Name | Zoledronic acid |
Synonyms | Orazol BPH 91 Aclasta Reclast CGP-4244 CGP-42446 ZOLEDRONATE sMall aMount Zoledronic acid Zoledronic Acid API 2-(imidazole-1-yl)-1-acetic acid HCl 2-(Imidazol-1-yl)-1-hydroxyethane-1,1-diphosphonic Acid [1-hydroxy-2-(1h-imidazol-1-yl)-ethylidene]bisphosphonic acid [1-hydroxy-2-(1H-imidazol-1-yl)ethane-1,1-diyl]bis(phosphonic acid) |
CAS | 118072-93-8 |
EINECS | 1806241-263-5 |
InChI | InChI=1/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) |
Molecular Formula | C5H10N2O7P2 |
Molar Mass | 272.09 |
Density | 2.13±0.1 g/cm3(Predicted) |
Melting Point | 193-2040C (dec) |
Boling Point | 764.0±70.0 °C(Predicted) |
Flash Point | 415.8°C |
Solubility | Soluble in Water (up to 2 mg/ml). |
Vapor Presure | 1.53E-24mmHg at 25°C |
Appearance | solid |
Color | White or off-white |
pKa | 1.41±0.10(Predicted) |
Storage Condition | Sealed in dry,Room Temperature |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in distilled water may be stored at -20° for up to 2 months. |
Refractive Index | 1.718 |
MDL | MFCD00867791 |
Physical and Chemical Properties |
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Use | For antineoplastic agents |
Hazard Symbols | Xi - Irritant |
Risk Codes | R21/22 - Harmful in contact with skin and if swallowed. R36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S24/25 - Avoid contact with skin and eyes. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. |
HS Code | 2933399090 |
Pharmacological effects | Zoledronic acid is the third generation bisphosphonate compound and is an effective inhibitor of bone resorption. The drug can inhibit osteoclast activity, induce osteoclast apoptosis, prevent the reabsorption of mineral bone and cartilage by combining with bone, and inhibit the osteoclast activity caused by various stimulating factors released by tumor cells Increase and release of bone calcium, which can effectively control hypercalcemia. |
Indications | [Trade Name] Zoledronic Acid, Aikeshu, Ailang, Arenin, Bolaining, Gai Ning, Miluda, Suqi, Tianqing Yitai, Yilida, Zetai, Zhenda, Zhuolai, Zorui, Zomei. 1) Malignant hypercalcemia: Hypercalcemia is a metabolic complication of malignant tumors. When the serum calcium in the body is higher than 3.75mmol/L, a hypercalcemia crisis may occur, which may eventually cause death. Zoledronic acid can treat hypercalcemia by inhibiting bone resorption, reducing blood calcium levels, and increasing urinary calcium excretion. 14 patients with tumor hypercalcemia were treated with zoledronic acid. The final results showed that zoledronic acid was 100% to reduce blood calcium to normal during the observation period, the median effective remission time was 5.07d, and the median remission maintenance time was 22.30d. It has been shown by studies that 4 mg of zoledronic acid is recommended for the initial dose of hypercalcemia and 8mg of zoledronic acid is recommended for relapsed or refractory hypercalcemia. 2) Bone metastasis: Zoledronic acid is a new generation of potent nitrogen-containing bisphosphonates. It has been used in foreign clinical practice to treat a variety of tumor bone metastasis-related complications, including multiple myeloma, breast cancer, Lung cancer, etc. Polymyeloma (MM) is a malignant plasma cell disease in which tumor cells originate from plasma cells in the bone marrow, and plasma cells are cells in which lymphocytes develop to the final functional stage. Therefore, multiple myeloma can be classified as B- cell lymphoma. In previous clinical studies, bisphosphonates can reduce hypercalcemia in tumor patients, reduce the occurrence of pathological fractures, and relieve pain in bone metastases. Zoledronic acid is the third bisphosphonate drug, which has been proved to be the drug with the strongest anti-bone resorption ability. 94 patients with myeloma were randomly divided into experimental group and control group. The control group was treated with standard chemotherapy, while the experimental group was treated with standard chemotherapy combined with zoledronic acid. The results showed that the five-year disease-free survival rate of the experimental group was relatively high. At present, zoledronic acid is mainly used as an adjuvant drug for tumor treatment, for the treatment of bone metastasis and other complications. However, with the development of clinical trials, studies have found that zoledronic acid has a significant effect on the treatment of malignant tumors. |
use | is an anti-tumor drug treatment of malignant tumor bone metastasis |