trametinib + afuresertib

This is a combination of the MEK1/2 inhibitor trametinib and the AKT inhibitor afuresertib intended to achieve dual blockade of the MAPK and PI3K/AKT pathways in cancer. In a phase I study in advanced solid tumors and multiple myeloma, continuous daily dosing was poorly tolerated; an intermittent schedule with continuous trametinib and afuresertib given Days 1–10 of a 28‑day cycle was more tolerable, with common adverse events including diarrhea, acneiform dermatitis, and rash, and limited clinical activity observed (one partial response and some stable disease) [phase I, NCT01476137].[1] Reviews of combination strategies similarly note poor tolerability and limited efficacy for trametinib plus afuresertib across advanced solid tumors.[3]

Other names

trametinib plus afuresertibtrametinib and afuresertib