Tolerability, pharmacokinetics, and pharmacodynamics of mirogabalin in healthy subjects: Results from phase 1 studies

Pharmacology Research & Perspectives
Karen BrownHamim Zahir

Abstract

Three phase 1 pharmacokinetic (PK)/pharmacodynamics (PD) studies were conducted in healthy men and women to further characterize the safety, tolerability, and PK/PD of mirogabalin administration with or without food and to guide the dose selection and regimen for phase 2 and 3 clinical development. The 3 studies included 2 randomized, double-blind, placebo-controlled, single- and multiple-ascending-dose studies, and 1 open-label, crossover study to evaluate the PK of mirogabalin administered under fasting and fed (high-fat meal) conditions. Forty-eight and 47 healthy volunteers completed the single- and multiple-dose studies, respectively. Thirty subjects were enrolled and completed the food effect study. Mirogabalin was well tolerated in the fed and fasted states. The most frequent treatment-emergent adverse events (TEAEs)-dizziness and somnolence-were expected based on mirogabalin's mechanism of action. Subjects receiving the highest mirogabalin doses (50 and 75 mg single dose) showed greater dizziness and sedation and higher rates of TEAEs than subjects receiving 3-30 mg. After oral administration, mirogabalin was rapidly absorbed (time to maximum concentration, ∼1 hour) and eliminated through urine unchanged (61%-72% urinar...Continue Reading

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Citations

Feb 20, 2019·Drugs·Emma D Deeks
Jan 1, 2021·The Korean Journal of Pain·Jae-Yeon KimKyung-Hoon Kim
Jan 26, 2021·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Naotoshi YamamuraVijay Vashi
Feb 13, 2021·Pharmaceuticals·Renata ZajączkowskaJerzy Wordliczek

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Methods Mentioned

BETA
urine
sedation

Clinical Trials Mentioned

NCT02318706
NCT02318719

Software Mentioned

Phoenix WinNonlin

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