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[Bropirimine (U-54461S) phase I clinical studies]
14th Dept. of Internal Medicine, School of Medicine, Teikyo University.
Gan to Kagaku Ryoho. Cancer & Chemotherapy
|December 1, 1996
Summary
Bropirimine, an oral interferon inducer, showed tolerability in cancer patients during Phase I studies. Consecutive day dosing effectively induced interferon and suggested potential antitumor activity, warranting further investigation.
Area of Science:
- Oncology
- Pharmacology
- Immunology
Background:
- Bropirimine (U-54461S) is a novel oral antitumor agent with interferon (IFN) inducing and direct antiproliferative properties.
- Phase I studies are crucial for evaluating novel cancer therapeutics' safety and pharmacokinetic profiles.
Purpose of the Study:
- To assess the safety and pharmacokinetics of bropirimine tablets in cancer patients.
- To measure interferon concentrations following bropirimine administration.
- To explore preliminary clinical antitumor efficacy.
Main Methods:
- Single and multiple-dose studies of bropirimine tablets were conducted in cancer patients.
- Dosing regimens included single doses (0.25-3g) and multiple doses (1-2g) over one or consecutive days.
- Adverse events, laboratory abnormalities, IFN levels, and tumor response were monitored.
Main Results:
- Bropirimine was generally well-tolerated, with common adverse events including malaise, fever, and nausea.
- Interferon induction was observed in 18.8% of patients with one-day dosing and 85.7% with consecutive-day dosing.
- Two cases showed tumor size reduction and symptom improvement with one-day dosing.
Conclusions:
- A regimen of 1g bropirimine orally every two hours, three times daily for three consecutive days, followed by a four-day drug-free interval, was determined to be tolerable.
- This regimen demonstrated potential for interferon induction and preliminary antitumor effects, supporting its advancement to early Phase II studies.