Sofpironium bromide

Sofpironium bromide, sold under the brand name Ecclock among others, is a medication used to treat hyperhidrosis (excessive sweating).[1] It is an anticholinergic and is applied to the skin.[1]

Sofpironium bromide
Clinical data
Trade namesEcclock, Sofdra
Other namesBBI-4000, BBI 4000
License data
Routes of
administration		Topical
ATC code
  • None
Legal status
Legal status
Identifiers
  • [(3R)-1-(2-Ethoxy-2-oxoethyl)-1-methylpyrrolidin-1-ium-3-yl] (2R)-2-cyclopentyl-2-hydroxy-2-phenylacetate bromide
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC22H32BrNO5
Molar mass470.404 g·mol−1
3D model (JSmol)
  • CCOC(=O)C[N+]1(CC[C@H](C1)OC(=O)[C@@](C2CCCC2)(C3=CC=CC=C3)O)C.[Br-]
  • 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
  • Key:FIAFMTCUJCWADZ-JOFREBOKSA-M

It was approved in Japan in 2020, for the treatment of primary axillary hyperhidrosis.[2][3][4] It was approved for medical use in the United States in June 2024.[1][5]

Medical uses

Sofpironium bromide is indicated for the treatment of primary axillary hyperhidrosis.[1]

Mechanism of action

Sofpironium bromide is an anticholinergic agent that reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands.[4] It is a retrometabolically-designed drug (or "soft drug") based on glycopyrronium bromide,[6][7] meaning it has been designed to exert the desired effects at the site of administration, after which it is quickly converted into an inactive non-toxic metabolite upon entering systemic circulation avoiding the typical anticholinergic side-effects caused by off-site action.

Society and culture

Brand names

Sofpironium bromide is the international nonproprietary name.[8]

It is marketed as Ecclock in Japan and as Sofdra in the US.

References
  1. "Sofdra (sofpironium) topical gel, 12.45%" (PDF). Archived (PDF) from the original on 20 June 2024. Retrieved 20 June 2024.
  2. Paik J (December 2020). "Sofpironium Bromide: First Approval". Drugs. 80 (18): 1981–1986. doi:10.1007/s40265-020-01438-1. PMID 33236266. S2CID 227155835.
  3. Gregoriou S, Campanati A, Rigopoulos D, Maria Offidani A, Stratigos A, Kontochristoulos G (May 2021). "Investigational topical anticholinergics in clinical development for the treatment of hyperhidrosis". Expert Opinion on Investigational Drugs. 30 (5): 479–482. doi:10.1080/13543784.2021.1900114. PMID 33691553. S2CID 232187568.
  4. Yokozeki H, Fujimoto T, Abe Y, Igarashi M, Ishikoh A, Omi T, et al. (March 2021). "A phase 3, multicenter, randomized, double-blind, vehicle-controlled, parallel-group study of 5% sofpironium bromide (BBI-4000) gel in Japanese patients with primary axillary hyperhidrosis". The Journal of Dermatology. 48 (3): 279–288. doi:10.1111/1346-8138.15668. PMC 7986147. PMID 33410265.
  5. "FDA Approves Sofdra topical gel" (Press release). Botanix Pharmaceuticals. 20 June 2024. Archived from the original on 20 June 2024. Retrieved 20 June 2024.
  6. Huang F, Brown CE, Wu WM, Juhász A, Ji F, Bodor N (October 2003). "Design, pharmacokinetic, and pharmacodynamic evaluation of a new class of soft anticholinergics". Pharmaceutical Research. 20 (10): 1681–9. doi:10.1023/a:1026160023030. PMID 14620526. S2CID 20657068.
  7. Ji F, Wu W, Dai X, Mori N, Wu J, Buchwald P, et al. (November 2005). "Synthesis and pharmacological effects of new, N-substituted soft anticholinergics based on glycopyrrolate". J. Pharm. Pharmacol. 57 (11): 1427–35. doi:10.1211/jpp.57.11.0008. PMID 16259775.
  8. World Health Organization (2017). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 77". WHO Drug Information. 31 (1). hdl:10665/330984.


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