A Rising Single Oral Dose Study to Investigate the Tolerability, Pharmacokinetics and Dopamine ß-hydroxylase (DßH) Inhibition Profile of BIA 5-453 in Healthy Male Volunteers

NCT02845037 Phase 1 COMPLETED

The purpose of this study is to assess the safety and tolerability of BIA 5-453 after single oral doses

Details

Lead sponsor	Bial - Portela C S.A.
Phase	Phase 1
Status	COMPLETED
Enrolment	80
Start date	2007-05
Completion	2007-09

Conditions

• Hypertension
• Chronic Heart Failure

Interventions

• BIA 5-453
• Placebo

Primary outcomes

• Maximum observed plasma concentration (Cmax) — Day 1 pre-dose then at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60, and 72 hours post-dose
  Mean BIA 5-453 plasma pharmacokinetic parameters ± SD following single doses of 2, 10, 20, 50, 100, 200, 400, 600, 900 and 1200 mg of BIA 5-453 in 10 groups of 6 healthy volunteers each
• Time to reach Cmax (Tmax) — Day 1 pre-dose then at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60, and 72 hours post-dose
  Mean BIA 5-453 plasma pharmacokinetic parameters ± SD following single doses of 2, 10, 20, 50, 100, 200, 400, 600, 900 and 1200 mg of BIA 5-453 in 10 groups of 6 healthy volunteers each
• Area under the plasma concentration-time curve from time 0 to the time of last quantifiable concentration (AUC0-t) — Day 1 pre-dose then at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60, and 72 hours post-dose
  Mean BIA 5-453 plasma pharmacokinetic parameters ± SD following single doses of 2, 10, 20, 50, 100, 200, 400, 600, 900 and 1200 mg of BIA 5-453 in 10 groups of 6 healthy volunteers each
• Area under the plasma concentration-time curve from time 0 to the infinity (AUC0-∞) — Day 1 pre-dose then at 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60, and 72 hours post-dose
  Mean BIA 5-453 plasma pharmacokinetic parameters ± SD following single doses of 2, 10, 20, 50, 100, 200, 400, 600, 900 and 1200 mg of BIA 5-453 in 10 groups of 6 healthy volunteers each
• % of subjects with at least one adverse event — through study completion, an average of 72 hours
  Adverse events were continuously monitored from screening until the follow-up visit.
• % of subjects by dose group with at least one treatment-emergent adverse event (TEAEs) — through study completion, an average of 72 hours
  Treatment emergent adverse events (TEAE) were defined as adverse events which did not exist before dosing and appeared in the 72 hours following treatment administration or which was present before administration and worsened in the 72 hours following treatment administration.

Countries

France