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Crisaborole

Class: Anti-inflammatory Agents
Chemical Name: 4-[(1-hydroxy-3H-2,1-benzoxaborol-5-yl)oxy]benzonitrile
Molecular Formula: C14H10BNO3
CAS Number: 1073669-75-6
Brands: Eucrisa

Introduction

Crisaborole is an anti-inflammatory agent.1

Uses for Crisaborole

Crisaborole has the following uses:

Crisaborole is a phosphodiesterase 4 inhibitor indicated for topical treatment of mild to moderate atopic dermatitis in patients 2 years of age and older.1

Crisaborole Dosage and Administration

General

Crisaborole is available in the following dosage form(s) and strength(s):

Ointment, 2%.1

Dosage

It is essential that the manufacturer's labeling be consulted for more detailed information on dosage and administration of this drug. Dosage summary:

  • Apply a thin layer twice daily to affected areas.1

  • For topical use only.1

  • Not for ophthalmic, oral, or intravaginal use.1

Cautions for Crisaborole

Contraindications

Known hypersensitivity to crisaborole or any component of the formulation.1

Warnings/Precautions

Hypersensitivity Reactions

Hypersensitivity reactions, including contact urticaria, have occurred in patients treated with crisaborole. Hypersensitivity should be suspected in the event of severe pruritus, swelling and erythema at the application site or at a distant site. If signs and symptoms of hypersensitivity occur, discontinue crisaborole immediately and initiate appropriate therapy.1

Specific Populations

Pregnancy

Risk Summary:There is no available data with crisaborole in pregnant women to inform the drug-associated risk for major birth defects and miscarriage. In animal reproduction studies, there were no adverse developmental effects 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)]. 1

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.1

Animal Data: Rat and rabbit embryofetal development was assessed after oral administration of crisaborole. Crisaborole did not cause adverse effects to the fetus at oral doses up to 300 mg/kg/day in pregnant rats during the period of organogenesis (5 times the MRHD on an AUC comparison basis). No treatment-related fetal malformations were noted after oral treatment with crisaborole in pregnant rats at doses up to 600 mg/kg/day (18 times the MRHD on an AUC comparison basis) during the period of organogenesis. Maternal toxicity was produced at the high dose of 600 mg/kg/day in pregnant rats and was associated with findings of decreased fetal body weight and delayed skeletal ossification. Crisaborole did not cause adverse effects to the fetus at oral doses up to the highest dose tested of 100 mg/kg/day in pregnant rabbits during the period of organogenesis (3 times the MRHD on an AUC comparison basis).1

In a prenatal/postnatal development study, pregnant rats were treated with crisaborole at doses of 150, 300, and 600 mg/kg/day by oral gavage during gestation and lactation (from gestation day 7 through day 20 of lactation). Crisaborole did not have any adverse effects on fetal development at doses up to 600 mg/kg/day (18 times the MRHD on an AUC comparison basis). Maternal toxicity was produced at the high dose of 600 mg/kg/day in pregnant rats and was associated with findings of stillbirths, pup mortality, and reduced pup weights. 1

Lactation

There is no information available on the presence of crisaborole 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 crisaborole to women who are breastfeeding. Crisaborole is systemically absorbed. The lack of clinical data during lactation precludes a clear determination of the risk of crisaborole to a breastfed infant. Therefore, the developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for crisaborole and any potential adverse effects on the breastfed infant from crisaborole or from the underlying maternal condition.1

Pediatric Use

The safety and effectiveness of crisaborole have been established in pediatric patients age 2 years and older for topical treatment of mild to moderate atopic dermatitis. Use of crisaborole 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 crisaborole in pediatric patients below the age of 2 years have not been established.1

Geriatric Use

Clinical studies of crisaborole did not include sufficient numbers of subjects age 65 and over to determine whether they respond differently from younger subjects.1

Common Adverse Effects

The most common adverse reaction occurring in ≥1% of subjects is application site pain.1

Drug Interactions

Specific Drugs

It is essential that the manufacturer's labeling be consulted for more detailed information on interactions with this drug, including possible dosage adjustments. Interaction highlights:

Please see product labeling for drug interaction information.

Actions

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 for the treatment of atopic dermatitis is not well defined.1

Advice to Patients

Advise the patient or caregivers to read the FDA-approved patient labeling (Patient Information).1

Hypersensitivity Reactions:

Advise patients to discontinue crisaborole and seek medical attention immediately if signs or symptoms of hypersensitivity occur.1

Administration Instructions:

Advise patients or caregivers that crisaborole is for external use only and is not for ophthalmic, oral, or intravaginal use. 1

Additional Information

AHFS First Release. For additional information until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the manufacturer's labeling be consulted for more detailed information on usual uses, dosage and administration, cautions, precautions, contraindications, potential drug interactions, laboratory test interferences, and acute toxicity.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Crisaborole

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Topical

Ointment

20 mg /1 g

Eucrisa

Anacor Pharmaceuticals Inc.

AHFS Drug Information. © Copyright 2017, Selected Revisions February 21, 2017. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

References

1. Anacor Pharmaceuticals, Inc.. Eucrisa (crisaborole) TOPICAL prescribing information. 2016 Dec.

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