Cabotegravir (GSK744, GSK1265744)
Molecular Weight(MW): 405.35
Cabotegravir (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor against a broad range of HIV subtypes, and inhibits the HIV-1 integrase catalyzed strand transfer reaction with IC50 of 3.0 nM. Phase 2.
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Choose Selective Integrase Inhibitors
|Description||Cabotegravir (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor against a broad range of HIV subtypes, and inhibits the HIV-1 integrase catalyzed strand transfer reaction with IC50 of 3.0 nM. Phase 2.|
GSK1265744 inhibits HIV replication with EC50 of 0.22 nM and 0.34-1.3 nM against HIV-1 Ba-L and NL432, respectively. GSK1265744 produces cytotoxicity with CC50 of 6.4, 5.0, 9.2, and 13 μM in proliferating IM-9, U-937, MT-4, and Molt-4 cell lines, respectively. 
|In vivo||GSK1265744 (50 mg/kg) treatment protects rhesus macaques against three high-dose SHIV challenges. |
In vitro strand transfer assay:The inhibitory concentrations of GSK1265744 is measured in a strand transfer assay using recombinant HIV IN. A complex of integrase and biotinylated donor DNA–streptavidin-coated SPA beads is formed by incubating 2 μM purified recombinant integrase with 0.66 μM biotinylated donor DNA–4 mg/mL streptavidin-coated SPA beads in 25 mM sodium MOPS pH 7.2, 23 mM NaCl, and 10 mM MgCl2 for 5 minutes at 37°C. These beads are spun down and preincubated with diluted INSTIs for 60 minutes at 37°C. Next, [3H]-labeled target DNA substrate is added to give a final concentration of 7 nM substrate, and the strand transfer reaction is incubated at 37°C for 25 to 45 minutes, which allowed for a linear increase in strand transfer of donor DNA to radiolabeled target DNA. The signal is read using a Wallac MicroBeta scintillation plate reader.
|In vitro||DMSO||38 mg/mL warmed (93.74 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02799264||Completed||Drug: Cabotegravir 30 mg||Infection Human Immunodeficiency Virus||ViiV Healthcare|Glaxosmithkline/Quintiles||June 2016||Phase 1|
|NCT02462772||Withdrawn||Drug: cabotegravir|Drug: Placebo||Human Immunodeficiency Virus||Centre for the AIDS Programme of Research in South Africa|ViiV Healthcare||October 2015||Phase 2|
|NCT02354937||Completed||Drug: GSK1265744 30 mg||Infection Human Immunodeficiency Virus|HIV Infections||ViiV Healthcare||July 13 2015||Phase 1|
|NCT02354950||Completed||Drug: GSK1265744 30mg||HIV Infections||ViiV Healthcare|GlaxoSmithKline||June 22 2015||Phase 1|
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