Drug intelligence / Profile preview

Dolutegravir + Tenofovir Alafenamide

Development stage
Unknown
Lead developer
Viatris
Modality
Small Molecules
Administration
Oral
01

Overview

The combination of dolutegravir and tenofovir alafenamide is a fixed-dose combination antiretroviral medication used to treat HIV/AIDS. This combination typically includes a third component, either emtricitabine or lamivudine, to create a complete HIV treatment regimen. Based on search results, this combination is available in two main formulations: 1. Dolutegravir + emtricitabine + tenofovir alafenamide (50mg/200mg/25mg) 2. Dolutegravir + lamivudine + tenofovir alafenamide (50mg/300mg/25mg) Dolutegravir is an integrase strand transfer inhibitor (INSTI), while tenofovir alafenamide is a nucleoside analog reverse transcriptase inhibitor (NRTI). When combined with either emtricitabine or lamivudine (both NRTIs), they form a complete antiretroviral therapy regimen for HIV-1 infection. The medication works by inhibiting HIV viral replication through multiple mechanisms, preventing the virus from integrating its genetic material into host cells and blocking reverse transcription. This combination helps increase CD4 T cell counts and reduces viral load in patients with HIV. Common side effects include nausea, headache, diarrhea, and insomnia. More serious potential adverse effects include hypersensitivity reactions, hepatotoxicity, and possible embryo-fetal toxicity. This combination received tentative FDA approval under PEPFAR (President's Emergency Plan for AIDS Relief) in 2018 and is used as a first-line treatment for HIV/AIDS in many countries.

02

Targets

Integrase allosteric pocket (HIV)Human immunodeficiency virus type 1 reverse transcriptaseOCT2 (Organic cation transporter 2)

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