Repositioning Candidate Details
| Candidate ID: | R0741 |
| Source ID: | DB05219 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Crisaborole |
| Synonyms: | Crisaborole |
| Molecular Formula: | C14H10BNO3 |
| SMILES: | OB1OCC2=C1C=CC(OC1=CC=C(C=C1)C#N)=C2 |
| Structure: |
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| DrugBank Description: | Crisaborole is a novel oxaborole approved by FDA on December 14, 2016 as Eucrisa, a topical treatment of for mild to moderate atopic dermatitis. This non-steroidal agent is efficacious in improving disease severity, reducing the risk of infection and reducing the signs and symptoms in patients 2 years old and older. It reduces the local inflammation in the skin and prevents further exacerbation of the disease with a good safety profile. Its structure contains a boron atom, which facilitates skin penetration and binding to the bimetal center of the phosphodiesterase 4 enzyme. It is currently under development as topical treatment of psoriasis. |
| CAS Number: | 906673-24-3 |
| Molecular Weight: | 251.05 |
| DrugBank Indication: | Intended for the topical treatment of mild to moderate atopic dermatitis in patients 2 years of age and older. |
| DrugBank Pharmacology: | Crisaborole has broad-spectrum anti-inflammatory activity by mainly targeting phosphodiesterase 4 (PDE4) enzyme that is a key regulator of inflammatory cytokine production. As this enzyme is expressed in keratinocytes and immune cells, crisaborole mediates an anti-inflammatory effect on almost all inflammatory cells. Topical application of this drug is useful as it potentiates the localization of this drug in the skin and this anti-inflammatory activity is in the low micromolar range. |
| DrugBank MoA: | Inhibition of PDE4 by crisaborole leads to elevated levels of cyclic adenosine monophosphate (cAMP). Increased intracellular levels of cAMP inhibit the NF-kB pathway and suppress the release of pro-inflammatory mediators such as TNF-alfa and various interleukins that play a causative role in psoriasis and atopic dermatitis. Suppression of downstream effects in different cell types may explain the therapeutic role of crisaborole in immune-mediated skin diseases. |
| Targets: | cAMP-specific 3',5'-cyclic phosphodiesterase 4A inhibitor; cAMP-specific 3',5'-cyclic phosphodiesterase 4B inhibitor; cAMP-specific 3',5'-cyclic phosphodiesterase 4C inhibitor; cAMP-specific 3',5'-cyclic phosphodiesterase 4D inhibitor |
| Inclusion Criteria: | Therapeutic strategy associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S05 | Anti-inflammatory | inflammatory | Bile acid; TNF-a inhibitor; Dual PPAR-α and -δ agonists; Toll-Like Receptor; (TLR)-4 antagonist; Caspase inhibitor; ASK-1 inhibitor | Ursodeoxycholic Acid; Pentoxifylline; Elafibranor; JKB-121; Emricasan; Selonsertib; | Details |
| Diseases ID | DO ID | Disease Name | Definition | Class |
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