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

Stem definition	Drug id	CAS RN
antivirals	4805	1051375-16-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: dolutegravir sodium tivicay dolutegravir GSK 1349572 S-349572	Dolutegravir 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. Molecular weight: 419.39 Formula: C20H19F2N3O5 CLOGP: 0.08 LIPINSKI: 0 HAC: 8 HDO: 2 TPSA: 99.18 ALOGS: -3.66 ROTB: 3 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

dolutegravir sodium
tivicay
dolutegravir
GSK 1349572
S-349572

Dolutegravir 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.

Molecular weight: 419.39
Formula: C20H19F2N3O5
CLOGP: 0.08
LIPINSKI: 0
HAC: 8
HDO: 2
TPSA: 99.18
ALOGS: -3.66
ROTB: 3

Status: ONP

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

Drug dosage:

Dose	Unit	Route
50	mg	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
fu (Fraction unbound in plasma)	0.00 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

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Approvals:

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Date	Agency	Company
Aug. 12, 2013	FDA	VIIV HLTHCARE
Jan. 16, 2014	EMA	VIIV HEALTHCARE BV
March 24, 2014	PMDA	ViiV Healthcare K.K.

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FDA Adverse Event Reporting System (Female)

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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
Abortion spontaneous	732.68	30.33	257	7381	46938	63434446
Exposure during pregnancy	707.03	30.33	352	7286	155195	63326189
Foetal exposure during pregnancy	673.16	30.33	219	7419	31743	63449641
Virologic failure	654.13	30.33	123	7515	1739	63479645
Maternal exposure during pregnancy	632.12	30.33	367	7271	219695	63261689
Pathogen resistance	363.84	30.33	95	7543	6303	63475081
Blood HIV RNA increased	357.42	30.33	64	7574	675	63480709
Foetal death	325.99	30.33	98	7540	10882	63470502
Viral mutation identified	266.36	30.33	58	7580	1752	63479632
Stillbirth	256.56	30.33	73	7565	6677	63474707

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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
Virologic failure	915.20	18.26	216	11488	3264	34941963
Immune reconstitution inflammatory syndrome	708.93	18.26	214	11490	8545	34936682
Blood HIV RNA increased	528.03	18.26	114	11590	1116	34944111
Viral mutation identified	390.96	18.26	106	11598	2848	34942379
Foetal exposure during pregnancy	299.80	18.26	176	11528	37925	34907302
Pathogen resistance	290.77	18.26	112	11592	9370	34935857
Congenital umbilical hernia	229.31	18.26	45	11659	259	34944968
Birth mark	177.07	18.26	33	11671	137	34945090
Treatment noncompliance	167.86	18.26	109	11595	27991	34917236
Drug resistance	146.14	18.26	97	11607	25830	34919397

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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
Virologic failure	1198.86	17.67	254	15777	3937	79724420
Immune reconstitution inflammatory syndrome	834.30	17.67	240	15791	13601	79714756
Blood HIV RNA increased	682.58	17.67	138	15893	1670	79726687
Viral mutation identified	526.87	17.67	128	15903	3730	79724627
Exposure during pregnancy	432.47	17.67	263	15768	100869	79627488
Pathogen resistance	422.68	17.67	144	15887	14198	79714159
Maternal exposure during pregnancy	402.09	17.67	281	15750	136257	79592100
Abortion spontaneous	397.14	17.67	167	15864	29340	79699017
Treatment noncompliance	284.17	17.67	159	15872	52109	79676248
Foetal death	199.29	17.67	71	15960	7973	79720384

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FDA Adverse Event Reporting System (Pediatric)

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Pharmacologic Action:

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Source	Code	Description
ATC	J05AJ03	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Integrase inhibitors
ATC	J05AR13	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HIV infections, combinations
ATC	J05AR21	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HIV infections, combinations
ATC	J05AR25	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HIV infections, combinations
ATC	J05AR27	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HIV infections, combinations
FDA EPC	N0000175887	Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor
FDA MoA	N0000000127	HIV Integrase Inhibitors
FDA MoA	N0000187061	Organic Cation Transporter 2 Inhibitors
FDA MoA	N0000191423	Multidrug and Toxin Extrusion Transporter 1 Inhibitors
MeSH PA	D019380	Anti-HIV Agents

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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

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.24	acidic
pKa2	12.47	acidic

