This study was designed to investigate the multiple-dose pharmacokinetics of a range of intransal doses of IS-159, a serotonin 1B/1D receptor agonist. Intranasal doses of 1, 2, 4 and 6 mg of IS-159 were administered twice at an interval of 4 hours to 17 healthy male and female subjects in a two-way crossover study. Plasma concentrations of IS-159 were determined from blood samples taken at regular intervals up to 24 hours after the first administration during both treatment periods. IS-159 was rapidly absorbed and eliminated with a t(max) of approximately 15 min and a t(1/2) of approximately 1.6 hours. With increasing dose, the exposure increased dose-proportionally, and IS-159 pharmacokinetics appear not to be influenced by gender and food intake. The results showed dose-proportional pharmacokinetics of IS-159 in the dose range tested and a low propensity for drug accumulation.

01 Aug 2000·Clinical Pharmacology & TherapeuticsQ2 · MEDICINE

Pronounced effect of caprylocaproyl macrogolglycerides on nasal absorption of IS-159, a peptide serotonin 1B/1D-receptor agonist

Q2 · MEDICINE

Article

Author: Jasper Dingemanse ; Olivier Blin ; Pascale Pisano ; Catherine Soubrouillard ; Jérôme Paris

OBJECTIVESThis double-blind, randomized, two-way crossover study in 12 healthy male subjects investigated the influence of caprylocaproyl macrogolglycerides on the pharmacokinetics of IS-159 (serotonin-carboxylmethyleneoxy-L-tyrosylglycinamide), a peptide serotonin 1B/1D-receptor agonist, after intranasal administration.METHODSA dose of 4 mg IS-159 was administered in a volume of 200 microL, once in the presence and once in the absence of 2% caprylocaproyl macrogolglycerides. Plasma concentrations of IS-159 were measured over a period of 12 hours for determination of pharmacokinetic parameters. Systemic and local tolerability were assessed at regular time points, the latter by rhinoscopy and visual analog scales.RESULTSCaprylocaproyl macrogolglycerides significantly increased the maximum plasma concentration (from 4.7 +/- 1.7 to 48 +/- 17 ng/mL) and the area under the plasma concentration-time curve (from 12 +/- 4.7 to 56 +/- 22 ng x h/mL) of IS-159. The time to maximum concentration (15 to 20 minutes) and the elimination half-life (2.0 to 2.3 hours) were not different between the two treatments. Rhinoscopic examination revealed no differences between treatments, but in the presence of caprylocaproyl macrogolglycerides subjects reported more local and systemic adverse events and on the visual analog scales greater nasal obstruction and rhinorrhea.CONCLUSION2% caprylocaproyl macrogolglyceride markedly increased the absorption of IS-159 through the nasal mucosa and elicited only mild irritant effects.

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Indication	Highest Phase	Country/Location	Organization	Date
Migraine Disorders	Phase 2	FR	Immunotech	-
Migraine Disorders	Phase 2	US	The Medicines Co.	-
Migraine Disorders	Phase 2	-	The Medicines Company (Spain) SL	-
Migraine Disorders	Phase 2	-	Immunotech Laboratories, Inc.	-

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