AJM347 / Eisai, Ensho Therap, EA Pharma - LARVOL DELTA

Safety, Pharmacokinetics, Food effect, and Pharmacodynamics of AJM347, a Selective α4β7 Integrin Antagonist: A First-in-Human Single- and Multiple-Ascending Dose Study in Healthy Male Volunteers. (PubMed, J Clin Pharmacol) - "Blood samples were collected to assess PK and PD (α4β7 receptor occupancy). Samples were also collected to measure lymphocyte counts in peripheral blood and cerebrospinal fluid (CSF)."

Clinical • First-in-human • Journal • P1 data • PK/PD data • CD4

[VIRTUAL] ORAL ALPHA 4 BETA 7 INTEGRIN ANTAGONIST AJM347 DEMONSTRATES SUSTAINED TARGET ENGAGEMENT IN A FIRST-IN-HUMAN STUDY IN HEALTHY VOLUNTEERS. (DDW 2021) - P1 | "These results demonstrated that AJM347 is clinically safe, tolerable well and orally available enough to maintain the almost complete and selective inhibition of MAdCAM-1 binding to α4β7 integrin on peripheral blood CD4+ T cells without affecting CSF lymphocyte counts. AJM347 could be a gut-selective and orally available treatment option for IBD. (ClinicalTrials.gov Identifier: NCT03133468)."

Clinical • P1 data • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • CD4

[VIRTUAL] PHARMACOLOGICAL CHARACTERIZATION OF AJM347: A NOVEL, ORALLY ACTIVE AND SMALL MOLECULAR PRODRUG OF ALPHA 4 BETA 7-SPECIFIC INTEGRIN ANTAGONIST FOR INFLAMMATORY BOWEL DISEASE (DDW 2021) - "In vitro studies show that CAN2281 is a highly potent and α4β7 integrin-selective inhibitor. In addition, its prodrug, AJM347 exhibits α4β7 integrin-selective pharmacological properties even in vivo. Finally AJM347 has completed Phase 1 trial and could be a gut-selective and orally available treatment option for IBD."

CNS Disorders • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Multiple Sclerosis • CD4 • IL10 • VCAM1