Tirbanibulin (Topical) (Monograph)

Brand name: Klisyri [Web]
Drug class: Skin and Mucous Membrane Agents, Miscellaneous

Medically reviewed by Drugs.com on Sep 28, 2023. Written by ASHP.

Introduction

Microtubule inhibitor; skin or mucous membrane agent.

Uses for Tirbanibulin (Topical)

Actinic keratosis

Indicated for topical treatment of actinic keratosis (AK) of the face or scalp.

Guidelines generally recommend tirbanibulin as an option for topical treatment of AK.

Tirbanibulin (Topical) Dosage and Administration

General

Dispensing and Administration Precautions

• After topical application of tirbanibulin, wash hands immediately with soap and water. Avoid application around the mouth and lips, and avoid transfer to the periocular area. Avoid washing or touching the treated area for approximately 8 hours after tirbanibulin application; after 8 hours, the area may be washed with mild soap.

• Avoid application until skin is healed from any prior drug, procedure, or surgery.

Administration

Topical Administration

Single-dose ointment packets for topical use only; not for oral or ophthalmic use.

Apply a sufficient amount evenly to cover up to a 25 cm² treatment field.

Dosage

Each 1% single-use ointment packet contains 2.5 mg of tirbanibulin in 250 mg.

Adults

Actinic keratosis

Topical

Apply sufficient amount to evenly cover up to 25 cm² treatment field on face or scalp once daily for 5 consecutive days.

Special Populations

Hepatic Impairment

No specific dosage recommendations at this time.

Renal Impairment

No specific dosage recommendations at this time.

Geriatric Use

No specific dosage recommendations at this time. No differences in safety or efficacy observed in geriatric patients; however, greater sensitivity cannot be ruled out.

Related/similar drugs

fluorouracil topical, Efudex, tirbanibulin topical, Carac, Tolak, Klisyri

Cautions for Tirbanibulin (Topical)

Contraindications

None.

Warnings/Precautions

Ophthalmic Adverse Reactions

May cause eye irritation.

Avoid transfer into the eyes and periocular area during and after application. Wash hands immediately after application. Flush eyes with water and seek medical care as soon as possible if accidental exposure occurs.

Local Skin Reactions

Local skin reactions, including severe reactions (erythema, flaking/scaling, crusting, swelling, vesiculation/pustulation and erosion/ulceration) may occur after topical application. Avoid use until skin is healed from any previous drug, procedure, or surgery. Irritation more likely if treatment area is occluded after topical application of tirbanibulin.

Specific Populations

Pregnancy

No available data on tirbanibulin use in pregnancy.

Animal data indicate potential fetal harm with increased systemic exposure of tirbanibulin.

Lactation

Not known whether tirbanibulin distributes into milk, affects milk production, or affects breast-fed infants.

Pediatric Use

Safety and efficacy not established.

Geriatric Use

Of 353 subjects with actinic keratosis treated with tirbanibulin in the Phase 3 trials, 70% were ≥65 years of age. No overall differences in safety or efficacy were observed between these subjects and younger adults; however, increased sensitivity of some older individuals cannot be ruled out.

Hepatic Impairment

Effects of hepatic impairment on pharmacokinetics of tirbanibulin not evaluated.

Renal Impairment

Effects of renal impairment on pharmacokinetics of tirbanibulin not evaluated.

Common Adverse Effects

Most common adverse reactions (incidence ≥2%): local skin reactions, application site pruritus, application site pain.

Drug Interactions

Formal drug interaction studies not conducted.

In vitro, principally metabolized by CYP3A4, and to a lesser extent, CYP2C8.

In vitro, no clinically meaningful effects on pharmacokinetics of drugs metabolized by CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, or CYP3A4, or drugs mediated by multidrug and toxin extrusion (MATE) transporter 1, MATE2-K, organic anion transporting polypeptide (OATP)1B1, OATP1B3, organic cation transporter (OCT)1, or OCT2.

Tirbanibulin (Topical) Pharmacokinetics

Absorption

Following topical application of a mean daily dose of 138 mg of tirbanibulin to a 25 cm² contiguous area of the balding scalp or face for 5 consecutive days, steady-state concentrations achieved within 72 hours.

Median time to achieve Cmax approximately 7 hours after application.

Low systemic exposure after 5 days of application; Cmax approximately 0.34 ng/mL ± 0.30 ng/mL and 0.18 ng/mL ± 0.10 ng/mL when applied to the face and scalp, respectively.

Distribution

Extent

Not known if present in human milk.

Plasma Protein Binding

88% bound.

Elimination

Metabolism

Primarily by CYP3A4, and to a lesser extent, CYP2C8.

Exposure to human hepatocytes in vitro generated KX2-5036 and KX2-5163, 2 pharmacologically inactive metabolites, and other unidentified metabolites.

Elimination Route

Method of excretion not fully explained.

Stability

Storage

Topical

Ointment

Store at 20–25°C; (excursions permitted between 15–30°C). Do not refrigerate or freeze.

Actions

Microtubule inhibitor; mechanism of action for the topical treatment of actinic keratosis unknown.

Advice to Patients

• Advise the patient to read the FDA-approved patient labeling and instructions for use. Discard the packet after a single use.

• Inform patients that tirbanibulin is not for ophthalmic use. Advise patients to avoid application around the eyes, and transfer of the drug into the eyes and to the periocular area. If accidental exposure occurs, advise patients to flush eyes with water and seek medical care.

• Inform patients that treatment with tirbanibulin may lead to local skin reactions.

• Advise patients that tirbanibulin is for topical use only. Advise patients to avoid application near and around the mouth and lips.

• Instruct patients to wash hands well after applying tirbanibulin.

• Instruct patients to avoid washing and touching the treated area for 8 hours after treatment. Following this time, patients may wash the area with a mild soap and water.

• Instruct patients to avoid inadvertent transfer of tirbanibulin to other areas, or to another person.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, 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.

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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