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Multiple-dose, placebo-controlled, phase I study of oral dolasetron
T L Hunt1, M Cramer, J Christy-Bittel
1Laboratories of Pharmaco LSR, Inc., Austin, Texas, USA.
Pharmacotherapy
|March 1, 1996
Summary
Oral dolasetron mesylate was well tolerated in healthy volunteers up to 200 mg/day. This new 5-HT3 antagonist demonstrated good safety and predictable pharmacokinetics, with mild adverse events.
Area of Science:
- Pharmacology
- Clinical Pharmacology
- Drug Safety
Background:
- 5-HT3 antagonists are crucial in managing nausea and vomiting.
- Dolasetron mesylate is a novel agent in this class.
Purpose of the Study:
- To assess the safety and tolerability of escalating oral doses of dolasetron mesylate.
- To characterize the pharmacokinetic profile of dolasetron mesylate.
Main Methods:
- A double-blind, placebo-controlled, randomized phase I study.
- Forty healthy male volunteers received single and multiple oral doses of dolasetron mesylate (25-200 mg) or placebo.
- Safety, tolerability, and pharmacokinetics were evaluated over 9 days.
Main Results:
- Dolasetron mesylate was well tolerated across all tested dose levels.
- Adverse events, primarily headache and constipation, were generally mild and not dose-dependent.
- No significant changes in laboratory values or vital signs were observed.
- Pharmacokinetics of the active metabolite were dose-independent.
Conclusions:
- Oral dolasetron mesylate is safe and well-tolerated in healthy volunteers at doses up to 200 mg/day.
- The drug exhibits predictable pharmacokinetics and a favorable safety profile.
- Dolasetron mesylate represents a promising option for antiemetic therapy.