Mometasone (0.1-3 mg/kg; intranasal) reduces the enhanced airway sensitivity to aerosolized methacholine and suppresses mild allergic lung inflammation in a dosage-dependent manner at the highest dose tested, 3 mg/kg. Allergen-induced rise in Penh in murine mice [3].

Absorption, Distribution and Excretion
The nasal spray is virtually undetectable in plasma. Metabolism/Metabolites Hepatic metabolism. Extensively metabolized into multiple metabolites. No major metabolite was detected in plasma. One of the minor metabolites generated after in vitro incubation is 6-hydroxymometasone furoate. In human liver microsomes, the generation of this metabolite is regulated by cytochrome P-450 3A4. Biological Half-Life 5.8 hours

Effects During Pregnancy and Lactation
◉ Overview of Medication Use During Lactation There are currently no studies on the use of topical mometasone preparations or mometasone nasal implants during lactation. Since only large-area application of potent corticosteroids is likely to have systemic effects on the mother, short-term use of topical corticosteroids or sustained-release implants is unlikely to pose a risk to the nursing infant through breast milk. However, a precautionary approach is to use the least potent medication on the smallest possible area of skin. It is especially important to ensure that the infant's skin does not come into direct contact with the treated area. Current guidelines allow the application of topical corticosteroids to the nipples immediately after breastfeeding to treat eczema, and the nipples should be gently cleaned before breastfeeding. Only water-soluble creams or gels should be applied to the breasts, as ointments may expose the infant to high concentrations of mineral oil through licking.
◉ Effects on Breastfed Infants
A mother applied a topical corticosteroid (isofluprednisolone acetate) with high mineralocorticoid activity to her nipples, resulting in QT interval prolongation, Cushing's syndrome-like symptoms, severe hypertension, growth retardation, and electrolyte imbalance in her 2-month-old breastfed infant. The mother had been using the cream due to nipple pain since birth.
◉ Effects on Lactation and Breast Milk
No published information was found as of the revision date.
◉ Summary of Medication Use During Lactation
No studies have been conducted on inhaled mometasone or mometasone nasal implants during lactation. Although measurements were not performed, the amount of inhaled and nasal corticosteroids absorbed into the maternal bloodstream and secreted into breast milk is likely too small to affect breastfed infants. Expert opinion is that inhaled, nasal, and oral corticosteroids are safe to use during lactation. See also topical mometasone.
◉ Effects on breastfed infants
There are currently no reports on corticosteroids.
◉ Effects on lactation and breast milk
As of the revision date, no relevant published information was found.

---

Protein binding
98% to 99% (concentration range 5 to 500 ng/mL).

[1]. Long-term, intermittent treatment of chronic hand eczema with mometasone furoate. Br J Dermatol. 1999 May;140(5):882-6.

[2]. Mometasone or Tiotropium in Mild Asthma with a Low Sputum Eosinophil Level. N Engl J Med. 2019 May 23;380(21):2009-2019.

[3]. Synergistic effect of formoterol and mometasone in a mouse model of allergic lung inflammation. Br J Pharmacol. 2007 Sep;152(1):83-90.

Mometasone is an 11β-hydroxysteroid, 17α-hydroxysteroid, 20-oxosteroid, 3-oxo-Δ1,Δ4-steroid, chlorosteroid, and tertiary α-hydroxy ketone. It possesses anti-inflammatory, dermatological, vasoconstrictive, and anti-allergic effects. Its function is related to Δ1-progesterone. Mometasone is a corticosteroid and is no longer used in medical products. However, mometasone furoate continues to be used. Mometasone is a corticosteroid. Its mechanism of action is as a glucocorticoid receptor agonist. Mometasone is a synthetic, topical glucocorticoid receptor (GR) agonist with anti-inflammatory, antipruritic, and vasoconstrictive effects. After administration, mometasone binds to cytoplasmic GR, subsequently activating GR-mediated gene expression. This leads to the synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators. Specifically, mometasone appears to induce the expression of phospholipase A2 inhibitory protein, thereby controlling the release of the inflammatory precursor arachidonic acid from the phospholipase membrane. Mometasone is a pregnadiene glycol derivative with anti-allergic and anti-inflammatory effects, used to treat asthma and allergic rhinitis. It is also used as a topical treatment for skin conditions. See also: mometasone furoate (in salt form); mometasone furoate monohydrate (its active ingredient). Drug Indications This inhaler is indicated for the maintenance and preventative treatment of asthma. This nasal spray is indicated for the treatment of nasal symptoms in seasonal and perennial allergic rhinitis. Mechanism of Action Free corticosteroids can cross cell membranes and bind with high affinity to specific cytoplasmic receptors. Its mechanisms of action include: reducing the release of acidic hydrolases from leukocytes, preventing macrophage aggregation at inflammatory sites, interfering with leukocyte adhesion to capillary walls, reducing capillary membrane permeability, reducing complement components, inhibiting the release of histamine and kinins, and interfering with scar tissue formation, thereby alleviating inflammation. The anti-inflammatory effects of corticosteroids are believed to be related to lipocortin, a phospholipase A2 inhibitory protein that controls the biosynthesis of potent inflammatory mediators such as prostaglandins and leukotrienes. In vitro studies have shown that mometasone furoate has approximately 12 times the binding affinity to human glucocorticoid receptors as dexamethasone, 7 times as much as triamcinolone, 5 times as much as budesonide, and 1.5 times as much as fluticasone.

---

Pharmacodynamics
Mometasone is a moderately potent synthetic glucocorticoid with anti-inflammatory, antipruritic, and vasoconstrictive effects. Studies in asthma patients have shown that mometasone has a good ratio of local to systemic activity due to its predominantly local action, extensive hepatic metabolism, and lack of active metabolites. While glucocorticoids are effective in treating asthma, they do not provide immediate relief from symptoms. The maximum improvement in symptoms after inhaled mometasone furoate may take one to two weeks or longer to achieve. After discontinuing glucocorticoids, asthma may remain stable for several days or longer. In vitro studies have shown that mometasone has approximately 12 times the binding affinity to human glucocorticoid receptors as dexamethasone, 7 times as much as triamcinolone, 5 times as much as budesonide, and 1.5 times as much as fluticasone. The clinical significance of these findings is unclear.

C22H28O4CL2

427.36132

520.142

105102-22-5

Mometasone-d5

441335

White to off-white solid powder

1.35g/cm3

586.6ºC at 760mmHg

220ºC (decomposes)

308.5ºC

4.47E-18mmHg at 25°C

1.603

4.869

2

4

2

28

806

8

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)O)C)O)Cl)C

QLIIKPVHVRXHRI-CXSFZGCWSA-N

InChI=1S/C22H28Cl2O4/c1-12-8-16-15-5-4-13-9-14(25)6-7-19(13,2)21(15,24)17(26)10-20(16,3)22(12,28)18(27)11-23/h6-7,9,12,15-17,26,28H,4-5,8,10-11H2,1-3H3/t12-,15+,16+,17+,19+,20+,21+,22+/m1/s1

(8S,9R,10S,11S,13S,14S,16R,17R)-9-chloro-17-(2-chloroacetyl)-11,17-dihydroxy-10,13,16-trimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-3-one

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~125 mg/mL (~292.49 mM)

Solubility in Formulation 1: ≥ 2.08 mg/mL (4.87 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

---

Solubility in Formulation 2: ≥ 2.08 mg/mL (4.87 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

---

View More

Solubility in Formulation 3: ≥ 2.08 mg/mL (4.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

---

 (Please use freshly prepared in vivo formulations for optimal results.)