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Tirbanibulin

Generic Name
Tirbanibulin
Brand Names
Klisyri
Drug Type
Small Molecule
Chemical Formula
C26H29N3O3
CAS Number
897016-82-9
Unique Ingredient Identifier
4V9848RS5G

Overview

Tirbanibulin (KX-O1 or KX2–391) is a dual inhibitor of Src Kinase and tubulin. On December 14, 2020, tirbanibulin was approved by the FDA for the topical treatment of actinic keratosis on the face or scalp. It is marketed under the brand name Klisyri. Actinic keratosis is a chronic condition characterized by lesions, which can potentially transform into invasive squamous cell carcinoma with a risk of 1% over 10 years. Tirbanibulin blocks the molecular pathways that promote the proliferation, survival, and metastasis of malignant cells. Tirbanibulin exhibits antitumour effects in vitro and in vivo and has been investigated for its antitumor efficacy in the management of various cancers, such as prostate cancer and breast cancer.

Indication

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

Associated Conditions

  • Actinic Keratoses of the face
  • Actinic Keratoses of the scalp

Research Report

Published: Aug 29, 2025

Tirbanibulin (Klisyri®): A Comprehensive Monograph on its Pharmacology, Clinical Efficacy, and Therapeutic Role in Dermatology

Executive Summary

Tirbanibulin is a first-in-class topical medication approved for the treatment of actinic keratosis (AK) on the face or scalp. Marketed under the brand name Klisyri®, it represents a significant advancement in dermatological therapy, distinguished by a novel, dual-action mechanism of action that inhibits both tubulin polymerization and Src kinase signaling.[1] This unique molecular activity allows for the targeted disruption of key pathways involved in the proliferation and survival of neoplastic keratinocytes characteristic of AK.[3]

The most notable clinical feature of Tirbanibulin is its remarkably short treatment duration, requiring only a once-daily application for five consecutive days.[5] This abbreviated regimen contrasts sharply with the weeks or months of therapy required for many established topical agents, addressing a critical unmet need for treatments that enhance patient adherence and satisfaction.[7] Its clinical profile is further defined by a favorable safety and tolerability profile. Adverse events are almost exclusively localized to the application site, consisting of predictable, transient, and manageable local skin reactions (LSRs) such as erythema and scaling, which typically resolve within a few weeks of treatment completion.[9]

Continue reading the full research report

Clinical Trials

Title
Posted
Study ID
Phase
Status
Sponsor
2025/06/08
Phase 1
Recruiting
Bruce Robinson, MD
2025/01/24
Phase 4
Recruiting
The Skin Center Dermatology Group
2023/11/18
Phase 3
Completed
2023/11/01
Phase 2
Recruiting
2023/09/07
Phase 4
Withdrawn
Medical University of Graz
2023/06/12
Phase 4
Completed
Medical University of Graz
2023/02/23
Phase 4
Completed
2023/02/06
Phase 2
Completed
2022/05/24
Phase 4
Active, not recruiting
2022/03/15
Phase 3
Completed

FDA Drug Approvals

Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
Almirall, LLC
16110-391
TOPICAL
10 mg in 1 g
12/18/2020

EMA Drug Approvals

HSA Drug Approvals

Approved Product
Manufacturer
Approval Number
Dosage Form
Strength
Approval Date
No HSA approvals found for this drug.

NMPA Drug Approvals

Approved Product
Company
Approval Number
Drug Type
Dosage Form
Approval Date
No NMPA approvals found for this drug.

PPB Drug Approvals

Approved Product
Registration No.
Company
Licence No.
Strength
Registration Date
No PPB approvals found for this drug.

TGA Drug Approvals

Approved Product
ARTG ID
Sponsor
Registration Type
Status
Registration Date
ONAKTA tirbanibulin 1% w/w ointment sachet
391198
Medicine
A
2/23/2024

Health Canada Drug Approvals

Approved Product
Company
DIN
Dosage Form
Strength
Market Date
ONAKTA
avir pharma inc.
02537818
Ointment - Topical
1 % / W/W
N/A

CIMA AEMPS Drug Approvals

Approved Product
Company
Registration Number
Pharmaceutical Form
Prescription Type
Status
No CIMA AEMPS (Spain) approvals found for this drug.

Philippines FDA Drug Approvals

Approved Product
Company
License Number
Dosage Form
Strength
Approval Date
No Philippines FDA approvals found for this drug.

Saudi SFDA Drug Approvals

Approved Product
Company
License Number
Dosage Form
Strength
Approval Date
No Saudi SFDA approvals found for this drug.

Malaysia NPRA Drug Approvals

Approved Product
Company
Registration Number
Dosage Form
Strength
Approval Date
No Malaysia NPRA approvals found for this drug.

UK EMC Drug Information

Medicine Name
MA Holder
MA Number
Pharmaceutical Form
Active Ingredient
Authorization Date
No UK EMC drug information found for this drug.

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