What type of inhibitor is raltegravir?
What type of inhibitor is raltegravir?
Raltegravir is the first approved human immunodeficiency virus type 1 (HIV-1) integrase inhibitor; it targets the strand transfer step of HIV-1 integration.
What does raltegravir target?
Therefore, there is a continued need for new classes of drugs. The integrase inhibitors target a viral enzyme that catalyses an essential process in the replication cycle of HIV – the insertion of HIV-1 proviral DNA into the host’s cellular genome.
How is raltegravir excreted?
Raltegravir is metabolized by uridine diphosphate-glucuronosyl-transferase (UGT) to a glucuronide metabolite, mainly by UGT1A1. The dose is eliminated in both the urine (32%) and feces (51%), with metabolite accounting for 23% and 0% in the urine and feces, respectively.
Is there another name for raltegravir?
Raltegravir, sold under the brand name Isentress, is an antiretroviral medication used, together with other medication, to treat HIV/AIDS.
What process does raltegravir inhibit?
Raltegravir is an antiretroviral drug used in the treatment of HIV-1 infection. The drug inhibits the activity of HIV-1 integrase, which impedes the insertion of HIV-1 DNA into the host cell genome. Integrase is a vital enzyme that catalyzes two reactions, which must occur for viral DNA insertion into the host DNA.
What is the role of integrase?
Integrase is the viral enzyme that catalyzes the integration of virally derived DNA into the host cell DNA in the nucleus, forming a provirus that can be activated to produce viral proteins.
Where does integrase come from?
HIV integrase is a 32 kDa protein produced from the C-terminal portion of the Pol gene product, and is an attractive target for new anti-HIV drugs.
What is the mechanism of action of raltegravir?
When should I take raltegravir?
Raltegravir (Isentress® HD) tablets are usually taken with or without food once a day. Take raltegravir at the same time(s) every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take raltegravir exactly as directed.
Who invented raltegravir?
Considering the experience that has been gathered since the 1980s of ARV drug development arrival of INSTIs as a new potent class of ARV signals a new era in the treatment of HIV. Development of a successful INSTI treatment was accomplished when raltegravir was discovered by Merck Sharp & Dohme Limited.
Is Raltegravir a competitive inhibitor?
Raltegravir and elvitegravir share the same mechanism of action against integrase: to bind to the active site of Mg2+ ions. Competitive inhibitors compete directly with viral DNA for binding to integrase in order to inhibit 3′-end processing.
