Crisaborole

Summary

Crisaborole (CHEMBL484785) is an approved small-molecule phosphodiesterase IV inhibitor (ATC D11AH06) targeting PDE1A, PDE4B, and PDE7A; indicated across 7 conditions including atopic eczema and psoriasis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: D11AH06
• Targets: 3 (PDE1A, PDE4B, PDE7A)
• Indications: 7 conditions
• Clinical trials: 32
• Chemistry: 251.05 Da · C14H10BNO3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL484785
Name	Crisaborole
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	44591583
ChEBI	CHEBI:134677
ATC	D11AH06
Molecular formula	C14H10BNO3
Molecular weight	251.05
InChIKey	USZAGAREISWJDP-UHFFFAOYSA-N

SMILES: B1(C2=C(CO1)C=C(C=C2)OC3=CC=C(C=C3)C#N)O

IUPAC name: 4-[(1-hydroxy-3H-2,1-benzoxaborol-5-yl)oxy]benzonitrile

ChEBI definition: A member of the class of benzoxaboroles that is 5-hydroxy-1,3-dihydro-2,1-benzoxaborole in which the phenolic hydrogen has been replaced by a 4-cyanophenyl group. A phosphodiesterase 4 inhibitor that is used for treatment of mild to moderate atopic dermatitis in children and adults.

Pharmacological roles (ChEBI): phosphodiesterase IV inhibitor, antipsoriatic, non-steroidal anti-inflammatory drug.

Also known as: AN-2728, AN2728, Crisaborol, Crisaborole, Eucrisa, Staquis, SID174007043, CRISABOROLE, crisaborole

Patent coverage: 631 distinct patent families (1,482 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 1,198 (81%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
PDE1A	phosphodiesterase 1A	Inhibition	5.21	0%	P54750
PDE4B	phosphodiesterase 4B	Inhibition		0.2%	Q07343
PDE7A	phosphodiesterase 7A	Inhibition	6.14	1.1%	Q13946

Broader ChEMBL bioactivity targets: 11 (assay-derived). Sample: Phosphodiesterase 4, Phosphodiesterase 3, Muscarinic acetylcholine receptor M1, Alpha-1A adrenergic receptor, cGMP-inhibited 3’,5’-cyclic phosphodiesterase 3A, 3’,5’-cyclic-AMP phosphodiesterase 4A, 3’,5’-cyclic-AMP phosphodiesterase 4B, 3’,5’-cyclic-AMP phosphodiesterase 4D, 3’,5’-cyclic-AMP phosphodiesterase 4C, High affinity 3’,5’-cyclic-AMP phosphodiesterase 7A.

Bioactivity

ChEMBL activities: 19 potent at pChembl ≥ 5 of 22 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
PDE4D	7.26	IC50	55	nM	CHEMBL_ACT_18795050
PDE4C	7.26	IC50	55	nM	CHEMBL_ACT_18795051
PDE4B	7.26	IC50	55	nM	CHEMBL_ACT_18795052
PDE4B	7.26	IC50	55	nM	CHEMBL_ACT_18795053
PDE4A	7.26	IC50	55	nM	CHEMBL_ACT_18795054
PDE4B	7.24	IC50	57.2	nM	CHEMBL_ACT_23173735
PDE4A	6.96	IC50	110	nM	CHEMBL_ACT_2414894
PDE4B	6.96	IC50	110	nM	CHEMBL_ACT_24999656
PDE4D	6.77	IC50	170	nM	CHEMBL_ACT_29243152
PDE4A	6.47	AC50	336.7	nM	CHEMBL_ACT_25207264
PDE4A	6.31	IC50	490	nM	CHEMBL_ACT_22875409
PDE4A	6.31	IC50	490	nM	CHEMBL_ACT_2416747
PDE4D	6.31	IC50	490	nM	CHEMBL_ACT_24896949
PDE7A	6.14	IC50	730	nM	CHEMBL_ACT_2414892
PDE4D	6.1	AC50	800	nM	CHEMBL_ACT_25185388
PDE4D	5.94	IC50	1140	nM	CHEMBL_ACT_25899676
ADRA1A	5.37	AC50	4316	nM	CHEMBL_ACT_25219001
PDE1A	5.21	IC50	6100	nM	CHEMBL_ACT_2414898
PDE3B	5.19	IC50	6400	nM	CHEMBL_ACT_2414896

Target pathways

Aggregated over 3 target gene(s): PDE1A, PDE4B, PDE7A.

