ISM033-154 / Insilico Medicine - LARVOL DELTA

Study of ISM5939 in Patients With Advanced and/or Metastatic Solid Tumors (clinicaltrials.gov) - P1 | N=159 | Not yet recruiting | Sponsor: InSilico Medicine Hong Kong Limited | Trial completion date: Dec 2029 ➔ Jun 2030 | Trial primary completion date: Dec 2028 ➔ Jun 2029

First-in-human • Trial completion date • Trial primary completion date • Solid Tumor

Oral ENPP1 inhibitor designed using generative AI as next generation STING modulator for solid tumors. (PubMed, Nat Commun) - "In murine syngeneic models across cancer types, ISM5939 synergizes with targeting the PD-1/PD-L1 axis and chemotherapy in suppressing tumor growth with good tolerance. Our findings provide evidence supporting ENPP1 as an innate immune checkpoint across solid tumors and reports an AI design-aided ENPP1 inhibitor, ISM5939, as a cutting-edge STING modulator for cancer therapy, paving a path for immunotherapy advancements."

Journal • Oncology • Solid Tumor • ENPP1 • STING

Study of ISM5939 in Patients With Advanced and/or Metastatic Solid Tumors (clinicaltrials.gov) - P1 | N=159 | Not yet recruiting | Sponsor: InSilico Medicine Hong Kong Limited

Metastases • New P1 trial • Oncology • Solid Tumor

ISM5939, a novel, potent, orally available, selective ENPP1 inhibitor enhances the anti-tumor effects of immune checkpoint inhibitors in syngeneic murine cancer models (SITC 2023) - "Conclusions ISM5939, is a novel, potent ENPP1 inhibitor that augments the effectiveness of anti-PD-L1 or anti-PD1 therapy in multiple syngeneic mouse tumor models, while exhibiting favorable safety and tolerability properties. Together, these data support further evaluation of ISM5939 as an anti-tumor agent."

Checkpoint inhibition • IO biomarker • Preclinical • Breast Cancer • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer