Class: Anti-inflammatory Agents, Miscellaneous
Chemical Name: Benzonitrile, 4-[(1,3-dihydro-1-hydroxy-2,1-benzoxaborol-5-yl)oxy]
Molecular Formula: 14H10BNO3
CAS Number: 906676-24-3
Anti-inflammatory agent; selective phosphodiesterase type 4 (PDE4) inhibitor.
Uses for Crisaborole
Topical treatment of mild to moderate atopic dermatitis (eczema) in adults and children ≥2 years of age.
Crisaborole Dosage and 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.
Children ≥2 years of age: Apply thin layer of 2% ointment to affected areas of skin twice daily.
Apply thin layer of 2% ointment to affected areas of skin twice daily.
No special population dosage recommendations.
Cautions for Crisaborole
Known hypersensitivity to crisaborole or any ingredient in the formulation.
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.
Data are inadequate regarding use of topical crisaborole in pregnant women.
Adverse embryofetal effects not observed in animal studies using oral crisaborole.
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.
Safety and efficacy not established in children <2 years of age.
Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.
Common Adverse Effects
Application site pain (burning, stinging).
Interactions for Crisaborole
Does not inhibit CYP isoenzyme 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, or 3A4; not expected to induce CYP isoenzymes.
Drug interactions not expected
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.
Reduction of pruritus occurs as early as 8 days after initiation of topical crisaborole.
Not known whether systemically absorbed crisaborole is distributed into human milk.
Plasma Protein Binding
Systemically absorbed drug is rapidly and extensively metabolized to inactive metabolites.
Systemically absorbed drug excreted principally in urine as inactive metabolites.
20–25°C (may be exposed to 15–30°C).
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, unlike other commercially available PDE4 inhibitors, is a boron-based benzoxaborole PDE4 inhibitor. The drug 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
Provide patient with a copy of the manufacturer's patient information with each prescription of the drug.
Advise patients that crisaborole should only be used as directed by a clinician.
Advise patients that crisaborole ointment is for external use only and that contact with the eyes should be avoided; importance of not using the drug orally or intravaginally.
Importance of washing hands immediately after applying crisaborole, unless the hands are being treated.
Advise patients to discontinue the drug and immediately contact a clinician if signs or symptoms of hypersensitivity (e.g., hives, itching, swelling, redness) occur.
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.
Importance of informing patients of other important precautionary information. (See Cautions.)
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.
AHFS DI Essentials™. © Copyright 2022, Selected Revisions May 21, 2018. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
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