Top Reactome pathways

4 total, by targets touching each:

Pathway	Targets	Genes
G alpha (s) signalling events	2	PDE1A, PDE7A
Cam-PDE 1 activation	1	PDE1A
DARPP-32 events	1	PDE4B
cGMP effects	1	PDE1A

Dominant GO biological processes

GO term	Targets
signal transduction	3
negative regulation of cAMP/PKA signal transduction	3
cAMP catabolic process	2
regulation of smooth muscle cell apoptotic process	1
cGMP catabolic process	1
regulation of smooth muscle cell proliferation	1
neutrophil homeostasis	1
neutrophil chemotaxis	1
positive regulation of type II interferon production	1
positive regulation of interleukin-2 production	1
T cell receptor signaling pathway	1
leukocyte migration	1
cellular response to lipopolysaccharide	1
cellular response to xenobiotic stimulus	1
cellular response to epinephrine stimulus	1

Indications & clinical

Indications

7 indications (2 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
atopic eczema	4	MONDO:0004980	EFO:0000274
psoriasis	2	MONDO:0005083	EFO:0000676
localized scleroderma	2	MONDO:0019562	EFO:1001361
alopecia areata	2	MONDO:0005340	EFO:0004192
dermatitis	2	MONDO:0002406	MONDO:0002406
vitiligo	2	MONDO:0008661	EFO:0004208

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 32.

