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crisaborole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	5201	906673-24-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: staquis crisaborole AN2728 eucrisa	Crisaborole is a phosphodiesterase 4 (PDE-4) inhibitor. PDE-4 inhibition results in increased intracellular cyclic adenosine monophosphate (cAMP) levels. The specific mechanism(s) by which crisaborole exerts its therapeutic action for the treatment of atopic dermatitis is not well defined. Molecular weight: 251.05 Formula: C14H10BNO3 CLOGP: 2.63 LIPINSKI: 0 HAC: 4 HDO: 1 TPSA: 62.48 ALOGS: -4.03 ROTB: 2 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

staquis
crisaborole
AN2728
eucrisa

Crisaborole is a phosphodiesterase 4 (PDE-4) inhibitor. PDE-4 inhibition results in increased intracellular cyclic adenosine monophosphate (cAMP) levels. The specific mechanism(s) by which crisaborole exerts its therapeutic action for the treatment of atopic dermatitis is not well defined.

Molecular weight: 251.05
Formula: C14H10BNO3
CLOGP: 2.63
LIPINSKI: 0
HAC: 4
HDO: 1
TPSA: 62.48
ALOGS: -4.03
ROTB: 2

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	0.11 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
Dec. 14, 2016	FDA	ANACOR PHARMS INC
March 27, 2020	EMA	Pfizer Europe MA EEIG

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Application site pain	2060.51	42.08	332	3577	3850	63481263
Burning sensation	684.75	42.08	214	3695	54193	63430920
Dermatitis atopic	283.75	42.08	74	3835	9650	63475463
Application site erythema	248.51	42.08	58	3851	4777	63480336
Drug ineffective	181.31	42.08	266	3643	1044499	62440614
Skin burning sensation	154.70	42.08	49	3860	12685	63472428
Eczema	146.85	42.08	60	3849	32231	63452882
Application site pruritus	129.14	42.08	33	3876	3951	63481162
Drug effective for unapproved indication	119.59	42.08	30	3879	3334	63481779
Application site swelling	106.72	42.08	20	3889	558	63484555

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Application site pain	1121.75	106.77	171	1548	1737	34953475
Burning sensation	422.54	106.77	110	1609	18284	34936928
Drug ineffective	205.28	106.77	171	1548	456580	34498632
Dermatitis atopic	197.65	106.77	47	1672	5300	34949912
Application site erythema	171.40	106.77	36	1683	2300	34952912

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Application site pain	2029.31	59.89	328	4008	4419	79735633
Burning sensation	627.15	59.89	198	4138	58434	79681618
Drug ineffective	367.78	59.89	363	3973	1080550	78659502
Application site erythema	340.18	59.89	74	4262	5036	79735016
Dermatitis atopic	290.35	59.89	74	4262	9982	79730070
Off label use	182.06	59.89	233	4103	906982	78833070
Application site pruritus	170.92	59.89	40	4296	3770	79736282
Condition aggravated	154.35	59.89	161	4175	500963	79239089
Eczema	153.81	59.89	64	4272	40754	79699298
Pruritus	143.78	59.89	139	4197	394509	79345543

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	D11AH06	DERMATOLOGICALS OTHER DERMATOLOGICAL PREPARATIONS OTHER DERMATOLOGICAL PREPARATIONS Agents for dermatitis, excluding corticosteroids
CHEBI has role	CHEBI:35475	non-steroidal anti-inflammatory agent
CHEBI has role	CHEBI:50748	antipsoriatic drug
CHEBI has role	CHEBI:68844	phosphodiesterase IV inhibitors
FDA EPC	N0000182961	Phosphodiesterase 4 Inhibitor
FDA MoA	N0000182960	Phosphodiesterase 4 Inhibitors

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Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Atopic dermatitis	indication	24079001	DOID:3310

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.8	acidic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
2%	EUCRISA	ANACOR PHARMS INC	N207695	Dec. 14, 2016	RX	OINTMENT	TOPICAL	8501712	Feb. 16, 2027	METHOD OF TREATING MILD TO MODERATE ATOPIC DERMATITIS.
2%	EUCRISA	ANACOR PHARMS INC	N207695	Dec. 14, 2016	RX	OINTMENT	TOPICAL	9682092	Feb. 16, 2027	METHOD OF TREATING MILD TO MODERATE ATOPIC DERMATITIS.
2%	EUCRISA	ANACOR PHARMS INC	N207695	Dec. 14, 2016	RX	OINTMENT	TOPICAL	8168614	Jan. 20, 2030	METHOD OF TREATING MILD TO MODERATE ATOPIC DERMATITIS.

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
2%	EUCRISA	ANACOR PHARMS INC	N207695	Dec. 14, 2016	RX	OINTMENT	TOPICAL	March 23, 2023	NEW PATIENT POPULATION
2%	EUCRISA	ANACOR PHARMS INC	N207695	Dec. 14, 2016	RX	OINTMENT	TOPICAL	Sept. 23, 2023	PEDIATRIC EXCLUSIVITY

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Phosphodiesterase 4	Enzyme	P27815 Q07343 Q08493 Q08499	PDE4A_HUMAN PDE4B_HUMAN PDE4C_HUMAN PDE4D_HUMAN	INHIBITOR	IC50	6.31	SCIENTIFIC LITERATURE	DRUG LABEL
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A	Enzyme	P54750	PDE1A_HUMAN		IC50	5.21	CHEMBL
High affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A	Enzyme	Q13946	PDE7A_HUMAN		IC50	6.14	CHEMBL
Beta-lactamase	Enzyme		Q93LQ9_KLEPN		IC50	6.17	CHEMBL

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External reference:

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ID	Source
017053	NDDF
10024	INN_ID
1865953	RXNORM
248463	MMSL
32196	MMSL
4036360	VANDF
44591583	PUBCHEM_CID
724007009	SNOMEDCT_US
763593001	SNOMEDCT_US
9151	IUPHAR_LIGAND_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Eucrisa	HUMAN PRESCRIPTION DRUG LABEL	1	55724-211	OINTMENT	20 mg	TOPICAL	NDA	27 sections
Eucrisa	HUMAN PRESCRIPTION DRUG LABEL	1	55724-211	OINTMENT	20 mg	TOPICAL	NDA	27 sections
Staquis	HUMAN PRESCRIPTION DRUG LABEL	1	0009-2211	OINTMENT	20 mg	TOPICAL	EXPORT ONLY	1 sections
Staquis	HUMAN PRESCRIPTION DRUG LABEL	1	0009-2211	OINTMENT	20 mg	TOPICAL	EXPORT ONLY	1 sections

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