KMN-159

KMN-159 is a synthetic small-molecule prostanoid EP4 receptor agonist developed by Cayman Chemical as a locally administered bone anabolic agent for orthopedic and dental applications.[6][15][13] It is a difluorolactam analog of prostaglandin E1 that acts as a potent, highly selective full agonist of the prostaglandin E2 EP4 receptor, with >5000‑fold selectivity over EP2 and nanomolar potency, and exhibits favorable pharmacokinetic properties and chemical stability suited to incorporation in biomaterial scaffolds.[6][7][4][10] By activating EP4 on osteoprogenitor and bone marrow cells, KMN-159 stimulates osteoblastic differentiation, upregulates markers such as alkaline phosphatase, type I collagen, and osteocalcin, and enhances bone formation and defect repair in preclinical models, achieving bone healing comparable to recombinant human BMP-2 when delivered locally via calcium phosphate, demineralized bone matrix, or mineralized collagen matrices.[6][1][3][16] The compound is being investigated preclinically as the active pharmaceutical ingredient in drug–device combinations to augment bone mass and improve outcomes in indications such as spinal fusion and dental implant osseointegration.[2][8][3][5]

Other names

11-deoxy-10,10-difluoro-8-aza-PGE1 analog