Pharmacokinetics, Safety, and Tolerability of a Single 5-Day Treatment of Tirbanibulin Ointment 1% in 100 cm 2 : A Phase 1 Maximal-Use Trial in Patients with Actinic Keratosis.

Autor: DuBois J; DermResearch, Inc., Austin, TX, USA., Jones TM; J&S Studies, Inc., College Station, TX, USA., Lee MS; Progressive Clinical Research, San Antonio, TX, USA., Falqués M; Almirall, Sant Feliu de Llobregat, Spain., Kiyasova V; Almirall, Sant Feliu de Llobregat, Spain., Jiménez G; Almirall, Barcelona, Spain., Otero R; Almirall, Sant Feliu de Llobregat, Spain., Jansat JM; Almirall, Sant Feliu de Llobregat, Spain., Aubets J; Almirall, Sant Feliu de Llobregat, Spain., Forconi RJ; International Clinical Research - US, LLC, Sanford, FL, USA.
Jazyk: angličtina
Zdroj: Clinical pharmacology in drug development [Clin Pharmacol Drug Dev] 2024 Feb; Vol. 13 (2), pp. 208-218. Date of Electronic Publication: 2024 Jan 07.
DOI: 10.1002/cpdd.1368
Abstrakt: Tirbanibulin ointment 1% is approved in the United States and Europe for the treatment of actinic keratosis with demonstrated efficacy, safety, and tolerability when applied over a field up to 25 cm 2 . This Phase 1 maximal-use trial determines the plasma pharmacokinetics, safety, and tolerability of tirbanibulin ointment 1% applied to 100 cm 2 of the face or balding scalp in adults with actinic keratosis. Twenty-eight patients self-applied tirbanibulin once daily for a single 5-day treatment course. On Day 5, the mean maximum plasma concentration was 1.06 ng/mL and area under the plasma concentration-time curve during a dosing interval was 16.2 ng • h/mL. Systemic exposure was approximately 4-fold higher than in a previous pharmacokinetic study with a 25 cm 2 field, consistent with the increase in the treated area. Tirbanibulin applied to a 100-cm 2 treatment field showed favorable safety and tolerability. The most common treatment-emergent adverse events were application site reactions (in 35.7% of patients). All treatment-emergent adverse events and most of the tolerability signs were mild/moderate and resolved or returned to baseline by Day 29. In summary, under maximal-use conditions, tirbanibulin ointment 1% was safe and well tolerated supporting its potential use over a field up to 100 cm 2 .
(© 2024 The Authors. Clinical Pharmacology in Drug Development published by Wiley Periodicals LLC on behalf of American College of Clinical Pharmacology.)
Databáze: MEDLINE
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