Drug intelligence / Profile preview

14C-bleximenib

Development stage
Unknown
Lead developer
Janssen Research & Development
Modality
Small Molecules
Administration
Oral
01

Overview

Bleximenib (JNJ-75276617) is an investigational, orally bioavailable small molecule inhibitor of the menin-KMT2A (lysine methyltransferase 2A) protein-protein interaction, developed by Janssen Research & Development. It is specifically designed for the treatment of acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL) harboring KMT2A rearrangements or NPM1 mutations. By binding to menin, the drug prevents its association with KMT2A, leading to the downregulation of critical leukemogenic drivers such as HOXA9 and MEIS1. The 14C-labeled version (14C-bleximenib) is a radiolabeled formulation used in Phase 1 clinical trials to conduct absorption, metabolism, and excretion (AME) studies, allowing researchers to track the drug's metabolic pathways and mass balance in human subjects.

Other names
radiolabeled bleximenib[14C]bleximenib14C-labeled bleximenib
02

Targets

Menin – KMT2A interaction site on menin

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