Phase distribution

Phase	Trials
PHASE4	10
PHASE2	9
PHASE3	6
Not specified	4
PHASE1	2
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07352566	PHASE4	NOT_YET_RECRUITING	Utilization of a Microdevice for Psoriasis and Atopic Dermatitis
NCT07437534	PHASE4	NOT_YET_RECRUITING	Comparative Evaluation of the Safety and Effectiveness of Crisaborole Ointment (2%) Versus Tacrolimus Ointment (0.1%) for the Topical Treatment of Atopic Dermatitis
NCT07438509	PHASE4	NOT_YET_RECRUITING	Efficacy of Crisaborole 2% Cream Versus Placebo in Mild to Moderate Atopic Eczema
NCT03539601	PHASE4	TERMINATED	A Study of Crisaborole Ointment 2%; Crisaborole Vehicle; TCS and TCI in Subjects Aged ≥ 2 Years, With Mild-moderate AD
NCT03567980	PHASE4	COMPLETED	A Proof of Concept Clinical Trial Evaluating the Safety and Efficacy of Eucrisa (Crisaborole) in Patients With Seborrheic Dermatitis
NCT03832010	PHASE4	COMPLETED	Steroid-reducing Effects of Crisaborole
NCT03868098	PHASE4	COMPLETED	Different Application Rates of Crisaborole Ointment 2% in Adults With Mild to Moderate Atopic Dermatitis
NCT04023084	PHASE4	COMPLETED	Response of Children With Atopic Dermatitis (Eczema) to Eucrisa
NCT04214197	PHASE4	UNKNOWN	Study of Crisaborole Ointment 2% in Mild to Moderate Atopic Dermatitis
NCT05200403	PHASE4	TERMINATED	Improvement In Scratch Behavior And Sleep In Patients With Atopic Dermatitis
NCT07162896	PHASE3	NOT_YET_RECRUITING	Crisaborole 2% Versus Tacrolimus 0.1% in Children With Mild to Moderate Atopic Dermatitis
NCT03645057	PHASE3	COMPLETED	ASPIRE: PROs & Caregiver Burden in Children With Atopic Dermatitis
NCT04040192	PHASE3	COMPLETED	A Study to Evaluate Long-Term Maintenance Treatment With Once Daily Crisaborole Ointment 2% in Pediatric and Adult Participants With Mild-to-Moderate Atopic Dermatitis
NCT04360187	PHASE3	COMPLETED	Crisaborole for Chinese and Japanese Subjects (≥2 Years of Age) With Mild to Moderate Atopic Dermatitis
NCT04498403	PHASE3	TERMINATED	A Study of the Long-Term Safety of Crisaborole Ointment, 2% in Japanese Pediatric and Adult Participants With Mild to Moderate Atopic Dermatitis
NCT05016284	PHASE3	WITHDRAWN	Comparison of JW-100 and EUCRISA for the Treatment of Atopic Dermatitis
NCT00755196	PHASE2	COMPLETED	Safety and Efficacy Study of A Novel Ointment to Treat Plaque Type Psoriasis
NCT00759161	PHASE2	COMPLETED	Safety and Efficacy Study of A Novel Ointment to Treat Plaque Type Psoriasis
NCT01029405	PHASE2	COMPLETED	Safety and Efficacy Study of a Novel Ointment to Treat Plaque Type Psoriasis
NCT03351114	PHASE2	COMPLETED	Pilot Study Evaluating the Efficacy of a Topical PDE4 Inhibitor for Morphea
NCT04091087	PHASE2	COMPLETED	Study Evaluating Efficacy and Safety of Crisaborole in Adults With Stasis Dermatitis
NCT04194814	PHASE2	COMPLETED	Skin bioMARkers for Atopic Eczema Therapy Evaluation
NCT04299503	PHASE2	WITHDRAWN	Topical Crisaborole in Patients with Alopecia Areata
NCT05298033	PHASE2	COMPLETED	Study of Efficacy, Safety and Tolerability of Crisaborole and PF-07038124 With and Without NBUVB in Vitiligo
NCT06118047	PHASE2	UNKNOWN	Crisaborole Ointment for Skin Toxicity Induced by Cetuximab
NCT01258088	PHASE1	COMPLETED	Safety Study of Ointment for the Treatment of Plaque-type Psoriasis
NCT03250663	PHASE1	COMPLETED	Eucrisa for Atopic Dermatitis
NCT04800185	EARLY_PHASE1	COMPLETED	Characterizing Skin Microbiome Change in Atopic Dermatitis
NCT07519174	Not specified	NOT_YET_RECRUITING	A Randomized Controlled Trial Comparing the Effectiveness and Safety of Topical Tacrolimus 0.03% Versus Crisaborole 2% in Patients With Mild to Moderate Atopic Dermatitis Over 8 Weeks
NCT03770858	Not specified	COMPLETED	Wearable Skin Sensors to Assess Nocturnal Scratch Behavior
NCT04008784	Not specified	COMPLETED	Improvement of Short Term Outcome of Mild to Moderate Atopic Dermatitis Using a Combination of Crisaborole and a Concomitant Topical Corticosteroid Over a 8 Week Period
NCT07537751	Not specified	COMPLETED	Crisaborole vs Fluticasone Propionate in Mild to Moderate Atopic Dermatitis

