Crisaborole (Topical) (Monograph)

Brand name: Eucrisa
Drug class: Phosphodiesterase-4 Inhibitors

Medically reviewed by Drugs.com on Feb 10, 2025. Written by ASHP.

Introduction

Anti-inflammatory agent; selective phosphodiesterase type 4 (PDE4) inhibitor.

Uses for Crisaborole (Topical)

Atopic Dermatitis

Topical treatment of mild to moderate atopic dermatitis (eczema) in adults and children ≥3 months of age.

Clinical practice guidelines recommend topical corticosteroids and other topical treatments (e.g., calcineurin inhibitors, crisaborole) in patients who fail to response to treatment with topical moisturizers alone.

Crisaborole (Topical) Dosage and Administration

Administration

Topical Administration

Apply topically as a 2% ointment.

For external use only. Do not administer orally, vaginally, or topically to the eye.

Apply evenly as a thin layer to affected areas of skin.

Wash hands after applying, unless hands are being treated.

Dosage

Pediatric Patients

Atopic Dermatitis

Topical

Children ≥3 months of age: Apply thin layer of 2% ointment to affected areas of skin twice daily. Consider reducing application frequency to once daily once clinical effect achieved.

Adults

Atopic Dermatitis

Topical

Apply thin layer of 2% ointment to affected areas of skin twice daily. Consider reducing application frequency to once daily once clinical effect achieved.

Special Populations

Hepatic Impairment

No dosage recommendations at this time.

Renal Impairment

No dosage recommendations at this time.

Geriatric Patients

No dosage recommendations at this time.

Cautions for Crisaborole (Topical)

Contraindications

• Known hypersensitivity to crisaborole or any ingredient in the formulation.

Warnings/Precautions

Hypersensitivity Reactions

Hypersensitivity reactions (e.g., urticaria) reported.

Suspect hypersensitivity if severe pruritus, swelling, and erythema occur at site of application or at distant site.

If signs and symptoms of hypersensitivity occur, discontinue immediately and initiate appropriate treatment.

Specific Populations

Pregnancy

Insufficient data regarding use of topical crisaborole in pregnant women.

Adverse embryofetal effects not observed in animal studies using oral crisaborole.

Lactation

Not known whether systemically absorbed crisaborole is distributed into human milk, affects human milk production, or affects breast-fed infants.

Consider benefits of breast-feeding and importance of the drug to the woman; also consider potential adverse effects on the breast-fed infant from the drug or underlying maternal condition.

Pediatric Use

Safety and efficacy not established in children <3 months of age.

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.

Hepatic Impairment

No formal pharmacokinetic studies to date.

Renal Impairment

No formal pharmacokinetic studies to date.

Common Adverse Effects

Most common adverse effect (≥1%) is application site pain (burning or stinging).

Drug Interactions

Crisaborole and initial metabolite do not inhibit CYP isoenzymes 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, or 3A4; not expected to induce CYP isoenzymes. Weak CYP1A2 and 2B6 inhibition and moderate CYP2C8 and 2C9 inhibition with subsequent metabolite.

Crisaborole and initial metabolite do not inhibit UGT isoenzymes 1A1, 1A4, 1A6, 1A9, 2B7, or 2B15. Weak UGT1A1 inhibition and moderate UGT1A9 inhibition with subsequent metabolite.

Crisaborole and initial metabolite do not inhibit P-glycoprotein (P-gp), organic anionic or cationic transporters, or breast cancer resistance protein (BCRP) at clinically relevant concentrations. At therapeutic concentrations, subsequent metabolite is expected to inhibit BCRP.

Specific Drugs

Crisaborole (Topical) Pharmacokinetics

Absorption

Bioavailability

Rapidly absorbed systemically following topical application to the skin.

Following topical application of crisaborole 2% ointment (approximately 3 mg/cm²) twice daily for 8 days in pediatric patients 2–17 years of age with atopic dermatitis, plasma concentrations of the drug were detectable in all patients. Mean peak plasma concentration was 127 ng/mL; steady-state plasma concentrations were attained by day 8. For pediatric patients 4 to <24 months of age, mean peak plasma concentration was 188 ng/mL.

Onset

Reduction of pruritus occurs as early as 8 days after initiation of topical crisaborole.

Distribution

Extent

Not known whether systemically absorbed crisaborole is distributed into human milk.

Plasma Protein Binding

97%.

Elimination

Metabolism

Systemically absorbed drug is rapidly and extensively metabolized to inactive metabolites.

Elimination Route

Systemically absorbed drug excreted principally in urine as inactive metabolites.

Stability

Storage

Topical

Ointment

20–25°C (may be exposed to 15–30°C); keep tube tightly closed.

Actions

• Boron-based benzoxaborole PDE4 inhibitor.

• PDE4 is a phosphodiesterase expressed in inflammatory cells associated with atopic dermatitis and is involved in metabolism of cyclic adenosine-3',5'-monophosphate (cAMP).

• Selective inhibition of PDE4 results in accumulation of intracellular cAMP, a modulator of inflammatory responses, which can downregulate inflammatory responses by inhibiting expression of inflammatory cytokines, thereby reducing inflammation in patients with atopic dermatitis.

• Crisaborole preferentially inhibits PDE4 and suppresses tumor necrosis factor (TNF; TNF-α), interleukin-2 (IL-2), interleukin-4 (IL-4), interleukin-5 (IL-5), interleukin-13 (IL-13), interleukin-17 (IL-17), interleukin-22 (IL-22), interleukin-23 (IL-23), and interferon-γ secretion from human leukocytes.

• Exact mechanism(s) of action of crisaborole in the management of atopic dermatitis not elucidated.

Advice to Patients

• Advise the patient or caregiver to read the FDA-approved patient labeling (Patient Information).

• Advise patients that crisaborole should only be used as directed by a clinician.

• Advise patients that crisaborole ointment is for external use only, that contact with the eyes should be avoided, and that the drug should not be used orally or intravaginally.

• Advise patients to discontinue the drug and immediately contact a clinician if signs or symptoms of hypersensitivity (e.g., hives, itching, swelling, redness) occur.

• Advise patients to inform their clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary and herbal supplements, as well as any concomitant illnesses.

• Advise patients to inform clinician if they are or plan to become pregnant or plan to breast-feed.

• Advise patients of other important precautionary information.

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

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.

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Frequently asked questions

• What are the most common skin conditions? (with photos)

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