Authors: Frida Ponthan, Thomas Kedward, Valentina Ubertini, Gary Beale, Cath Booth
Published: 2025-04-21
DOI: 10.1158/1538-7445.am2025-5208
Source: Full article
Dysregulated cell division is one of the most important hallmarks of cancer. Cyclindependent kinases (CDKs), involved in cell cycle regulation, have been identified to be overexpressed in many cancers. The development of CDK inhibitors has emerged as a promising and novel approach for cancer treatment in both solid and hematological malignancies. However, first generation pan-CDKIs, which initially showed reliable results in vitro and in Phase I trials, lacked selectivity. Many were discontinued due to adverse effects, including Gastrointestinal (GI) toxicity, and reduced efficacy in vivo. The development of specific CDKIs, which can provide optimum therapeutic outcomes with good efficacy and reduced off-target effects are therefore needed.