cobicistat Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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: 3.98
  • 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

Approvals:

DateAgencyCompanyOrphan
Aug. 27, 2012 FDA GILEAD SCIENCES INC

FDA Adverse Event Reporting System (Female)

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
Maternal exposure during pregnancy 131.52 33.57 41 692 14822 2342530
Abortion spontaneous 105.99 33.57 34 699 13411 2343941
Drug interaction 87.06 33.57 36 697 29127 2328225
Weight increased 81.92 33.57 32 701 22305 2335047
Virologic failure 77.69 33.57 13 720 273 2357079
Exposure during pregnancy 71.36 33.57 30 703 25189 2332163
Rash 70.81 33.57 39 694 59519 2297833
Blood HIV RNULL increased 61.58 33.57 9 724 74 2357278
Nausea 61.57 33.57 45 688 112144 2245208
Cushing's syndrome 52.75 33.57 11 722 778 2356574
Multiple-drug resistance 52.00 33.57 9 724 232 2357120
Viral mutation identified 51.49 33.57 9 724 246 2357106
Product use complaint 48.46 33.57 9 724 348 2357004
Genotype drug resistance test positive 45.64 33.57 7 726 82 2357270
Drug resistance 39.61 33.57 11 722 2613 2354739
Viral load increased 37.96 33.57 7 726 260 2357092
Vomiting 35.18 33.57 27 706 71575 2285777

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
Viral load increased 326.97 34.48 62 2043 522 1744154
Blood HIV RNULL increased 179.62 34.48 32 2073 181 1744495
Weight increased 165.31 34.48 68 2037 11289 1733387
Immune reconstitution inflammatory syndrome 164.20 34.48 42 2063 1507 1743169
Rash 161.50 34.48 99 2006 38594 1706082
Drug interaction 152.05 34.48 85 2020 27873 1716803
Nausea 136.22 34.48 99 2006 51097 1693579
Blood creatinine increased 102.64 34.48 52 2053 13894 1730782
Product dose omission 97.24 34.48 59 2046 22381 1722295
Headache 94.54 34.48 68 2037 34308 1710368
Diarrhoea 87.12 34.48 78 2027 53774 1690902
Drug ineffective 72.24 34.48 76 2029 63725 1680951
Genotype drug resistance test positive 71.75 34.48 16 2089 313 1744363
Myalgia 67.27 34.48 41 2064 15617 1729059
Drug resistance 66.76 34.48 25 2080 3205 1741471
Treatment noncompliance 64.94 34.48 28 2077 5173 1739503
Product use complaint 62.29 34.48 14 2091 284 1744392
Arthralgia 61.14 34.48 45 2060 23399 1721277
Glomerular filtration rate decreased 60.42 34.48 19 2086 1438 1743238
Fatigue 58.25 34.48 61 2044 50720 1693956
Product dispensing error 57.92 34.48 19 2086 1647 1743029
CD4 lymphocytes decreased 51.84 34.48 13 2092 427 1744249
Abnormal dreams 51.67 34.48 18 2087 1873 1742803
Depression 50.32 34.48 35 2070 16634 1728042
Therapy cessation 49.61 34.48 20 2085 3119 1741557
Vomiting 47.42 34.48 48 2057 38267 1706409
Renal tubular disorder 47.33 34.48 14 2091 861 1743815
Abdominal discomfort 44.73 34.48 26 2079 9055 1735621
Cushing's syndrome 43.13 34.48 12 2093 592 1744084
Progressive multifocal leukoencephalopathy 42.47 34.48 15 2090 1624 1743052
Amniotic band syndrome 40.37 34.48 6 2099 7 1744669
Pruritus 40.03 34.48 35 2070 23187 1721489
Dysphagia 39.49 34.48 25 2080 10143 1734533
Osteoporosis 39.42 34.48 14 2091 1541 1743135
Suicidal ideation 38.30 34.48 23 2082 8495 1736181
Insurance issue 36.86 34.48 9 2096 264 1744412
Glycosuria 36.48 34.48 9 2096 276 1744400
Inability to afford medication 36.33 34.48 8 2097 147 1744529
Acute kidney injury 34.73 34.48 39 2066 34905 1709771

