Insilico Medicine announced the first patient enrollment and dosing in the Phase III GENESIS-IPF-3 study of Rentosertib (ISM001-055/INS018_055), its lead AI-generated small-molecule inhibitor targeting TNIK for idiopathic pulmonary fibrosis (IPF).

The 52-week, prospective, randomized, double-blind, placebo-controlled trial plans to recruit 320 participants across 47 clinical centers in China. The primary endpoint is the annual rate of decline in forced vital capacity (FVC), while the key secondary endpoint is time to first disease-progression event. Peking Union Medical College Hospital enrolled and dosed the first patient, with Shanghai Pulmonary Hospital initiating enrollment on the same day.

GENESIS-IPF-3 is led by Professor Xu Zuojun (Peking Union Medical College Hospital) with co-leading principal investigators Academician Zhong Nanshan (Chinese Academy of Engineering) and Dr. Chen Chang (Shanghai Pulmonary Hospital).

Rentosertib, discovered through Insilico’s generative AI platform Pharma.AI, aims to halt or reverse lung fibrosis by inhibiting TNIK. In the earlier GENESIS-IPF Phase IIa trial, the compound showed a favorable safety profile and dose-dependent efficacy trends; results were published in Nature Medicine in June 2025.

IPF affects about 5 million people worldwide and carries a median survival of 3 to 4 years, underscoring the need for disease-modifying therapies beyond existing antifibrotic treatments.

Insilico Medicine, listed on the Hong Kong Stock Exchange on 30 December 2025, applies AI and automation across fibrosis, oncology, immunology, pain, obesity, and metabolic disorders, as well as non-pharmaceutical sectors including advanced materials and agriculture.