Last updated on: 15.12.2021

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Tirbanibulin is a topical microtubule inhibitor with a selective antiproliferative mechanism of action.

Pharmacodynamics (Effect)
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Tirbanibulin is not only a "non-ATP-competitive inhibitor of proto-oncogenic non-receptor tyrosine kinase(SRC)" but also a potent tubulin inhibitor (see microtubules below).

Tirbanibulin inhibits the SRC signaling pathway. Tyrosine kinase SRC, formerly known as C-SRC, (SRC=is the acronym for "cellular and sarcoma") is a tyrosine-protein kinase that is present associated with the cell membrane. SRC is a protooncogene and is considered the best studied protooncogene ever.

In cell-based experiments, tirbanibulin has been shown to induce tubulin depolymerization and cell cycle arrest in G2/M phase at low nanomolar concentrations. It acts similarly to colchicine (Niu L et al. 2019). Here, it reversibly binds to the colchicine binding site on β-tubulin, triggering a cellular effect (G2/M cell cycle arrest). The reversible binding of tirbanibulin explains its clinically low toxicity (Niu L et al. 2019).

Field of application/use
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Tirbanibulin, applied in ointment form, is indicated for the field therapy of non-hyperkeratotic, non-hypertrophic actinic keratoses (Olsen grade I) on the face or scalp in adults. Tirbanibulin comes in ointment form and is for topical use only.

Dosage and method of use
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Tirbanibulin ointment should be applied in a thin layer to the treatment area of up to 25 cm2 once daily on the face or scalp for a treatment cycle of five consecutive days. Approximately eight weeks after the start of treatment, the therapeutic effect can be assessed.

The treatment area should be cleaned with water and a mild soap before application and should then be dried. The ointment should then be squeezed from the disposable sachet onto a fingertip and applied in a thin layer evenly over the entire treatment area, up to a maximum of 25 cm2. It is recommended to apply the ointment daily at approximately the same time each day. The treated area should not be washed or touched for a period of about 8 hours.

Caution: Wash hands with soap and water before and immediately after applying the ointment!

Undesirable effects
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  • The most commonly reported adverse reactions were local skin reactions. At the application site, these included: Erythema (91%)
  • scaling (82%)
  • crusting (46%)
  • swelling (39%)
  • Erosion/ulceration (12%)
  • Pain (10%)
  • Itching (9%)
  • Vesicle/pustule formation (8%)

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Klisyri ® 10 mg /g ointment

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Tirbanibulin was approved for medical use in the United States in December 2020. It is the first representative of a new class of active substances (first in class) in this area of application. Approval for the European Union followed in July 2020.

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  1. S3 guideline Actinic keratosis and squamous cell carcinoma of the skin. AWMF guideline 032/022OL; March 2020.
  2. Blauvelt A et al (2021) Phase 3 trials of tirbanibulin ointment for actinic keratosis. N Engl J Med 2021; 384: 512-20.
  3. Klisyri (Almirall) package insert: https://image.wub service.uk/resources/static/des/210901/12/85/128549.pdf.
  4. Niu L et al (2019) Reversible binding of the anticancer drug KXO1 (tirbanibulin) to the colchicine-binding site of β-tubulin explains KXO1's low clinical toxicity. J Biol Chem 294:18099-18108.

Incoming links (1)


Outgoing links (3)

Colchicine; Microtubules; SRC;

Last updated on: 15.12.2021