Rentosertib becomes the first end-to-end AI-designed drug to enter Phase III

In July 2026, Insilico Medicine launched a phase III trial involving 320 patients in 47 centers for the treatment of idiopathic pulmonary fibrosis based on its AI platform.

On July 7, 2026, Insilico Medicine announced the start of a Phase III trial for rentosertib, a TNIK inhibitor for the treatment of idiopathic pulmonary fibrosis. The trial involves 320 patients in 47 centers in China, with the main criterion of the evolution of forced vital capacity over 52 weeks.

The event is presented as a first: it is the first drug whose biological target and molecule have both been identified by an artificial intelligence platform to reach the stage of late testing. Phase IIa results, published in Nature Medicine in 2025, showed a comparable group tolerance and a dose-dependent signal on lung function, with an average change in forced vital capacity of +98.4 mL at 60 mg daily, compared to -20.3 mL on placebo.

This isolated advance must not mask the general state of the sector. A count presented to ASCO in 2026 included 117 AI-derived therapeutic assets entered clinical trials in 63 companies; Of these, 60 had completed phase 1, but only 8 had completed phase 2. To date, no AI-designed drugs have received marketing authorisation.