Моногидрат Минодроновой кислоты

What is this

Minodronic acid monohydrate is a third generation nitrogen-containing bisphosphonate, a pharmaceutical substance. The development code is YM-529. The structure contains two phosphonate residues at the total carbon and an imidazopyridine fragment carrying nitrogen atoms - it is this that determines the high activity of the compound compared to early bisphosphonates without nitrogen.

Basic Attributes

• CAS No: 155648-60-5
• Chemical formula: C9H12N2O7P2 H2O
• Molecular Weight: 340.165
• Exact weight: 340.022522
• EU number: 1592732-453-0
• RTECS number: SZ8562470
• PSA Specifications: 154
• XLogP3: −0.186

Pharmacological group and mechanism

Bone resorption inhibitor. The target is farnesyl diphosphate synthase, an enzyme of the mevalonate pathway. Its blockade deprives the osteoclast of isoprenoids necessary for the prenylation of small GTPases, which disrupts the organization of the cell cytoskeleton and its resorptive function. After administration, the substance selectively accumulates in bone tissue; the acid that the osteoclast secretes into the lacuna during bone resorption releases the bisphosphonate from the matrix, and it is absorbed by this particular cell. In terms of suppression of bone resorption, minodronic acid is approximately 1000 times superior to etidronate and 10–100 times superior to alendronic acid.

Application

• treatment of osteoporosis; drug approved in Japan
• According to published data, this is the first drug to show a statistically significant reduction in the incidence of fractures compared with placebo in a Japanese patient population
• substance for the production of finished dosage forms and reference standard for pharmaceutical analysis

Safety Information

• Hazard Statements: H301
• Precautions: P201, P202, P261, P264, P270, P271, P280, P281, P301 + P310, P302 + P352, P304 + P340, P305 + P351 + P338, P308 + P313, P312, P321, P330, P332 + P313, P337 + P313, P362, P403 + P233, P405, P501
• Packing group: III
• Hazard category: 6.1
• UN transport code: 2811

Storage and handling

Tightly closed container, dry room. The substance crystallizes with one molecule of water, so excess moisture and heat can change the hydration state and the results of the analysis. Hanging is carried out under a hood, wearing gloves and safety glasses; dust is not allowed; residues are collected as pharmaceutical waste.