GFH547 / GenFleet Therap - LARVOL DELTA

GFH547: An orally bioavailable, cyclophilin A-hijacking panRAS(on) inhibitor with broad spectrum anti-tumor activities (AACR 2024) - "KRAS has recently become druggable with the approval of two KRAS G12C inhibitors - sotorasib and adagrasib. The compound demonstrated strong therapeutic activities in tumors with activating RAS and RTK mutations/alterations. Based on these promising results, we are advancing a CypA-binding panRAS(on) inhibitor into the clinic as targeted therapy for cancers addicted to RAS pathways."

Late-breaking abstract • Oncology • BRAF • EGFR • FGFR2 • HRAS • KRAS • NRAS

GenFleet Therapeutics Announces Broad-spectrum Activity of GFH547, an Oral panRAS (ON) Inhibitor, and Its Potential to Overcome Resistance against SIIP-based KRAS Inhibitors in Late-breaking Research Abstract of 2024 AACR Annual Meeting (PRNewswire) - "GenFleet Therapeutics...announced the latest findings of GFH547, an oral panRAS (ON) inhibitor, in a late-breaking research abstract at the 2024 American Association for Cancer Research (AACR) Annual Meeting....The deep inhibition of KRAS pathway was observed following a single oral administration of GFH547 in KRAS mutant CDX tumors. GFH547 also demonstrates dose-dependent anti-tumor activity and drives tumor regression in KRAS mutant tumor models....GFH547 is resistant to RTK activation by EGF stimulation which attenuates potency of current mainstream SIIP-based KRAS inhibitors. It is also effective to cells carrying secondary KRAS mutations causing acquired resistance to SIIP-based KRAS inhibitors. Overall, GFH547 demonstrates promising bioavailability, kinase selectivity and safety in the preclinical research."

Late-breaking abstract • Preclinical • Oncology