MES-1007

MES-1007 is a bone-targeted, bi-specific small-molecule drug-conjugate prodrug of a potent prostaglandin E2 EP4 receptor agonist, designed to deliver an anabolic EP4 agonist specifically to bone in order to stimulate bone formation while minimizing systemic side effects.[1][2][3][8] The molecule consists of an EP4 agonist covalently linked to a bisphosphonate-based bone-targeting moiety, leading to rapid blood clearance, high uptake into bone, and slow release of the active EP4 agonist from bone with an approximate half-life of 7 days.[3][8] Preclinical studies in models of osteogenesis imperfecta and other bone conditions show that MES-1007 alone increases bone formation rate and, in combination with the bisphosphonate zoledronate, produces additive improvements in trabecular and cortical bone parameters and mechanical strength, consistent with EP4-mediated bone anabolic activity.[3][5] MES-1007 was originally developed at Simon Fraser University and is being advanced by Mesentech under license, with development focused on bone diseases such as osteoporosis, osteogenesis imperfecta, and bone loss in Duchenne muscular dystrophy, and has completed IND-enabling and early safety evaluations with a substantially higher NOAEL than non-targeted EP4 agonists.[1][2][3][5][8]

Other names

Mes-1007Mes1007Mes 1007