Eucrisa (crisaborole)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Crisaborole, a selective phosphodiesterase type 4 (PDE4) inhibitor, is an anti-inflammatory agent.
Crisaborole, a selective phosphodiesterase type 4 (PDE4) inhibitor, is an anti-inflammatory agent. PDE4 is a phosphodiesterase expressed in inflammatory cells associated with atopic dermatitis and is involved in the 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.
Unlike other commercially available PDE4 inhibitors, crisaborole is a boron-based benzoxaborole PDE4 inhibitor. The drug preferentially inhibits PDE4 and suppresses tumor necrosis factor (TNF; TNF-alpha), 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-gamma secretion from human leukocytes. The exact mechanism(s) of action of crisaborole in the management of atopic dermatitis has not been fully elucidated.
Crisaborole is rapidly absorbed systemically following topical application to the skin. In a study in pediatric patients 2-17 years of age with mild to moderate atopic dermatitis involving 27-92% of body surface area, topical application of 3 mg/cm2 of crisaborole 2% ointment to lesions twice daily for 8 days resulted in detectable plasma concentrations of the drug in all patients. The mean peak plasma concentration of crisaborole in these patients was 127 ng/mL and steady-state plasma concentrations of the drug were attained by day 8.
In a study in pediatric patients 4 months to <24 months of age, the mean peak plasma concentration of crisaborole was 188 ng/mL. Crisaborole is 97% bound to human plasma protein based on an in vitro study. Following systemic absorption, crisaborole is rapidly and extensively metabolized to inactive metabolites.
The drug is initially converted to 5-(4-cyanophenoxy)-2-hydroxyl benzylalcohol (metabolite 1) by hydrolysis and then further metabolized by oxidation to 5-(4-cyanophenoxy)-2-hydroxyl benzoic acid (metabolite 2). Systemically absorbed crisaborole is excreted principally in the urine as the inactive metabolites.
USES: This medication is used to treat eczema. It reduces swelling, redness, and itching on the skin.
Generic name: crisaborole
Pronunciation: (KRIS-a-BOR-ole)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Eucrisa
Indications
The following indications are listed for Eucrisa:
- Atopic Dermatitis
Also known as: Atopic Eczema, Disseminated Neurodermatitis.
Dosing
No dosing information is available for this tab.
Crisaborole is applied topically to the skin as a 2% ointment.
Crisaborole ointment is for external use only and should not be used orally, ophthalmically, or vaginally; contact with the eyes should be avoided.
A thin layer of crisaborole ointment should be applied to affected areas of skin.
Hands should be washed after applying the ointment, unless the hands are being treated.
Keep the tube of ointment tightly closed when not in use. Store at 20-25oC.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
In vitro studies indicate that crisaborole and its initial metabolite are not expected to inhibit cytochrome P-450 (CYP) isoenzymes 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, or 3A4. In vitro studies also indicate that the subsequent metabolite does not inhibit CYP2C19, 2D6, or 3A4, but is a weak inhibitor of CYP1A2 and 2B6 and a moderate inhibitor of CYP2C8 and 2C9. Crisaborole and its metabolites are not expected to induce CYP isoenzymes.
In vitro studies indicate that crisaborole and its initial metabolite do not inhibit uridine disphosphate (UDP)-glucuronosyltransferase (UGT) isoenzymes 1A1, 1A4, 1A6, 1A9, 2B7, or 2B15. In vitro studies also indicate that the subsequent metabolite does not inhibit UGT1A4, 1A6, 2B7, or 2B15, but is a weak inhibitor of UGT1A1 and a moderate inhibitor of UGT1A9.
In vitro studies indicate that crisaborole and its metabolites are not expected to have clinically significant interactions with P-glycoprotein substrates and organic anionic or cationic transporters. In vitro studies also indicate that crisaborole and its initial metabolite are not expected to inhibit breast cancer resistance protein (BCRP), but its subsequent metabolite is expected to inhibit BCRP at therapeutic concentrations.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity to crisaborole or any ingredient in the formulation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects occurring in >=1% of patients receiving topical crisaborole for the treatment of atopic dermatitis include application site pain (burning or stinging).
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of topical crisaborole have not been established in pediatric patients younger than 3 months of age.
Safety and efficacy of crisaborole for the topical treatment of mild to moderate atopic dermatitis in pediatric patients 3 months of age and older is supported by evidence from 2 multicenter, randomized, double-blind, parallel-group, vehicle-controlled trials that included 1313 pediatric patients 2-17 years of age, a safety and pharmacokinetics trial that included 137 pediatric patients 3 months to <2 years of age, and another clinical trial with an open-label period of up to 8 weeks that included 327 pediatric patients 5 months to <18 years of age.
Data are inadequate regarding the use of topical crisaborole in pregnant women.
Animal reproduction studies with oral crisaborole have not revealed evidence of fetal harm at exposures greater than those attained with the maximum recommended human topical dosage.
It is not known whether systemically absorbed crisaborole is distributed into human milk, affects human milk production, or affects breast-fed infants.
The benefits of breast-feeding and the importance of topical crisaborole to the woman should be considered along with potential adverse effects on the breast-fed infant from the drug or from the underlying maternal condition.
The manufacturer makes no specific dosage recommendations for geriatric patients.
Clinical studies of topical crisaborole did not include sufficient numbers of patients 65 years of age and older to determine whether geriatric patients respond differently than younger patients.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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