Indication:
HIGHLIGHTS OF PRESCRIBING INFORMATION
These highlights do not include all the information needed to use
EUCRISA safely and effectively. See full prescribing information for
EUCRISA.
EUCRISA (crisaborole) ointment, 2%, for topical use
Initial U.S. Approval: 2016
INDICATIONS AND USAGE
EUCRISA is a phosphodiesterase 4 inhibitor indicated for topical treatment of
mild to moderate atopic dermatitis in patients 2 years of age and older.
DRUG INNOVATION - NOVEL DRUG APPROVALS FOR 2016
No Drug Name Active Ingredient Approval Date FDA-Approved use
on Approval date
20. Eucrisa Crisaborole 12/14/2016
To treat mild to moderate ezema (atopic dermatitis) in
patients two years of age and older
Press release
Drug Trials Snapshot
Adverse Reaction:
ADVERSE REACTIONS
The most common adverse reaction occurring in =1% in subjects is
application site pain.
Contra-Indications:
CONTRAINDICATIONS
Known hypersensitivity to crisaborole or any component of the formulation.
WARNINGS AND PRECAUTIONS
Hypersensitivity reactions: If signs and symptoms of hypersensitivity occur,
discontinue EUCRISA immediately and initiate appropriate therapy.
Dosages/ Overdosage Etc:
INDICATIONS AND USAGE
EUCRISA is a phosphodiesterase 4 inhibitor indicated for topical treatment of
mild to moderate atopic dermatitis in patients 2 years of age and older.
DOSAGE AND ADMINISTRATION
Apply a thin layer twice daily to affected areas.
For topical use only.
Not for ophthalmic, oral, or intravaginal use.
DOSAGE FORMS AND STRENGTHS
Ointment, 2%.
Patient Information:
PATIENT COUNSELING INFORMATION
Advise the patient or caregivers to read the FDA-approved patient labeling (Patient
Information).
Hypersensitivity Reactions:
Advise patients to discontinue EUCRISA and seek medical attention immediately if signs or
symptoms of hypersensitivity occur
Administration Instructions:
Advise patients or caregivers that EUCRISA is for external use only and is not for
ophthalmic, oral, or intravaginal use.
Manufactured for:
Anacor Pharmaceuticals, Inc.
Palo Alto, CA 94303 USA
Issued: 12/2016
EUCRISA is a trademark of Anacor Pharmaceuticals, Inc.
© 2016 Anacor Pharmaceuticals, Inc.
Pharmacology/ Pharmacokinetics:
CLINICAL PHARMACOLOGY
1. Mechanism of Action
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
2. Pharmacokinetics
Absorption
The pharmacokinetics (PK) of EUCRISA were investigated in 33 pediatric
subjects 2 to 17 years of age with mild to moderate atopic dermatitis and
a mean ± SD body surface area involvement of 49 ± 20% (range 27% to 92%).
In this study, subjects applied approximately 3 mg/cm2 of EUCRISA ointment
(dose range was approximately 6 g to 30 g per application)
twice daily for 8 days.
Systemic concentrations of crisaborole were at steady state by Day 8.
Based on the ratios of AUC0-12 between Day 8 and Day 1, the mean
accumulation factor for crisaborole was 1.9.
Metabolism
Crisaborole is substantially metabolized into inactive metabolites. The major
metabolite 5-(4-cyanophenoxy)-2-hydroxyl benzylalcohol (metabolite 1),
is formed via hydrolysis;this metabolite is further metabolized into downstream
metabolites, among which 5-(4-cyanophenoxy)-2-hydroxyl benzoic acid
(metabolite 2), formed via oxidation, is also a major metabolite.
PK of metabolites 1 and 2 were assessed in the PK study described above
and the systemic concentrations were at or near steady state by Day 8.
Based on the ratios of AUC0-12 between Day 8 and Day 1, the mean
accumulation factors for metabolites 1 and 2 were 1.7 and 6.3, respectively.
Excretion
Renal excretion of metabolites is the major route of elimination.
Pregnancy and lactation:
USE IN SPECIFIC POPULATIONS
1. Pregnancy
Risk Summary
There is no available data with EUCRISA in pregnant women to inform the
drug-associated risk for major birth defects and miscarriage.
In animal reproduction studies, there were no adverse developmental effect
observed with oral administration of crisaborole in pregnant rats and rabbits
during organogenesis at doses up to 5 and 3 times, respectively, the
maximum recommended human dose (MRHD) .
The background risk of major birth defects and miscarriage for the indicated
population is unknown. All pregnancies carry some risk of birth defect, loss
or other adverse outcomes.
The background risk of major birth defects in the U.S. general population
is 2% to 4% and of miscarriage is 15% to 20% of clinically recognized pregnancies.
2. Lactation
Risk Summary
There is no information available on the presence of EUCRISA in human milk,
the effects of the drug on the breastfed infant, or the effects of the drug on milk
production after topical application of EUCRISA to women who are breastfeeding.
EUCRISA is systemically absorbed.
Therefore, the developmental and health benefits of breastfeeding should be
considered along with the mother’s clinical need for EUCRISA and any potential
adverse effects on the breastfed infant from EUCRISA or from the underlying
maternal condition.
3. Pediatric Use
The safety and effectiveness of EUCRISA have been established in pediatric
patients age 2 years and older for topical treatment of mild to moderate
atopic dermatitis
Use of EUCRISA in this age group is supported by evidence from two multicenter,
randomized,double-blind, parallel-group, vehicle-controlled 28-day trials which
included 1,313 pediatric subjects 2 years and older
The safety and effectiveness of EUCRISA in pediatric patients below the
age of 2 years have not been established.
4. Geriatric Use
Clinical studies of EUCRISA did not include sufficient numbers of subjects age 65 and over
to determine whether they respond differently from younger subjects.
Manufacturer Details