Bone Abstracts

Introduction: Standard clinical treatments for postmenopausal osteoporosis utilize resorption-inhibiting drugs such as bisphosphonates, which selectively bind to bone mineral but also suppress bone formation over time. Prostaglandin E2 (PGE2) has bone-anabolic effects in vivo, but its clinical utility is hindered by side effects upon systemic administration. Since PGE2 acts on bone via the EP4 receptor, our approach utilizes a specific...

Introduction: Prostaglandin E2 has bone-anabolic effects through EP4 receptor but its clinical utility is hindered by gastrointestinal side effects. To avoid these side effects, EP4 agonists (EP4a) were covalently linked to the bisphosphonate alendronate (ALN) to create two ALN-EP4a conjugate drugs, C1 and C2. When administered systemically, C1 and C2 will be target delivered to bone through ALN, where local hydrolytic enzymes liberate EP4a from ALN to exert bone an...