Drug intelligence / Profile preview

BI97D6

Development stage
Preclinical
Lead developer
Sanford Burnham Prebys Medical Discovery Institute
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

BI97D6 is a small molecule BH3 mimetic and an apogossypolone derivative developed as a pan-inhibitor of anti-apoptotic BCL2 family proteins. It binds with high affinity to MCL1, BCL2, BCL-XL, and BFL1, thereby disrupting their interaction with pro-apoptotic proteins like BIM and BAX. This inhibition triggers BAX conformational changes and leads to mitochondrial-mediated apoptosis. BI97D6 has demonstrated potent activity against Acute Myeloid Leukemia (AML) cell lines and primary AML samples, including those with high MCL1 expression or FLT3 mutations, and effectively targets leukemia stem cells. The compound was identified through research at the Sanford-Burnham Medical Research Institute and the University of Texas MD Anderson Cancer Center.

Other names
apogossypolone derivative BI97D6
02

Targets

MCL1 (Myeloid cell leukemia sequence 1)BCL2A1 (B-cell lymphoma 2-related protein A1)BCL2L1 (B-cell lymphoma-extra large protein)

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