Design and synthesis of bone-selective osteogenic oxysterol-bisphosphonate analog

DESCRIPTION (provided by applicant): Osteoporosis affects 10 million Americans and another 34 million are osteopenic and at risk for developing osteoporosis. Bone fractures, the most important complication of osteoporosis, cause substantial morbidity andmortality in the aging population as well as significant socio-economic cost. Since the 1960's, bisphosphonate drug therapy has produced modest clinical benefits such as improved bone density and reduced fracture risk by slowing osteoclastic bone resorption. To this date, all marketed therapies for osteoporosis as well as the majority of potential new treatments under clinical investigation aim to reduce the level of bone resorption in osteoporotic patients. Anti-resorptive drug therapy has been most effective in treating early and mild cases of the disease, unlike severe osteoporosis, where a massive loss of bone mineral density has already occurred. New strategies are urgently needed for intervention in osteoporosis, particularly in severe cases of th