Istisociclib

Istisociclib is an orally bioavailable, selective inhibitor of cyclin-dependent kinase 9 (CDK9), the catalytic subunit of the RNA polymerase II (RNA Pol II) elongation factor positive transcription elongation factor b (PTEF-b; PTEFb). Its mechanism of action involves blocking the phosphorylation and kinase activity of CDK9, which in turn prevents PTEF-b-mediated activation of RNA Pol II. This inhibition leads to the downregulation of gene transcription for various anti-apoptotic proteins and oncogenic transcription factors, including MYC and androgen receptor (AR). The ultimate effect is the induction of cell cycle arrest and apoptosis, thereby preventing tumor cell proliferation. Initially developed by Kronos Bio, Inc. for its potential antineoplastic activity, its clinical development was later discontinued by Kronos Bio due to safety concerns. However, its clinical assets were subsequently acquired by Ignota Labs with the intent to revive and further develop the drug.

Other names

KB-130742KB130742KB 130742