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
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

Molecule

Description

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:

Dose	Unit	Route
0.15	g	O

ADMET properties:

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Property	Value	Reference
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

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Approvals:

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

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FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

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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	129.15	42.81	60	384	225886	34730601
Immune reconstitution inflammatory syndrome	79.19	42.81	19	425	8740	34947747
Viral load increased	59.28	42.81	12	432	2515	34953972

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FDA Adverse Event Reporting System (Geriatric)

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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	160.92	45.77	72	530	415111	79328675
Immune reconstitution inflammatory syndrome	75.06	45.77	18	584	13823	79729963
Gastroschisis	63.95	45.77	7	595	30	79743756
Foetal growth abnormality	54.94	45.77	6	596	25	79743761
Foetal exposure during pregnancy	49.95	45.77	11	591	5779	79738007

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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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
CHEBI has role	CHEBI:50183	P450 inhibitors
FDA EPC	N0000191001	Cytochrome P450 3A Inhibitor
FDA MoA	N0000182137	Cytochrome P450 2D6 Inhibitors
FDA MoA	N0000185503	P-Glycoprotein Inhibitors

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

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

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🐶 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)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
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	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;300MG	STRIBILD	GILEAD SCIENCES INC	N203100	Aug. 27, 2012	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;300MG	STRIBILD	GILEAD SCIENCES INC	N203100	Aug. 27, 2012	RX	TABLET	ORAL	8633219	April 30, 2030	TREATMENT OF HIV INFECTION

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Orange Book exclusivity data (new drug applications)

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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, 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

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Cytochrome P450 3A	Enzyme	P08684 P20815 P24462 Q9HB55	CP3A4_HUMAN CP3A5_HUMAN CP3A7_HUMAN CP343_HUMAN	INHIBITOR	Ki	6.03		SCIENTIFIC LITERATURE	DRUG LABEL
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	4.23		CHEMBL

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External reference:

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ID	Source
014623	NDDF
1306284	RXNORM
213129	MMSL
25151504	PUBCHEM_CID
28748	MMSL
4031664	VANDF
710109003	SNOMEDCT_US
714771003	SNOMEDCT_US
7535	IUPHAR_LIGAND_ID
9266	INN_ID

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Pharmaceutical products:

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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
EVOTAZ	HUMAN PRESCRIPTION DRUG LABEL	2	0003-3641	TABLET	150 mg	ORAL	NDA	30 sections
Genvoya	HUMAN PRESCRIPTION DRUG LABEL	4	61958-1901	TABLET	150 mg	ORAL	NDA	32 sections
Genvoya	HUMAN PRESCRIPTION DRUG LABEL	4	70518-0568	TABLET	150 mg	ORAL	NDA	31 sections
PREZCOBIX	HUMAN PRESCRIPTION DRUG LABEL	2	50090-1723	TABLET, FILM COATED	150 mg	ORAL	NDA	29 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
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

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