Klisyri (tirbanibulin)
Topical Antineoplastic Alkylating Agents Topical Ointment In Packet (Ea)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Tirbanibulin, a microtubule inhibitor, is a skin or mucous membrane agent.
Although tirbanibulin is a microtubule inhibitor, the mechanism of action by which tirbanibulin is effective for the treatment of actinic keratosis (AK) is unknown.
Following topical application of a mean daily dose of 138 mg of tirbanibulin to a 25 cm2 contiguous area of the balding scalp or face for 5 consecutive days, steady-state concentrations are achieved within 72 hours. Systemic exposure after 5 days of application is low; maximum plasma concentrations are approximately 0.34 ng/mL +- 0.30 ng/mL and 0.18 ng/mL +- 0.10 ng/mL when applied to the face and scalp, respectively. The median time to achieve maximum serum concentrations is approximately 7 hours after application.
Tirbanibulin is 88% bound to plasma proteins, and its binding is independent of plasma concentrations from 0.01-10 mcg/mL. Exposure to human hepatocytes in vitro generated 2 inactive metabolites of tirbanibulin, KX2-5036 and KX2-5163, and other unidentified metabolites. The method by which tirbanibulin undergoes excretion has not been fully characterized in humans.
USES: This medication is used to treat a certain skin condition (actinic keratosis) on the face or scalp area.
Generic name: tirbanibulin
Pronunciation: (TIR-ban-i-BUE-lin)
Drug class: Topical Antineoplastic Alkylating Agents
Therapeutic class: Dermatological
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Klisyri
Indications
The following indications are listed for Klisyri:
- Actinic Keratosis On The Face Or Scalp
Dosing
Each single-use 1% ointment packet contains 2.5 mg of tirbanibulin in 250 mg.
Tirbanibulin is available as single-dose ointment packets for topical use only; not for oral or ophthalmic use. A sufficient amount of tirbanibulin should be evenly applied to cover up to a 25 cm2 treatment field.
Store at 20-25degreesC (excursions permitted between 15-30degreesC). Do not refrigerate or freeze.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Klisyri 1% (250 Mg) Oint Pkt | Maintenance | Apply 1 packet to the affected area(s) on the face and/or scalp by topical route once daily for 5 consecutive days. |
| Klisyri 1% (350 Mg) Oint Pkt | Maintenance | Apply 1 packet to the affected area(s) on the face and/or scalp by topical route once daily for 5 consecutive days. |
No dosing information is available for this tab.
Drug interactions
No formal drug interaction studies have been conducted with tirbanibulin.
In vitro, tirbanibulin is principally metabolized by cytochrome P-450 (CYP) isoenzyme 3A4, and to a lesser extent, CYP2C8. Findings from in vitro studies suggest that tirbanibulin has no clinically meaningful effects on the pharmacokinetics of drugs metabolized by CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, or CYP3A4. Tirbanibulin also does not have clinically meaningful effects on drugs mediated by multidrug and toxin extrusion (MATE) transporter 1, MATE2-K, organic anion transporting polypeptide (OATP)1B1, OATP1B3, organic cation transporter (OCT)1, or OCT2.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
None.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
- No disease contraindications
Adverse reactions
The most common adverse reactions reported in >=2% of patients receiving tirbanibulin include local skin reactions, application site pruritus, and application site pain.
There are no severe adverse reactions for this drug.
More Frequent
- Acute pain at drug application site
- Pruritus of skin
Less Frequent
- Erythema
- Localized edema
- Skin crusting
- Skin scaling
- Superficial skin ulcer
Rare or Very Rare
- Blistering skin
Precautions
No enhanced messaging available.
The safety and efficacy of tirbanibulin have not been established in patients <18 years of age; however, actinic keratosis (AK) is generally not seen within the pediatric population.
No data are available on the use of tirbanibulin in pregnancy to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.
Animal reproductive data have shown tirbanibulin administered to rats during the period of organogenesis atleast 74 times the systemic exposure associated with the maximum recommended human dose (MRHD) results in an increased number of fetal deaths and malformations. Oral administration of tirbanibulin to rabbits during organogenesis at an exposure approximately 159 times the systemic exposure associated with the MRHD was associated with reduced mean fetal weight and size.
No data are available on the presence of tirbanibulin in human or animal milk. The effects of tirbanibulin on the breastfed child and its effects on milk production are unknown.
Consider the benefits of breastfeeding along with the mother's clinical need for the drug and any potential adverse effects from tirbanibulin on the breastfed child.
The manufacturer makes no specific dosage recommendations at this time. No differences in safety or efficacy have been observed between geriatric and younger adult patients; however, sensitivity of some older individuals cannot be ruled out. ,
Out of the 353 subjects with AK who received treatment with tirbanibulin in Phase 3 trials, 246 (70%) were >65 years of age. No overall differences in safety or efficacy were observed between these patients and younger adult patients. Other reported clinical experience has not identified differences in response, but greater sensitivity of some older individuals cannot be ruled out.
ICD codes
| Code | Type | Description |
|---|---|---|
| Actinic keratosis on the face or scalp | ||
| L57.0 | ICD10CM | Actinic keratosis |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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