2711 T3D2669 Zoledronate Zoledronate (zoledronic acid, marketed by Novartis under the trade names Zometa and Reclast) is a bisphosphonate. Zometa is used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer. It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases. An annual dose of Zoledronate may also prevent recurring fractures in patients with a previous hip fracture. Zoledronate is a single 5 mg infusion for the treatment of Paget's disease of bone. In 2007, the FDA also approved Reclast for the treatment of postmenopausal osteoporosis. 118072-93-8 68740 C5H10N2O7P2 271.996320 White powder. Sparingly soluble Intravenous. Poorly absorbed (oral absorption is about 1% of what intravenous absorption is). The action of zoledronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Zoledronate also targets farnesyl pyrophosphate (FPP) synthase. Nitrogen-containing bisphosphonates such as zoledronate appear to act as analogues of isoprenoid diphosphate lipids, thereby inhibiting FPP synthase, an enzyme in the mevalonate pathway. Inhibition of this enzyme in osteoclasts prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are essential for the post-translational farnesylation and geranylgeranylation of small GTPase signalling proteins. This activity inhibits osteoclast activity and reduces bone resorption and turnover. In postmenopausal women, it reduces the elevated rate of bone turnover, leading to, on average, a net gain in bone mass. Zoledronate does not inhibit human P450 enzymes in vitro and does not undergo biotransformation in vivo. Route of Elimination: In 64 patients with cancer and bone metastases, on average (&#177; s.d.) 39 &#177; 16% of the administered zoledronic acid dose was recovered in the urine within 24 hours, with only trace amounts of drug found in urine post-Day 2. Half Life: 146 hours No indication of carcinogenicity to humans (not listed by IARC). For the treatment of hypercalcemia of malignancy. Also for the treatment of patients with multiple myeloma and patients with documented bone metastases from solid tumors, in conjunction with standard antineoplastic therapy. In May of 2007, the drug was approved for treatment of Paget's Disease. There is no experience of acute overdose. Two patients received zoledronate (32 mg) over 5 minutes in clinical trials. Neither patient experienced any clinical or laboratory toxicity. Overdosage may cause clinically significant hypocalcemia, hypophosphatemia, and hypomagnesemia. 2009-07-15T20:44:41Z 2026-03-27T00:45:52Z Zoledronate 46557 ZOLEDRONATE Zoledronic Acid DB00399 ZOL true OC(CN1C=CN=C1)(P(O)(O)=O)P(O)(O)=O C5H10N2O7P2 InChI=1S/C5H10N2O7P2/c8-5(15(9,10)11,16(12,13)14)3-7-2-1-6-4-7/h1-2,4,8H,3H2,(H2,9,10,11)(H2,12,13,14) XRASPMIURGNCCH-UHFFFAOYSA-N 272.0896 271.996323708 Exogenous Solid -4.2 HMDB14543 CHEMBL924 61986 <p>Judith Aronhime, Revital Lifshitz-Liron, &#8220;Zoledronic acid crystal forms, zoledronate sodium salt crystal forms, amorphous zoledronate sodium salt, and processes for their preparation.&#8221; U.S. Patent US20050054616, issued March 10, 2005.</p> CHEM002114 DTXSID0042668 NS00006387 [1-hydroxy-2-(1H-imidazol-1-yl)-1-phosphonoethyl]phosphonic acid