Dolutegravir

Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor — ANTIINFECTIVES FOR SYSTEMIC USE

Key facts

Dolutegravir is an onp drug in the Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2013. Its mechanism of action is classified as HIV Integrase Inhibitors, Multidrug and Toxin Extrusion Transporter 1 Inhibitors and Organic Cation Transporter 2 Inhibitors. DrugCentral lists 8 molecular targets, including pol, Integrase and pol. Recorded indications include Human immunodeficiency virus infection.

• Approval status: onp (first approved 2013 by the FDA).
• Drug class: Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor.
• Mechanism of action: HIV Integrase Inhibitors; Multidrug and Toxin Extrusion Transporter 1 Inhibitors; Organic Cation Transporter 2 Inhibitors.
• Molecular targets: pol, Integrase, pol and TMEM97 (8 listed in DrugCentral).
• Indications: Human immunodeficiency virus infection.
• ATC code: J05AJ03 (Integrase inhibitors).
• Molecular formula: C20H19F2N3O5; molecular weight 419.38 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Human immunodeficiency virus infection

Mechanism & targets

• Mechanism of action (MoA): HIV Integrase Inhibitors; Multidrug and Toxin Extrusion Transporter 1 Inhibitors; Organic Cation Transporter 2 Inhibitors
• Established pharmacologic class: Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor

Molecular targets (8)

Target	Gene	Action	Activity
Integrase	pol	unknown	EC50 8.64
Integrase	—	unknown	IC50 8.57
Integrase	pol	inhibitor	IC50 8.13
Transmembrane protein 97	TMEM97	unknown	Ki 7.75
Sigma intracellular receptor 2	Tmem97	unknown	Ki 7.50
Sigma non-opioid intracellular receptor 1	SIGMAR1	unknown	Ki 7.15
Sigma non-opioid intracellular receptor 1	Sigmar1	unknown	Ki 6.66
Vesicular acetylcholine transporter	Slc18a3	unknown	Ki 5.34

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2014-03-24	PMDA	—	ViiV Healthcare K.K.	Yes
2014-01-16	EMA	—	VIIV HEALTHCARE BV
2013-08-12	FDA	—	VIIV HLTHCARE

ATC classification

ATC code	Therapeutic hierarchy
J05AJ03	ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Integrase inhibitors
J05AR13	ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Antivirals for treatment of HIV infections, combinations
J05AR21	ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Antivirals for treatment of HIV infections, combinations
J05AR25	ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Antivirals for treatment of HIV infections, combinations
J05AR27	ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Antivirals for treatment of HIV infections, combinations
J05AR29	ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Antivirals for treatment of HIV infections, combinations

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: UGT1A1 · Informative PGx
• FDA label: UGT1A1 · Informative PGx
• HCSC label: UGT1A1 · Informative PGx
• Swissmedic label: CYP3A4, CYP3A5, NR1I2, UGT1A1 · Informative PGx

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Virologic failure	3744.8
Viral mutation identified	2277.1
Pathogen resistance	2118.8
Blood HIV RNA increased	2021.5
Foetal exposure during pregnancy	1959.4
Immune reconstitution inflammatory syndrome	1495.1
Exposure during pregnancy	1175.7
Foetal death	844.2
Food allergy	704.0
Treatment noncompliance	703.8
Congenital umbilical hernia	699.7
Abortion spontaneous	651.8

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Dolutegravir is on its molecule page.

• Molecular formula: C₂₀H₁₉F₂N₃O₅
• Molecular weight: 419.38 g/mol
• CAS number: 1051375-16-6
• InChIKey: RHWKPHLQXYSBKR-BMIGLBTASA-N
• PubChem CID: 54726191

C[C@@H]1CCO[C@H]2CN3C=C(C(=O)NCC4=C(F)C=C(F)C=C4)C(=O)C(O)=C3C(=O)N12

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Dolutegravir used for?

DrugCentral lists the following indications for Dolutegravir: Human immunodeficiency virus infection.

How does Dolutegravir work?

Dolutegravir is classified as HIV Integrase Inhibitors, Multidrug and Toxin Extrusion Transporter 1 Inhibitors and Organic Cation Transporter 2 Inhibitors; its molecular targets in DrugCentral include pol, Integrase, pol (inhibitor) and TMEM97.

When was Dolutegravir first approved?

Dolutegravir was first approved by the FDA in 2013.

What drug class does Dolutegravir belong to?

Dolutegravir is in the Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor class.

What is the chemical formula of Dolutegravir?

Dolutegravir has the molecular formula C20H19F2N3O5 and a molecular weight of 419.38 g/mol.

Sources

• DrugCentral drug card 4805 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1213165 — compound record and bioactivity
• PubChem CID 54726191 — chemical identifiers
• DrugBank DB08930 — drug record
• FDA UNII DKO1W9H7M1 — substance identity
• DailyMed: FDA labels for Dolutegravir — current prescribing information (label search)
• UniProt Q5BJF2 (TMEM97) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.