Insilico Medicine Licenses AI-Discovered Oral PHD Inhibitor ISM4808 to TaiGen for CKD Anemia in Greater China in Multi-Million Dollar Deal

VCBeat learned at the earliest opportunity that on December 12, a clinical-stage biopharmaceutical technology company powered by generative artificial intelligenceInsilico Medicine, and market-oriented new drug R&D companiesTaiGen*-KY (4157), and its wholly-ownedBeijing Subsidiary Taijing Pharmaceutical R&D (hereinafter referred to as “Taijing”)，Announced the exclusive out-licensing collaboration for its pipeline.

Pursuant to the terms of the agreement, TaiGen Biotechnology will receiveExclusive rights to develop, commercialize, and sublicense the PHD inhibitor ISM4808 in Greater China (including mainland China, Hong Kong, Macau, and Taiwan), Insilico Medicine is eligible to receive an upfront payment, development- and sales-based milestone payments, and tiered royalties based on net sales, etc.Total transaction volume reached tens of millions of US dollars。

Studies have shown that chronic kidney disease (CKD) causes more than 1.5 million deaths annually, and over one in seven patients with kidney disease suffers from anemia due to reduced erythropoietin (EPO) production and shortened red blood cell lifespan. However, anemia cannot be completely cured; current therapies mainly focus on symptomatic treatment, aiming to alleviate symptoms such as fatigue, shortness of breath, body pain, dizziness/syncope, with the goal of improving patients' quality of life.

ISM4808 was nominated as a PHD inhibitor candidate in 2022, with “best-in-class” potential. It targets the HIF-α pathway, which has been recognized by the Nobel Prize, and enhances erythropoiesis by inducing EPO production and improving iron utilization for the treatment of anemia associated with chronic kidney disease.Notably, the novel structure of ISM4808 was powered by Insilico Medicine’s proprietary Chemistry42 engine, with its design, synthesis, and testing completed within 12 months prior to candidate drug nomination.In January 2024, the discovery and development journey of the ISM4808 series was published in the Journal of Medicinal Chemistry, highlighting the novelty and efficiency of Insilico Medicine’s AI-driven drug discovery workflow.

In preclinical studies, ISM4808 demonstrated robust efficacy in both in vitro and in vivo experiments, with its lower effective dose validated in a rat model of chronic kidney disease. Furthermore, ISM4808 exhibited favorable oral druggability, characterized by excellent in vitro ADME properties, superior pharmacokinetic (PK) profiles in animal models, as well as a higher maximum tolerated dose and a wider safety margin. The project received clinical trial approval from China’s Center for Drug Evaluation (CDE) in 2023.

Dr. Feng Ren, Co-CEO and Chief Scientific Officer of Insilico Medicinestated, “We are delighted to partner with TaiGen Biotechnology. Previously, empowered by our AI platform, Insilico Medicine efficiently nominated two novel small-molecule inhibitors targeting PHD for different indications. Among them, ISM5411, a candidate molecule for the treatment of inflammatory bowel disease, has completed two Phase I clinical trials under the leadership of Insilico Medicine. The results demonstrated favorable safety profiles, further strengthening our confidence in targeting the PHD mechanism. We are very pleased that another candidate drug targeting this pathway, ISM4808, will be further developed by TaiGen, a partner with extensive R&D experience and strong commercialization capabilities. I believe that TaiGen’s robust drug development capabilities and clinical resources will help accelerate the project’s progress, bringing AI-driven therapies to patients with unmet clinical needs sooner.”

TaiGen Biotechnology Chairman Huang Guo-LongIt stated, “We are delighted to establish this strategic partnership with Insilico Medicine, whose innovations driven by its generative AI platform are truly impressive. In mainland China, there are over one million dialysis patients, and the market for PHD inhibitor drugs is experiencing explosive growth, with its size expanding from RMB 50 million to RMB 2.45 billion in just five years. Moreover, oral medications are gradually replacing traditional injectable drugs to meet clinical needs for convenience and adherence. This licensing agreement aligns perfectly with our mission of developing innovative drugs, and TaiGen Biotechnology will be committed to advancing the clinical development of this project.”

Insilico Medicine is a global pioneer in biotechnology powered by generative artificial intelligence, leveraging its proprietary Pharma.AI platform and advanced automated laboratories to accelerate drug discovery and drive innovation in the life sciences sector. By integrating artificial intelligence and automation technologies, Insilico Medicine is delivering innovative therapeutic solutions for unmet medical needs in areas such as fibrosis, oncology, immunology, pain, obesity, and metabolic disorders. Ten molecules from Insilico Medicine’s AI-discovered pipeline have received regulatory approval for clinical trials. Among these, Rentosertib (formerly ISM001-055), the most advanced candidate, is a potential first-in-class therapy for idiopathic pulmonary fibrosis that has completed Phase 2a clinical studies with encouraging positive results. Furthermore, Insilico Medicine is exploring frontier fields, including breakthroughs in aging research, sustainable chemistry, and agricultural innovation.