cobicistat 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| enzyme inhibitors | 4299 | 1004316-88-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.15 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Hosey CM, Chan R, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Drug interaction | 73.21 | 36.46 | 38 | 303 | 197347 | 29376839 |
| Immune reconstitution inflammatory syndrome | 72.62 | 36.46 | 17 | 324 | 7785 | 29566401 |
| Viral load increased | 50.65 | 36.46 | 10 | 331 | 2039 | 29572147 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Drug interaction | 117.53 | 45.24 | 53 | 367 | 362030 | 64136282 |
| Immune reconstitution inflammatory syndrome | 68.92 | 45.24 | 16 | 404 | 12454 | 64485858 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| 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 | 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 |
| 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 |
| CHEBI has role | CHEBI:50183 | P450 inhibitors |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Human immunodeficiency virus infection | indication | 86406008 | DOID:526 |
| Coronavirus infection | off-label use | 186747009 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 6.58 | Basic |
| pKa2 | 3.62 | Basic |
| pKa3 | 2.45 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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;800MG;200MG;EQ 10MG BASE | SYMTUZA | JANSSEN PRODS | N210455 | July 17, 2018 | RX | TABLET | ORAL | 7803788 | Feb. 2, 2022 | 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 | 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;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;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 | 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 | 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;800MG | 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;800MG | 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-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;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 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 PHARMACOKINETIC ENHANCER THAT INIBITS 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 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Cytochrome P450 3A | Enzyme | INHIBITOR | Ki | 6.03 | SCIENTIFIC LITERATURE | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| 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 |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| EVOTAZ | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0003-3641 | TABLET | 150 mg | ORAL | NDA | 30 sections |
| EVOTAZ | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0003-3641 | TABLET | 150 mg | ORAL | NDA | 30 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 | 30 sections |
| PREZCOBIX | HUMAN PRESCRIPTION DRUG LABEL | 2 | 59676-575 | TABLET, FILM COATED | 150 mg | ORAL | NDA | 30 sections |
| Symtuza | HUMAN PRESCRIPTION DRUG LABEL | 4 | 59676-800 | TABLET, FILM COATED | 150 mg | ORAL | NDA | 34 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 |
| 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 |
| Tybost | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61958-1401 | TABLET, FILM COATED | 150 mg | ORAL | NDA | 31 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 |