Tirbanibulin

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

• KLISYRI is indicated for the topical field treatment of actinic keratosis on the face or scalp. KLISYRI is a microtubule inhibitor indicated for the topical treatment of actinic keratosis of the face or scalp.

• None. None.contraindicated

For topical use only; not for oral or ophthalmic use. Apply KLISYRI evenly to cover up to 100 cm 2 treatment field on the face or balding scalp once daily for 5 consecutive days using 1 unit-dose packet per application. Wash hands immediately with soap and water after application. Avoid washing and touching the treated area for approximately 8 hours after application of KLISYRI. Following this time, the area may be washed with a mild soap. Avoid transfer of KLISYRI to the periocular area [see Warnings and Precautions ( 5.1 )] . Avoid application near and around the mouth and lips. For topical use; not for oral or ophthalmic use. ( 2 ) Apply KLISYRI to the treatment field on the face or scalp once daily for 5 consecutive days using 1 unit-dose packet per application. ( 2 )

Ophthalmic Adverse Reactions: May cause eye irritation upon ocular exposure. Avoid transfer of the drug into the eyes and to the periocular area. If accidental exposure occurs, flush eyes with water and seek medical care. ( 5.1 ) Local Skin Reactions: Local skin reactions can occur including severe reactions (e.g., vesiculation/pustulation, erosion/ulceration) in the treated area. Avoid use until skin is healed from any previous drug or surgical treatment. ( 5.2 ) 5.1 Ophthalmic Adverse Reactions KLISYRI 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. 5.2 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 KLISYRI [see Adverse Reactions ( 6.1 )] . Occlusion after topical application of KLISYRI is more likely to result in irritation. Avoid use until skin is healed from any previous drug, procedure, or surgical treatment.

Most common adverse reactions (incidence ≥2%) are local skin reactions, application site pruritus, and application site pain. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Almirall, at 1-866-665-2782 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. Two double-blind, vehicle-controlled clinical trials were conducted in 702 adult subjects with actinic keratosis on the face or scalp. Subjects were randomized 1:1 to KLISYRI or vehicle. Subjects enrolled in the trials had 4 to 8 clinically typical, visible, and discrete AK lesions in a contiguous area of 25 cm 2 on the face or scalp. Subjects’ average age was 70 years (range 45 to 96 years) and they were predominantly White (99%), male (87%), with Fitzpatrick skin types I or II (72%) and actinic keratosis on the face (68%) or scalp (32%). Treatment groups were comparable across all demographics and baseline characteristics, including AK lesion count and distribution on the face or scalp. In the controlled trials, local skin reactions (LSRs) were collected independent of adverse events.

8.1 Pregnancy Risk Summary There are no available data with KLISYRI 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 19 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 41 times the exposure associated with the MRHD ( see Data ). 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.

Metabolism

Absorption Following topical treatment of a mean daily dose of 348 mg (range: 224 to 435 mg) of KLISYRI to a 100 cm 2 contiguous area of the face or balding scalp, once daily for 5 consecutive days. On Day 5, systemic exposure to tirbanibulin had a mean±SD maximum plasma concentration (C max ) of 1.32±0.74 ng/mL and 0.71±0.31 ng/mL, and a mean±SD area under the plasma concentration from time zero to 24 hours (AUC 24 ) of 19.6±8.1 h∗ng/mL and 11.7±4.4 h∗ng/mL, in subjects who received the face and scalp topical treatment, respectively.

• Dec 14, 2020NDANDA213189Almirall

1. 1Drug Ineffective4620%
2. 2Application Site Erythema3415%
3. 3Erythema239.9%
4. 4Drug Intolerance208.6%
5. 5Adverse Drug Reaction177.3%
6. 6Application Site Exfoliation177.3%
7. 7Application Site Vesicles166.9%
8. 8Application Site Pain135.6%
9. 9Off Label Use135.6%
10. 10Pruritus125.2%
11. 11Application Site Dryness104.3%
12. 12Application Site Pruritus104.3%
13. 13Blister93.9%
14. 14Burning Sensation83.4%
15. 15Skin Burning Sensation83.4%

The 10 most recently updated of 19 ClinicalTrials.gov registrations naming Tirbanibulin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Efficacy and Safety of Cryotherapy Followed by Tirbanibulin Ointment for Actinic Keratosis on the Scalp and Forehead
  Not yet recruiting · Phase 3 · Interventional · 59 enrolled · University Hospital, Lille
  NCT07273656updated 2026-05-22
• Tirbanibulin for Pediatric Warts
  Recruiting · Phase 4 · Interventional · 10 enrolled · The Skin Center Dermatology Group
  NCT06791525updated 2026-04-23
• A Study to Evaluate the Efficacy and Safety of Tirbanibulin Ointment in Adult Participants With Actinic Keratosis
  Completed · Phase 3 · Interventional · 280 enrolled · Almirall, S.A.
  NCT06135415updated 2026-03-25
• Treating Basal and Squamous Cell Carcinomas With Fractional Laser and Tirbanibulin Ointment
  Recruiting · Phase 1 · Phase 2 · Interventional · 100 enrolled · Bruce Robinson, MD
  NCT07010692updated 2025-09-17
• Investigation of the Efficacy and Tolerability of Topical Applied Tirbanibulin on Actinic Keratoses With Downward-directed Proliferation Patterns
  Recruiting · Observational · 20 enrolled · Thomas Dirschka
  NCT06648447updated 2025-07-09
• KX01 Ointment Phase 1 Study in Patients With Plaque Type Psoriasis
  Completed · Phase 1 · Interventional · 28 enrolled · PharmaEssentia
  NCT05522816updated 2025-07-02
• A Study of Tirbanibulin on the Wellbeing of Participants With Actinic Keratoses
  Completed · Phase 4 · Interventional · 334 enrolled · Almirall, S.A.
  NCT05741294updated 2025-02-20
• A Study of Tirbanibulin Ointment and Diclofenac Sodium Gel for the Treatment of Adult Participants With Actinic Keratosis on the Face or Scalp
  Active not recruiting · Phase 4 · Interventional · 447 enrolled · Almirall, S.A.
  NCT05387525updated 2025-02-11
• Patient and Clinician Reported Outcomes for Tirbanibulin Effectiveness and Safety in Actinic Keratosis
  Completed · Observational · 300 enrolled · Almirall, S.A.
  NCT05260073updated 2024-09-20
• Proof of Concept Study to Access Superficial Basal Cell Carcinoma in Adults
  Completed · Phase 2 · Interventional · 5 enrolled · Austin Institute for Clinical Research
  NCT05713760updated 2024-07-19

Frequently asked questions

How does Tirbanibulin work?

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

What is Tirbanibulin used for?

According to FDA labeling, Tirbanibulin carries indications including: KLISYRI is indicated for the topical field treatment of actinic keratosis on the face or scalp. KLISYRI is a microtubule inhibitor indicated for the topical treatment of actinic keratosis of the face or scalp.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Tirbanibulin?

Tirbanibulin is classified as Other chemotherapeutics, Microtubule Inhibitor, Microtubule Inhibition.

What are the brand names for Tirbanibulin?

Tirbanibulin is marketed under brand names including Klisyri.

What are the contraindications for Tirbanibulin?

Tirbanibulin labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.