Pharmacologic Action:

SourceCodeDescription
ATC V03AX03 VARIOUS
ALL OTHER THERAPEUTIC PRODUCTS
ALL OTHER THERAPEUTIC PRODUCTS
Other therapeutic products
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
FDA MoA N0000190114 Cytochrome P450 3A Inhibitors
FDA EPC N0000191001 Cytochrome P450 3A Inhibitor
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000182137 Cytochrome P450 2D6 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
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 D065692 Cytochrome P-450 CYP3A Inhibitors
MeSH PA D065607 Cytochrome P-450 Enzyme Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D065606 Metabolic Side Effects of Drugs and Substances

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Human immunodeficiency virus infection indication 86406008 DOID:526
Coronavirus infection off-label use 186747009

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 STRIBILD GILEAD SCIENCES INC N203100 Aug. 27, 2012 RX TABLET ORAL 6642245 Nov. 4, 2020 TREATMENT OF HIV INFECTION
150MG GENVOYA GILEAD SCIENCES INC N207561 Nov. 5, 2015 RX TABLET ORAL 6642245 Nov. 4, 2020 TREATMENT OF HIV INFECTION
150MG SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 6642245 Nov. 4, 2020 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 GENVOYA GILEAD SCIENCES INC N207561 Nov. 5, 2015 RX TABLET ORAL 7803788 Feb. 2, 2022 TREATMENT OF HIV INFECTION
150MG SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 7803788 Feb. 2, 2022 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 STRIBILD GILEAD SCIENCES INC N203100 Aug. 27, 2012 RX TABLET ORAL 8592397 Jan. 13, 2024 TREATMENT OF HIV INFECTION
150MG STRIBILD GILEAD SCIENCES INC N203100 Aug. 27, 2012 RX TABLET ORAL 8716264 Jan. 13, 2024 TREATMENT OF HIV INFECTION
150MG STRIBILD GILEAD SCIENCES INC N203100 Aug. 27, 2012 RX TABLET ORAL 9457036 Jan. 13, 2024 TREATMENT OF HIV INFECTION
150MG STRIBILD GILEAD SCIENCES INC N203100 Aug. 27, 2012 RX TABLET ORAL 9744181 Jan. 13, 2024 TREATMENT OF HIV INFECTION
150MG STRIBILD GILEAD SCIENCES INC N203100 Aug. 27, 2012 RX TABLET ORAL 7176220 Aug. 27, 2026 TREATMENT OF HIV INFECTION
150MG GENVOYA GILEAD SCIENCES INC N207561 Nov. 5, 2015 RX TABLET ORAL 7176220 Aug. 27, 2026 TREATMENT OF HIV INFECTION
150MG STRIBILD GILEAD SCIENCES INC N203100 Aug. 27, 2012 RX TABLET ORAL 7635704 Oct. 26, 2026 TREATMENT OF HIV INFECTION
150MG 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 RX TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV INFECTION USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE
150MG 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 STRIBILD GILEAD SCIENCES INC N203100 Aug. 27, 2012 RX TABLET ORAL 9891239 Sept. 3, 2029 TREATMENT OF HIV INFECTION
150MG 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
150MG EVOTAZ BRISTOL-MYERS SQUIBB 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 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 GENVOYA GILEAD SCIENCES INC N207561 Nov. 5, 2015 RX TABLET ORAL 9891239 Sept. 3, 2029 TREATMENT OF HIV INFECTION
150MG 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 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 INIBITS CYTOCHROME P450 MONOOXYGENASE IN ADULTS WHO ARE VIROLOGICALLY SUPPRESSED ON A STABLE ANTIRETROVIRAL REGIMEN FOR AT LEAST 6 MONTHS
150MG 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 STRIBILD GILEAD SCIENCES INC N203100 Aug. 27, 2012 RX TABLET ORAL 8633219 April 24, 2030 TREATMENT OF HIV INFECTION
150MG GENVOYA GILEAD SCIENCES INC N207561 Nov. 5, 2015 RX TABLET ORAL 8633219 April 24, 2030 TREATMENT OF HIV INFECTION
150MG GENVOYA GILEAD SCIENCES INC N207561 Nov. 5, 2015 RX TABLET ORAL 8754065 Aug. 15, 2032 TREATMENT OF HIV INFECTION
150MG GENVOYA GILEAD SCIENCES INC N207561 Nov. 5, 2015 RX TABLET ORAL 9296769 Aug. 15, 2032 TREATMENT OF HIV INFECTION
150MG 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 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

