ISM5411 / Insilico Medicine - LARVOL DELTA

Study Evaluating ISM5411 Administered Orally to Subjects With Active Ulcerative Colitis (clinicaltrials.gov) - P2 | N=80 | Recruiting | Sponsor: InSilico Medicine Hong Kong Limited

New P2 trial • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis

THERAPEUTIC EFFICACY OF ISM012-042(ISM5411)IN T CELL TRANSFER-INDUCED COLITIS IN MICE (UEGW 2025) - "ISM012-042, administered preventively or therapeutically, alone or with anti-TNF-α, effectively mitigated chronic T cell transfer-induced colitis by preserving colon integrity, and suppressing pro-inflammatory T cell subsets and cytokines, suggesting its potential as a versatile IBD therapy."

Preclinical • Crohn's disease • Fibrosis • Gastroenterology • Gastrointestinal Disorder • Immunology • Infectious Disease • Inflammation • Inflammatory Bowel Disease • GATA3 • IFNG • IL17A • IL6

ISM5411, A NOVEL GUT-RESTRICTIVE PROLYL HYDROXYLASE-2 INHIBITOR FOR INFLAMMATORY BOWEL DISEASE: RANDOMIZED, DOUBLE-BLINDED, PLACEBO-CONTROLLED FIRST-IN-HUMAN PHASE I STUDY TO EVALUATE SAFETY, TOLERABILITY AND PK PROFILES (UEGW 2025) - "ISM5411 tablets were safe and well-tolerated and demonstrated good gut-restrictive property, consistent with the intended PK profile. Another Phase I study in China was also completed. Phase 2a proof of concept study of ISM5411 is under planned in patients with ulcerative colitis to explore the safety, PK and clinical efficacy."

Clinical • First-in-human • P1 data • Crohn's disease • Gastroenterology • Gastrointestinal Disorder • Hematological Disorders • Immunology • Inflammation • Inflammatory Bowel Disease • Ulcerative Colitis • HIF1A

Insilico Received Positive Topline Results from Two Phase 1 Trials of ISM5411, New Drug Designed Using Generative AI for the Treatment of Inflammatory Bowel Disease (PRNewswire) - P1 | N=79 | NCT06012578 | Sponsor: InSilico Medicine Hong Kong Limited | N=48 | CTR20241789 | Sponsor: Insilicon Intelligence Technology (Shanghai) Co., Ltd. | "The data indicates that ISM5411 was generally safe and well tolerated across all dose groups of two Phase I studies, with no reports of serious adverse events or treatment-related adverse events (TRAEs) leading to discontinuation...The observed human PK of ISM5411 in healthy volunteers was in line with the Company's preclinical modeling, with no significant drug accumulation observed after 14 days of multiple administration across all dosing groups. ISM5411 also exhibited a favorable PK profile....Based on these results, Insilico Medicine expects to initiate a Phase 2 proof-of-concept study evaluating ISM5411 in active ulcerative colitis patients in the second half of 2025."

New P2 trial • P1 data • Inflammatory Bowel Disease • Ulcerative Colitis

Intestinal mucosal barrier repair and immune regulation with an AI-developed gut-restricted PHD inhibitor. (PubMed, Nat Biotechnol) - "Here we used a multimodel multimodal generative artificial intelligence platform to design an orally gut-restricted selective PHD1 and PHD2 inhibitor that exhibits favorable safety and pharmacokinetic profiles in preclinical studies. ISM012-042 restores intestinal barrier function and alleviates gut inflammation in multiple experimental colitis models."

Journal • Gastroenterology • Gastrointestinal Disorder • Hematological Disorders • Immunology • Inflammation • Inflammatory Bowel Disease

Nature Biotechnology | Generative Chemistry Enables Insilico to Develop Gut-Restricted PHD Inhibitors Promising for Intestinal Mucosal Barrier Repair and Immunomodulation (PRNewswire) - "Recently, scientists at Insilico Medicine utilized the comprehensive generative chemistry engine Chemistry42 to discover a novel gut-restricted PHD inhibitor that shows promise for repairing the intestinal mucosal barrier and regulating immune responses in IBD. The study, published in Nature Biotechnology, highlights the role of Chemistry42 and its submodules in supporting drug candidate design and optimization....At the time of this publication, two Phase 1 clinical trials of ISM5411 for the treatment of IBD are being conducted in parallel in Australia and China."

Preclinical • Trial status • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis

Study Evaluating ISM5411 Administered Orally to Healthy Volunteers (clinicaltrials.gov) - P1 | N=79 | Completed | Sponsor: InSilico Medicine Hong Kong Limited | Recruiting ➔ Completed

Trial completion

Insilico Medicine Announces First-in-Human Study for Orally PHD Inhibitor ISM5411 for Inflammatory Bowel Disease (IBD) (PRNewswire-Asia) - "Insilico Medicine...announced that the company has initiated the first-in-human study for ISM5411, a potentially first-in-class PHD inhibitor for the treatment of inflammatory bowel disease (IBD)....The ongoing Phase I study is designed to evaluate the safety, tolerability, pharmacokinetics and food effects of ISM5411 at increasing oral doses in 76 healthy subjects, with the first dose in healthy volunteers now completed in Australia. To further evaluate ISM5411 in wider populations, Insilico plans to conduct global multi-center Phase Ib trials in patients with ulcerative colitis following the Phase Ia study."

Trial status • Immunology • Inflammatory Bowel Disease