CHIR-124 / Novartis - LARVOL DELTA

The Human Chk1 Inhibitor CHIR-124 Shows Multistage Activity Against Plasmodium falciparum via Dual Inhibition of Pf Ark1 and Hemozoin Formation. (PubMed, bioRxiv) - "This is further supported by in vitro drug combination experiments, morphological studies and resistance generation attempts. This study demonstrates the feasibility of designing dual Plasmodium kinase/hemozoin formation inhibitors active against resistant strains with decreased resistance risks in the fight against malaria."

Journal • Infectious Disease • Malaria • AURKA

A high-throughput approach to identify BRCA1-downregulating compounds to enhance PARP inhibitor sensitivity. (PubMed, iScience) - "Three compounds, N-acetyl-N-acetoxy chlorobenzenesulfonamide (NANAC), A-443654, and CHIR-124, were validated to reduce BRCA1 protein levels and sensitize breast cancer cells to the toxic effects of olaparib. These results suggest that BRCA1-HiBiT reporter cells hold promise in developing agents to improve the clinical utility of PARPi."

Journal • Breast Cancer • Oncology • Solid Tumor • BRCA1

Overcoming MK1775 resistance in upper gastrointestinal cancers with combined WEE1 and CHK1 inhibition (AACR 2024) - "Notably, combining the WEE1 inhibitor with the CHK1 inhibitor CHIR124 effectively inhibited CHK1 kinase activity and abrogated STAT3 phosphorylation, DNA binding, and transcriptional activity in UGC cells. Our study underscores the potential of combining WEE1 and CHK1 inhibitors to effectively combat MK1775 resistance in UGC, offering a promising direction for improved treatment strategies and patient outcomes in these challenging malignancies."

Esophageal Adenocarcinoma • Esophageal Cancer • Gastric Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor • WEE1