biostudies-literatureUnknown16(7)Fukuda TEli Lilly and Company<h4>Introduction</h4>This study aimed to assess the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of single and multiple doses of the ketohexokinase inhibitor LY3522348 in healthy participants.<h4>Methods</h4>This first-in-human phase 1 study evaluated LY3522348, a highly selective, oral dual inhibitor of human ketohexokinase (KHK) isoforms C and A. The study was conducted in two parts: a single-ascending dose (SAD) study and a multiple-ascending dose (MAD) study, including a drug-drug interaction analysis with midazolam. Participants in the SAD study received single oral doses of LY3522348 ranging from 5 to 380 mg, while participants in the MAD study received once-daily doses of 50 mg, 120 mg, and 290 mg for 14 days.<h4>Results</h4>A total of 65 healthy participanDiabetes therapy : research, treatment and education of diabetes and related disorders1399-1415https://www.ebi.ac.uk/biostudies/studies/S-EPMC12182541biostudies-literatureLY3522348, A New Ketohexokinase Inhibitor: A First-in-Human Study in Healthy Adults.PMC12182541Morse BLDurham TBKonig MQian HRWang WFukuda TLaBell ESHaupt AThompson BRBrouwers BBenson CTMacKrell JfalseLY3522348, A New Ketohexokinase Inhibitor: A First-in-Human Study in Healthy Adults.<h4>Introduction</h4>This study aimed to assess the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of single and multiple doses of the ketohexokinase inhibitor LY3522348 in healthy participants.<h4>Methods</h4>This first-in-human phase 1 study evaluated LY3522348, a highly selective, oral dual inhibitor of human ketohexokinase (KHK) isoforms C and A. The study was conducted in two parts: a single-ascending dose (SAD) study and a multiple-ascending dose (MAD) study, including a drug-drug interaction analysis with midazolam. Participants in the SAD study received single oral doses of LY3522348 ranging from 5 to 380 mg, while participants in the MAD study received once-daily doses of 50 mg, 120 mg, and 290 mg for 14 days.<h4>Results</h4>A total of 65 healthy participan2025-01-01T00:00:00Z2025 Jul2026-06-01T07:58:02.788Z2026-04-08T10:38:35.059ZS-EPMC121825414035884910.1007/s13300-025-01752-5