Mometasone Furoate

Mometasone Furoate

Cat Number
API83919237
CAS Number
83919-23-7

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CAS Number
83919-23-7
EINECS
617-501-0
Storage
Store at room temperature
Synonyms
Asmanex; Elocon; Sinuva; Asmanex HFA; Asmanex Twisthaler; SCH 32088
Molecular Formula
C27H30Cl2O6
Molecular Weight
521.4
Smiles
C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@@]4([C@]3([C@H](C[C@@]2([C@]1(C(=O)CCl)OC(=O)C5=CC=CO5)C)O)Cl)C
Appearance
White to off-white powder
Melting Point
218-220℃
Boiling Point
655.5℃ at 760 mmHg
General Description
Mometasone furoate is a medium-to-high potency synthetic corticosteroid available in multiple formulations. It is characterized by high lipophilicity and a low potential for systemic absorption when applied locally. The furoate ester enhances receptor binding and prolongs tissue retention.
Mechanism of Action
Mometasone binds to glucocorticoid receptors with approximately 20-fold higher affinity than dexamethasone, leading to potent anti-inflammatory and immunosuppressive effects. It reduces inflammatory cytokine production (IL-4, IL-5, IL-13), inhibits eosinophil chemotaxis, and downregulates adhesion molecule expression on endothelial cells. In the lung and nasal mucosa, this reduces edema, mucus secretion, and airway hyperresponsiveness. The drug has minimal atrophogenic effect on skin compared to other potent steroids.
Application
Intranasal mometasone is indicated for allergic rhinitis (seasonal and perennial) and nasal polyps. The topical cream is approved for atopic dermatitis, psoriasis, and other steroid-responsive dermatoses. Inhaled mometasone via dry powder inhaler is used for prophylactic asthma management.

Mometasone furoate, a chlorinated 17‑furoate ester of hydrocortisone, exhibits greater anti‑inflammatory activity and longer duration of action than betamethasone. Clinical trials show comparable or superior efficacy in adults and children with various dermatologic conditions. It is well tolerated with only transient mild‑to‑moderate local effects. Due to high lipophilicity, low percutaneous absorption, and rapid hepatic biotransformation, systemic availability is very low, with no significant hypothalamic‑pituitary‑adrenal axis suppression. Its molecular biotransformation in skin results in lower affinity for dermal cells than epidermal cells, contributing to low atrophogenicity. Sensitization is rare. Mometasone furoate is a highly efficacious potent corticosteroid with low risk of local and systemic adverse effects.

Fig. 1 Changes in hydrocortisone leading to the formation of mometasone furoate. (Spada F, <i>et al</i>., 2018) Fig. 1 Changes in hydrocortisone leading to the formation of mometasone furoate. (Spada F, et al., 2018)

References

  1. Spada F, et al. Comparative safety and efficacy of topical mometasone furoate with other topical corticosteroids. Australas J Dermatol. 2018;59(3):e168-e174.

Does Mometasone Furoate require protection from light during storage?

Yes, it is photosensitive. UV light can cause photodegradation of the furoate ester and the steroid nucleus. Store in light-resistant containers.

What is the recommended storage temperature for Mometasone Furoate?

Store at controlled room temperature (15-25°C). Avoid temperatures above 30°C, which can accelerate hydrolysis and oxidation.

Is Mometasone Furoate stable in nasal spray and topical formulations?

Yes, it shows excellent stability when formulated with preservatives (e.g., benzalkonium chloride) and protected from light. We provide long-term stability data.

How is the impurity mometasone (free alcohol) monitored during stability?

This primary hydrolysis product is specifically quantified using a stability-indicating HPLC method, ensuring it remains within pharmacopoeial limits.
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