cobicistat 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
enzyme inhibitors 4299 1004316-88-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • GS-9350
  • tybost
  • cobicistat
  • GS 9350
A carbamate and thiazole derivative that functions as a CYTOCHROME P450 CYP3A INHIBITOR to enhance the concentration of ANTI-HIV AGENTS, with which it is used in combination, for the treatment of HIV INFECTIONS.
  • Molecular weight: 776.03
  • Formula: C40H53N7O5S2
  • CLOGP: 4.66
  • LIPINSKI: 2
  • HAC: 12
  • HDO: 3
  • TPSA: 138.02
  • ALOGS: -5.79
  • ROTB: 20
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.15 g O

ADMET properties:

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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK7,MET,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PRKDC,SIK3,TEK 22
kinase-selectivity-class AXL,GRK2 2
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 49.888 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 Moderate 0.67
rat-kpuu-brain Rat brain Kpuu 0.003 % High 1

Approvals:

DateAgencyCompanyOrphan
Aug. 27, 2012 FDA GILEAD SCIENCES INC
March 25, 2013 PMDA Japan Tobacco Inc.
Sept. 19, 2013 EMA Gilead Sciences Ireland UC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

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
Drug interaction 263.90 39.38 111 570 266888 42353766
Immune reconstitution inflammatory syndrome 101.59 39.38 25 656 10118 42610536
Serotonin syndrome 78.45 39.38 25 656 25820 42594834
Viral load increased 54.44 39.38 12 669 2985 42617669

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
Drug interaction 365.41 49.42 139 768 500044 110088348
Immune reconstitution inflammatory syndrome 106.37 49.42 25 882 16201 110572191
Serotonin syndrome 103.09 49.42 32 875 59121 110529271
Adrenal insufficiency 78.29 49.42 24 883 42366 110546026
Gastroschisis 63.35 49.42 7 900 30 110588362
Foetal exposure during pregnancy 56.74 49.42 13 894 7492 110580900
Foetal growth abnormality 54.43 49.42 6 901 25 110588367
Renal dysplasia 49.63 49.42 6 901 63 110588329

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J05AR09 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations
ATC J05AR14 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations
ATC J05AR15 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
ATC J05AR22 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations
ATC V03AX03 VARIOUS
ALL OTHER THERAPEUTIC PRODUCTS
ALL OTHER THERAPEUTIC PRODUCTS
Other therapeutic products
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000998 Antiviral Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D019380 Anti-HIV Agents
MeSH PA D065607 Cytochrome P-450 Enzyme Inhibitors
MeSH PA D065692 Cytochrome P-450 CYP3A Inhibitors
FDA MoA N0000182137 Cytochrome P450 2D6 Inhibitors
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000190107 Organic Anion Transporting Polypeptide 1B1 Inhibitors
FDA MoA N0000190108 Organic Anion Transporting Polypeptide 1B3 Inhibitors
FDA MoA N0000190113 Breast Cancer Resistance Protein Inhibitors
FDA MoA N0000190114 Cytochrome P450 3A Inhibitors
FDA EPC N0000191001 Cytochrome P450 3A Inhibitor
FDA MoA N0000191423 Multidrug and Toxin Extrusion Transporter 1 Inhibitors
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:35441 antiinfective agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35718 antifungal agent
CHEBI has role CHEBI:38068 antimalarial
CHEBI has role CHEBI:50183 P450 inhibitor
CHEBI has role CHEBI:50864 insulin-sensitizing drug
CHEBI has role CHEBI:64946 anti-HIV agent

Related Drugs by ATC class:

J05AR Antivirals for treatment of HIV infections, combinations 19 drugs
abacaviratazanavirbictegravirdarunavirdolutegravirdoravirineefavirenzelvitegraviremtricitabinelamivudinelopinavirnevirapine show all 19 →
V03AX Other therapeutic products 2 drugs
difelikefalinnalfurafine

