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

Stem definitionDrug idCAS RN
antivirals 4300 697761-98-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • GS-9137
  • GS9137
  • JTK303
  • JTK-303
  • JTK 303
  • GS 9137
  • elvitegravir
Elvitegravir 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 HIV-1 DNA into host genomic DNA, blocking the formation of the HIV-1 provirus and propagation of the viral infection. Elvitegravir does not inhibit human topoisomerases I or II.
  • Molecular weight: 447.89
  • Formula: C23H23ClFNO5
  • CLOGP: 4.56
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 87.07
  • ALOGS: -4.84
  • ROTB: 7

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Aug. 27, 2012 FDA GILEAD SCIENCES INC
March 25, 2013 PMDA Japan Tobacco Inc.

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 J05AJ02 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Integrase inhibitors
ATC J05AR09 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations
ATC J05AR18 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations
FDA MoA N0000000127 HIV Integrase Inhibitors
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 D004791 Enzyme Inhibitors
MeSH PA D019429 Integrase Inhibitors
FDA EPC N0000175887 Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor
FDA MoA N0000185507 Cytochrome P450 2C9 Inducers

Drug Use (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 6.37 acidic
pKa2 12.88 acidic
pKa3 3.44 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
150MG;150MG;200MG;EQ 10MG BASE GENVOYA GILEAD SCIENCES INC N207561 Nov. 5, 2015 RX TABLET ORAL 7803788 Feb. 2, 2022 TREATMENT OF HIV INFECTION
150MG;150MG;200MG;300MG STRIBILD GILEAD SCIENCES INC N203100 Aug. 27, 2012 RX TABLET ORAL 8592397 Jan. 13, 2024 TREATMENT OF HIV INFECTION
150MG;150MG;200MG;300MG STRIBILD GILEAD SCIENCES INC N203100 Aug. 27, 2012 RX TABLET ORAL 8716264 Jan. 13, 2024 TREATMENT OF HIV INFECTION
150MG;150MG;200MG;300MG STRIBILD GILEAD SCIENCES INC N203100 Aug. 27, 2012 RX TABLET ORAL 9457036 Jan. 13, 2024 TREATMENT OF HIV INFECTION
150MG;150MG;200MG;300MG STRIBILD GILEAD SCIENCES INC N203100 Aug. 27, 2012 RX TABLET ORAL 9744181 Jan. 13, 2024 TREATMENT OF HIV INFECTION
150MG VITEKTA GILEAD SCIENCES INC N203093 Sept. 24, 2014 DISCN TABLET ORAL 7176220 Aug. 27, 2026 TREATMENT OF HIV INFECTION
85MG VITEKTA GILEAD SCIENCES INC N203093 Sept. 24, 2014 DISCN TABLET ORAL 7176220 Aug. 27, 2026 TREATMENT OF HIV INFECTION
150MG;150MG;200MG;300MG STRIBILD GILEAD SCIENCES INC N203100 Aug. 27, 2012 RX TABLET ORAL 7176220 Aug. 27, 2026 TREATMENT OF HIV INFECTION
150MG;150MG;200MG;EQ 10MG BASE GENVOYA GILEAD SCIENCES INC N207561 Nov. 5, 2015 RX TABLET ORAL 7176220 Aug. 27, 2026 TREATMENT OF HIV INFECTION
150MG VITEKTA GILEAD SCIENCES INC N203093 Sept. 24, 2014 DISCN TABLET ORAL 7635704 Oct. 26, 2026 TREATMENT OF HIV INFECTION
85MG VITEKTA GILEAD SCIENCES INC N203093 Sept. 24, 2014 DISCN TABLET ORAL 7635704 Oct. 26, 2026 TREATMENT OF HIV INFECTION
150MG;150MG;200MG;300MG STRIBILD GILEAD SCIENCES INC N203100 Aug. 27, 2012 RX TABLET ORAL 7635704 Oct. 26, 2026 TREATMENT OF HIV INFECTION
150MG;150MG;200MG;EQ 10MG BASE GENVOYA GILEAD SCIENCES INC N207561 Nov. 5, 2015 RX TABLET ORAL 7635704 Oct. 26, 2026 TREATMENT OF HIV INFECTION
150MG;150MG;200MG;300MG STRIBILD GILEAD SCIENCES INC N203100 Aug. 27, 2012 RX TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV INFECTION USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE
150MG;150MG;200MG;300MG STRIBILD GILEAD SCIENCES INC N203100 Aug. 27, 2012 RX TABLET ORAL 9891239 Sept. 3, 2029 TREATMENT OF HIV INFECTION
150MG;150MG;200MG;EQ 10MG BASE GENVOYA GILEAD SCIENCES INC N207561 Nov. 5, 2015 RX TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV INFECTION USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE
150MG;150MG;200MG;EQ 10MG BASE GENVOYA GILEAD SCIENCES INC N207561 Nov. 5, 2015 RX TABLET ORAL 9891239 Sept. 3, 2029 TREATMENT OF HIV INFECTION
150MG;150MG;200MG;300MG STRIBILD GILEAD SCIENCES INC N203100 Aug. 27, 2012 RX TABLET ORAL 8633219 April 30, 2030 TREATMENT OF HIV INFECTION
150MG;150MG;200MG;EQ 10MG BASE GENVOYA GILEAD SCIENCES INC N207561 Nov. 5, 2015 RX TABLET ORAL 8633219 April 30, 2030 TREATMENT OF HIV INFECTION
150MG;150MG;200MG;EQ 10MG BASE GENVOYA GILEAD SCIENCES INC N207561 Nov. 5, 2015 RX TABLET ORAL 8754065 Aug. 15, 2032 TREATMENT OF HIV INFECTION
150MG;150MG;200MG;EQ 10MG BASE GENVOYA GILEAD SCIENCES INC N207561 Nov. 5, 2015 RX TABLET ORAL 9296769 Aug. 15, 2032 TREATMENT OF HIV INFECTION

