Boehringer Ingelheim advances first pan-KRAS inhibitor into clinical testing

Boehringer Ingelheim presented promising preclinical data from its pan-KRAS program including the novel, oral inhibitor BI 1701963 at the AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics in Boston, USA.

Based on these results the compound has been advanced to Phase I clinical testing alone and in combination with trametinib in patients with different types of advanced solid tumors with KRAS mutations.

KRAS mutations occur in one in seven of all human metastatic cancers making it the most frequently mutated cancer-causing oncogene, with mutation rates of more than 90 percent in pancreatic cancers, more than 40 percent in colorectal cancers and more than 30 percent in lung adenocarcinomas. It has evaded attempts to develop inhibitors for almost 40 years. Only recently have promising compounds targeting the specific KRAS mutation G12C entered the clinic. There are however many KRAS gene mutations beyond G12C that drive tumor growth.

“Our pan-KRAS inhibitor has been designed to target a broad range of oncogenic KRAS variants, including all major G12 and G13 oncoproteins. Effective targeting of the most prevalent KRAS mutant alleles that have so far proved elusive could enable us to develop much needed new therapy regimens for patients with gastrointestinal and lung cancers who have limited treatment options available,” said Norbert Kraut, Ph.D., Head of Global Cancer Research at Boehringer Ingelheim.

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