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||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00920426||Completed||Infection Human Immunodeficiency Virus||ViiV Healthcare|Shionogi|GlaxoSmithKline||June 9 2009||Phase 2|
|NCT03164564||Recruiting||HIV Infections||National Institute of Allergy and Infectious Diseases (NIAID)||November 7 2017||Phase 3|
|NCT03149848||Completed||Infection Human Immunodeficiency Virus||ViiV Healthcare|GlaxoSmithKline||June 6 2017||Phase 1|
|NCT01641809||Active not recruiting||Infection Human Immunodeficiency Virus||ViiV Healthcare|GlaxoSmithKline||August 6 2012||Phase 2|
|NCT02951052||Active not recruiting||Infection Human Immunodeficiency Virus||ViiV Healthcare|Janssen Pharmaceuticals|GlaxoSmithKline||October 28 2016||Phase 3|
|NCT03299049||Active not recruiting||HIV Infections||ViiV Healthcare|Janssen Research and Development||October 27 2017||Phase 3|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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