Crisaborole

Phosphodiesterase 4 Inhibitor — DERMATOLOGICALS

Key facts

Crisaborole is an onp drug in the Phosphodiesterase 4 Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2016. Its mechanism of action is classified as Phosphodiesterase 4 Inhibitors. DrugCentral lists 4 molecular targets, including PDE4A|PDE4B|PDE4C|PDE4D, KPC-2 and PDE7A. Recorded indications include Atopic dermatitis.

• Approval status: onp (first approved 2016 by the FDA).
• Drug class: Phosphodiesterase 4 Inhibitor.
• Mechanism of action: Phosphodiesterase 4 Inhibitors.
• Molecular targets: PDE4A|PDE4B|PDE4C|PDE4D, KPC-2, PDE7A and PDE1A (4 listed in DrugCentral).
• Indications: Atopic dermatitis.
• ATC code: D11AH06 (Agents for dermatitis, excluding corticosteroids).
• Molecular formula: C14H10BNO3; molecular weight 251.05 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Atopic dermatitis

Mechanism & targets

• Mechanism of action (MoA): Phosphodiesterase 4 Inhibitors
• Established pharmacologic class: Phosphodiesterase 4 Inhibitor

Molecular targets (4)

Target	Gene	Action	Activity
Phosphodiesterase 4	PDE4A|PDE4B|PDE4C|PDE4D	inhibitor	IC50 6.31
Beta-lactamase	KPC-2	unknown	IC50 6.17
High affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A	PDE7A	unknown	IC50 6.14
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A	PDE1A	unknown	IC50 5.21

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2020-03-27	EMA	—	Pfizer Europe MA EEIG
2016-12-14	FDA	—	ANACOR PHARMS INC

ATC classification

ATC code	Therapeutic hierarchy
D11AH06	DERMATOLOGICALS › OTHER DERMATOLOGICAL PREPARATIONS › OTHER DERMATOLOGICAL PREPARATIONS › Agents for dermatitis, excluding corticosteroids

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Application site pain	4447.4
Burning sensation	1781.0
Dermatitis atopic	867.2
Drug ineffective	693.1
Application site erythema	507.7
Eczema	331.2
Drug effective for unapproved indication	297.6
Skin burning sensation	285.1
Pruritus	272.0
Pain	236.8
Dry skin	218.5
Condition aggravated	216.2

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Crisaborole is on its molecule page.

• Molecular formula: C₁₄H₁₀BNO₃
• Molecular weight: 251.05 g/mol
• CAS number: —
• InChIKey: USZAGAREISWJDP-UHFFFAOYSA-N
• PubChem CID: 44591583

OB1OCC2=CC(OC3=CC=C(C=C3)C#N)=CC=C12

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Crisaborole used for?

DrugCentral lists the following indications for Crisaborole: Atopic dermatitis.

How does Crisaborole work?

Crisaborole is classified as Phosphodiesterase 4 Inhibitors; its molecular targets in DrugCentral include PDE4A|PDE4B|PDE4C|PDE4D (inhibitor), KPC-2, PDE7A and PDE1A.

When was Crisaborole first approved?

Crisaborole was first approved by the FDA in 2016.

What drug class does Crisaborole belong to?

Crisaborole is in the Phosphodiesterase 4 Inhibitor class.

What is the chemical formula of Crisaborole?

Crisaborole has the molecular formula C14H10BNO3 and a molecular weight of 251.05 g/mol.

Sources

• DrugCentral drug card 5201 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL484785 — compound record and bioactivity
• PubChem CID 44591583 — chemical identifiers
• DrugBank DB05219 — drug record
• FDA UNII Q2R47HGR7P — substance identity
• DailyMed: FDA labels for Crisaborole — current prescribing information (label search)
• UniProt Q13946 (PDE7A) — target protein
• UniProt P54750 (PDE1A) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

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