Tirbanibulin

Tirbanibulin, sold under the brand name Klisyri, is a medication for the treatment of actinic keratosis on the face or scalp.[1][2]

Tirbanibulin

Clinical data
Trade names	Klisyri
Other names	KX2-391
License data	US DailyMed: Tirbanibulin
Routes of administration	Topical
Drug class	Microtubule inhibitor
ATC code	D06BX03 (WHO)
Legal status
Legal status	US: ℞-only [1][2]
Identifiers
IUPAC name N-benzyl-2-[5-[4-(2-morpholin-4-ylethoxy)phenyl]pyridin-2-yl]acetamide
CAS Number	897016-82-9
PubChem CID	23635314
DrugBank	DB06137
ChemSpider	24633341
UNII	4V9848RS5G
KEGG	D11691
ChEMBL	ChEMBL571546
PDB ligand	DN0 (PDBe, RCSB PDB)
CompTox Dashboard (EPA)	DTXSID30237862
Chemical and physical data
Formula	C26H29N3O3
Molar mass	431.536 g·mol^−1
3D model (JSmol)	Interactive image
SMILES C1COCCN1CCOC2=CC=C(C=C2)C3=CN=C(C=C3)CC(=O)NCC4=CC=CC=C4
InChI InChI=1S/C26H29N3O3/c30-26(28-19-21-4-2-1-3-5-21)18-24-9-6-23(20-27-24)22-7-10-25(11-8-22)32-17-14-29-12-15-31-16-13-29/h1-11,20H,12-19H2,(H,28,30) Key:HUNGUWOZPQBXGX-UHFFFAOYSA-N

The most common side effects include local skin reactions, application site pruritus, and application site pain.[1][2]

Tirbanibulin was approved for medical use in the United States in December 2020.[2][3][4] The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication.[5]

It functions as a mitotic inhibitor.[6]

Medical uses

Tirbanibulin is indicated for the topical treatment of actinic keratosis of the face or scalp.[1][2]

History

The U.S. Food and Drug Administration (FDA) approved tirbanibulin based on evidence from two clinical trials (Trial 1/ NCT03285477 and Trial 2/NCT03285490) of 702 adults with actinic keratosis on the face or scalp.[2] The trials were conducted at 62 sites in the United States.[2] Participants received once daily treatment with either tirbanibulin or inactive control ointment for 5 consecutive days to the single predetermined area where they had actinic keratosis.[2] Neither the participants nor the health care providers knew which treatment was being given until after the trial was completed.[2] The benefit of tirbanibulin in comparison to control was assessed after 57 days by comparing the percentage of participants who did not have any actinic keratosis on the treatment area (100% clearance).[2]

References

1. "Klisyri- tirbanibulin ointment". DailyMed. Retrieved 8 January 2021.
2. "Drug Trials Snapshot: Klisyri". U.S. Food and Drug Administration (FDA). 14 December 2020. Retrieved 8 January 2021. This article incorporates text from this source, which is in the public domain.
3. "Drug Approval Package: Klisyri". U.S. Food and Drug Administration (FDA). 28 December 2020. Retrieved 8 January 2021.
4. "Athenex Announces FDA Approval of Klisyri (Tirbanibulin) for the Treatment of Actinic Keratosis on the Face or Scalp" (Press release). Athenex Inc. 15 December 2020. Retrieved 15 December 2020 – via GlobeNewswire.
5. "New Drug Therapy Approvals 2020". U.S. Food and Drug Administration (FDA). 31 December 2020. Retrieved 17 January 2021.
6. Niu L, Yang J, Yan W, Yu Y, Zheng Y, Ye H, et al. (November 2019). "Reversible binding of the anticancer drug KXO1 (tirbanibulin) to the colchicine-binding site of β-tubulin explains KXO1's low clinical toxicity". The Journal of Biological Chemistry. 294 (48): 18099–18108. doi:10.1074/jbc.RA119.010732. PMID 31628188.

External links

• "Tirbanibulin". Drug Information Portal. U.S. National Library of Medicine.
• Clinical trial number NCT03285477 for "A Multi-Center Study to Evaluate the Efficacy and Safety of KX2-391 Ointment 1% on AK on Face or Scalp (AK003)" at ClinicalTrials.gov
• Clinical trial number NCT03285490 for "A Multi-Center Study to Evaluate the Efficacy and Safety of KX2-391 Ointment 1% on AK on Face or Scalp (AK004)" at ClinicalTrials.gov