Crisaborole topical

Crisaborole is a phosphodiesterase-4 (PDE-4) inhibitor, mainly acting on phosphodiesterase 4B (PDE4B), which causes inflammation. Chemically, Crisaborole is a phenoxybenzoxaborole. It contains a boron atom that helps penetrate the skin and is essential for its binding activity. Inhibition of PDE4B appears to suppress the release of tumor necrosis factor alpha (TNFα), interleukin-12 (IL-12), IL-23 and other cytokines, proteins believed to be involved in the immune response and inflammation. It is indicated for topical treatment of mild to moderate atopic dermatitis in pediatric patients 3 months of age and older.

• Mild to moderate atopic dermatitis (patients 3 months and older)

The active ingredient, Crisaborole, is a phosphodiesterase-4 (PDE-4) inhibitor, mainly acting on phosphodiesterase 4B (PDE4B), which causes inflammation. Chemically, Crisaborole is a phenoxybenzoxaborole. It contains a boron atom that helps penetrate the skin and is essential for its binding activity. Inhibition of PDE4B appears to suppress the release of tumor necrosis factor alpha (TNFα), interleukin-12 (IL-12), IL-23 and other cytokines, proteins believed to be involved in the immune response and inflammation.

Phosphodiesterase (PDE)-4 inhibitor; results in increased intracellular cyclic adenosine monophosphate (cAMP) levels. The specific mechanism by which crisaborole exerts its therapeutic action for atopic dermatitis is not well defined, although cAMP is thought to decrease the proinflammatory response (eg, cytokine release) associated with atopic dermatitis.

Adult Dose (Topical): Mild to moderate atopic dermatitis: Apply a thin layer to affected area(s) twice daily.

Pediatric Dose (>2 years): Apply a thin layer to affected area(s) twice daily.

Pediatric Dose (3 months-2 years): Apply a thin layer to affected area(s) twice daily.

Topical Administration: Apply thin layer of ointment to affected areas twice daily. Wash hands after applying ointment, unless hands are being treated. For topical use only; not for ophthalmic, oral, or intravaginal use.

If you miss a dose of Crisaborole, apply it as soon as you remember. However, if it is almost time for your next application, skip the missed dose. Do not double the dose.

Common Side Effects (1-10%): Application site pain, burning, or stinging (4%)

Rare Side Effects (<1%): Contact urticaria

Allergic Reactions: Severe pruritus, swelling, and erythema at the application site or at a distant site.

• Hypersensitivity reactions reported, including contact urticaria; signs and symptoms may include severe pruritus, swelling, and erythema at the application site or at a distant site. Discontinue immediately and initiate appropriate therapy if hypersensitivity suspected.
• For topical use only; not for ophthalmic, oral, or intravaginal use.

• History of hypersensitivity to crisaborole or any component of the formulation.

In vitro studies using human liver microsomes indicated that under the conditions of clinical use, Crisaborole and metabolite 1 are not expected to inhibit cytochrome P450 (CYP) 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A4. In vitro human liver microsomes studies for metabolite 2 showed that it did not inhibit activities of CYP2C19, 2D6, and 3A4.

No food interactions have been found or established.

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 3 and 2 times, respectively, the maximum recommended human dose (MRHD).

There is no information available on the presence of crisaborole in human milk. Crisaborole is systemically absorbed. The lack of clinical data during lactation precludes a clear determination of the risk of crisaborole to a breastfed infant.

Pediatric dose: 3 months and older: Apply a thin layer to affected area(s) twice daily. Safety and efficacy in children under 3 months have not been established.

Limited information is available regarding dose adjustment for elderly patients.

For topical use, no dose adjustment is required in renal or hepatic impairment.

Information on Crisaborole overdosage is not available.

Do not store above 30°C temperature. Keep away from light and out of reach of children.

Crisaborole