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

The HARRT regiments were based on 2 reverse transcriptase inhibitors (mainly Combivir, Truvada, or Kivexa) and either a nonnucleoside reverse transcriptase inhibitor (Efaviranze) or a boosted protease inhibitor (mainly Kaletra, boosted Atazanavir, or boosted Darunavir) or an integrase inhibitor (Isentress). [source, 2016]
Among HIV-1 IN inhibitors, Raltegravir (RAL; Isentress, Merck) was the first integrase strand transfer inhibitor (INSTI) licensed in 2007 by the U.S. [source, 2015]
Raltegravir (MK-0518), developed by Merck and Co, Inc. (Whitehouse Station, NJ, USA), was the first HIV-1 IN inhibitor approved by the US Food and Drug Administration (FDA), in 2007. [source, 2014]
Raltegravir (also known as MK0518, Isentress) is a first-in-its-class oral integrase inhibitor and has demonstrated potent efficacy against multidrug-resistant HIV-1 and was initially approved by the FDA in 2007 to treat treatment-experienced HIV-1-infected patients [11]. [source, 2014]
The first approved HIV-1 IN inhibitor is raltegravir (MK-0518), obtained from the optimization of DKA lead compounds containing hydroxy-8-(1,6)-7-naphthyridine carboxamide and N-alkyl-5-hydroxypyrimidinone groups [9]–[14]. [source, 2014]
PubMed and EMBASE search terms were “HIV-1 [mesh] OR HIV infections [mesh] NOT pregnancy [mesh] AND ((dolutegravir OR GSK1349572) OR (Efavirenz OR Sustiva OR Stocrin OR DMP-266) OR (raltegravir OR Isentress OR MK-0518) OR (elvitegravir OR GS-9137 OR JTK-303) OR (rilpivirine OR Edurant OR TMC 278) OR (Darunavir OR Prezista OR TMC-114) OR (atazanavir OR Reyataz OR BMS-232632) OR (lopinavir OR ABT-378 OR Aluviran OR Koletra OR Kaletra) OR (Atripla OR Quad OR Stribild OR Eviplera OR Complera))”. [source, 2014]
Raltegravir (RAL, MK-0518, Isentress, Merck & Co., Inc.) was the first INSTI approved in 2007 [5]. [source, 2014]
Raltegravir or Isentress is the first antiretroviral integrase inhibitor approved by the US Food and Drug Administration in 2009 [1] and the European Medicines Agency in 2007 [2]. [source, 2014]
The dosage of raltegravir (Isentress, Merck & Co., Inc., Whitehouse Station, NJ, USA) was determined based on the human therapeutic dosing (400 mg twice daily, orally), for the average human body weight of 60 kg [22] and multiplying by 10, because it has been described that experimental animals are generally less vulnerable than humans, by a factor of approximately 10 [23]. [source, 2014]
The QDMRK study (MK-0518 protocol 071) compared 800 mg of RAL taken once daily (QD) or 400 mg of RAL taken twice daily (BID), both in combination with FTC/TDF in an international, double-blind, phase 3, randomized trial [30]. [source, 2014]