Find, compare & contact
Odanacatib API Manufacturers & Suppliers

General Description:

Odanacatib, identified by CAS number 603139-19-1, is a notable compound with significant therapeutic applications. Odanacatib is an inhibiter of cathepsin K which was originally developed be Merck & Co as a new treatment for osteoporosis . The drug made it to phase III trials before abandoned due to increased stroke.

Indications:

This drug is primarily indicated for: Investigated for use/treatment in osteoporosis . Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Odanacatib undergoes metabolic processing primarily in: The major metabolite is the product of hydroxylation by CYP3A4 and CYP2C8 . This metabolite is active but is 25 times less effective at inhibiting cathepsin K than odanacatib. The other metabolites are produced through glutathione conjugation, hydrolysis, dealkylation, glucuronidation, oxidation, and cyclization. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Odanacatib are crucial for its therapeutic efficacy: Tmax of 2-6h . The absolute bioavailabilities observed with 30mg and 50 mg doses are 70% and 30% respectively. When taken with high fat meals the 50mg dose's bioavailability increases to 49% and tmax increases to 10.5h . The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Odanacatib is an important consideration for its dosing schedule: Apparent half life observed to be 87.3-94.7h . This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Odanacatib exhibits a strong affinity for binding with plasma proteins: 97.5% bound to plasma proteins . This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Odanacatib from the body primarily occurs through: 16.9% excreted in urine. 74.5% excreted in feces. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Odanacatib is distributed throughout the body with a volume of distribution of: 100L. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Odanacatib is a critical factor in determining its safe and effective dosage: Total clearance of 0.8L/h . It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Odanacatib exerts its therapeutic effects through: Increases bone mineral density and reduces risk of fractures in osteoporosis . The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Odanacatib functions by: Odanacatib inhibits cathepsin K, likely by binding to its active site . Cathepsin K is a cysteine protease enzyme which is secreted by osteoclasts . Cathepsin K is responsible for the breakdown of collagen in the bone matrix as part of bone resorption. The inhibition of this enzyme results in decreased bone resorption without affecting bone deposition resulting in increased bone mineral density. This increased bone mineral density strengthens the bone which leads to fewer fractures in osteoporosis. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Odanacatib belongs to the class of organic compounds known as leucine and derivatives. These are compounds containing leucine or a derivative thereof resulting from reaction of leucine at the amino group or the carboxy group, or from the replacement of any hydrogen of glycine by a heteroatom, classified under the direct parent group Leucine and derivatives. This compound is a part of the Organic compounds, falling under the Organic acids and derivatives superclass, and categorized within the Carboxylic acids and derivatives class, specifically within the Amino acids, peptides, and analogues subclass.

Categories:

Odanacatib is categorized under the following therapeutic classes: Benzene Derivatives, Cytochrome P-450 CYP2C8 Substrates, Cytochrome P-450 CYP3A Substrates, Cytochrome P-450 CYP3A4 Substrates, Cytochrome P-450 Substrates, P-glycoprotein substrates. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.