mAChR3/4/5

In addition to undergoing oxidative metabolism through CYP2D6 and CYP3A4, sopironium bromide is mostly metabolized by non-enzymatic hydrolysis [1].

By reducing the contractile activity of guinea pig ileal tissue in a concentration-dependent manner, sofpironium bromide demonstrates anticholinergic action. In a rat model, solopidium bromide decreased footpad sweating caused by the muscarinic receptor agonist pilocarpine [1].

Important Safety Information
Sofdra is for external use only under the skin. Wash your hands immediately after applying Sofdra. Do not touch your armpits after applying Sofdra. Sofdra is flammable. Keep away from heat and open flames when applying Sofdra.
Who should not use Sofdra?
Do not use Sofdra if you have certain conditions that may be exacerbated by taking anticholinergic drugs, such as glaucoma, severe ulcerative colitis (UC) or certain other serious bowel problems associated with severe UC, myasthenia gravis, and Sjögren's syndrome.
What information should I tell my healthcare provider before using Sofdra?
• Inform your healthcare provider about all your health conditions, including bladder or kidney problems, difficulty urinating, whether you are pregnant or breastfeeding, or planning to become pregnant or breastfeed. It is currently unknown whether Sofdra will harm the fetus or pass into breast milk. • Inform your healthcare provider about all medications you are taking, including prescription and over-the-counter drugs, especially any anticholinergic drugs. What are the possible side effects of Sofdra? Serious side effects may include: • Blurred vision. If you experience blurred vision, stop using Sofdra immediately and contact your healthcare provider. Do not drive, operate machinery, or engage in hazardous work until your vision is clear. • New or worsening urinary retention. If you experience difficulty urinating, frequent urination, weak or dribbling urine, a full bladder, or difficulty urinating, stop using Sofdra immediately and contact your healthcare provider. The most common side effects of Sofdra include dry mouth; blurred vision; pain, redness, swelling, itching, and irritation under the armpits; dilated pupils (mydriasis); and difficulty urinating. These are not all possible side effects of Sofdra. For medical advice regarding side effects, consult your doctor. https://www.cliniexpert.com/article/983.html

[1]. Sofpironium Bromide: First Approval. Drugs. 2020 Dec;80(18):1981-1986.

Sofosfoam bromide is a small molecule drug currently in Phase IV clinical trials and was first approved in 2024 for the treatment of hyperhidrosis. The U.S. Food and Drug Administration (FDA) has approved 12.45% sofosfoam bromide topical gel (Sofdra; Botanix) for the treatment of primary axillary hyperhidrosis in adults and children aged 9 years and older. It is estimated that approximately 10 million people in the United States suffer from hyperhidrosis, characterized by abnormally excessive sweating that exceeds the amount needed to regulate body temperature. The press release notes that this disproportionate sweating can have a profound impact on quality of life, including work productivity, daily activities, emotional health, and interpersonal relationships. It is the third most common skin condition after acne and atopic dermatitis. “We are very pleased to provide a new treatment option for the 10 million people in the United States suffering from primary axillary hyperhidrosis,” said Vince Ippolito, Executive Chairman of Botanix, in a press release. "As the first and currently only new chemical entity, Sofdra represents a novel treatment option for dermatologists to treat this disabling condition." This approval is based on the results of two pivotal Phase 3 CARDIGAN trials evaluating the safety and efficacy of sofosfoam bromide compared to excipients. The CARDIGAN I study enrolled 350 participants who were randomly assigned to either once-daily application of 15% sofosfoam bromide gel or once-daily application of the excipient gel. The primary efficacy endpoints were: the number of participants with a ≥2-point improvement in the total score of the seven items on the Hyperhidrosis Disease Severity Scale (HDSM-Ax) from baseline, and the change in weighted sweat secretion (GSP) from baseline. Enrolled participants were required to be at least 9 years old, diagnosed with primary axillary hyperhidrosis with symptoms lasting at least 6 months, an HDSM-Ax score of 3 or 4, a minimum bilateral axillary GSP of 50 mg, and a total bilateral axillary GSP of at least 150 mg. The CARDIGAN I and II studies enrolled a total of 701 patients. In both trials, sopirome bromide treatment met all primary and secondary endpoints, with clinically and statistically significant improvements in HDSM-Ax 7 and GSP scores from baseline. Botanix plans to launch a patient experience program in the third quarter of fiscal year 2024 to ensure eligible patients receive treatment as early as possible. These patients will become the first commercial users of sopirome bromide, guided by telemedicine and Medicare reimbursement processes, with full availability expected in early fourth quarter. “The approval of sopirome bromide is exciting news for the hyperhidrosis community, who have long suffered from a lack of effective and convenient treatment options,” said Dr. David Pariser, a founding member of the International Hyperhidrosis Society and former president of the American Academy of Dermatology, in a press release. "The emergence of a new topical treatment regimen is exciting; it is well-tolerated, highly effective, and easy to use, and is expected to be welcomed by patients and doctors alike."
Primary hyperhidrosis is caused by abnormal nerve signals triggering overactivity of eccrine sweat glands, typically affecting the palms, soles, and armpits, and sometimes the face. It has no definitive cause but may have a familial tendency. Secondary hyperhidrosis is caused by underlying diseases or certain medications and can lead to sweating all over the body. According to the Mayo Clinic, diabetes, menopause, thyroid disease, certain types of cancer, neurological disorders, and infections can all cause secondary hyperhidrosis.
https://www.pharmacytimes.com/view/fda-approves-sofpironium-first-treatment-for-primary-axillary-hyperhidrosis

C22H32BRNO5

470.397186279297

469.146

C, 56.17; H, 6.86; Br, 16.99; N, 2.98; O, 17.01

1628106-94-4

1628251-49-9 (cation);1628106-94-4 (bromide); 2409055-48-5

86301316

White to off-white solid powder

1

6

9

29

555

2

[Br-].O(C([C@](C1C=CC=CC=1)(C1CCCC1)O)=O)[C@@H]1CC[N+](C)(CC(=O)OCC)C1

FIAFMTCUJCWADZ-JOFREBOKSA-M

InChI=1S/C22H32NO5.BrH/c1-3-27-20(24)16-23(2)14-13-19(15-23)28-21(25)22(26,18-11-7-8-12-18)17-9-5-4-6-10-17;/h4-6,9-10,18-19,26H,3,7-8,11-16H2,1-2H3;1H/q+1;/p-1/t19-,22+,23?;/m1./s1

3-((R)-2-cyclopentyl-2-hydroxy-2-phenylacetoxy)-1-(2-ethoxy-2-oxoethyl)-1-methylpyrrolidin-1-ium bromide

BBI4000; Ecclock; 1628106-94-4; Sofdra; BBI-4000; Sofpironium bromide [USAN];BBI-4000; Sofpironium bromide

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

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

DMSO : ~100 mg/mL (~212.59 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.31 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 25.0 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.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (5.31 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 25.0 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.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (5.31 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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