Crisaborole

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Crisaborole.svg
Systematic (IUPAC) name
(5-(4-Cyanophenoxy)-1-hydroxy-1,3-dihydro-2,1-benzoxaborole)
Clinical data
Legal status
  • Investigational New Drug
Routes of
administration		 Topical (ointment)
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
Molecular mass 251.045100 g/mol
  • B1(c2ccc(cc2CO1)Oc3ccc(cc3)C#N)O
  • InChI=1S/C14H10BNO3/c16-8-10-1-3-12(4-2-10)19-13-5-6-14-11(7-13)9-18-15(14)17/h1-7,17H,9H2
  • Key:USZAGAREISWJDP-UHFFFAOYSA-N

Crisaborole (INN,[1] USAN, codenamed AN2728) is a non-steroidal, topical 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]

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.[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]

Clinical trials

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

References

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  1. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  2. ↑ 2.0 2.1 Lua error in package.lua at line 80: module 'strict' not found.
  3. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  4. ↑ 4.0 4.1 4.2 4.3 4.4 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
  5. ↑ Lua error in package.lua at line 80: module 'strict' not found.
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