb. 7, 2023 NEW CHEMICAL ENTITY
EQ 50MG BASE;200MG;EQ 25MG BASE BIKTARVY GILEAD SCIENCES INC N210251 Feb. 7, 2018 RX TABLET ORAL Feb. 7, 2023 NEW CHEMICAL ENTITY
EQ 50MG BASE;200MG;EQ 25MG BASE BIKTARVY GILEAD SCIENCES INC N210251 Feb. 7, 2018 RX TABLET ORAL Feb. 24, 2024 LABELING REVISIONS RELATED TO CLINICAL STUDIES
EQ 50MG BASE;200MG;EQ 25MG BASE BIKTARVY GILEAD SCIENCES INC N210251 Feb. 7, 2018 RX TABLET ORAL June 18, 2026 FOR HIV-1 INFECTION IN PEDIATRIC PTS AT LEAST 25 KG W/ NO ANTIRETROVIRAL (ARV) TX HX OR TO REPLACE CURRENT ARV REGIMEN FOR VIROLOGICALLY-SUPPRESSED ON STABLE ARV W/ NO HX TX FAILURE AND NO KNOWN SUBSTITUTIONS ASSOCIATED W/ RESISTANCE TO BIC, FTC, OR TAF
EQ 30MG BASE;120MG;EQ 15MG BASE BIKTARVY GILEAD SCIENCES INC N210251 Oct. 7, 2021 RX TABLET ORAL Oct. 7, 2028 A COMPLETE REGIMEN FOR THE TREATMENT OF HUMAN IMMUNODEFICIENCY VIRUS TYPE 1 (HIV-1) INFECTION IN PEDIATRIC PATIENTS WEIGHING 14 KG TO LESS THAN 25 KG WHO HAVE NO ANTIRETROVIRAL TREATMENT HISTORY OR TO REPLACE THE CURRENT ANTIRETROVIRAL REGIMEN IN THOSE WHO ARE VIROLOGICALLY-SUPPRESSED (HIV-1 RNA LESS THAN 50 COPIES PER ML) ON A STABLE ANTIRETROVIRAL REGIMEN WITH NO HISTORY OF TREATMENT FAILURE AND NO KNOWN SUBSTITUTIONS ASSOCIATED WITH RESISTANCE TO THE INDIVIDUAL COMPONENTS OF BIKTARVY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Integrase Enzyme INHIBITOR IC50 8.13 SCIENTIFIC LITERATURE DRUG LABEL
Integrase Enzyme IC50 8.12 CHEMBL

External reference:

IDSource
8GB79LOJ07 UNII
1807988-02-8 SECONDARY_CAS_RN
C4507568 UMLSCUI
CHEBI:172943 CHEBI
KLQ PDB_CHEM_ID
CHEMBL3989866 ChEMBL_ID
90311989 PUBCHEM_CID
DB11799 DRUGBANK_ID
CHEMBL3989867 ChEMBL_ID
D10909 KEGG_DRUG
10133 INN_ID
11575 IUPHAR_LIGAND_ID
33694 MMSL
d08735 MMSL
017460 NDDF
017461 NDDF
772193003 SNOMEDCT_US
772194009 SNOMEDCT_US
816103009 SNOMEDCT_US
4037318 VANDF
1999660 RXNORM
C000620396 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Biktarvy HUMAN PRESCRIPTION DRUG LABEL 3 50090-6247 TABLET 50 mg ORAL NDA 33 sections
Biktarvy HUMAN PRESCRIPTION DRUG LABEL 3 61958-2501 TABLET 50 mg ORAL NDA 35 sections
Biktarvy HUMAN PRESCRIPTION DRUG LABEL 3 61958-2501 TABLET 50 mg ORAL NDA 35 sections
Biktarvy HUMAN PRESCRIPTION DRUG LABEL 3 61958-2505 TABLET 30 mg ORAL NDA 35 sections
Biktarvy HUMAN PRESCRIPTION DRUG LABEL 3 61958-2505 TABLET 30 mg ORAL NDA 35 sections
Biktarvy HUMAN PRESCRIPTION DRUG LABEL 3 70518-3080 TABLET 50 mg ORAL NDA 34 sections