2023
DOI: 10.1002/cpdd.1236
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Single‐ and Multiple‐dose Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of ASP1128, a Novel Peroxisome Proliferator‐activated Receptor δ Modulator, in Healthy Participants

Abstract: Peroxisome proliferator‐activated receptor δ (PPARδ) plays a central role in modulating mitochondrial function in ischemia‐reperfusion injury. ASP1128, a potent and selective modulator of PPARδ, is currently under investigation for treating acute kidney injury. This randomized, first‐in‐human study assessed the safety, tolerability, pharmacokinetics, and pharmacodynamics of ASP1128 administered intravenously in healthy participants. Forty‐nine participants received a single dose of ASP1128 0.3–10 mg (n = 37) o… Show more

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Cited by 2 publications
(4 citation statements)
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“…Based on the positive preclinical and phase-1 results, 7 , 8 , 9 treatment effect was assumed for 100 mg ASP1128 in the clinical setting. Reasons for an absence of this treatment effect on renal outcomes of ASP1128 can be related to issues with the compound (dosing, timing of treatment), the study (disbalance in confounding factors, population, and sample size), or both.…”
Section: Discussionmentioning
confidence: 99%
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“…Based on the positive preclinical and phase-1 results, 7 , 8 , 9 treatment effect was assumed for 100 mg ASP1128 in the clinical setting. Reasons for an absence of this treatment effect on renal outcomes of ASP1128 can be related to issues with the compound (dosing, timing of treatment), the study (disbalance in confounding factors, population, and sample size), or both.…”
Section: Discussionmentioning
confidence: 99%
“…The 100 mg dose was considered safe and well tolerated in the phase-1 study 1128-CL-0101 with up to 7 days multiple dosing (3–100 mg) in healthy nonelderly and elderly patients, and ASP1128 plasma concentration increased dose proportionally. 9 PPARδ or fatty acid oxidation target gene upregulation revealed optimal results for 100 mg at all time points in single and multiple dosing. 9 The treatment period up to 72 hours postsurgery and related gene upregulation was assumed to cover the period when AKI usually occurs in relation to injury sustained during cardiac surgery, and the peak of SCr and related biomarkers.…”
Section: Methodsmentioning
confidence: 96%
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