Raltegravir (CAS 518048-05-0) Suppliers and Product Information

Raltegravir is an HIV integrase strand transfer inhibitor used to treat HIV-1 infection in combination with other antiretroviral drugs. It works by inhibiting HIV integrase, an enzyme essential for viral replication. Raltegravir is formulated as the potassium salt for oral administration and is marketed under the brand name Isentress.

Frequently Asked Questions about Raltegravir

Q: What is the mechanism of action of Raltegravir?

A: Raltegravir inhibits HIV-1 integrase, preventing the integration of viral DNA into the host cell genome. It specifically inhibits the strand transfer activity of HIV-1 integrase with high selectivity.

Q: What are the common side effects of Raltegravir?

A: The most common side effects include diarrhea, nausea, headache, and fatigue. In rare cases, muscle-related issues such as myopathy and rhabdomyolysis have been reported.

Q: Are there any significant drug interactions with Raltegravir?

A: Raltegravir's concentration may be reduced by rifampicin. It should be avoided with fosamprenavir, and its absorption may be affected by orlistat. Omeprazole and famotidine may increase its concentration.

Q: How is Raltegravir metabolized and excreted?

A: Raltegravir is primarily metabolized through hepatic glucuronidation mediated by the UGT 1A1 enzyme. It is excreted in both feces (51%) and urine (32%) as unaltered compound and its glucuronide.