Phase I and pharmacological studies of adriamycin administered intraperitoneally to patients with ovarian cancer.

Robert F. Ozols, Robert C. Young, James L. Speyer, Paul H. Sugarbaker, Raymond F. Greene, Jean Jenkins, Charles E. Myers

PubMed · 1982 · 223 citations · 0 references

Concepts

Abstract

Abstract A Phase I study of Adriamycin administered i.p. was performed in 10 ovarian cancer patients who were refractory to systemic chemotherapy. Adriamycin was infused in 2 liters of Inpersol via a semipermanent Tenckhoff dialysis catheter. Adriamycin was administered for a 4-hr dwell every 2 weeks with concentrations ranging from 9 to 54 µm. The dose-limiting toxicity of i.p. Adriamycin was a sterile peritonitis. Severe abdominal pain with ascites and adhesions was observed at concentrations greater than 36 µm. There were three objective responses, and two other patients had a marked reduction in ascites formation while on treatment. The objective responses were in patients who had small volume ( Adriamycin concentrations were measured by high-pressure liquid chromotography. A mean of 85% of the drug was absorbed over the 4-hr dwell time. The concentrations attained i.p. have been demonstrated previously to be cytotoxic to human ovarian cancer cells from untreated patients or from patients who had relapsed after treatment with a non-Adriamycin combination. Plasma levels peaked within the first hr after i.p. instillation. Plasma levels were markedly lower than corresponding peritoneal concentrations. The maximum pharmacological advantage (peak peritoneal concentration/peak plasma concentration) was 474, while the 4-hr peritoneal level was 166 times higher than the corresponding plasma level after an i.p. dose of 40 mg/2 liters (36 /µm). The peak plasma levels after a 60-mg/2 liters (54 µm) dose were 10 times lower than after a 60-mg i.v. dose. The recommended starting dose for a Phase II trial is 27 to 36 µm (30 to 40 mg Adriamycin per 2 liters Inpersol) with a 4-hr dwell every 2 to 3 weeks for six cycles.