Zoledronate

Zoledronic acid
Clinical data


AHFS/Drugs.com	Monograph
MedlinePlus	a605023
License data	EU EMA: Reclast US FDA: Zoledronic_acid
Pregnancy category	D (U.S.)
Routes of administration	Intravenous
ATC code	M05BA08 (WHO)
Legal status
Legal status	℞-only (U.S.)
Pharmacokinetic data
Protein binding	22%
Metabolism	Nil
Biological half-life	146 hours
Excretion	Renal (partial)
Identifiers
IUPAC name [1-hydroxy-2-(1H-imidazol-1-yl)ethane-1,1-diyl]bis(phosphonic acid)
CAS Number	118072-93-8
PubChem (CID)	68740
IUPHAR/BPS	3177
DrugBank	DB00399
ChemSpider	61986
UNII	70HZ18PH24^Y
KEGG	D08689^N
ChEMBL	CHEMBL924^Y
PDB ligand ID	ZOL (PDBe, RCSB PDB)
Chemical and physical data
Formula	C₅H₁₀N₂O₇P₂
Molar mass	272.09 g/mol
3D model (Jmol)	Interactive image
SMILES O=P(O)(O)C(O)(Cn1ccnc1)P(=O)(O)O
InChI 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) Key:XRASPMIURGNCCH-UHFFFAOYSA-N
^NY (what is this?)

Zoledronic acid (INN) or zoledronate is a bisphosphonate drug given intravenously to treat some bone diseases. It is sold under many trade names worldwide.

Zoledronic acid slows down bone resorption, allowing the bone-forming cells time to rebuild normal bone and allowing bone remodeling.

Zometa is used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer, as well as for treating osteoporosis. It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases.

It can be administered at home rather than in hospital. Such administration has shown safety and quality-of-life benefits in breast cancer patients with bone metastases.

Marketed as Aclasta (in Australia) or Reclast (in the US), zoledronic acid may be given as a 5 mg infusion once per year for treatment of osteoporosis in men and post-menopausal women at increased risk of fracture.

In 2007, the U.S. Food and Drug Administration (FDA) also approved Reclast for the treatment of postmenopausal osteoporosis.

As Reclast a single dose of 5 mg is used for the treatment of Paget's disease.

Side-effects can include fatigue, anemia, muscle aches, fever, and/or swelling in the feet or legs. Flu-like symptoms are commonly experienced after the first zoledronate infusion, although not subsequent infusions, and are thought to occur because of its potential to activate human γδ T cells (gamma/delta T cells).

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Wikipedia