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
EQ 50MG BASE;300MG	DOVATO	VIIV HLTHCARE	N211994	April 8, 2019	RX	TABLET	ORAL	11234985	Jan. 24, 2031	TREATMENT OF HIV INFECTION
EQ 50MG BASE;EQ 25MG BASE	JULUCA	VIIV HLTHCARE	N210192	Nov. 21, 2017	RX	TABLET	ORAL	7125879	April 21, 2025	TREATMENT OF HIV INFECTION
EQ 50MG BASE;EQ 25MG BASE	JULUCA	VIIV HLTHCARE	N210192	Nov. 21, 2017	RX	TABLET	ORAL	10426780	Jan. 24, 2031	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
EQ 50MG BASE;300MG	DOVATO	VIIV HLTHCARE	N211994	April 8, 2019	RX	TABLET	ORAL	Aug. 6, 2023	TO REPLACE THE CURRENT ANTIRETROVIRAL REGIMEN IN THOSE WHO ARE VIROLOGICALLY SUPRESSED (HIV-1 RNA LESS THAN 50 COPIES PER ML) ON A STABLE ANTIRETROVIRAL REGIMEN WITH NO HISTORY OF TREATMENT FAILURE
EQ 600MG BASE;EQ 50MG BASE;300MG	TRIUMEQ	VIIV HLTHCARE	N205551	Aug. 22, 2014	RX	TABLET	ORAL	June 15, 2026	INFORMATION ADDED TO THE LABELING REGARDING THE RESULT OF STUDY 205860
EQ 600MG BASE;EQ 50MG BASE;300MG	TRIUMEQ	VIIV HLTHCARE	N205551	Aug. 22, 2014	RX	TABLET	ORAL	Dec. 15, 2026	PEDIATRIC EXCLUSIVITY
EQ 60MG BASE;EQ 5MG BASE;30MG	TRIUMEQ PD	VIIV HLTHCARE	N215413	March 30, 2022	RX	TABLET, FOR SUSPENSION	ORAL	June 15, 2026	NEW PATIENT POPULATION
EQ 60MG BASE;EQ 5MG BASE;30MG	TRIUMEQ PD	VIIV HLTHCARE	N215413	March 30, 2022	RX	TABLET, FOR SUSPENSION	ORAL	Dec. 15, 2026	PEDIATRIC EXCLUSIVITY

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Transmembrane protein 97	Enzyme	Q5BJF2	TMM97_HUMAN		Ki	7.75	CHEMBL
Integrase	Enzyme		Q7ZJM1_9HIV1	INHIBITOR	IC50	8.13	SCIENTIFIC LITERATURE	CHEMBL
Sigma non-opioid intracellular receptor 1	Membrane other		SGMR1_CAVPO		Ki	7.15	CHEMBL
Vesicular acetylcholine transporter	Transporter		VACHT_RAT		Ki	5.34	CHEMBL
Integrase	Enzyme		Q76353_9HIV1		IC50	8.57	CHEMBL
Sigma non-opioid intracellular receptor 1	Membrane receptor		SGMR1_RAT		Ki	6.66	CHEMBL
Sigma intracellular receptor 2	Unclassified		SGMR2_RAT		Ki	7.50	CHEMBL
Integrase	Unclassified		P89582_9HIV2		EC50	8.64	CHEMBL

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External reference:

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ID	Source
DLU	PDB_CHEM_ID
015174	NDDF
015175	NDDF
1051375-19-9	SECONDARY_CAS_RN
1433867	RXNORM
205031	MMSL
29613	MMSL
30505	MMSL
4032640	VANDF
54726191	PUBCHEM_CID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Dolutegravir	HUMAN PRESCRIPTION DRUG LABEL	1	65015-353	TABLET, FOR SUSPENSION	10 mg	ORAL	Export only	1 sections
Dolutegravir	HUMAN PRESCRIPTION DRUG LABEL	1	65015-353	TABLET, FOR SUSPENSION	10 mg	ORAL	Export only	1 sections
Dovato	HUMAN PRESCRIPTION DRUG LABEL	2	49702-246	TABLET, FILM COATED	50 mg	ORAL	NDA	29 sections
Dovato	HUMAN PRESCRIPTION DRUG LABEL	2	49702-246	TABLET, FILM COATED	50 mg	ORAL	NDA	29 sections
Dovato	HUMAN PRESCRIPTION DRUG LABEL	2	49702-246	TABLET, FILM COATED	50 mg	ORAL	NDA	29 sections
Dovato	HUMAN PRESCRIPTION DRUG LABEL	2	49702-246	TABLET, FILM COATED	50 mg	ORAL	NDA	29 sections
Juluca	HUMAN PRESCRIPTION DRUG LABEL	2	49702-242	TABLET, FILM COATED	50 mg	ORAL	NDA	28 sections
Juluca	HUMAN PRESCRIPTION DRUG LABEL	2	49702-242	TABLET, FILM COATED	50 mg	ORAL	NDA	28 sections
Juluca	HUMAN PRESCRIPTION DRUG LABEL	2	49702-242	TABLET, FILM COATED	50 mg	ORAL	NDA	28 sections
Juluca	HUMAN PRESCRIPTION DRUG LABEL	2	49702-242	TABLET, FILM COATED	50 mg	ORAL	NDA	28 sections

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