Crisaborole
 | |
| Systematic (IUPAC) name | |
|---|---|
|
(5-(4-Cyanophenoxy)-1-hydroxy-1,3-dihydro-2,1-benzoxaborole) | |
| Clinical data | |
| Routes of administration | Topical (ointment) |
| Legal status | |
| Legal status |
|
| Identifiers | |
| CAS Number | 906673-24-3 |
| PubChem | CID 44591583 |
| DrugBank | DB05219 |
| ChemSpider | 24701949 |
| UNII | Q2R47HGR7P |
| Synonyms | 4-[(1-hydroxy-1,3-dihydro-2,1-benzoxaborol-5-yl)oxy]benzonitrile |
| Chemical data | |
| Formula | C14H10BNO3 |
| Molar mass | 251.045100 g/mol |
| |
| |
Crisaborole (INN,[1] USAN, codenamed AN2728) is a non-steroidal boron-containing drug candidate that as of 2015 was under development by Anacor Pharmaceuticals for the topical treatment of psoriasis and atopic dermatitis (atopic eczema).[2][3][4] It is a phosphodiesterase-4 inhibitor, mainly acting on phosphodiesterase 4B (PDE4B).[4] Chemically, crisaborole is a phenoxybenoxaborole;[4] the boron atom is essential for its binding activity.[5] 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] As of 2015, Anacor was conducting a Phase III clinical trial for the treatment of mild-to-moderate atopic dermatitis,[2] and some Phase II trials had been completed for the treatment of psoriasis.[4]
See also
- Phosphodiesterase
- Tavaborole (trade name Kerydin) — a structurally related drug developed by Anacor, approved for the treatment of onychomycosis
References
- ↑ "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.
- 1 2 "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: 1236–1242. PMID 19876791.
- 1 2 3 4 5 Moustafa F, Feldman SR. A review of phosphodiesterase-inhibition and the potential role for phosphodiesterase 4-inhibitors in clinical dermatology. Dermatol Online J. 2014 May 16;20(5):22608. PMID 24852768
- ↑ Akama, T. (May 2008). "Structure-activity studies of AN2728 and AN2898, novel oxaborole compounds with anti- inflammatory activity" (PDF). International Investigative Dermatology Conference.