Raltegravir

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Description:
Raltegravir (MK-0518, brand name Isentress) is an antiretroviral drug produced by Merck & Co., used to treat HIV infection. It received approval by the U.S. Food and Drug Administration (FDA) in October 2007, the first of a new class of HIV drugs, the integrase inhibitors, to receive such approval.

Mechanism

Raltegravir targets integrase, an HIV enzyme that integrates the viral genetic material into human chromosomes, a critical step in the pathogenesis of HIV. The drug is metabolized away via glucuronidation.

Dosage

Raltegravir is taken orally twice daily. Doses of 200, 400, and 600 mg have been studied.

At the 2007 Conference on Retroviruses and Opportunistic Infections, researchers presented Phase III data showing that 77% of patients taking the 400 mg dose of raltegravir plus other antiretroviral drugs reached HIV viral loads below 400 copies, nearly twice as many compared with a control group.

Indications

Raltegravir was initially approved only for use in individuals whose infection has proven resistant to other HAART drugs. As with any HAART medication, raltegravir...
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