Insilico Medicine has announced that first-in-human phase 1 trial data for ISM6331, its novel Artificial Intelligence (AI)-designed pan-TEAD inhibitor, has been accepted for a Rapid Oral presentation at the European Society for Medical Oncology (ESMO) Congress 2026, taking place from October 23-27, 2026, in Madrid, Spain.

Feng Ren, PhD, Co-CEO and Chief Scientific Officer (CSO), Insilico Medicine, said, "TEAD has long been recognised as an attractive target in hard-to-treat solid tumors, but small-molecule inhibition has historically posed significant design challenges. The selection of ISM6331 for a Rapid Oral presentation at ESMO 2026 highlights the potential of our AI-generated platform to target complex oncogenic drivers like the Hippo pathway and represents a promising pan-TEAD approach that we are eager to share with the community."

ISM6331 is a novel, potent, small-molecule pan-TEAD inhibitor discovered and designed using Insilico Medicine's proprietary generative AI-powered drug discovery platform, Chemistry42. The molecule targets TEAD transcription factors, the principal downstream effectors of the Hippo signaling pathway, a critical regulator of cell proliferation, survival, tissue homeostasis, and therapeutic resistance across a broad range of solid tumors.

Although the Hippo pathway has long been recognised as a promising therapeutic target in oncology, developing effective small-molecule TEAD inhibitors has remained a significant medicinal chemistry challenge. ISM6331 was designed to selectively inhibit pan-TEAD activity and is being evaluated in a global, multicenter phase 1 clinical trial in patients with malignant mesothelioma and other advanced solid tumors. The study is assessing ISM6331 safety, tolerability, pharmacokinetics, and preliminary antitumor activity to inform its continued clinical development.

Halle Zhang, PhD, Vice President (VP), Clinical Development–Oncology, Insilico Medicine, said, "Presenting our first-in-human phase 1 study at ESMO marks an important clinical milestone for ISM6331. Patients with advanced mesothelioma and other Hippo-driven solid tumors face limited therapeutic options. These preliminary clinical findings provide early encouragement as we evaluate ISM6331's safety, pharmacokinetics, and initial antitumor activity to inform our ongoing clinical development strategies."