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

DiseaseRelationSNOMED_IDDOID
Human immunodeficiency virus infection indication 86406008 DOID:526
Malignant Melanoma with BRAF V600E Mutation indication 830150003
Coronavirus infection off-label use 186747009




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.58 Basic
pKa2 3.62 Basic
pKa3 2.45 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
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;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 TYBOST GILEAD SCIENCES INC N203094 Sept. 24, 2014 DISCN TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV INFECTION USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE
90MG TYBOST GILEAD SCIENCES INC N203094 June 20, 2025 DISCN 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 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;EQ 675MG BASE PREZCOBIX JANSSEN PRODS N205395 March 21, 2025 RX TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV INFECTION IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 25KG USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE
150MG;EQ 800MG BASE PREZCOBIX JANSSEN PRODS N205395 Jan. 29, 2015 RX TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV INFECTION IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 25KG USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE
150MG;EQ 800MG BASE PREZCOBIX JANSSEN PRODS N205395 Jan. 29, 2015 RX TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV INFECTION IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 40KG USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE
150MG;EQ 800MG BASE PREZCOBIX JANSSEN PRODS N205395 Jan. 29, 2015 RX TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV INFECTION USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE
EQ 300MG BASE;150MG EVOTAZ BRISTOL N206353 Jan. 29, 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 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;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV-1 INFECTION USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE IN ADULTS WHO ARE VIROLOGICALLY SUPPRESSED ON A STABLE ANTIRETROVIRAL REGIMEN FOR AT LEAST 6 MONTHS
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV-1 INFECTION USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE IN ADULTS WHO HAVE NO PRIOR ANTIRETROVIRAL TREATMENT HISTORY
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV-1 INFECTION USING A COMPOSITION CONTAINING A PK ENHANCER THAT INHIBITS CY P450 MONOXYGENASE IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 40KG WHO ARE VIROLOGICALLY SUPPRESSED ON A STABLE ARV REGIMEN FOR AT LEAST 6 MONTHS
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV-1 INFECTION USING A COMPOSITION CONTAINING A PK ENHANCER THAT INHIBITS CY P450 MONOXYGENASE IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 40KG WHO HAVE NO PRIOR ARV TREATMENT HISTORY
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 8148374 Sept. 3, 2029 TX OF HIV1 INFECTION USING A COMPOSITION CONTAINING A PK ENHANCER THAT INHIBITS CY P450 MONOXYGENASE IN ADULTS & PEDIATRIC PATIENTS AT LEAST 40KG HAVING NO PRIOR ARV TX HISTORY OR ARE VIROLOGICALLY SUPPRESSED ON A STABLE ARV REGIMEN FOR AT LEAST 6 MO
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 8148374 Sept. 3, 2029 TX OF HIV-1 INFECTION USING A COMPOSITION CONTAINING A PK ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENATES IN ADULTS WHO HAVE NO PRIOR ANTIRETROVIRAL TX HISTORY OR ARE VIROLOGICALLY SUPPRESSED ON A STABLE ANTIRETROVIRAL REGIMEN FOR AT LEAST 6 MONTHS
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
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 8754065 Aug. 15, 2032 TREATMENT OF HIV-1 INFECTION IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 40 KG WHO HAVE NO PRIOR ANTIRETROVIRAL TREATMENT HISTORY OR ARE VIROLOGICALLY SUPPRESSED ON A STABLE ANTIRETROVIRAL REGIMEN FOR AT LEAST 6 MONTHS
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 8754065 Aug. 15, 2032 TREATMENT OF HIV-1 INFECTION IN ADULTS WHO HAVE NO PRIOR ANTIRETROVIRAL TREATMENT HISTORY OR ARE VIROLOGICALLY SUPPRESSED ON A STABLE ANTIRETROVIRAL REGIMEN FOR AT LEAST 6 MONTHS
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 9296769 Aug. 15, 2032 TREATMENT OF HIV-1 INFECTION IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 40 KG WHO HAVE NO PRIOR ANTIRETROVIRAL TREATMENT HISTORY OR ARE VIROLOGICALLY SUPPRESSED ON A STABLE ANTIRETROVIRAL REGIMEN FOR AT LEAST 6 MONTHS
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 9296769 Aug. 15, 2032 TREATMENT OF HIV-1 INFECTION IN ADULTS WHO HAVE NO PRIOR ANTIRETROVIRAL TREATMENT HISTORY OR ARE VIROLOGICALLY SUPPRESSED ON A STABLE ANTIRETROVIRAL REGIMEN FOR AT LEAST 6 MONTHS
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 10786518 July 19, 2038 TREATMENT OF HIV-1 INFECTION IN ADULT OR PEDIATRIC PATIENTS (>=40 KG) WITH <50 COPIES/ML HIV-1 RNA AFTER >= 6 MONTHS ON PRIOR ANTIRETROVIRAL REGIMEN AND NO KNOWN DARUNAVIR OR TENOFOVIR RESISTANCE-ASSOCIATED SUBSTITUTIONS

