Document Detail

Barusiban, an effective long-term treatment of oxytocin-induced preterm labor in nonhuman primates.
MedLine Citation:
PMID:  16914691     Owner:  NLM     Status:  MEDLINE    
Preterm labor (PTL) affects up to 25% of human pregnancies in developing countries, but there are few therapeutic options. Based on the key role of oxytocin (OXT) in labor and parturition, OXT antagonists are a potentially useful class of drugs for PTL. Barusiban is a new selective, potent, and long-acting OXT receptor antagonist. In this study barusiban was given by continuous i.v. infusion to monkeys during the last 3 wk of pregnancy; the monkeys were also given daily doses of OXT to induce uterine contractions and simulate PTL. Barusiban effectively suppressed OXT-induced PTL-like contractions and prevented early delivery. In contrast, fenoterol (a beta2-adrenoceptor [beta2-AR] agonist used as a comparative control) did not inhibit uterine contractions in this model. Barusiban was particularly effective in maintaining low intrauterine pressure (IUP) near the end of pregnancy, which is when IUP in both OXT controls and fenoterol-treated females increased substantially. Although barusiban delayed the onset of labor, it did not prevent normal delivery. These data demonstrate the safety and efficacy of barusiban in reducing uterine contractility in response to repeated OXT challenge, and suggest that barusiban may be therapeutically effective in long-term treatment of PTL.
Torsten M Reinheimer; Gary J Chellman; John C Resendez; Julie K Meyer; Walter H Bee
Publication Detail:
Type:  Journal Article     Date:  2006-08-16
Journal Detail:
Title:  Biology of reproduction     Volume:  75     ISSN:  0006-3363     ISO Abbreviation:  Biol. Reprod.     Publication Date:  2006 Nov 
Date Detail:
Created Date:  2006-10-23     Completed Date:  2007-02-26     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0207224     Medline TA:  Biol Reprod     Country:  United States    
Other Details:
Languages:  eng     Pagination:  809-14     Citation Subset:  IM    
Ferring Pharmaceuticals A/S, International PharmaScience Center, Department of Non-Clinical Development, Copenhagen S, 2300 Denmark.
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MeSH Terms
Adrenergic beta-Agonists / pharmacokinetics,  therapeutic use*
Fenoterol / pharmacokinetics,  therapeutic use*
Labor, Obstetric / drug effects
Macaca fascicularis
Obstetric Labor, Premature / drug therapy*
Oligopeptides / administration & dosage,  pharmacokinetics,  therapeutic use*
Oxytocin / pharmacology
Receptors, Oxytocin / antagonists & inhibitors*
Time Factors
Reg. No./Substance:
0/Adrenergic beta-Agonists; 0/Oligopeptides; 0/Receptors, Oxytocin; 0/barusiban; 13392-18-2/Fenoterol; 50-56-6/Oxytocin

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