Ibandronate: the evolution of a once-a-month oral therapy for postmenopausal osteoporosis.

摘要

Bisphosphonates have been shown to be highly effective in preventing and treating postmenopausal osteoporosis (PMO) and the associated risk of fracture. However, poor adherence with bisphosphonate therapies for PMO results in a high incidence of otherwise preventable fractures. The chronicity of this condition requires long-term treatment, but fewer than one in two women remains on daily bisphosphonate therapy for 1 yr. A good way to reduce the risk of osteoporotic fractures is through development of equally efficacious formulations with more convenient dosing regimens. Weekly formulations of bisphosphonates have been introduced that demonstrate comparable efficacy to daily formulations with slightly improved adherence. Recently, a new formulation utilizing a third-generation nitrogen-containing bisphosphonate--ibandronate--has been approved with a monthly dosing regimen. The pharmacokinetics and high potency of ibandronate, similar with other bisphosphonates, facilitate lower mg doses and longer-interval dosing frequencies with similar efficacy and enhanced tolerability. Preclinical studies and clinical trials have consistently demonstrated that it is the total cumulative dose of ibandronate that determines efficacy. The convenience of once-monthly dosing may ultimately improve adherence and clinical outcomes among the growing population of postmenopausal women at risk of osteoporosis.