trametinib + navitoclax

Trametinib + navitoclax is an investigational combination therapy being evaluated by the National Cancer Institute (NCI) for the treatment of advanced solid tumors harboring KRAS or NRAS mutations. Trametinib is a highly selective, reversible, allosteric inhibitor of MEK1 and MEK2 (mitogen-activated protein kinase kinase), which are key components of the MAPK/ERK signaling pathway. Navitoclax (ABT-263) is an orally bioavailable small molecule that inhibits the pro-survival BCL-2 family proteins, including BCL-2, BCL-XL, and BCL-W. By combining a MEK inhibitor with a BCL-2 family inhibitor, the regimen aims to induce apoptosis and overcome the resistance often seen with MEK inhibitor monotherapy in RAS-mutated cancers. Clinical trials have focused on indications such as pancreatic, colorectal, non-small cell lung, and gynecologic cancers.

Other names

trametinib and navitoclaxtrametinib/navitoclax