Crisaborole

Crisaborole
Clinical data
Routes of
administration		 Topical (ointment)
Legal status
Legal status
  • Investigational New Drug
Identifiers
Synonyms 4-[(1-hydroxy-1,3-dihydro-2,1-benzoxaborol-5-yl)oxy]benzonitrile
CAS Number 906673-24-3
PubChem (CID) 44591583
DrugBank DB05219
ChemSpider 24701949
UNII Q2R47HGR7P
Chemical and physical data
Formula C14H10BNO3
Molar mass 251.045100 g/mol
3D model (Jmol) Interactive image

Crisaborole (INN,[1] USAN, codenamed AN2728) is a non-steroidal, topical drug candidate that as of 2016 is under development by Anacor Pharmaceuticals for the topical treatment of psoriasis and atopic dermatitis (atopic eczema).[2][3][4][5]

Mechanism of action

It is a phosphodiesterase-4 inhibitor, mainly acting on phosphodiesterase 4B (PDE4B), which causes inflammation.[4] Chemically, crisaborole is a phenoxybenoxaborole.[4] It contains a boron atom that helps penetrate the skin and is essential for its binding activity.[6] Inhibition of PDE4B appears to suppress the release of tumor necrosis factor alpha (TNFα), interleukin-12 (IL-12), IL-23 and other cytokines, proteins believed to be involved in the immune response and inflammation.[4]

Clinical trials

As of 2016, two Phase III clinical trials for the treatment of mild-to-moderate atopic dermatitis have been completed,[5] and some Phase II trials had been completed for the treatment of psoriasis.[4]

See also

References

  1. ↑ "WHO Drug Information, Vol. 29, No. 3, 2015. International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 74" (PDF). World Health Information. p. 391. Retrieved 26 April 2016.
  2. ↑ "Anacor Pharmaceuticals: Crisaborole". Anacor Pharmaceuticals, Inc. Retrieved 26 April 2016.
  3. ↑ Nazarian, R (2009). "AN-2728, a PDE4 inhibitor for the potential topical treatment of psoriasis and atopic dermatitis". Curr Opin Investig Drugs. 11 (11): 1236–1242. PMID 19876791.
  4. 1 2 3 4 5 Moustafa, F; Feldman, S. R. (2014). "A review of phosphodiesterase-inhibition and the potential role for phosphodiesterase 4-inhibitors in clinical dermatology". Dermatol Online J. 20 (5): 22608. PMID 24852768.
  5. 1 2 H. Spreitzer (16 August 2016). "Neue Wirkstoffe - Crisaborol". Österreichische Apothekerzeitung (in German) (17/2016).
  6. ↑ Akama, T. (May 2008). "Structure-activity studies of AN2728 and AN2898, novel oxaborole compounds with anti- inflammatory activity" (PDF). International Investigative Dermatology Conference.
This article is issued from Wikipedia - version of the 11/8/2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.