The evaluation of drug rechallenge: the casopitant Phase III program

Regul Toxicol Pharmacol. 2010 Dec;58(3):539-43. doi: 10.1016/j.yrtph.2010.09.014. Epub 2010 Oct 13.

Abstract

Drug rechallenge (or reinitiation), following an event of drug-induced liver injury, is associated with 13% mortality in prospective series. Rechallenge generally results in much more rapid injury than the initial liver event. The neurokinin-1 antagonist casopitant or its placebo was administered cyclically with ondansetron and dexamethasone in two randomized chemotherapy-induced nausea and vomiting clinical trials in nearly 3000 subjects. Grade 3 ALT elevations were observed in up to 2% of subjects receiving casopitant or placebo treatment. Similar rates of positive rechallenge were observed in the casopitant 8/29 (28%) and placebo groups 2/8 (25%), with no Grade 4 ALT elevations, hypersensitivity or liver-related serious adverse events. Publishing available rechallenge data (positive and negative) will advance our clinical understanding. Rechallenge should only be considered when the potential drug benefit exceeds the risk.

Publication types

  • Clinical Trial, Phase III
  • Multicenter Study
  • Randomized Controlled Trial

MeSH terms

  • Administration, Oral
  • Antiemetics / administration & dosage
  • Antiemetics / adverse effects*
  • Antineoplastic Agents / adverse effects
  • Dexamethasone / administration & dosage
  • Dexamethasone / adverse effects*
  • Dose-Response Relationship, Drug
  • Female
  • Humans
  • Male
  • Nausea / chemically induced
  • Nausea / drug therapy
  • Neurokinin-1 Receptor Antagonists*
  • Ondansetron / administration & dosage
  • Ondansetron / adverse effects
  • Piperazines / administration & dosage
  • Piperazines / adverse effects*
  • Piperidines / administration & dosage
  • Piperidines / adverse effects*
  • Serotonin Antagonists / administration & dosage
  • Serotonin Antagonists / adverse effects
  • Vomiting / chemically induced
  • Vomiting / drug therapy

Substances

  • Antiemetics
  • Antineoplastic Agents
  • Neurokinin-1 Receptor Antagonists
  • Piperazines
  • Piperidines
  • Serotonin Antagonists
  • casopitant
  • Ondansetron
  • Dexamethasone