Pharmacokinetics and tolerability of single escalating doses of fampridine sustained-release tablets in patients with multiple sclerosis: a Phase I-II, open-label trial

Clinical Therapeutics
T Vollmer, Herbert R Henney

Abstract

Fampridine (4-aminopyridine) is a potassium channel-blocking agent that has been reported to have therapeutic potential for improving walking and mobility in patients with multiple sclerosis (MS). A sustained-release (SR) formulation of fampridine was developed to improve the agent's pharmacokinetic profile by extending its t((1/2)) relative to that of immediate-release fampridine. The primary study objective was to examine the pharmacokinetics of fampridine SR tablets after single escalating doses in patients with MS. Tolerability was evaluated as a secondary end point. This multicenter, Phase I-II, open-label trial evaluated the dose proportionality and tolerability of 4 single doses of fampridine SR (5, 10, 15, and 20 mg) in patients with MS. There was a 4-day washout between doses. Blood samples were collected immediately before drug administration, hourly for the first 8 hours after administration, and at 10, 12, 14, 18, and 24 hours after administration. The pharmacokinetic parameters evaluated included C(max), T(max), AUC, elimination rate constant, apparent elimination t((1/2)), and apparent CL/F. Twelve-lead ECGs were obtained at baseline (0.5 hour before dosing) and at 1, 4, 12, and 24 hours after drug administration ...Continue Reading

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