Overview
Dolutegravir is an HIV-1 integrase inhibitor that blocks the strand transfer step of the integration of the viral genome into the host cell (INSTI). The effect of this drug has no homology in human host cells, which gives it excellent tolerability and minimal toxicity. Dolutegravir was developed by ViiV Healthcare and FDA-approved on August 12, 2013. On November 21, 2017, dolutegravir, in combination with rilpivirine, was approved as part of the first complete treatment regimen with only two drugs for the treatment of adults with HIV-1 named Juluca.
Indication
Dolutegravir is indicated in combination with other antiretroviral agents for the treatment of patients with HIV-1 infection that comply with the characteristics of being adults or children aged 12 years and older and present at least a weight of 40 kg. The FDA combination therapy approval of dolutegravir and rilpivirine is indicated for adults with HIV-1 infections whose virus is currently suppressed (< 50 copies/ml) on a stable regimen for at least six months, without history of treatment failure and no known substitutions associated to resistance to any of the two components of the therapy. Dolutegravir is also available in combination with lamivudine and abacavir for the treatment of adult and pediatric patients with HIV-1 who weigh ≥10kg.
Associated Conditions
- Human Immunodeficiency Virus Type 1 (HIV-1) Infection
Research Report
Dolutegravir: A Comprehensive Pharmacological and Clinical Review
1. Introduction
1.1. Overview of Dolutegravir as an Antiretroviral Agent
Dolutegravir (DrugBank ID: DB08930, CAS Number: 1051375-16-6) is a second-generation integrase strand transfer inhibitor (INSTI) that has become a cornerstone in the contemporary management of Human Immunodeficiency Virus type 1 (HIV-1) infection. As a small molecule antiviral agent, dolutegravir is administered in combination with other antiretroviral drugs to suppress viral replication. Its primary mechanism of action involves blocking the strand transfer step of viral genome integration into the host cell's DNA [User Query]. This targeted viral process has no direct counterpart in human cellular mechanisms, a characteristic that contributes significantly to dolutegravir's generally favorable tolerability and minimal toxicity profile observed in clinical practice.[1] This specificity for a viral enzyme is a highly desirable attribute for antiretroviral agents intended for long-term administration, as is typical in HIV-1 management, potentially reducing the burden of off-target effects often associated with older drug classes.
1.2. Development and Key Approval Milestones
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/05/13 | Phase 4 | Not yet recruiting | UBATEC | ||
2025/02/03 | Not Applicable | Not yet recruiting | Federal University of São Paulo | ||
2025/01/22 | Phase 4 | Not yet recruiting | |||
2024/12/24 | Phase 3 | Not yet recruiting | |||
2024/07/11 | Phase 3 | Not yet recruiting | |||
2024/06/10 | Phase 1 | Completed | Humanis Saglık Anonim Sirketi | ||
2024/02/28 | Phase 1 | Recruiting | |||
2024/08/19 | Phase 3 | Recruiting | |||
2023/09/29 | Phase 2 | Recruiting | Shanxi Kangbao Biological Product Co., Ltd. | ||
2023/08/15 | Phase 2 | Recruiting | PENTA Foundation |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| No FDA approvals found for this drug. | |||||
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
Authorised | 1/16/2014 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| TIVICAY DISPERSIBLE TABLET 5 MG | SIN16504P | TABLET, FOR SUSPENSION | 5.00 mg | 5/30/2022 | |
| TIVICAY TABLET 50MG | SIN14579P | TABLET, FILM COATED | 50mg | 7/31/2014 | |
| TRIUMEQ FILM COATED TABLET 50mg/600mg/300mg | SIN15100P | TABLET, FILM COATED | 50 mg | 10/14/2016 | |
| DOVATO FILM-COATED TABLET 50MG/300MG | SIN15989P | TABLET, FILM COATED | 50 mg | 8/13/2020 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| TRIUMEQ dolutegravir (as sodium) 50 mg/abacavir (as sulfate) 600 mg/lamivudine 300 mg tablet bottle | 218644 | Medicine | A | 1/14/2015 | |
| JULUCA dolutegravir (as sodium) 50 mg/ rilpivirine (as hydrochloride) 25 mg tablet bottle | 291356 | Medicine | A | 6/20/2018 | |
| TIVICAY dolutegravir (as sodium) 50 mg film-coated tablet bottle | 205212 | Medicine | A | 1/17/2014 |
Health Canada Drug Approvals
Approved Product | Company | DIN | Dosage Form | Strength | Market Date |
|---|---|---|---|---|---|
| No Health Canada approvals found for this drug. | |||||
CIMA AEMPS Drug Approvals
Approved Product | Company | Registration Number | Pharmaceutical Form | Prescription Type | Status |
|---|---|---|---|---|---|
| No CIMA AEMPS (Spain) approvals found for this drug. | |||||
Philippines FDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Philippines FDA approvals found for this drug. | |||||
Saudi SFDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Saudi SFDA approvals found for this drug. | |||||
Malaysia NPRA Drug Approvals
Approved Product | Company | Registration Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Malaysia NPRA approvals found for this drug. | |||||
UK EMC Drug Information
Medicine Name | MA Holder | MA Number | Pharmaceutical Form | Active Ingredient | Authorization Date |
|---|---|---|---|---|---|
| No UK EMC drug information found for this drug. | |||||
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