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

Stem definition	Drug id	CAS RN
HIV integrase inhibitors	5440	1051375-10-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: cabotegravir cabotegravir sodium vocabria GSK1265744	Cabotegravir is an HIV-1 antiretroviral drug. Cabotegravir inhibits HIV integrase by binding to the integrase active site and blocking the strand transfer step of retroviral deoxyribonucleic acid (DNA) integration which is essential for the HIV replication cycle. It is indicated in combination with rilpivirine, an HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI), as a complete regimen for the treatment of HIV-1 infection in adults to replace the current antiretroviral regimen in those who are virologically suppressed on a stable antiretroviral regimen with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine. Molecular weight: 405.36 Formula: C19H17F2N3O5 CLOGP: -0.12 LIPINSKI: 0 HAC: 8 HDO: 2 TPSA: 99.18 ALOGS: -3.56 ROTB: 3 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

cabotegravir
cabotegravir sodium
vocabria
GSK1265744

Cabotegravir is an HIV-1 antiretroviral drug. Cabotegravir inhibits HIV integrase by binding to the integrase active site and blocking the strand transfer step of retroviral deoxyribonucleic acid (DNA) integration which is essential for the HIV replication cycle. It is indicated in combination with rilpivirine, an HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI), as a complete regimen for the treatment of HIV-1 infection in adults to replace the current antiretroviral regimen in those who are virologically suppressed on a stable antiretroviral regimen with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine.

Molecular weight: 405.36
Formula: C19H17F2N3O5
CLOGP: -0.12
LIPINSKI: 0
HAC: 8
HDO: 2
TPSA: 99.18
ALOGS: -3.56
ROTB: 3

Status: ONP

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

Drug dosage:

Dose	Unit	Route
30	mg	O
10	mg	P

ADMET properties:

None

Approvals:

Date	Agency	Company
Dec. 17, 2020	EMA	ViiV Healthcare B.V.
Jan. 21, 2021	FDA	Viiv HLTHCARE
May 31, 2022	PMDA	ViiV Healthcare K.K

FDA Adverse Event Reporting System (Female)

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
Viral load increased	322.14	50.96	47	820	1327	63486828
Injection site nodule	123.45	50.96	24	843	3811	63484344
Injection site pain	120.12	50.96	50	817	129750	63358405
Virologic failure	100.34	50.96	18	849	1844	63486311
Blood HIV RNA increased	94.70	50.96	15	852	724	63487431
Exposure during pregnancy	74.48	50.96	38	829	155509	63332646
Pathogen resistance	57.27	50.96	14	853	6384	63481771
Product use in unapproved therapeutic environment	55.73	50.96	6	861	9	63488146

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
Viral load increased	650.07	43.11	113	1771	2414	34952633
Injection site pain	330.58	43.11	110	1774	38895	34916152
Product dose omission issue	169.08	43.11	95	1789	119616	34835431
Product use in unapproved therapeutic environment	131.82	43.11	17	1867	33	34955014
Virologic failure	112.56	43.11	28	1856	3452	34951595
Injection site nodule	110.12	43.11	24	1860	1659	34953388
Product complaint	107.01	43.11	30	1854	5860	34949187
Blood HIV RNA increased	94.36	43.11	20	1864	1210	34953837
Pathogen resistance	57.66	43.11	21	1863	9461	34945586
Viral mutation identified	53.40	43.11	15	1869	2939	34952108
Wrong technique in device usage process	53.07	43.11	13	1871	1499	34953548
Inappropriate schedule of product administration	50.67	43.11	35	1849	62261	34892786
Product administered at inappropriate site	48.02	43.11	13	1871	2223	34952824

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
Viral load increased	425.57	34.49	70	1561	2878	79739879
Product dose omission issue	182.22	34.49	92	1539	247445	79495312
Injection site pain	143.49	34.49	64	1567	129774	79612983
Blood HIV RNA increased	112.35	34.49	21	1610	1787	79740970
Virologic failure	89.26	34.49	20	1611	4171	79738586
Pathogen resistance	77.78	34.49	23	1608	14319	79728438
Product use in unapproved therapeutic environment	76.51	34.49	9	1622	24	79742733
Product complaint	74.98	34.49	22	1609	13327	79729430
Injection site nodule	64.17	34.49	15	1616	3765	79738992
Viral mutation identified	53.49	34.49	13	1618	3845	79738912
Exposure via skin contact	41.65	34.49	7	1624	322	79742435
Blood HIV RNA below assay limit	36.42	34.49	4	1627	4	79742753
Product administration error	35.95	34.49	16	1615	31830	79710927

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	J05AJ04	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Integrase inhibitors
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	D019428	HIV Integrase Inhibitors
MeSH PA	D019429	Integrase Inhibitors
FDA EPC	N0000175887	Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor
FDA MoA	N0000190110	Organic Anion Transporter 1 Inhibitors
FDA MoA	N0000190111	Organic Anion Transporter 3 Inhibitors

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

Disease	Relation	SNOMED_ID	DOID
Human immunodeficiency virus I infection	indication	40780007

