Definition

An orally bioavailable inhibitor of the anti-apoptotic proteins B-cell lymphoma-2 (Bcl-2) and Bcl-extra large (Bcl-XL), with potential pro-apoptotic and antineoplastic activities. Upon oral administration, Bcl-2/Bcl-XL inhibitor LP-118 selectively targets, binds to and inhibits the activity of Bcl-2 and Bcl-XL. This restores apoptotic processes in tumor cells. Bcl-2 and Bcl-XL, Bcl-2 family proteins overexpressed in many cancers, play important roles in the negative regulation of apoptosis. Their expression is associated with increased drug resistance and tumor cell survival.