Mometasone furoate API Manufacturers

General Description:

Mometasone furoate, identified by CAS number 83919-23-7, is a notable compound with significant therapeutic applications. Mometasone furoate is a corticosteroid drug that can be used for the treatment of asthma, rhinitis, and certain skin conditions. It has a glucocorticoid receptor binding affinity 22 times stronger than and higher than many other corticosteroids as well. Mometasone furoate is formulated as a dry powder inhaler, nasal spray, and ointment for its different indications.

Indications:

This drug is primarily indicated for: Inhaled mometasone furoate is indicated for prophylaxis of asthma in patients ≥4 years. Applied topically as an ointment, mometasone furoate is indicated for symptomatic treatment of dermatitis and pruritis in patients ≥2 years. Mometasone furoate nasal spray is available both over-the-counter (OTC) and by prescription. The OTC nasal spray formulation of mometasone furoate is indicated for the treatment of upper respiratory allergic symptoms (e.g. rhinorrhea, sneezing) in patients ≥2 years of age. The prescription formulation is indicated for the treatment of chronic rhinosinusitis with nasal polyps in patients ≥18 year old and for the and prophylaxis of seasonal allergic rhinitis in patients ≥12 years old. It is also approved in combination with for the symptomatic treatment of seasonal allergic rhinitis in patients ≥12 years. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Mometasone furoate undergoes metabolic processing primarily in: Metabolism of mometasone furoate is largely performed hepatically by cytochrome P450 3A4 producing a number of metabolites. Some of these metabolites include free mometasone and 6-beta-hydroxy-mometasone furoate. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Mometasone furoate are crucial for its therapeutic efficacy: The mean time to peak concentration is 1.0 to 2.5 hours. Bioavailability has been reported as <1% but studies of repeat doses of inhaled corticosteroids suggest a bioavailability of 11%. The 0.1% ointment may have a bioavailability of 0.7%. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Mometasone furoate is an important consideration for its dosing schedule: The terminal half life of an inhaled dose is approximately 5 hours though it has been reported as 5.8 hours by other sources. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Mometasone furoate exhibits a strong affinity for binding with plasma proteins: 98% to 99% (in vitro concentration of 5 to 500ng/mL). This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Mometasone furoate from the body primarily occurs through: For an inhaled dose, approximately 74% is excreted in the feces and 8% is excreted in the urine. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Mometasone furoate is distributed throughout the body with a volume of distribution of: Steady state volume of distribution of 152L. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Mometasone furoate is a critical factor in determining its safe and effective dosage: The clearance rate of mometasone furoate is not readily available, though it may be close to 90L/h. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Mometasone furoate exerts its therapeutic effects through: Mometasone is a synthetic corticosteroid with an affinity for glucocorticoid receptors 22 times higher than that of . Mometasone furoate also has a lower affinity to mineralocorticoid receptors than natural corticosteroids, making it more selective in its action. Mometasone furoate diffuses across cell membranes to activate pathways responsible for reducing inflammation. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Mometasone furoate functions by: In asthma, mometasone is believed to inhibit mast cells, eosinophils, basophils, and lymphocytes. There is also evidence of inhibition of histamine, leukotrienes, and cytokines. Corticosteroids diffuse across cell membranes into the cytosol of cells where they bind to glucocorticoid receptors to produce their activity. Mometasone furoate has a particularly high receptor affinity compare to other corticosteroids, 22 times higher than that of . Mometasone furoate binding to a glucocorticoid receptor causes conformational changes in the receptor, separation from chaperones, and the receptor moves to the nucleus. Once at the nucleus, receptors dimerize and bind to a DNA sequence known as the glucocorticoid response element which either increases expression of anti-inflammatory molecules or inhibits expression of pro-inflammatory molecules (such as interleukins 4 and 5). Mometasone furoate also reduces inflammation by blocking transcription factors such as activator-protein-1 and nuclear factor kappa B (NF-kappaB). This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Mometasone furoate belongs to the class of organic compounds known as gluco/mineralocorticoids, progestogins and derivatives. These are steroids with a structure based on a hydroxylated prostane moiety, classified under the direct parent group Gluco/mineralocorticoids, progestogins and derivatives. This compound is a part of the Organic compounds, falling under the Lipids and lipid-like molecules superclass, and categorized within the Steroids and steroid derivatives class, specifically within the Pregnane steroids subclass.

Categories:

Mometasone furoate is categorized under the following therapeutic classes: Adrenal Cortex Hormones, Adrenals, Adrenergics, Inhalants, Anti-Allergic Agents, Anti-Inflammatory Agents, Corticosteroids, Corticosteroids, Dermatological Preparations, Corticosteroids, Potent (Group III), Cytochrome P-450 CYP2C8 Inhibitors, Cytochrome P-450 CYP2C8 Inhibitors (strength unknown), Cytochrome P-450 CYP2C8 Inhibitors (strong), Cytochrome P-450 CYP3A Inducers, Cytochrome P-450 CYP3A Substrates, Cytochrome P-450 CYP3A4 Inducers, Cytochrome P-450 CYP3A4 Inducers (strength unknown), Cytochrome P-450 CYP3A4 Substrates, Cytochrome P-450 CYP3A5 Inducers, Cytochrome P-450 CYP3A5 Inducers (strength unknown), Cytochrome P-450 Enzyme Inducers, Cytochrome P-450 Enzyme Inhibitors, Cytochrome P-450 Substrates, Dermatologicals, Drugs for Obstructive Airway Diseases, Fused-Ring Compounds, Glucocorticoids, Hyperglycemia-Associated Agents, Immunosuppressive Agents, Nasal Preparations, Pregnadienes, Steroids, Thyroxine-binding globulin inhibitors. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Experimental Properties:

Further physical and chemical characteristics of Mometasone furoate include:

• Water Solubility: Insoluble
• Melting Point: 215-228
• logP: 4.115