ChemicalBook > CAS DataBase List > Zoledronic acid

Zoledronic acid

Product Name
Zoledronic acid
CAS No.
118072-93-8
Chemical Name
Zoledronic acid
Synonyms
Zoledronic;ZOLEDRONATE;ZoMeta;Reclast;Zoledronic Acid API;Orazol;BPH 91;Aclasta;ZOL 446;CGP-4244
CBNumber
CB4395643
Molecular Formula
C5H10N2O7P2
Formula Weight
272.09
MOL File
118072-93-8.mol
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Zoledronic acid Property

Melting point:
193-2040C (dec)
Boiling point:
764.0±70.0 °C(Predicted)
Density 
2.13±0.1 g/cm3(Predicted)
storage temp. 
Sealed in dry,Room Temperature
solubility 
Soluble in Water (up to 2 mg/ml).
form 
solid
pka
1.41±0.10(Predicted)
color 
White or off-white
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.
CAS DataBase Reference
118072-93-8(CAS DataBase Reference)
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Safety

Hazard Codes 
Xi
Risk Statements 
21/22-36/37/38
Safety Statements 
24/25-36/37/39
HS Code 
2933399090
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H317May cause an allergic skin reaction

H319Causes serious eye irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P272Contaminated work clothing should not be allowed out of the workplace.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P333+P313IF SKIN irritation or rash occurs: Get medical advice/attention.

P363Wash contaminated clothing before reuse.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Tocris
Product number
6111
Product name
Zoledronic Acid
Purity
≥98%(HPLC)
Packaging
10
Price
$70
Updated
2021/12/16
Tocris
Product number
6111
Product name
Zoledronic Acid
Purity
≥98%(HPLC)
Packaging
50
Price
$290
Updated
2021/12/16
TRC
Product number
Z623505
Product name
Zoledronic Acid
Packaging
250mg
Price
$1065
Updated
2021/12/16
TRC
Product number
Z623505
Product name
Zoledronic Acid
Packaging
5mg
Price
$75
Updated
2021/12/16
TRC
Product number
Z623505
Product name
Zoledronic Acid
Packaging
25mg
Price
$215
Updated
2021/12/16
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Zoledronic acid Chemical Properties,Usage,Production

Description

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.

Chemical Properties

White Solid

Originator

Zometa,Novartis Pharma,Switz

Uses

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.

Uses

Bisphosphonate antiresorptive agent

Uses

bone resorption inhibitor

Definition

ChEBI: An imidazole compound having a 2,2-bis(phosphono)-2-hydroxyethane-1-yl substituent at the 1-position.

Manufacturing Process

With stirring and under reflux, 8.6 g (0.053 mole) of imidazol-4-yl acetic acid hydrochloride, 7.1 ml of 85% phosphoric acid and 25 ml of chlorobenzene are heated to 100°C. Then 13.9 ml of phosphorus trichloride are added dropwise at 100°C, whereupon evolution of gas occurs. Over the course of 30 min a dense mass precipitates from the reaction mixture. The batch is heated for 3 hours to 100°C and the supernatant chlorobenzene is removed by decantation. With stirring and under reflux, the residual viscous mass is heated to the boil for 3 hours with 40 ml of 9 N hydrochloric acid. The batch is filtered hot with the addition of carbon and the filtrate is diluted with acetone, whereupon the crude 2-(imidazol-4-yl)-1-hydroxy-ethane-1,1- diphosphonic acid precipitates. This product is recrystallised from water. Melting point: 238-240°C (dec.).

brand name

Zometa (Novartis).

Therapeutic Function

Bone calcium regulator

Biological Functions

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.

Clinical Use

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.

Drug interactions

Potentially hazardous interactions with other drugs
Other nephrotoxic drugs: use with caution as can enhance nephrotoxicity

Metabolism

Zoledronic acid is not metabolised and is excreted unchanged via the kidney. Over the first 24 hours, 39 ± 16
% of the administered dose is recovered in the urine, while the remainder is principally bound to bone tissue.

storage

Store at +4°C

References

1) Green?et al. (1994),?Preclinical pharmacology of CGP 42446, a new, potent, heterocyclic bisphosphonate compound; J. Bone Miner. Res.,?9?745 2) Deeks and Perry (2008)?Zoledronic acid: a review of its use in the treatment of osteoporosis; Drugs Aging,?25?963 3) Perry and Figgitt (2004),?Zoledronic acid: a review of its use in patients with advanced cancer; Drugs,?64?1197 4) Koto?et al. (2010)?Zoledronic acid inhibits proliferation of human fibrosarcoma cells with induction of apoptosis and shows combined effects with other anticancer agents; Oncol. Rep.,?24?233 5) Tonyali?et al. (2010)?The role of zoledronic acid in the adjuvant treatment of breast cancer: current perspectives; Expert Opin. Pharmacother.,?11?2715

Zoledronic acid Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Zoledronic acid manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD
Product
Zoledronic acid 118072-93-8
Price
US $1.00/g
Min. Order
100g
Purity
≥98%
Supply Ability
100kg/month
Release date
2021-06-10
Hebei Weibang Biotechnology Co., Ltd
Product
Zoledronic acid 118072-93-8
Price
US $1.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
10 mt
Release date
2024-10-25
Hebei Fengjia New Material Co., Ltd
Product
Zoledronic acid 118072-93-8
Price
US $20.00/kg
Min. Order
1kg
Purity
0.99
Supply Ability
100 tons
Release date
2024-08-09

118072-93-8, Zoledronic acidRelated Search:


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