APR-246

APR-246 (PRIMA-1MET) is a methylated derivative of PRIMA-1 that restores mutant p53 activity, acts synergistically with chemotherapeutic agents to inhibit tumor cell proliferation; also restores the pro-apoptotic function to mutant TAp63γ and TAp73β in tumor cells but has less effect on TAp73α; induces mutant p53-dependent mitochondria-mediated apoptosis through activation of caspase-2 with subsequent cytochrome c release and further activation of downstream caspase-9 and caspase-3; inhibits tumor xenograft growth in vivo.Ovarian Cancer Phase 2 Clinical.