@article{Maher:2026:10.1183/23120541.00469-2025,
author = {Maher, TM and Chen, MC and Korth, CC and Elenko, E and Harnett, MD and Garg, V and Graham, CS},
doi = {10.1183/23120541.00469-2025},
journal = {ERJ Open Res},
title = {A phase 1 pharmacokinetics study of deupirfenidone (LYT-100) in healthy older adults.},
url = {http://dx.doi.org/10.1183/23120541.00469-2025},
volume = {12},
year = {2026}
}

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TY  - JOUR
AB  - BACKGROUND: Deupirfenidone, a selectively deuterated form of pirfenidone, is being developed for idiopathic pulmonary fibrosis (IPF), where tolerability limits current antifibrotic use. Deupirfenidone retains the biological activity of pirfenidone, and the differentiated pharmacokinetic (PK) profile may be associated with improved tolerability. METHODS: A phase 1, three-part, randomised, double-blind study was conducted to identify phase 2 doses. The safety, tolerability, steady-state PK and food effect profile of deupirfenidone were assessed in healthy older adults. Part 1 was a crossover study comparing deupirfenidone 850mg twice daily to pirfenidone 801mg three times daily. Part 2 was a crossover study comparing deupirfenidone 550mg three times daily to pirfenidone 801mg three times daily. Part 3 was a parallel study of deupirfenidone 550mg three times daily titrated to deupirfenidone 824mg three times daily versus placebo. RESULTS: Deupirfenidone 850mg twice daily met the equivalence criterion to pirfenidone 801mg three times daily for area-under-the-curve (AUC); however, maximum measured concentration (C max) and treatment-emergent adverse events (TEAEs) were higher with deupirfenidone. Deupirfenidone 550mg three times daily met equivalence criterion to pirfenidone 801mg three times daily for AUC; however, C max was lower. Frequency of gastrointestinal (GI) and nervous system (NS) TEAEs for deupirfenidone in the fed state was 40% lower than for pirfenidone. When deupirfenidone was titrated from 550mg three times daily to 824mg three times daily, PK parameters increased without increases in GI or NS TEAEs. CONCLUSIONS: Results suggest evaluating a dose for deupirfenidone in healthy older adults of between 550mg three times daily and 825mg three times daily. Both doses are being evaluated in a 26-week, phase 2b study in patients with IPF.
AU  - Maher,TM
AU  - Chen,MC
AU  - Korth,CC
AU  - Elenko,E
AU  - Harnett,MD
AU  - Garg,V
AU  - Graham,CS
DO  - 10.1183/23120541.00469-2025
PY  - 2026///
SN  - 2312-0541
TI  - A phase 1 pharmacokinetics study of deupirfenidone (LYT-100) in healthy older adults.
T2  - ERJ Open Res
UR  - http://dx.doi.org/10.1183/23120541.00469-2025
UR  - https://www.ncbi.nlm.nih.gov/pubmed/41846675
VL  - 12
ER  - 

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