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
150MG TYBOST GILEAD SCIENCES INC N203094 Sept. 24, 2014 DISCN TABLET ORAL Aug. 22, 2026 INDICATED TO INCREASE SYSTEMIC EXPOSURE OF ATAZANAVIR IN COMBINATION WITH OTHER ANTIRETROVIRAL AGENTS IN THE TREATMENT OF HIV-1 INFECTION IN PEDIATRIC PATIENTS WEIGHING AT LEAST 35 KG

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Cytochrome P450 3A Enzyme INHIBITOR Ki 6.03 SCIENTIFIC LITERATURE DRUG LABEL
ATP-binding cassette sub-family G member 2 Transporter IC50 4.23 CHEMBL
Replicase polyprotein 1ab Enzyme Kd 5.66 CHEMBL

External reference:

IDSource
D09881 KEGG_DRUG
4031664 VANDF
C3177235 UMLSCUI
CHEBI:72291 CHEBI
CHEMBL2095208 ChEMBL_ID
D000069547 MESH_DESCRIPTOR_UI
DB09065 DRUGBANK_ID
7535 IUPHAR_LIGAND_ID
9266 INN_ID
LW2E03M5PG UNII
25151504 PUBCHEM_CID
1306284 RXNORM
213129 MMSL
28748 MMSL
d07897 MMSL
014623 NDDF
710109003 SNOMEDCT_US
714771003 SNOMEDCT_US
A1APA PDB_CHEM_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
EVOTAZ HUMAN PRESCRIPTION DRUG LABEL 2 0003-3641 TABLET 150 mg ORAL NDA 30 sections
PREZCOBIX HUMAN PRESCRIPTION DRUG LABEL 2 50090-1723 TABLET, FILM COATED 150 mg ORAL NDA 29 sections
Stribild HUMAN PRESCRIPTION DRUG LABEL 4 53808-0887 TABLET, FILM COATED 150 mg ORAL NDA 30 sections
PREZCOBIX HUMAN PRESCRIPTION DRUG LABEL 2 59676-575 TABLET, FILM COATED 150 mg ORAL NDA 35 sections
PREZCOBIX PED HUMAN PRESCRIPTION DRUG LABEL 2 59676-577 TABLET, FOR SUSPENSION 90 mg ORAL NDA 35 sections
PREZCOBIX HUMAN PRESCRIPTION DRUG LABEL 2 59676-578 TABLET, FILM COATED 150 mg ORAL NDA 35 sections
Symtuza HUMAN PRESCRIPTION DRUG LABEL 4 59676-800 TABLET, FILM COATED 150 mg ORAL NDA 34 sections
Stribild HUMAN PRESCRIPTION DRUG LABEL 4 61958-1201 TABLET, FILM COATED 150 mg ORAL NDA 31 sections
Tybost HUMAN PRESCRIPTION DRUG LABEL 1 61958-1401 TABLET, FILM COATED 150 mg ORAL NDA 32 sections
Tybost HUMAN PRESCRIPTION DRUG LABEL 1 61958-1402 TABLET, FILM COATED 90 mg ORAL NDA 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