Molecular Weight(MW): 444.42
Raltegravir (MK-0518) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM in cell-free assays, respectively. It shows greater than 1000-fold selectivity for HIV-1 IN over several related Mg2+-dependent enzyme such as HCV polymerase, HIV reverse transcriptase, HIV RNaseH and human α-, β-, γ-polymerases.
Cited by 12 Publications
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a: HCV, hepatitis C virus; HBV, hepatitis B virus. B: PI, protease inhibitor; NRTI, nucleoside reverse transcriptase inhibitor; NNRTI, nonnucleoside reverse transcriptase inhibitor; IN, integrase inhibitor. c: n=3. d: The EC50 for samatasvir in the presence of 45% human serum was 25 pM.
Antimicrob Agents Chemother, 2014, 58(8): 4431-42. Raltegravir (MK-0518) purchased from Selleck.
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|Description||Raltegravir (MK-0518) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM in cell-free assays, respectively. It shows greater than 1000-fold selectivity for HIV-1 IN over several related Mg2+-dependent enzyme such as HCV polymerase, HIV reverse transcriptase, HIV RNaseH and human α-, β-, γ-polymerases.|
|Features||The 1st approved human immunodeficiency virus type 1 (HIV-1) integrase inhibitor.|
PFV IN carrying the S217H substitution is 10-fold less susceptible to Raltegravir with IC50 of 900 nM. PFV IN displays 10% of WT activity and is inhibited by Raltegravir with an IC50 of 200 nM, indicating a ~twofold decrease in susceptibility to the IN strand transfer inhibitor (INSTI) compared with WT IN. S217Q PFV IN is as sensitive to Raltegravir as the WT enzyme.  Raltegravir is metabolized by glucuronidation, not hepatically. Raltegravir has potent in vitro activity against HIV-1, with a 95% inhibitory concentration of 31?0 nM, in human T lymphoid cell cultures. Raltegravir is also active against HIV-2 when Raltegravir is tested in CEMx174 cells, with an IC95 of 6 nM. Raltegravir metabolism occurs primarily through glucuronidation. Drugs that are strong inducers of the glucuronidation enzyme, UGT1A1, significantly reduce Raltegravir concentrations and should not be used. Raltegravir exhibits weak inhibitory effects on hepatic cytochrome P450 activity. Raltegravir does not induce CYP3A4 RNA expression or CYP3A4-dependent testosterone 6-β-hydroxylase activity.  Raltegravir cellular permeativity is reduced in the presence of magnesium and calcium.  Raltegravir and related HIV-1 integrase (IN) strand transfer inhibitors (INSTIs efficiently block viral replication.  In acutely infected human lymphoid CD4+ T-cell lines MT-4 and CEMx174, SIVmac251 replication is efficiently inhibited by Raltegravir, which shows an EC90 in the low nanomolar range. 
|In vivo||Raltegravir induces viro-immunological improvement of nonhuman primates with progressing SIVmac251 infection. One non-human primate shows an undetectable viral load following Raltegravir monotherapy. |
PFV integration assay:For quantitative strand transfer assays, donor DNA substrate is formed by annealing HPLC grade oligonucleotides 5′-GACTCACTATAGGGCACGCGTCAAAATTCCATGACA and 5′-ATTGTCATG GAATTTTGACGCGTGCCCTATAGTGAGTC. Reactions (40 μL) contains 0.75 μM PFV IN, 0.75 μM donor DNA, 4 nM (300 ng) supercoiled pGEM9-Zf(−) target DNA, 125 mM NaCl, 5 mM MgSO4, 4 μM ZnCl2, 10 mM DTT, 0.8% (vol/vol) DMSO, and 25 mM BisTris propane–HCl, pH 7.45. Raltegravir is added at indicated concentrations. Reactions are initiated by addition of 2 μL PFV IN diluted in 150 mM NaCl, 2 mM DTT, and 10 mM Tris-HCl, pH 7.4, and stopped after 1 hour at 37 °C by addition of 25 mM EDTA and 0.5% (wt/vol) SDS. Reaction products, deproteinized by digestion with 20 μg proteinase K for 30 minutes at 37 °C followed by ethanol precipitation, are separated in 1.5% agarose gels and visualized by staining with ethidium bromide. Integration products are quantified by quantitative real-time PCR, using Platinum SYBR Green qPCR SuperMix and three primers: 5′-CTACTTACTCTAGCTTCCCGGCAAC, 5′-TTCGCCAGTTAATAGTTTGCGCAAC, and 5′-GACTCACTATAGGGCACGCGT. PCR reactions (20 μL) contained 0.5 μM of each primer and 1 μL diluted integration reaction product. Following a 5-min denaturation step at 95 °C, 35 cycles are carried out in a CFX96 PCR instrument, using 10 seconds denaturation at 95 °C, 30 seconds annealing at 56 °C and 1 minutes extension at 68 °C. Standard curves are generated using serial dilutions of WT PFV IN reaction in the absence of INSTI.
-  Hare S, et al. Proc Natl Acad Sci U S A. 2010, 107(46), 20057-20062.
-  Hicks C, et al. Clin Infect Dis. 2009, 48(7), 931-939.
-  Moss DM, et al. Antimicrob Agents Chemother. 2012, 56(6), 3020-3026.
|In vitro||DMSO||88 mg/mL (198.01 mM)|
|In vivo||30% PEG400+0.5% Tween80+5% propylene glycol||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01867320||Recruiting||HTLV-I Infection||National Institute of Neurological Disorders and Stroke (NINDS)|National Institutes of Health Clinical Center (CC)||May 6, 2013||Early Phase 1|
|NCT02437110||Enrolling by invitation||Amyotrophic Lateral Sclerosis||National Institute of Neurological Disorders and Stroke (NINDS)|National Institutes of Health Clinical Center (CC)||April 23, 2015||Phase 1|
|NCT02655471||Not yet recruiting||HTLV-I Infections|Tropical Spastic Paraparesis||Universidad Peruana Cayetano Heredia|Merck Sharp & Dohme Corp.||March 2016||Early Phase 1|
|NCT02150993||Recruiting||HIV-2 Infection||French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)||January 2016||Phase 2|Phase 3|
|NCT02336074||Recruiting||HIV||Imperial College London|Medical Research Council|University of Oxford|University of Cambridge|Chelsea and Westminster NHS Foundation Trust|Royal Free Hospital NHS Foundation Trust|Brighton and Sussex University Hospitals NHS Trust|Guys and St Thomas NHS Foundation Trust|Central and North West London NHS Foundation Trust||November 2015||Phase 2|
|NCT02577042||Recruiting||Aging-related Inflammation in HIV-infected Patients||Fundacio Lluita Contra la SIDA||October 2015||Phase 4|
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