|Chemical and physical data|
|Molar mass||251.045100 g/mol|
|3D model (Jmol)||Interactive image|
Crisaborole (INN, 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).
Mechanism of action
It is a phosphodiesterase-4 inhibitor, mainly acting on phosphodiesterase 4B (PDE4B), which causes inflammation. Chemically, crisaborole is a phenoxybenoxaborole. It contains a boron atom that helps penetrate the skin and is essential for its binding activity. 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.
- Tavaborole (trade name Kerydin) — a structurally related topical antifungal developed by Anacor
- "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.
- "Anacor Pharmaceuticals: Crisaborole". Anacor Pharmaceuticals, Inc. Retrieved 26 April 2016.
- 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.
- 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.
- H. Spreitzer (16 August 2016). "Neue Wirkstoffe - Crisaborol". Österreichische Apothekerzeitung (in German) (17/2016).
- Akama, T. (May 2008). "Structure-activity studies of AN2728 and AN2898, novel oxaborole compounds with anti- inflammatory activity" (PDF). International Investigative Dermatology Conference.