Pharmacokinetics and Safety Evaluation of the Transglutaminase 2 Inhibitor Suvigletistat in Healthy Chinese, Japanese, and White/European Participants.
6 affiliations
- 1Clinical Pharmacology Pharmacometrics Systems and Tools, GSK R&D, Melbourne, VIC, Australia.
- 2Respiratory Immunology & Inflammation Research Unit, GSK, Stevenage, UK.
- 3Safety Evaluation and Risk Management, GSK, Poznań, Poland.
- 4Safety Evaluation and Risk Management, GSK, London, UK.
- 5Early Development Statistics, GSK, Bengaluru, Karnataka, India.
- 6Clinical Pharmacology and Quantitative Medicine, GSK, Stevenage, UK.
Abstract
This Phase I, randomized, placebo-controlled, double-blind study (NCT06625489) evaluated pharmacokinetics (PK), safety, and tolerability of the transglutaminase 2 inhibitor suvigletistat in Chinese, Japanese, and White/European participants. Eligible participants: aged 18-50 years, healthy, and of Chinese, Japanese, or White/European ancestry. Thirty-six participants (12 per ancestry group) were randomized 3:1 to receive suvigletistat (160 mg single oral dose) or placebo. Suvigletistat was rapidly absorbed (median time to maximum observed drug concentration [Cmax]: 0.67-0.75 h), and geometric mean half-life ranged from 1.93 to 2.58 h across ancestry groups. Suvigletistat systemic exposure was similar across all ancestries; geometric least squares mean ratios versus White/European participants for Cmax were 0.99 and 1.06 in participants of Chinese and Japanese ancestry, respectively. Similarly, area under the concentration-time curve from time zero to infinity ratios were 0.94 and 1.06. Suvigletistat geometric mean elimination half-life was comparable in Chinese (1.93 h), Japanese (2.23 h), and White/European participants (2.58 h). There were no serious adverse events or deaths. There were no clinically meaningful findings in laboratory values, vital signs, or electrocardiograms. No clinically meaningful differences in suvigletistat PK were observed between ancestry groups, providing evidence of low ethnic sensitivity for a drug with cytochrome P450 3A4-dependent metabolism.
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BibTeX
@article{nand2026pharmacokinetics,
title = {{Pharmacokinetics and Safety Evaluation of the Transglutaminase 2 Inhibitor Suvigletistat in Healthy Chinese, Japanese, and White/European Participants.}},
author = {Romina A Nand and Hannah Woodcock and Kasia A Okrojek-Swiderek and Yolanda Alvarez and Mohak Sharda and Anubha Gupta},
journal = {Clinical pharmacology in drug development},
year = {2026},
month = oct,
doi = {10.1002/cpdd.70113},
url = {https://europepmc.org/article/MED/42905102},
note = {CC BY-NC-ND},
}
RIS
TY - JOUR
TI - Pharmacokinetics and Safety Evaluation of the Transglutaminase 2 Inhibitor Suvigletistat in Healthy Chinese, Japanese, and White/European Participants.
AU - Romina A Nand
AU - Hannah Woodcock
AU - Kasia A Okrojek-Swiderek
AU - Yolanda Alvarez
AU - Mohak Sharda
AU - Anubha Gupta
PY - 2026
DA - 2026/10/01
JO - Clinical pharmacology in drug development
DO - 10.1002/cpdd.70113
UR - https://europepmc.org/article/MED/42905102
AB - This Phase I, randomized, placebo-controlled, double-blind study (NCT06625489) evaluated pharmacokinetics (PK), safety, and tolerability of the transglutaminase 2 inhibitor suvigletistat in Chinese, Japanese, and White/European participants. Eligible participants: aged 18-50 years, healthy, and of Chinese, Japanese, or White/European ancestry. Thirty-six participants (12 per ancestry group) were randomized 3:1 to receive suvigletistat (160 mg single oral dose) or placebo. Suvigletistat was rapidly absorbed (median time to maximum observed drug concentration [Cmax]: 0.67-0.75 h), and geometric mean half-life ranged from 1.93 to 2.58 h across ancestry groups. Suvigletistat systemic exposure was similar across all ancestries; geometric least squares mean ratios versus White/European participants for Cmax were 0.99 and 1.06 in participants of Chinese and Japanese ancestry, respectively. Similarly, area under the concentration-time curve from time zero to infinity ratios were 0.94 and 1.06. Suvigletistat geometric mean elimination half-life was comparable in Chinese (1.93 h), Japanese (2.23 h), and White/European participants (2.58 h). There were no serious adverse events or deaths. There were no clinically meaningful findings in laboratory values, vital signs, or electrocardiograms. No clinically meaningful differences in suvigletistat PK were observed between ancestry groups, providing evidence of low ethnic sensitivity for a drug with cytochrome P450 3A4-dependent metabolism.
SN - 2160-763X
SN - 2160-7648
ER -