AV-101, a novel inhaled dry-powder formulation of imatinib, in healthy adult participants: a phase 1 single and multiple ascending dose study
| Autor: | Hunter Gillies, Ralph Niven, Benjamin T. Dake, Murali M. Chakinala, Jeremy P. Feldman, Nicholas S. Hill, Marius M. Hoeper, Marc Humbert, Vallerie V. McLaughlin, Martin Kankam |
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| Jazyk: | angličtina |
| Rok vydání: | 2023 |
| Předmět: | |
| Zdroj: | ERJ Open Research, Vol 9, Iss 2 (2023) |
| Druh dokumentu: | article |
| ISSN: | 2312-0541 23120541 |
| DOI: | 10.1183/23120541.00433-2022 |
| Popis: | Background Oral imatinib has been shown to be effective, but poorly tolerated, in patients with advanced pulmonary arterial hypertension (PAH). To maintain efficacy while improving tolerability, AV-101, a dry powder inhaled formulation of imatinib, was developed to deliver imatinib directly to the lungs. Methods This phase 1, placebo-controlled, randomised single ascending dose (SAD) and multiple ascending dose (MAD) study evaluated the safety/tolerability and pharmacokinetics of AV-101 in healthy adults. The SAD study included five AV-101 cohorts (1 mg, 3 mg, 10 mg, 30 mg, 90 mg) and placebo, and a single-dose oral imatinib 400-mg cohort. The MAD study included three AV-101 cohorts (10 mg, 30 mg, 90 mg) and placebo; dosing occurred twice daily for 7 days. Results 82 participants (SAD n=48, MAD n=34) were enrolled. For the SAD study, peak plasma concentrations of imatinib occurred within 3 h of dosing with lower systemic exposure compared to oral imatinib (p |
| Databáze: | Directory of Open Access Journals |
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