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Integrase Enzyme INHIBITOR IC50 8.14 CHEMBL CHEMBL
Gag-Pol polyprotein Polyprotein IC50 8 WOMBAT-PK
Reverse transcriptase/RNaseH Enzyme IC50 4.04 CHEMBL
Reverse transcriptase Enzyme IC50 4.04 CHEMBL
Integrase Enzyme IC50 8.75 CHEMBL

External reference:

IDSource
4031665 VUID
N0000185512 NUI
D06677 KEGG_DRUG
4031665 VANDF
CHEBI:72289 CHEBI
ELV PDB_CHEM_ID
CHEMBL204656 ChEMBL_ID
C509700 MESH_SUPPLEMENTAL_RECORD_UI
11574 IUPHAR_LIGAND_ID
8871 INN_ID
DB09101 DRUGBANK_ID
4GDQ854U53 UNII
5277135 PUBCHEM_CID
1306286 RXNORM
28749 MMSL
d07898 MMSL
014621 NDDF
708828000 SNOMEDCT_US
714795001 SNOMEDCT_US
C2606637 UMLSCUI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Stribild HUMAN PRESCRIPTION DRUG LABEL 4 53808-0887 TABLET, FILM COATED 150 mg ORAL NDA 30 sections
Stribild HUMAN PRESCRIPTION DRUG LABEL 4 61958-1201 TABLET, FILM COATED 150 mg ORAL NDA 31 sections
Stribild Access HUMAN PRESCRIPTION DRUG LABEL 4 61958-1202 TABLET, FILM COATED 150 mg ORAL Export only 32 sections
Stribild Access HUMAN PRESCRIPTION DRUG LABEL 4 61958-1202 TABLET, FILM COATED 150 mg ORAL Export only 32 sections
Genvoya HUMAN PRESCRIPTION DRUG LABEL 4 61958-1901 TABLET 150 mg ORAL NDA 32 sections
Stribild HUMAN PRESCRIPTION DRUG LABEL 4 69189-1201 TABLET, FILM COATED 150 mg ORAL NDA 30 sections
Genvoya HUMAN PRESCRIPTION DRUG LABEL 4 70518-0568 TABLET 150 mg ORAL NDA 31 sections