Overview
Bictegravir is a next-generation integrase inhibitor developed by Gilead Sciences for HIV-1 treatment. It blocks viral DNA integration into host cells, a critical step in the HIV lifecycle. Approved by the FDA in 2018, it is often combined with emtricitabine and tenofovir alafenamide in single-tablet regimens like Biktarvy®. Its advantages include once-daily dosing, minimal drug interactions, and efficacy against resistant strains. As a cornerstone of modern antiretroviral therapy (ART), it is widely used in both treatment-naïve and experienced patients.
Physical and Chemical Properties
Bictegravir is a white crystalline powder with a molecular weight of 449.38 g/mol. It is sparingly soluble in water but dissolves well in dimethyl sulfoxide (DMSO), a property leveraged in pharmaceutical formulations. The compound exhibits stability under recommended storage conditions (2-8°C). Its chemical structure features a trifluoromethyl group and a pyridinol moiety, contributing to its high binding affinity for the HIV integrase enzyme.
Main Applications
Bictegravir is exclusively used in HIV-1 therapy, typically in fixed-dose combinations such as Biktarvy® (with emtricitabine/tenofovir alafenamide). It is prescribed for adults and pediatric patients weighing ≥25 kg. Clinical trials demonstrate its non-inferiority to dolutegravir-based regimens, with fewer side effects like weight gain. Its high genetic barrier to resistance makes it a preferred choice in first-line ART, particularly in resource-limited settings due to its tolerability.
Safety and Storage
As a pharmaceutical intermediate, bictegravir requires careful handling. Use gloves, goggles, and respiratory protection to avoid exposure. In case of contact, rinse skin/eyes immediately with water. Store in sealed containers at 2-8°C, protected from moisture and light. Stability studies indicate degradation under excessive heat (>40°C) or humidity. Dispose of waste per local hazardous material regulations.
B2B Procurement Guide
Buyers should prioritize suppliers with GMP certification and proven API manufacturing expertise. Confirm CAS 1611493-60-7 and request certificates of analysis (CoA) for purity (typically ≥98%). Bulk pricing varies by volume and supplier location. Negotiate contracts with pharmaceutical-grade producers in India or China, where most generic versions originate. Monitor regulatory updates, as patents may affect availability in certain regions.
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