Hong Kong-based Insilico Medicine has announced positive results from two Phase I studies of ISM5411 (NCT06012578), a novel gut-restricted and prolyl hydroxylase domain (PHD)-specific inhibitor designed and optimised using the company’s AI platform Chemistry42.

The drug is being considered for the treatment of inflammatory bowel disease (IBD) and was nominated as a preclinical candidate for the illness in January 2022. This followed a 12-month period during which the generative AI-powered drug design platform synthesised and screened approximately 115 molecules.

The two Phase I studies took place in Australia and China, with 76 and 48 patients, respectively. The trials included three arms: single-ascending dose, multiple-ascending dose and food effects (FE). They investigated the safety, tolerability, pharmacokinetics (PK) and FE of ISM5411.

The results demonstrated that ISM5411 was generally safe and well tolerated across all dose groups, with no reports of serious adverse events (AEs) or treatment-related AEs leading to discontinuation. Insilico reported that treatment-emergent AEs were comparable between treatment groups and pooled placebo and most were grade 1.

No clinically significant increases in red blood cell count or haemoglobin were reported.

The results also demonstrated that the human PK of ISM5411 matched expectations based on preclinical modelling and no significant drug accumulation was observed over a 14-day administration period. ISM5411 exhibited a favourable PK profile for validating gut-restrictive properties, with very low systemic exposure and a high faecal / plasma ratio in healthy volunteers.

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Following the results, Insilico has announced that it will initiate a Phase II proof-of-concept study this year, considering ISM5411 as a treatment for active ulcerative colitis, a chronic form of IBD.

The use of AI in the development of ISM5411 is part of Insilico’s broader R&D model, which relies on its Chemistry42 platform. Insilico also used its AI offering in the research and development of ISM001_055 (formerly INS018_055), its lead drug pipeline, which is currently in Phase II trials (NCT05938920).

Chemistry42 is commercially available and sits within Insilico’s Pharma.ai discovery suite. It is used to streamline hit identification, hit-to-lead and lead optimisation programmes.

AI in drug discovery is a rapidly developing area with already many successful cases. In February 2020, BenevolentAI used its AI drug discovery platform to identify approved drugs that could potentially be used against Covid-19 infection. It identified baricitinib (already approved for the treatment of rheumatoid arthritis) as a potential treatment. In subsequent trials, the drug was found to reduce the risk of death when given to hospitalised patients with severe Covid-19.

GlobalData’s drugs database is currently tracking more than 3,000 drugs that have reportedly been developed or repurposed using AI, although recent analysis noted that the majority of them are in the early stages of development – either discovery or preclinical.

Commenting on the topic recently, GlobalData’s senior director of market research and strategic intelligence Urte Jakimaviciute said: “The fact that most AI-driven drugs are in early stages suggests that more companies are increasingly turning to AI to explore and expand their drug pipelines.

“This trend also reflects the industry’s growing reliance on AI to enhance R&D productivity. As the industry continues to recognise the potential of AI, this technology is set to become even more essential.”

GlobalData is the parent company of Clinical Trials Arena.