Insilico Medicine said it has completed a $110 million Series E financing, the proceeds of which are intended to help the artificial intelligence (AI) drug developer accelerate development of its pipeline and its AI platform.
“On one side, resources will focus on refining AI models and algorithms, alongside updates and expansions to its state-of-the-art robotics lab to further automate and streamline R&D processes,” Insilico founder and CEO Alex Zhavoronkov, PhD, told GEN. “On the other side, Insilico will focus on advancing the clinical validation of its flagship candidate for idiopathic pulmonary fibrosis treatment and accelerating the exploration of other independently developed and co-developed drug pipelines, driving impactful innovations in healthcare.”
Insilico’s idiopathic pulmonary fibrosis (IPF) candidate is the company’s lead pipeline program Rentosertib—previously ISM001-055 and initially called INS018_055—an internally developed drug candidate developed using generative AI. Rentosertib is designed to treat IPF by targeting Traf2- and NCK-interacting kinase (TNIK), a serine/threonine kinase whose activation plays a crucial role in cellular processes that include signal transduction pathways essential for fibrosis development.
Last month, researchers from Insilico and two partner institutions published a study concluding that Rentosertib was the first to show anti-aging properties and that its mechanism of action offered a promising therapeutic approach for treating age-related diseases.
“This study further strengthens the potential of INS018_055 as a longevity therapeutic by implicating TNIK in the cellular senescence hallmark of aging,” the researchers concluded, using the drug candidate’s original name, in “AI-Driven Robotics Laboratory Identifies Pharmacological TNIK Inhibition as a Potent Senomorphic Agent,” a study published in Aging and Disease. The Insilico researchers were joined by investigators from China’s Suzhou Hospital of Nanjing Medical University, as well as from the Buck Institute for Research on Aging.
Positive Phase IIa results
Last November, Insilico announced positive topline results from a Phase IIa trial conducted across 21 sites in China (NCT05938920), showing encouraging clinical efficacy for Rentosertib as measured by dose-dependent improvements in forced vital capacity (FVC) at 12 weeks. The largest improvement was seen in the 60 mg QD [once daily] cohort.
Insilico is working to validate findings from the Phase IIa and earlier clinical studies through a parallel Phase IIa trial (NCT05975983) now enrolling patients in the United States. The study is projected to enroll a total of 60 patients and achieve primary completion in February 2026.
Rentosertib leads Insilico’s wholly owned drug discovery portfolio of 30 assets generated through its Pharma.AI platform, of which 10 have received investigational new drug (IND) clearance to begin clinical trials. Last month, Insilico announced key benchmarks for its internal preclinical candidate programs showing a reduced average time to nomination of 12 to 18 months, vs. 2-1/2 to 4 years for traditional drug discovery methods, while enabling the synthesis and testing of only 60 to 200 molecules per program.
Pharma.AI includes two function-specific platforms, the target identification engine PandaOmics and the generative chemistry engine, Chemistry42. Also within Pharma.AI are innovative engines powered by large language models (LLMs), including Nach01, a multimodal foundation model for natural and chemical languages, and Dora, a multi-agent generative research assistant. Insilico recently deployed the first bipedal humanoid AI scientist within Life Star1, the company’s Pharma.AI-connected fully robotic lab, designed to further optimize and automate research workflows.
The Series E financing has lifted Insilico’s total valuation to more than $1 billion—what investors call “unicorn” status—compared with the company’s valuation of $895 million after it completed its $95 million Series D round in 2022.
Zhavoronkov said the Series E was “heavily oversubscribed, drawing exceptional interest from prominent investors.”
Hong Kong-based Value Partners Group, one of Asia’s largest independent asset management firms, led the $110 million Series E financing, with what Insilico called strong participation from industry- and technology-focused new investors, plus continued support from several existing investors.
Leadership position
“With a proven track record and a leadership position in AI-driven drug development, Insilico is at the forefront of transforming the industry,” stated Chuen Yan Leung, PhD, partner (Healthcare Investments) with Value Partners and a member of Insilico’s board. “We believe that Insilico’s advancements will not only accelerate the development of life-saving therapies but also redefine the future of biopharmaceutical R&D.”
Beyond venture financing, Insilico has generated revenue through four out-licensing deals for pipeline candidates with three biopharma partners totaling a combined up to $2.1 billion:
• Exelixis: Developing the cancer-fighting oral small molecule ISM3091 (now XL309), a ubiquitin-specific peptidase 1 (USP1) inhibitor, under a partnership launched with Insilico receiving $80 million upfront in 2023. In December 2024, Insilico received a $10 million clinical milestone payment for XL309, now in a Phase I trial (NCT05932862).
• Fosun Pharma: Co-developing ISM8207, a small molecule glutaminyl-peptide cyclotransferase-like protein (QPCTL) inhibitor which Insilico says is potentially first-in-class, as a treatment for advanced malignant tumors, such as those with high engagement of the CD47-Signal Regulatory Protein α (SIRPα) axis, in a Phase I trial (CTR20240727) that dosed its first patient last year.
• Menarini Group: Menarini’s Stemline Therapeutics subsidiary received global rights in January to develop a second Insilico-discovered candidate, a preclinical small molecule targeting what the companies called high unmet needs in oncology. In 2024, Menarini won global rights to the first candidate MEN2312, a small molecule KAT6 inhibitor being developed to treat breast cancer and other oncology indications.
Insilico has also generated milestone payments from collaborations totaling up to $1.4 billion. The biggest is an up-to-$1.2 billion, up-to-six target strategic research collaboration with Sanofi. The others include a sustainable fuels partnership with Saudi Aramco (whose Aramco Ventures includes Prosperity7 Ventures, a $1 billion VC fund that led the Series D round), and a collaboration of undisclosed value with South Korean-based Therasid Bioscience to develop first-in-class drugs to treat metabolic dysfunction-associated steatohepatitis (MASH).
