Boehringer Ingelheim Pharma GmbH & Co. KG and Vanderbilt University have synthesized annulated 2-amino-3-cyano thiophenes and derivatives acting as KRAS GTPase and its mutant inhibitors reported to be useful for the treatment of cancer.
KRAS Q61H mutation has been found in pancreatic ductal adenocarcinoma (PDAC), colorectal cancer (CRC), and non-small-cell lung cancer (NSCLC) among other solid tumors. In healthy cells, RAS proteins switch between ON and OFF states during signal transduction, but in cancer, mutations in RAS genes or regulators install RAS proteins in ON state permanently.
Researchers at 1200 Pharma LLC have undertaken preclinical analysis of KRAS G12C inhibitors in clinical phases with the aim of finding an explanation for the differences observed in therapeutic efficacy in tumor sites other than lung, including lung-derived metastases. Results pointed to potency and pharmacokinetics as key drivers of efficacy.
Shanghai Allist Pharmaceuticals Co. Ltd. has discovered pyridopyrimidines acting as GTPase KRAS mutant inhibitors reported to be useful for the treatment of cancer.
Innovent Biologics Inc. has inked a $312 million licensing deal for the development and commercialization of Genfleet Therapeutics Inc.’s KRAS G12C inhibitor, GFH-925, in mainland China, Hong Kong, Macau and Taiwan. Innovent also has additional option-in rights for global development and commercialization.
Genhouse Bio Co. Ltd. closed a series A financing round to raise more than ¥200 million (US$31 million) to support phase I studies of KRAS inhibitor GH-35 and SHP2 inhibitor GH-21 in China. The startup expects to enroll patients in trials testing the two compounds in the second half of this year, CEO Wang Kuifeng told BioWorld in an exclusive interview.
