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

Raltegravir was registered under the trademark Isentress TM ; it is manufactured in the form of 400 mg tablets for twice-daily oral administration. [source, 2011]
To date, only one IN inhibitor has been licensed for use in HIV-1 treatment; this being raltegravir which is marketed under the brand name Isentress® (Merck & Co., Inc., White house station, NJ) and was also formerly called MK-0518. [source, 2011]
Raltegravir (MK-0518; Isentress, Merck) was the first integrase (IN) inhibitor approved for treatment of HIV infection [1], while other compounds such as GS-9137 [2], S-1360 [3], and L-870,810 [4] are at different stages of development. [source, 2011]
Two DKA derivatives Raltegravir (MK-0518) [21] and Elvitegravir (GS-9137) have been recently approved as anti-AIDS drug or in clinical trials [22]. [source, 2011]
Clinical formulations of these drugs in tablet form (Maraviroc (Selzentry) 150 mg, Pfizer Labs; Raltergravir (Isentress) 400 mg, Merck & Co) were freshly dissolved in distilled water each day prior to oral gavage. [source, 2010]
In October 2007, raltegravir (MK-0518; Isentress, Merck, Whitehouse Station, NJ) was the first approved HIV-1 integrase inhibitor; it targets the strand transfer step of HIV-1 integration. [source, 2010]
After years of sustained effort, Merck and Co. successfully developed raltegravir (RAL, Isentress® also known as MK-0518), which was approved by the FDA in late 2007 as the first IN inhibitor (Table 1). [source, 2010]
Raltegravir is the first integrase inhibitor to get into the clinic and the MK-0518 Expanded Access Program (EAP) started in Italy in 2007, so that most patients now have an observation period of two years. [source, 2010]
They now include the integrase inhibitor raltegravir (Isentress), recently approved by the US Food and Drug Administration (FDA) for ART-naïve patients, in combination with the NRTIs tenofovir (TDF) and emtricitabine (FTC) [13]. [source, 2010]
For example, one recent MD study of HIV integrase revealed a previously uncharacterized binding trench that was subsequently exploited in the design of Isentress (raltegravir), an HIV drug approved by the FDA in 2007 [24]. [source, 2010]