Insilico Medicine reports first human data for AI-designed TEAD inhibitor ISM6331 in mesothelioma

What's the deal? Insilico Medicine, the generative-AI drug discovery company, presented first-in-human Phase 1 data for ISM6331 — an oral cancer drug designed with its Chemistry42 AI platform — at the ESMO cancer congress in Madrid on 26 October 2026. In patients with mesothelioma (an aggressive cancer of the lining of the lungs) who had already failed a median of two prior treatments, the drug shrank tumours in 40% of evaluable patients at the 130 mg daily dose, and in 18.2% across all dose levels, with disease control in 68.2% of evaluable patients.

Why it matters: ISM6331 targets TEAD proteins, a family of growth regulators downstream of the Hippo pathway that the industry long considered "too hard" to drug. The results are an early sign that generative AI can design clinical-grade molecules against difficult targets: responses appeared as early as week 8 — including in patients who had already been through five or six prior lines of therapy — and the drug was well tolerated, with no dose-limiting toxicities reported from 15 mg through 130 mg. Insilico holds US FDA orphan drug and fast track designations for ISM6331 in mesothelioma and plans to move into a Phase 2a randomised dose-optimisation study.

Read more: PR Newswire, 26 October 2026