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Xemilofiban/orbofiban: insight into drug development

R Anders1, J Kleiman, N Nicholson

  • 1Searle/Pharmacia Pharmaceuticals, 5200 Old Orchard Road, OO-II-3102, Skokie, IL 60077, USA. robert.j.anders@monsanto.com

Cardiovascular Drug Reviews
|August 3, 2001
PubMed

Insights

Oral glycoprotein IIb/IIIa receptor antagonists like xemilofiban and orbofiban were evaluated for chronic use in unstable angina. Despite promising mechanisms, pivotal trials did not demonstrate significant clinical benefits.

Area of Science:

  • Cardiology
  • Pharmacology
  • Thrombosis

Background:

  • Intravenous glycoprotein IIb/IIIa receptor antagonists show success in acute settings like unstable angina and percutaneous interventions.
  • The potential for chronic platelet aggregation inhibition led to the development of oral agents for longer-term use.

Purpose of the Study:

  • To review and evaluate the development programs of oral glycoprotein IIb/IIIa receptor antagonists, specifically xemilofiban and orbofiban.
  • To understand the selection process for therapeutic targets based on pharmacokinetic and pharmacodynamic profiles.
  • To analyze pivotal Phase III trial results and identify reasons for the lack of demonstrated benefit.

Main Methods:

  • Review of development programs for xemilofiban and orbofiban.
  • Analysis of pharmacokinetic and pharmacodynamic data.
  • Evaluation of pivotal Phase III clinical trial outcomes.

Main Results:

  • The development of oral glycoprotein IIb/IIIa antagonists was explored for chronic administration in cardiovascular conditions.
  • Pivotal Phase III trials for xemilofiban and orbofiban were conducted to assess efficacy and safety.
  • These agents did not show significant clinical benefit in the trials reviewed.

Conclusions:

  • Despite a strong theoretical basis and promising initial research, oral glycoprotein IIb/IIIa receptor antagonists did not translate into significant clinical benefits in Phase III trials.
  • Further investigation into the complex pharmacokinetic and pharmacodynamic responses was insufficient to overcome the lack of efficacy.
  • The development of these specific agents for chronic use in unstable angina was ultimately unsuccessful.

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