Rentosertib

ISM3830, An oral, highly selective small molecule CBLB inhibitor ISM0676, an innovative oral small molecule GIPR antagonist ISM5059, an innovative peripherally restricted small molecule NLRP3 inhibitor ISM6166, an innovative oral broad-spectrum pan-KRAS inhibitor ISM001-055 (Rentosertib), a small molecule TNIK inhibitor for treating idiopathic pulmonary fibrosis (IPF). The Phase IIa GENESIS-IPF study demonstrated strong safety and tolerability, with a dose-dependent improvement in lung function. This represents the first clinical proof-of-concept for an AI-discovered drug. ISM5411 (Garutadustat), a gut-restricted small molecule PHD1/2 inhibitor for inflammatory bowel disease (IBD) treatment. A Phase IIa clinical study named BETHESDA was launched, where first patient dosing was completed. ISM6331, a non-covalent small molecule pan-TEAD inhibitor for solid tumor treatment. Preclinical data showed broad-spectrum anti-tumor activity at low doses with favorable safety. Global multicenter Phase I trial initiated with first patient dosed. ISM3412, a small molecule MAT2A inhibitor for MTAP-deleted tumor treatment; preclinical studies demonstrated ideal efficacy, selectivity, druggability and combination potential. Initiated global multicenter Phase I trial and completed first patient dosing. ISM001-055 (Rentosertib)-Inhalation, an inhalable formulation of the TNIK inhibitor for treating idiopathic pulmonary fibrosis. Features potential advantages of high technical barriers, low efficacious dose, large safety window, and minimal side effects. IND application has been submitted for clinical trial.

Insilico Medicine and Tenacia Biotechnology have expanded their AI-driven CNS collaboration, adding a second discovery-stage program targeting an undisclosed biological target implicated in neurological disease. The expanded agreement carries additional deal value of up to USD 94.75 million. Cambridge, Massachusetts-based Insilico Medicine (3696.HK), a clinical-stage AI biotechnology company listed on the Hong Kong Stock Exchange, will deploy its Pharma.AI generative AI drug discovery platform to design a differentiated small-molecule candidate. Hong Kong-based Tenacia Biotechnology, a commercial-stage biopharmaceutical company founded in 2022 by Bain Capital, will fund the work and receive rights to the resulting candidate. Under the expanded terms, Insilico is eligible to receive near-term and milestone payments from Tenacia totaling up to USD 94.75 million. The specific breakdown between upfront, development, regulatory, and commercial milestones was not disclosed. Royalty rates, profit-sharing arrangements, and geographic rights allocation were not detailed in the announcement. The expansion builds on an initial collaboration launched in March 2025, in which the two companies combined Insilico’s Pharma.AI platform with Tenacia’s CNS-focused scientific expertise and proprietary data assets. That first program focused on designing small-molecule inhibitors with blood-brain barrier permeability for central nervous system treatment and is described as progressing on schedule. The biological target for both programs remains undisclosed. The second program aims to generate a molecule with a distinct pharmacological profile against the same target, advancing it to preclinical candidate nomination. No candidate molecule has been identified or nominated under the expanded agreement. The program is entirely at the discovery stage, with no IND-enabling studies, clinical trial registrations, or regulatory designations reported. Insilico’s Pharma.AI platform integrates three modules: PandaOmics for target identification, Chemistry42 for generative molecular design, and Inclinico for clinical trial outcome prediction. The platform uses reinforcement learning, generative adversarial networks, and variational autoencoders to design novel molecular structures rather than screen existing compound libraries. Insilico’s lead internal asset, rentosertib (ISM001-055), a TNIK inhibitor for idiopathic pulmonary fibrosis, reported positive Phase IIa topline results in November 2024, with data published in Nature Medicine. For Tenacia, the deal deepens its pipeline in neurological disorders. The company has positioned itself as a neuroscience-focused platform in China, backed by Bain Capital’s investment and life science network. Adding a second differentiated molecule against the same CNS target provides optionality in clinical development and may reduce late-stage attrition risk by allowing selection among candidates with varying pharmacokinetic or selectivity profiles. Insilico has been expanding its generative AI drug development partnerships in the CNS space. In early 2026, the company entered a co-development agreement with Hygtia Therapeutics, a Fosun Pharma joint venture, to advance ISM8969, an NLRP3-targeting candidate for Parkinson’s disease. That program received US FDA clearance to initiate clinical trials in January 2026, with a 50/50 global rights structure and total payments exceeding HKD 500 million. Separately, Insilico announced a collaboration with China Medical System in February 2026 covering CNS and autoimmune disease programs. Your email address will not be published. Required fields are marked * Comment * Name * Email * Website