Cabotegravir Impurities

General Information

Cabotegravir Impurities and Cabotegravir 

Daicel Pharma synthesizes Cabotegravir impurities of exceptional quality, such as Cabotegravir impurity 1, Cabotegravir Intermediate-1, Cabotegravir RR Isomer, Cabotegravir RS Isomer, and Cabotegravir SS Isomer. These impurities are crucial to assess the purity, reliability, and safety of Cabotegravir, an active pharmaceutical ingredient. Besides, Daicel Pharma provides custom synthesis of Cabotegravir impurities to meet clients’ demands for worldwide delivery.

Cabotegravir [CAS: 1051375-10-0], also known as GSK1265744A, is a medication for treating HIV-1 infection. It is an integrase inhibitor, often prescribed alongside the non-nucleoside reverse transcriptase inhibitor rilpivirine. Cabotegravir helps in the treatment of HIV-1 infection in individuals who have viral suppression.

Cabotegravir: Use and Commercial Availability 

Cabotegravir is a prescription drug in two forms and is available under two brand names. Vocabria is an oral tablet in combination with another HIV medication called rilpivirine (Edurant) for short-term HIV-1 treatment in adults, virologically suppressed. Apretude is an extended-release injectable form of Cabotegravir that treats at-risk adults and adolescents weighing at least 35 Kg for pre-exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 infection.

Cabotegravir Structure and Mechanism of Action

The chemical name of Cabotegravir is (3S,11aR)-N-[(2,4-Difluorophenyl)methyl]-2,3,5,7,11,11a-hexahydro-6-hydroxy-3-methyl-5,7-dioxooxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide. Its chemical formula is C₁₉H₁₇F₂N₃O₅, and its molecular weight is approximately 405.4 g/mol.

Cabotegravir binds to the HIV integrase active site and inhibits HIV integrase. It blocks the strand transfer step of retroviral deoxyribonucleic acid (DNA) integration for the HIV replication cycle.

Cabotegravir Impurities and Synthesis

Like any other pharmaceutical substance, Cabotegravir may contain impurities that affect its safety and efficacy. These impurities form during the synthesis¹, purification, and storage of the drug substance. They can include process-related impurities, such as starting materials, reagents, intermediates, and degradation products that arise due to the chemical or physical instability of the drug substance or its formulation. The presence of impurities can pose potential risks to patients, such as toxicity, reduced potency, or adverse effects. So, it is essential to control and monitor the levels of impurities in Cabotegravir to ensure that it meets the quality and safety standards required for pharmaceutical products.

Daicel Pharma offers a Certificate of Analysis (CoA) for Cabotegravir impurity standards, such as Cabotegravir impurity 1, Cabotegravir Intermediate-1, Cabotegravir RR Isomer, Cabotegravir RS Isomer, and Cabotegravir SS Isomer, generated from an analytical facility compliant with cGMP standards. The CoA includes a comprehensive characterization report comprising data from techniques like 1H NMR, 13C NMR, IR, MASS, and HPLC purity². Furthermore, on request, we can provide additional data like 13C-DEPT and CHN. Daicel Pharma can synthesize unknown Cabotegravir impurities or degradation products. A complete characterization report accompanies every delivery.