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
150MG STRIBILD GILEAD SCIENCES INC N203100 Aug. 27, 2012 RX TABLET ORAL Jan. 27, 2020 NEW PATIENT POPULATION
150MG SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL July 17, 2020 NEW COMBINATION
150MG GENVOYA GILEAD SCIENCES INC N207561 Nov. 5, 2015 RX TABLET ORAL Sept. 25, 2020 NEW PATIENT POPULATION
150MG GENVOYA GILEAD SCIENCES INC N207561 Nov. 5, 2015 RX TABLET ORAL Nov. 5, 2020 NEW CHEMICAL ENTITY
150MG SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL Nov. 5, 2020 NEW CHEMICAL ENTITY
150MG GENVOYA GILEAD SCIENCES INC N207561 Nov. 5, 2015 RX TABLET ORAL Dec. 10, 2021 DOSING RECOMMENDATION FOR THE USE OF ELVITEGRAVIR/COBICISTAT/EMTRICITABINE/TENOFOVIR ALAFENAMIDE FIXED DOSE COMBINATION IN HIV-1 INFECTED ADULT PATIENTS WITH END-STAGE-RENAL DISEASE WHO ARE RECEIVING CHRONIC HEMODIALYSIS
150MG TYBOST GILEAD SCIENCES INC N203094 Sept. 24, 2014 RX TABLET ORAL Aug. 22, 2022 NEW PATIENT POPULATION
150MG TYBOST GILEAD SCIENCES INC N203094 Sept. 24, 2014 RX 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

External reference:

IDSource
D000069547 MESH_DESCRIPTOR_UI
C3858034 UMLSCUI
D09881 KEGG_DRUG
714771003 SNOMEDCT_US
1306284 RXNORM
014623 NDDF
28748 MMSL
d07897 MMSL
4031664 VANDF
710109003 SNOMEDCT_US
LW2E03M5PG UNII
9266 INN_ID
DB09065 DRUGBANK_ID
CHEBI:72291 CHEBI
7535 IUPHAR_LIGAND_ID
CHEMBL2095208 ChEMBL_ID
25151504 PUBCHEM_CID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
EVOTAZ HUMAN PRESCRIPTION DRUG LABEL 2 0003-3641 TABLET 150 mg ORAL NDA 18 sections
Stribild HUMAN PRESCRIPTION DRUG LABEL 4 53808-0887 TABLET, FILM COATED 150 mg ORAL NDA 19 sections
PREZCOBIX HUMAN PRESCRIPTION DRUG LABEL 2 59676-575 TABLET, FILM COATED 150 mg ORAL NDA 19 sections
Symtuza HUMAN PRESCRIPTION DRUG LABEL 3 59676-800 TABLET, FILM COATED 150 mg ORAL NDA 20 sections
Stribild HUMAN PRESCRIPTION DRUG LABEL 4 61958-1201 TABLET, FILM COATED 150 mg ORAL NDA 20 sections
Stribild Access HUMAN PRESCRIPTION DRUG LABEL 4 61958-1202 TABLET, FILM COATED 150 mg ORAL Export only 20 sections
Tybost HUMAN PRESCRIPTION DRUG LABEL 1 61958-1401 TABLET, FILM COATED 150 mg ORAL NDA 19 sections
Genvoya HUMAN PRESCRIPTION DRUG LABEL 3 61958-1901 TABLET 150 mg ORAL NDA 20 sections
Stribild HUMAN PRESCRIPTION DRUG LABEL 4 69189-1201 TABLET, FILM COATED 150 mg ORAL NDA 20 sections
Genvoya HUMAN PRESCRIPTION DRUG LABEL 3 70518-0568 TABLET 150 mg ORAL NDA 20 sections