ISM8001 / Insilico Medicine - LARVOL DELTA

Discovery and preclinical characterization of ISM8001, a covalent and selective FGFR2/FGFR3 dual inhibitor with strong monotherapy anti-tumor activity against advanced solid tumors (AACR 2024) - "The second generation of FGFR inhibitors currently undergoing clinical evaluation such as RLY-4008 and LOXO-435 are primarily focused on achieving selectivity against either the FGFR2 or FGFR3 isoform, which may narrow their clinical potential. Results of 28-day non-clinical toxicology studies in rat and dog showed a safety window of approximately 2-5 fold based on efficacious exposure in different models. Taken together, these data support the clinical development of ISM8001 as a novel, selective FGFR2/FGFR3 dual inhibitor for the potential tissue-agnostic therapy of advanced solid tumors with FGFR2/3 aberrations."

Metastases • Monotherapy • Preclinical • Biliary Cancer • Bladder Cancer • Cholangiocarcinoma • Endometrial Cancer • Gastric Cancer • Gastrointestinal Cancer • Genito-urinary Cancer • Oncology • Solid Tumor • Urothelial Cancer • FGFR1 • FGFR2 • FGFR3 • FGFR4

Insilico announces the expansion of its oncology pipelines and delivers the new generation FGFR2/3 inhibitor (Eurekalert) - "The nomination of the new generation of FGFR2/3 inhibitor for the treatment of tissue-agnostic solid tumors, bringing the total number of PCCs nominated by Insilico in 2023 to six....Insilico Medicine...announced the nomination of ISM8001, a novel molecule targeting FGFR2/3 for the treatment of tissue-agnostic solid tumors bringing the total number of PCCs nominated in 2023 to six....ISM8001 is an orally available, highly selective dual inhibitor targeting FGFR2/3, and sparing FGFR1/4. The compound demonstrated superior potency in multiple FGFR2/3-driven efficacy models, and also in gatekeeper and molecular brake mutant-resistant models. It also showed favorable DMPK profiles, low efficacious dose, and desirable safety margin to support higher human dose."

New molecule • Preclinical • Oncology • Solid Tumor