RP04340 / Risen (Suzhou) Biosci - LARVOL DELTA

Discovery and Characterization of RP04340: A Highly Potent and Orally Active Pan-KRAS PROTAC Degrader. (PubMed, J Med Chem) - "In mouse xenograft models (KRAS G12C, G12D, and G12V), once-daily oral administration of RP04340 resulted in tumor regression and longer-lasting tumor suppression compared to the clinical-stage pan-RAS inhibitor RMC-6236. With its promising efficacy and druglike properties, RP04340 represents a compelling candidate for KRAS-driven cancers."

Journal • Oncology • Targeted Protein Degradation • CRBN • HRAS • KRAS • NRAS

Preclinical studies of RP04340: an orally available and potent PROTAC compound targeting KRAS G12C/D/V mutant tumors (AACR 2025) - "Furthermore, tissue distribution studies in mouse showed significant accumulation of RP04340 in the lungs and pancreas after 15 days of consecutive dosing, supporting its suitability for treating cancers in these organs. In conclusion, RP04340, a PROTAC compound with compelling preclinical efficacy and favorable pharmacokinetic properties, represents a promising therapeutic candidate for KRAS G12C/D/V-driven cancers."

Preclinical • Colorectal Cancer • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Pancreatic Cancer • Pancreatic Ductal Adenocarcinoma • Solid Tumor • DUSP6 • KRAS

Title: Preclinical studies of RP04340: an orally available and potent PROTAC compound targeting KRAS G12C/D/V mutant tumors (ACCESSWIRE) - "Risen Pharma...announced poster presentations...at the American Association for Cancer Research (AACR) Annual Meeting 2025....Key findings in the presentation:...In vivo studies using mouse xenograft models (Miapaca-2, PK-59, and NCI-H727) demonstrated significant tumor growth inhibition following daily oral administration of RP04340 at doses of 25, 50, and 100 mg/kg, with a clear dose-response relationship. Pharmacokinetic analyses revealed that RP04340 accumulated preferentially in tumor tissues, achieving high intratumoral concentrations after repeated dosing."

Preclinical • Solid Tumor