molecules of the month


first-in-class, bioavailable BCL-XL inhibitor

oral efficacy in xenograft, led to ADC dev.

from SBDD of prior BH3 mimetics

ACS Med. Chem. Lett., Jul. 5, 2020

AbbVie, North Chicago, IL / Genentech

1 min read

A-1331852 is a highly potent, orally bioavailable inhibitor of BCL-XL, blocking a protein-protein interaction resulting in tumor cell apoptosis. The compound was an important tool compound for understanding the biology of BCL-family protein inhibitors (particularly around heme toxicities), and ultimately led to the development of an antibody-drug conjugate (ABBV-155) which recently entered Ph. I studies for solid tumors. Andrew Judd gave a great presentation on the BCL-XL story at last year’s Bay Area Chemistry Symposium highlighting this project, and I’m looking forward to seeing the ADC part of the story being published in the future.

request a trial

You don’t have time to read everything, but you can’t afford to fall behind.

Drug Hunter Premium is drug discovery, distilled, so you can quickly catch up and make informed decisions based on industry examples.

Get ahead now by requesting a trial.

already a member? log in: