Phase I safety, tolerability, and pharmacokinetic studies of tetramethylpyrazine nitrone in healthy Chinese volunteers.
pharmacokinetics
tetramethylpyrazine nitrone
tolerability
Journal
Drug development research
ISSN: 1098-2299
Titre abrégé: Drug Dev Res
Pays: United States
ID NLM: 8204468
Informations de publication
Date de publication:
02 2021
02 2021
Historique:
received:
23
04
2019
revised:
01
11
2019
accepted:
17
07
2020
pubmed:
31
8
2020
medline:
4
3
2022
entrez:
1
9
2020
Statut:
ppublish
Résumé
The purpose of this study was to investigate the safety, tolerability and pharmacokinetics of tetramethylpyrazine nitrone (TBN) in healthy Chinese volunteers. A single-ascending-dose (SAD) study where 68 subjects were randomized to a single dose of placebo or TBN (50, 100, 200, 400, 700, 1,000, 1,400, or 1,800 mg) through IV infusion over 30 min. A multiple-ascending-dose (MAD) study where 24 subjects received TBN twice daily (with 12 hr interval) for total 6.5 days at doses of either 700 or 1,400 mg. Adverse events were recorded and pharmacokinetic samples were collected during the whole study period. No serious adverse events were found in the study. All of the observed adverse events, including increased white blood cell (4.4% subjects) and neutrophil counts (4.4% subjects), and decreased hemoglobin levels (4.2% subjects), were laboratory test abnormalities. All the adverse events were mild and tolerable, and returned to normal without any intervention. In the SAD study, linear C TBN is well tolerated in healthy volunteers. Linear C
Sections du résumé
BACKGROUND
The purpose of this study was to investigate the safety, tolerability and pharmacokinetics of tetramethylpyrazine nitrone (TBN) in healthy Chinese volunteers.
METHODS
A single-ascending-dose (SAD) study where 68 subjects were randomized to a single dose of placebo or TBN (50, 100, 200, 400, 700, 1,000, 1,400, or 1,800 mg) through IV infusion over 30 min. A multiple-ascending-dose (MAD) study where 24 subjects received TBN twice daily (with 12 hr interval) for total 6.5 days at doses of either 700 or 1,400 mg. Adverse events were recorded and pharmacokinetic samples were collected during the whole study period.
RESULTS
No serious adverse events were found in the study. All of the observed adverse events, including increased white blood cell (4.4% subjects) and neutrophil counts (4.4% subjects), and decreased hemoglobin levels (4.2% subjects), were laboratory test abnormalities. All the adverse events were mild and tolerable, and returned to normal without any intervention. In the SAD study, linear C
CONCLUSIONS
TBN is well tolerated in healthy volunteers. Linear C
Substances chimiques
Neuroprotective Agents
0
Pyrazines
0
tetramethylpyrazine nitrone
0
Banques de données
ChiCTR
['ChiCTR1800016225', 'ChiCTR1800019627']
Types de publication
Clinical Trial, Phase I
Journal Article
Randomized Controlled Trial
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
97-107Informations de copyright
© 2020 Wiley Periodicals, LLC.
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