Preclinical Pharmacology, Antitumor Activity, and Development of Pharmacodynamic Markers for the Novel, Potent AKT Inhibitor CCT128930

    February 2011 in “ Molecular cancer therapeutics ”
    Timothy A. Yap, Michael I. Walton, Lisa-Jane K. Hunter, Melanie Valenti, Alexis de Haven Brandon, Paul D. Eve, Ruth Ruddle, Simon P. Heaton, Alan T. Henley, Lisa Pickard, Gowri Vijayaraghavan, John Caldwell, Neil T. Thompson, Wynne Aherne, Florence I. Raynaud, Suzanne A. Eccles, Paul Workman, Ian Collins, Michelle D. Garrett
    TLDR CCT128930 is a promising new drug that effectively targets and inhibits a cancer-related protein, showing potential for cancer treatment.
    CCT128930 was a novel, potent AKT inhibitor that showed high selectivity for AKT over PKA and significant antiproliferative activity in various tumor cell lines, including PTEN-null U87MG glioblastoma cells. It caused G1 arrest, inhibited AKT substrate phosphorylation, and demonstrated marked antitumor activity in U87MG and BT474 breast cancer xenografts. Pharmacokinetic studies indicated effective tumor concentrations, and a novel biomarker assay using hair follicles was developed to measure AKT inhibition, showing promise for clinical trials. The study concluded that CCT128930 had significant therapeutic potential as a selective AKT inhibitor.
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