tirbanibulin

Action and Spectrum

Actions and spectrum: 

Actions:  

This drug also prevents tubulin from polymerizing into microtubules, which disturbs the typical cytoskeleton of cell. Inhibition of cell cycle, reduced cell growth, and ultimately cell death can result from this. Tirbanibulin also works to eliminate and diminish abnormal skin cells by stopping proteins from being made in skin cells. In addition, actinic keratosis induced skin redness and swelling can be relieved by an anti-inflammatory mechanism that is possessed by tirbanibulin. 

Drug Interaction

Adverse Reaction

Adverse reactions 

1-10% 

Application site pruritus (9%) 

Vesiculation/pustulation, mild (7%) 

Erosion/ulceration, moderate (3%) 

Crusting, severe (2%) 

Erythema, severe (6%) 

Application site pain (10%) 

Erosion/ulceration, mild (9%) 

Swelling, moderate (9%) 

Flaking/scaling, severe (9%) 

>10% 

Crusting, mild (30%) 

Swelling, mild (29%) 

Flaking/scaling, mild (26%) 

Erythema, mild (22%) 

Crusting, moderate (14%) 

Erythema, moderate (63%) 

Flaking/scaling, moderate (47%) 

<1% 

Swelling, severe (<1%) 

Vesiculation/pustulation, moderate-to-severe (<1%) 

Black Box Warning

Black box warning 

The drug may irritate eyes, upon accidental contact, rinse eyes thoroughly with water 

Contraindication / Caution

Contraindications/Caution 

Contraindications 

Hypersensitivity 

Cautions 

Pregnancy 

Lactation 

Pregnancy / Lactation

Pregnancy & breastfeeding: 

Pregnancy consideration: 

US FDA pregnancy category: Not assigned 

Breastfeeding warnings: 

Data about the excretion of the drug into breast milk is not known  

Pregnancy category: 

• Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: There was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: There was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women. 
• Category D: Adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence, these categories of drugs need to be avoided by pregnant women. 
• Category N: No data for the drug under this category is available. 

Pharmacology

Pharmacology: 

The drug is an inhibitor or tubulin and a tyrosine kinase inhibitor.  

Pharmacodynamics: 

The drug has shown promising results in treating patients with actinic keratosis of the face or scalp. It achieves complete clearance of lesions by 57days in 44-54% of patients, compared to 5-13% who receive a placebo as observed in clinical trials. Tirbanibulin also inhibits primary growth of tumor and metastasis in animal models and human triple-negative breast cancer xenografts. It is also found to restore functional ERα expression in ERα-negative breast tumors when combined with tamoxifen and paclitaxel. 

Pharmacokinetics: 

Absorption: 

It has good bioavailability when given orally. A steady state concentration can be achieved upon topical administration by 72 hours. 

Distribution: 

88% of the drug is known to be bound to plasma proteins. 

Metabolism: 

In vitro studies suggest that the drug is metabolized mainly by CYP3A4 and to lesser extent by CYP2C8. KX2-5036 and KX2-5163 are the metabolites identified in individuals with actinic keratosis. 

Elimination and excretion: 

Most of the drug and its metabolites are known to be excreted in feces.  

Half-life: 4 hours 

Adminstartion

Administration: 

It should be applied directly on to the affected skin such as scalp or face due to actinic keratosis. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: tirbanibulin 

Pronounced: [TIR-ban-i-BUE-lin-TOP-i-kal] 

Why do we use tirbanibulin? 

This drug is used in the treatment of actinic keratosis on the face or scalp. This condition occurs due to long-term exposure to sun leading to precancerous situations.