Tirbanibulin Monograph for Professionals - Drugs.com

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# Tirbanibulin

Brand name: Klisyri
Drug class: Skin and Mucous Membrane Agents, Miscellaneous
Chemical name: N-benzyl-2-[5-[4-(2-morpholin-4-ylethoxy)phenyl]pyridin-2-yl]acetamide
Molecular formula: C26H29N3O3
CAS number: 1038395-65-1

Medically reviewed by Drugs.com on Jan 2, 2023. Written by ASHP.

## Introduction

Tirbanibulin, a microtubule inhibitor, is a skin or mucous membrane agent.

## Uses for Tirbanibulin

### Tirbanibulin has the following uses:

Tirbanibulin is indicated for the topical treatment of actinic keratosis of the face or scalp.

## Tirbanibulin Dosage and Administration

### General

Tirbanibulin is available in the following dosage form(s) and strength(s):

Ointment: 1% tirbanibulin, single-dose packets.

### Dosage

It is essential that the manufacturer's labeling be consulted for more detailed information on dosage and administration of this drug. Dosage summary:

#### Adults

##### Dosage and Administration

- For topical use; not for oral or ophthalmic use.

- Apply tirbanibulin to the treatment field on the face or scalp once daily for 5 consecutive days using 1 single-dose packet per application.

Detailed Tirbanibulin topical dosage information

## Cautions for Tirbanibulin

### Contraindications

None.

### Warnings/Precautions

#### Ophthalmic Adverse Reactions

Tirbanibulin may cause eye irritation.

Avoid transfer of the drug into the eyes and to the periocular area during and after application. Wash hands immediately after application. If accidental exposure occurs, instruct patient to flush eyes with water and seek medical care as soon as possible.

#### Local Skin Reactions

Local skin reactions, including severe reactions (erythema, flaking/scaling, crusting, swelling, vesiculation/pustulation and erosion/ulceration) in the treated area can occur after topical application of tirbanibulin. Avoid use until skin is healed from any previous drug, procedure, or surgical treatment. Occlusion after topical application of tirbanibulin is more likely to result in irritation.

#### Specific Populations

##### Pregnancy

Risk Summary: There are no available data with tirbanibulin use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes.

In animal reproduction studies, oral administration of tirbanibulin to pregnant rats during the period of organogenesis resulted in an increased incidence of fetal deaths and malformations at a systemic exposure that was at least 74 times the exposure associated with the maximum recommended human dose (MRHD). Oral administration of tirbanibulin to pregnant rabbits during the period of organogenesis resulted in reduced mean fetal weight and size at a systemic exposure that was 159 times the exposure associated with the MRHD.

The background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively.

Animal Data: Tirbanibulin induced fetal deaths and external, visceral, and skeletal malformations when administered orally to pregnant rats during the period of organogenesis at doses greater than or equal to 1.25 mg/kg/day, which resulted in systemic exposures at least 74 times the exposure associated with the MRHD on an area under the curve (AUC) comparison basis. Tirbanibulin had no apparent effects on fetal development in rats at a dose of 0.5 mg/kg/day, which resulted in systemic exposures 18 times the exposure associated with the MRHD.

Tirbanibulin reduced mean fetal weight and size (crown-rump length) when administered orally to pregnant rabbits during the period of organogenesis at a dose of 3 mg/kg/day, which resulted in a systemic exposure 159 times the exposure associated with the MRHD on an AUC comparison basis. Tirbanibulin had no apparent effects on fetal development in rabbits at a dose of 1 mg/kg/day, which resulted in systemic exposures 53 times the exposure associated with the MRHD.

Tirbanibulin was assessed for effects on peri- and post-natal development of rats in a study that involved oral administration to pregnant rats during the period of organogenesis through lactation at dosages up to 1.25 mg/kg/day. These dosages resulted in systemic exposures up to 74 times the exposure associated with the MRHD on an AUC comparison basis. No adverse effects on maternal function or developmental, neurobehavioral, or reproductive performance of offspring were observed.

##### Lactation

There are no data on lactational transfer of tirbanibulin to human or animal milk. The effects of tirbanibulin on the breastfed infant, or its effects on milk production, are unknown.

The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for tirbanibulin and any potential adverse effects on the breastfed child from tirbanibulin or from the underlying maternal condition.

##### Pediatric Use

The safety and effectiveness of tirbanibulin for actinic keratosis in subjects less than 18 years of age have not been established. Actinic keratosis is not a condition generally seen within the pediatric population.

##### Geriatric Use

Of the 353 subjects with actinic keratosis treated with tirbanibulin in the 2 controlled phase 3 trials, 246 (70%) were 65 years of age or older. No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.

### Common Adverse Effects

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

## Drug Interactions

### Specific Drugs

It is essential that the manufacturer's labeling be consulted for more detailed information on interactions with this drug, including possible dosage adjustments. Interaction highlights:

Please see product labeling for drug interaction information.

## Actions

Tirbanibulin is a microtubule inhibitor. The mechanism of action of tirbanibulin for the topical treatment of actinic keratosis is 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.

- Advise 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 eyes, mouth and lips.

- Instruct patients to wash hands well after applying tirbanibulin to avoid transfer of the drug into the eyes and to the periocular area after application.

- 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.

## Additional Information

AHFSfirstRelease™. For additional information until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the manufacturer's labeling be consulted for more detailed information on usual uses, dosage and administration, cautions, precautions, contraindications, potential drug interactions, laboratory test interferences, and acute toxicity.

## 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.

Tirbanibulin
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer
--- | --- | --- | --- | ---
Topical | Ointment | 1% | Klisyri | Almirall LLC

AHFS Drug Information. © Copyright 2023, Selected Revisions January 11, 2021. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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## More about tirbanibulin topical

- Reviews (1)
- Side effects
- Dosage information
- During pregnancy
- Drug class: topical antineoplastics
- Breastfeeding
- En español

### Patient resources

- Drug Information
- Tirbanibulin Topical application (Advanced Reading)

### Professional resources

#### Other brands

Klisyri

### Related treatment guides

- Actinic Keratosis

Medical Disclaimer