Are the bcl2 family inhibitors substrates for the multidrug resistance efflux pump mdr1?

The BH3 mimetic compounds, a novel class of targeted anti-cancer agents, are highly efficacious for the treatment of certain haematological malignancies. The BCL2 inhibitor, venetoclax, is the most advanced and has been approved for treating patients with high-risk chronic lymphocytic leukemia (CLL) in many countries. While highly effective, clinical resistance is emerging, and we anticipate that resistance to BH3 mimetic therapy will be a problem in the future.Unlike CLL, the BCL2 relative MCL1 is the key survival factor in multiple myeloma (MM) and clinical trials with inhibitors selective for MCL1 have started in patients with this disease.

Source: Experimental Hematology - July 31, 2019 Category: Hematology Authors: Farima Moghaddaskho, Yuan Yao, Christoffer Flensburg, Jia-Nan Gong, Christine White, Ian J. Majewski, Andrew Roberts, David Huang Tags: 3098 Source Type: research