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Safety, Tolerability, Pharmacokinetics, and Food Effects on TAC‐302 in Healthy Participants: Randomized, Double‐Blind, Placebo‐Controlled, Single‐Dose and Multiple‐Dose Studies
Author(s) -
Sesoko Shogo,
Huang Jinhong,
Okayama Takashige,
Nishida Erika,
Miyoshi Kazuhisa
Publication year - 2020
Publication title -
clinical pharmacology in drug development
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.711
H-Index - 22
eISSN - 2160-7648
pISSN - 2160-763X
DOI - 10.1002/cpdd.776
Subject(s) - medicine , tolerability , pharmacokinetics , placebo , double blind , pharmacology , randomized controlled trial , adverse effect , anesthesia , alternative medicine , pathology
TAC‐302 stimulates neurite outgrowth activity and is expected to restore urinary function in patients with lower urinary tract dysfunction. We conducted 2 phase 1, randomized, placebo‐controlled studies to confirm the safety and pharmacokinetics (PK) of TAC‐302 in healthy adult Japanese male volunteers. In the first‐in‐human single‐dose study (n = 60), TAC‐302 was administered at doses from 100 to 1200 mg after an overnight fast. The effects of a meal on the PK of TAC‐302 400 mg were also examined. A multiple‐dose study (n = 36) evaluated the effects of meal fat content on the PK of single doses of TAC‐302 (100, 200, or 400 mg) and multiple doses of TAC‐302 administered for 5 days (100, 200, and 400 mg twice daily). TAC‐302 showed linear PK up to doses of 1200 mg in the fasting state, and across the dose range of 100–400 mg in the fed state. No accumulation of TAC‐302 was observed. Food, particularly with high fat content, increased TAC‐302 plasma concentrations. No differences were observed in the adverse event incidence between the TAC‐302 and placebo groups in either study. TAC‐302 showed a wide safety margin.