Drug intelligence / Profile preview

BI 3706674

Development stage
Phase 1
Lead developer
Boehringer Ingelheim
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

BI 3706674 is an orally bioavailable small molecule inhibitor that directly targets the KRAS protein, including both wild-type (WT) and various mutant forms such as KRAS G12C and G12V. It acts as a non-covalent "OFF" inhibitor of KRAS, preferentially binding to the inactive GDP-bound state of the protein. By inhibiting oncogenic KRAS signaling, BI 3706674 disrupts pro-proliferative pathways in cancer cells, leading to anti-tumor activity. The drug is being developed primarily for the treatment of advanced cancers with KRAS wild-type amplification or specific mutations—most notably unresectable metastatic gastric, esophageal, and gastroesophageal junction adenocarcinoma. Preclinical studies have shown efficacy in models with high copy number amplification of wild-type KRAS and in tumors harboring certain mutant alleles[1][3][6][7]. Clinical trials are ongoing to evaluate its safety and efficacy as monotherapy in these patient populations[2][5]. Boehringer Ingelheim is the developer.

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