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

60 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
DIPYRIDAMOLE	ChEMBL + PubChem	Phase 4 (approved)	PDE1A, PDE4B, PDE7A
SILDENAFIL	ChEMBL + PubChem	Phase 4 (approved)	PDE1A, PDE4B, PDE7A
Tadalafil	ChEMBL + PubChem	Phase 4 (approved)	PDE1A, PDE4B, PDE7A
THEOPHYLLINE	ChEMBL + PubChem	Phase 4 (approved)	PDE1A, PDE4B, PDE7A
VARDENAFIL	ChEMBL + PubChem	Phase 4 (approved)	PDE1A, PDE4B, PDE7A
Milrinone	ChEMBL + PubChem	Phase 4 (approved)	PDE1A, PDE4B
PAPAVERINE	ChEMBL	Phase 3	PDE1A, PDE4B
ROLIPRAM	ChEMBL	Phase 2	PDE1A, PDE4B
ZAPRINAST	ChEMBL	Phase 2	PDE1A, PDE4B
NIMODIPINE	ChEMBL + PubChem	Phase 4 (approved)	PDE1A
APREMILAST	ChEMBL	Phase 4 (approved)	PDE4B
ENOXIMONE	ChEMBL	Phase 4 (approved)	PDE4B
ENSIFENTRINE	ChEMBL	Phase 4 (approved)	PDE4B
IBUDILAST	ChEMBL	Phase 4 (approved)	PDE4B
INAMRINONE	ChEMBL	Phase 4 (approved)	PDE4B
LOSARTAN	ChEMBL	Phase 4 (approved)	PDE4B
PENTOXIFYLLINE	ChEMBL	Phase 4 (approved)	PDE4B
ROFLUMILAST	ChEMBL	Phase 4 (approved)	PDE4B
VINPOCETINE	ChEMBL	Phase 4 (approved)	PDE1A
CILOMILAST	ChEMBL	Phase 3	PDE4B
MUFEMILAST	ChEMBL	Phase 3	PDE4B
TETOMILAST	ChEMBL	Phase 3	PDE4B
ZATOLMILAST	ChEMBL	Phase 3	PDE4B
ADIBENDAN	ChEMBL	Phase 2	PDE4B
AZD-6482	ChEMBL	Phase 2	PDE4B
BMS-911543	ChEMBL	Phase 2	PDE4B
BUFROLIN	ChEMBL	Phase 2	PDE1A
CARTAZOLATE	ChEMBL	Phase 2	PDE4B
CDC-801	ChEMBL	Phase 2	PDE4B
CILOSTAMIDE	ChEMBL	Phase 2	PDE1A
CIPAMFYLLINE	ChEMBL	Phase 2	PDE4B
DAXALIPRAM	ChEMBL	Phase 2	PDE4B
DENBUFYLLINE	ChEMBL	Phase 2	PDE4B
EDELINONTRINE	ChEMBL	Phase 2	PDE1A
ENPROFYLLINE	ChEMBL	Phase 2	PDE4B
ETAZOLATE	ChEMBL	Phase 2	PDE1A
FILAMINAST	ChEMBL	Phase 2	PDE4B
IDOXIFENE	ChEMBL	Phase 2	PDE1A
IDREBORMILAST	ChEMBL	Phase 2	PDE4B
IMAZODAN	ChEMBL	Phase 2	PDE4B
INDOLIDAN	ChEMBL	Phase 2	PDE4B
LIXAZINONE	ChEMBL	Phase 2	PDE4B
LOTAMILAST	ChEMBL	Phase 2	PDE4B
MK-0873	ChEMBL	Phase 2	PDE4B
NITRAQUAZONE	ChEMBL	Phase 2	PDE4B
ORISMILAST	ChEMBL	Phase 2	PDE4B
OXAGRELATE	ChEMBL	Phase 2	PDE1A
PELRINONE	ChEMBL	Phase 2	PDE4B
PICLAMILAST	ChEMBL	Phase 2	PDE4B
PUMAFENTRINE	ChEMBL	Phase 2	PDE4B
REVAMILAST	ChEMBL	Phase 2	PDE4B
STREPTONIGRIN	ChEMBL	Phase 2	PDE4B
TOCLADESINE	ChEMBL	Phase 2	PDE4B
TOFIMILAST	ChEMBL	Phase 2	PDE4B
TOVINONTRINE	ChEMBL	Phase 2	PDE1A
TRANIMILAST	ChEMBL	Phase 2	PDE4B
TREQUINSIN	ChEMBL	Phase 2	PDE4B
UK-500001	ChEMBL	Phase 2	PDE4B
ZARDAVERINE	ChEMBL	Phase 2	PDE4B
Cilostazol	PubChem	Approved	PDE1A