2-methyl-7-oxo-4,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidine-6-carboxylic acid cas 842954-97-6

The most widely known name of this chemical is Tirbanibulin. Its trade name is Klisyri®.
The following is a comprehensive introduction to Tirbanibulin:
1. Basic Information
· Chemical Name: (2Z)-N-(2-Amino-4-fluorophenyl)-5-[[3,4,5-trimethoxyphenyl]methoxy]-2-furanamine
· CAS Number: 842954-97-6
· Molecular Formula: C₂₂H₂₄FN₃O₅
· Molecular Weight: 429.44 g/mol
2. What is it?
Tirbanibulin is a small molecule, synthetic multi-target inhibitor. It is classified as a local treatment drug in medicine and is mainly used in dermatology.
3. Mechanism of Action
The mechanism of action of Tirbanibulin is highly unique. It inhibits the proliferation of cancer cells through two distinct pathways:
· Microtubulin polymerization inhibitor: It can inhibit the polymerization of microtubulin, thereby disrupting the formation of the spindle during the cell mitosis process and preventing the division of cancer cells.
· Src signaling pathway inhibitor: Src is a tyrosine kinase related to cell proliferation, differentiation, and survival. Tirbanibulin can inhibit the activity of Src, thereby interfering with the survival signals of cancer cells.
This dual inhibitory mechanism enables it to effectively target and eliminate rapidly proliferating abnormal keratinocytes.
4. Main Uses and Indications
Tirbanibulin is mainly used for the treatment of solar keratosis.
· Indications: Local treatment for solar keratosis on the face or scalp of adults.
· Usage: It is a topical ointment with a concentration of 1% (trade name: Klisyri®). The patient is required to apply it continuously for 5 days, once a day.
Solar keratosis is a precancerous skin condition caused by prolonged exposure to sunlight. If left untreated, there is a small but significant chance that it may develop into squamous cell carcinoma. Therefore, early intervention and treatment are of great importance.
5. Research and Development and Market Launch Status
· Research and Development Company: Developed by Athenex Company (formerly known as DARA BioSciences).
· Approval Authorities:
· US FDA: Approved for market launch in December 2020.
· European Medicines Agency: Subsequently, it also received approval.
· Clinical Trials: The results of the key Phase III clinical trial showed that after continuous use for 5 days, approximately half of the patients had complete clearance of lesions at 57 days, and the efficacy and safety were both excellent.
6. Advantages and Features
Compared with traditional treatments for solar keratosis (such as cryotherapy, 5-fluorouracil, imiquimod, etc.), Tirbanibulin has the following significant advantages:
· Short course: Only need to use for 5 consecutive days, with high patient compliance.
· Mild local reactions: Compared to other local therapies (such as 5-fluorouracil and imiquimod) which cause severe redness, erosion and discomfort, the local skin reactions of Tirbanibulin are usually milder and shorter in duration.
· Convenient to use: As an external ointment, it is easy to apply and highly targeted.
7. Safety and Side Effects
Tirbanibulin is generally safe. The side effects are mainly concentrated at the site of administration, and are usually mild to moderate in severity, and are temporary. Common side effects include:
· Itching at the application site
· Pain at the application site
· Skin irritation, redness (reddening)
· Scaling, scabbing
· Swelling or blistering of the skin
These reactions usually subside on their own within a few weeks after the treatment is completed.
Summary

CAS 842954-97-6 (Tirbanibulin) is an innovative small molecule drug used for local treatment of solar keratosis. Its dual mechanism of action, short treatment duration and good tolerance make it an important treatment option in the field of dermatology, providing doctors and patients with an efficient and convenient new alternative beyond traditional therapies.