ゾレドロン酸 化学特性,用途語,生産方法
効能
高カルシウム血症治療薬, 骨吸収抑制薬, ファルネシルピロリン酸合成酵素阻害薬
説明
Zoledronic acid is a white, crystalline powder that is available in vials for reconstitution for IV infusion over at
least 15 minutes. It does not undergo metabolic transformation and does not inhibit CYP450 enzymes.
Clearance of this agent is dependent on the patient's creatinine clearance, not on dose. Serum creatinine
levels should be evaluated before every treatment. Zolendronic acid is contraindicated in patients with severe
renal impairment.
化学的特性
White Solid
使用
Zoledronic acid induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho.
定義
ChEBI: An imidazole compound having a 2,2-bis(phosphono)-2-hydroxyethane-1-yl substituent at the 1-position.
生物学の機能
Zoledronic acid, a bisphosphonate, was approved by the U.S. FDA in 2001 for the treatment of hypercalcemia
of malignancy, a metabolic complication that can be life-threatening. Hypercalcemia of malignancy
can occur in up to 50% of patients diagnosed with advanced breast cancer, multiple myeloma, and nonsmall
cell lung cancer. This condition arises when chemical moieties produced by the tumor cause overstimulation of
osteoclasts. When there is an increase in bone degradation, there is a concomitant release of calcium into the
plasma. When serum concentrations of calcium rapidly elevate, the kidneys are unable to handle the overload,
and hypercalcemia results. This can lead to dehydration, nausea, vomiting, fatigue, and confusion. Zoledronic
acid effectively decreases plasma calcium concentrations via inhibition of bone resorption (inhibition of
osteoclastic activity and induction of osteoclast apoptosis). It also prevents the increase in osteoclastic activity
caused by tumor-based stimulatory factors. Additionally zoledronic acid has been approved by the U.S. FDA for
the treatment of multiple myeloma and bone metastases associated with solid tumor–based cancers (e.g.,
prostrate and lung). This agent is currently in late-stage clinical trials for the treatment and prevention of
osteoporosis and, if approved, will be formulated as a 5-mg, once-yearly IV infusion.
臨床応用
Zoledronic acid is most
commonly given to patients whose cancer is no longer responding to hormones, but it also may be
given to prevent the bone thinning and weakening that results from hormonal treatments.
ゾレドロン酸 上流と下流の製品情報
原材料
準備製品