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

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
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML)	CABENUVA KIT	VIIV HLTHCARE	N212888	Jan. 21, 2021	RX	SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	7125879	April 21, 2025	TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML)	CABENUVA KIT	VIIV HLTHCARE	N212888	Jan. 21, 2021	RX	SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	7125879	April 21, 2025	TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
EQ 30MG BASE	VOCABRIA	VIIV HLTHCARE	N212887	Jan. 21, 2021	RX	TABLET	ORAL	8410103	April 28, 2026	TREATMENT OF HIV-1 IN AN ADULT IN COMBINATION WITH RILPIVIRINE
EQ 30MG BASE	VOCABRIA	VIIV HLTHCARE	N212887	Jan. 21, 2021	RX	TABLET	ORAL	8410103	April 28, 2026	TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML)	CABENUVA KIT	VIIV HLTHCARE	N212888	Jan. 21, 2021	RX	SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	8410103	April 28, 2026	TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML)	CABENUVA KIT	VIIV HLTHCARE	N212888	Jan. 21, 2021	RX	SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	8410103	April 28, 2026	TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML)	CABENUVA KIT	VIIV HLTHCARE	N212888	Jan. 21, 2021	RX	SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	11389447	June 30, 2027	TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG BY MONTHLY ADMINISTRATION OF RILPIVIRINE SUSPENSION AS PART OF COMBINATION THERAPY
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML)	CABENUVA KIT	VIIV HLTHCARE	N212888	Jan. 21, 2021	RX	SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	11389447	June 30, 2027	TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG BY MONTHLY ADMINISTRATION OF RILPIVIRINE SUSPENSION AS PART OF COMBINATION THERAPY
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML)	CABENUVA KIT	VIIV HLTHCARE	N212888	Jan. 21, 2021	RX	SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	11224597	Sept. 15, 2031	TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML)	CABENUVA KIT	VIIV HLTHCARE	N212888	Jan. 21, 2021	RX	SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	11224597	Sept. 15, 2031	TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 30MG BASE	VOCABRIA	VIIV HLTHCARE	N212887	Jan. 21, 2021	RX	TABLET	ORAL	Jan. 31, 2025	REVISION TO THE LABELING TO INCLUDE RESULTS FROM CLINICAL STUDY 207966 ATLAS-2M
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML)	CABENUVA KIT	VIIV HLTHCARE	N212888	Jan. 21, 2021	RX	SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	Jan. 31, 2025	NEW DOSING SCHEDULE FOR CABOTEGRAVIR/RILPIVRINE INJECTION EVERY 2 MONTHS
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML)	CABENUVA KIT	VIIV HLTHCARE	N212888	Jan. 21, 2021	RX	SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	Jan. 31, 2025	NEW DOSING SCHEDULE FOR CABOTEGRAVIR/RILPIVRINE INJECTION EVERY 2 MONTHS
EQ 30MG BASE	VOCABRIA	VIIV HLTHCARE	N212887	Jan. 21, 2021	RX	TABLET	ORAL	March 29, 2025	NEW PATIENT POPULATION
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML)	CABENUVA KIT	VIIV HLTHCARE	N212888	Jan. 21, 2021	RX	SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	March 29, 2025	NEW PATIENT POPULATION
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML)	CABENUVA KIT	VIIV HLTHCARE	N212888	Jan. 21, 2021	RX	SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	March 29, 2025	NEW PATIENT POPULATION
EQ 30MG BASE	VOCABRIA	VIIV HLTHCARE	N212887	Jan. 21, 2021	RX	TABLET	ORAL	Jan. 21, 2026	NEW CHEMICAL ENTITY
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML)	CABENUVA KIT	VIIV HLTHCARE	N212888	Jan. 21, 2021	RX	SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	Jan. 21, 2026	NEW CHEMICAL ENTITY
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML)	CABENUVA KIT	VIIV HLTHCARE	N212888	Jan. 21, 2021	RX	SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	Jan. 21, 2026	NEW CHEMICAL ENTITY
600MG/3ML (200MG/ML)	APRETUDE	VIIV HLTHCARE	N215499	Dec. 20, 2021	RX	SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	Jan. 21, 2026	NEW CHEMICAL ENTITY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Integrase	Enzyme		Q7ZJM1_9HIV1	INHIBITOR	IC50	8.52		DRUG LABEL	DRUG LABEL
Integrase	Enzyme		Q76353_9HIV1		IC50	8.52		CHEMBL

External reference:

ID	Source
D10548	KEGG_DRUG
HMH0132Z1Q	UNII
1051375-13-3	SECONDARY_CAS_RN
C4310385	UMLSCUI
CHEBI:172944	CHEBI
CHEMBL2403238	ChEMBL_ID
54713659	PUBCHEM_CID
DB11751	DRUGBANK_ID
CHEMBL3137330	ChEMBL_ID
11386	IUPHAR_LIGAND_ID
018236	NDDF
018309	NDDF
1145127006	SNOMEDCT_US
1145347005	SNOMEDCT_US
1217148000	SNOMEDCT_US
4040009	VANDF
2475076	RXNORM
340100	MMSL
38935	MMSL
38937	MMSL
d09653	MMSL
C584914	MESH_SUPPLEMENTAL_RECORD_UI
9903	INN_ID

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Vocabria	HUMAN PRESCRIPTION DRUG LABEL	1	49702-248	TABLET, FILM COATED	30 mg	ORAL	NDA	27 sections
Vocabria	HUMAN PRESCRIPTION DRUG LABEL	1	49702-248	TABLET, FILM COATED	30 mg	ORAL	NDA	27 sections
Vocabria	HUMAN PRESCRIPTION DRUG LABEL	1	49702-248	TABLET, FILM COATED	30 mg	ORAL	NDA	27 sections