Insilico Medicine Doses First Patient in Phase III Rentosertib Trial

CAMBRIDGE, Mass., Sept. 9, 2026 /CourierPR/ -- Insilico Medicine has dosed the first patient in GENESIS-IPF-3, a Phase III clinical trial for Rentosertib, a drug candidate discovered and developed using generative artificial intelligence (AI). The trial, led by Professor Zuojun Xu of Peking Union Medical College Hospital, Chinese Academy of Medical Sciences, aims to systematically evaluate the efficacy and safety of Rentosertib in patients with idiopathic pulmonary fibrosis (IPF).

The 52-week, multi-center, randomized, double-blind, placebo-controlled, parallel-group study will enroll 320 participants across 47 centers in China. The primary endpoint is the annual rate of decline in forced vital capacity (FVC) over the 52-week period. The key secondary endpoint is the time to the first occurrence of any disease progression event. This Phase III study builds on promising results from the 12-week Phase IIa study, which showed improvements in lung function among IPF patients.

Professor Xu commented, "TNIK, the target driven by AI, had never previously been linked to fibrosis. This perhaps indicates that AI is carving out a path distinct from traditional research paradigms in target discovery for complex diseases. Dosing the first patient marks another key clinical milestone for Rentosertib."

Insilico Medicine has published several peer-reviewed papers documenting the milestones of Rentosertib's development, from target identification to Phase IIa positive results. In 2024, a Nature Biotechnology publication detailed the AI-driven early discovery process of Rentosertib. In 2025, a Nature Medicine study reported the Phase IIa results, demonstrating a promising dose-dependent efficacy trend. Most recently, in 2026, a Nature Biotechnology study revealed a consistent reduction in biological age after Rentosertib dosage, across six independent biological aging clocks.

Carol Satler, MD, PhD, Senior Vice President for Clinical Development, Non-Oncology at Insilico Medicine, stated, "I believe Rentosertib will be transformative to patient care in the field of IPF, and AI has enabled this breakthrough with higher speed and reduced cost, which could make a lot of difference in the future of drug discovery."

The company's dual-purpose therapeutic strategy has proven to be a sustainable commercial model. Insilico reported total revenue of approximately $106 million in the first half of 2026, a 287% year-over-year increase, and achieved its first profitable half-year since listing, with an adjusted net profit exceeding $51 million. This milestone was driven by a series of out-licensing, co-development, and R&D collaborations with global partners, including Eli Lilly, Servier, Takeda, SK Biopharmaceuticals, Qilu Pharmaceutical, Hygtia Therapeutics, CMS, and Tenacia. As of the latest practicable date, the total contract value of transactions announced by Insilico in 2026 reached approximately $7.3 billion, pushing the cumulative contract value of its major collaborations since 2021 to approximately $11 billion.

Insilico's AI-driven R&D front is also advancing. The company has nominated nine development candidates within nine months of 2026 as of late August, setting a new company record for annual pipeline productivity and achieving eight clinical milestones across its proprietary and co-developed programs. The primary focus remains on Rentosertib, the world's first drug candidate discovered and developed using generative AI, which is now in a Phase III trial evaluating its efficacy in treating IPF.

The U.S. Food and Drug Administration granted Orphan Drug Designation to Rentosertib for IPF in February 2023. The program's discovery-to-clinic development was published in Nature Biotechnology, its Phase IIa clinical results were published in Nature Medicine, and its medicinal chemistry was published in the Journal of Medicinal Chemistry. Recently, Rentosertib has demonstrated potential to reverse biological age, with the data and analysis results supported by six different aging clock models published in Nature Biotechnology.

Insilico Medicine is a pioneering global biotechnology company dedicated to integrating artificial intelligence and automation technologies to accelerate drug discovery, drive innovation in the life sciences, and extend healthy longevity to people on the planet. The company was listed on the Main Board of the Hong Kong Stock Exchange on December 30, 2025, under the stock code 03696.HK.