molibresib

Molibresib is an orally bioavailable, selective small molecule inhibitor of the BET (bromodomain and extra-terminal) family of bromodomain-containing proteins, including BRD2, BRD3, and BRD4. By mimicking acetylated histones, it interferes with the recognition of acetylated histones by BET proteins, disrupting chromatin remodeling and gene expression. This inhibition can prevent the expression of certain growth-promoting genes and may lead to inhibition of tumor cell growth. Molibresib was developed primarily for the treatment of advanced solid tumors and hematologic malignancies such as NUT midline carcinoma, breast cancer (including triple-negative), prostate cancer (castration-resistant), small cell lung cancer, gastrointestinal stromal tumor, acute myeloid leukemia, and other solid tumors. The drug was developed by GlaxoSmithKline but has been discontinued in clinical development for all indications[1][2][5][6].

Other names

Bet inhibitor gsk525762Molibresib besylate