Latest research on MK-0518

Raltegravir 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) on 12 October 2007, the first of a new class of HIV drugs, the integrase inhibitors, to receive such approval. [Wikipedia]

Latest findings

Chemical optimisation of these compounds led to naphthyridine derivatives and L-900612 or MK-0518 (raltegravir) as a promising candidate compound. [source, 2009]
• Merck and Company announced it would cut its price of Stocrin (Efavirenz) in Mexico by 40% from 777 pesos per patient monthly to 468 pesos (roughly from US $77.50 to US $46), and on Isentress (raltegravir) by 30% from 9.05 pesos to 6.85 pesos per patient monthly (approximately US $903 to US $683). [source, 2009]
Further modifications of these compounds led to the synthesis of a new naphthyridine derivative, raltegravir (formerly known as L-900612 and MK-0518) and its emergence as a candidate for further development. [source, 2008]
With twice daily dosing, pharmacokinetic steady state is achieved within approximately the first 2 days of dosing (Isentress 2007; Isentress FDA Briefing Document 2007; Kassahun et al 2006). [source, 2008]
The major mechanism of clearance of raltegravir in human beings is metabolism via UGT1A1-mediated glucuronidation (Isentress 2007; Isentress FDA Briefing Document 2007; Kassahun et al 2006, 2007). [source, 2008]
No adjustment of dosing is necessary for age, gender, body mass index, HIV infection status, hepatic and renal function (Isentress 2007; Isentress FDA Briefing Document 2007). [source, 2008]
Thus, it is expected that interactions with drugs metabolized by the CYP450 system, including protease inhibitors and non-nucleoside reverse transcriptase inhibitors, are unlikely (Isentress FDA Briefing Document 2007). [source, 2008]
A number of HIV-1 IN inhibitors have been identified and few have been clinically examined including GS-9137 [1-3] and MK-0518 [4]. [source, 2008]
Recent examples include the development of inhibitors for MAP kinase p38 (50) and PTP1B (51) that have entered clinical trials and the recently approved HIV integrase inhibitor, raltegravir (marketed as Isentress, Merck, Whitehouse Station, NJ, USA) (52,53). [source, 2008]
Therefore, the development or availability of new drugs such as Fuzeon, the HIV-1 integrase inhibitor raltegravir (MK-0518) (Grinsztejn et al. 2007) and the CCR5 antagonist maraviroc (Stephenson, 2007) that remain active against drug resistant virus is essential for the continuing success of HAART (Yeni, 2006). [source, 2007]