Phase I trial of an interleukin-2 fusion toxin (DAB486IL-2) in hematologic malignancies: complete response in a patient with Hodgkin's disease refractory to chemotherapy

Cancer. 1994 Feb 15;73(4):1276-85. doi: 10.1002/1097-0142(19940215)73:4<1276::aid-cncr2820730424>3.0.co;2-d.

Abstract

Background: DAB486IL-2 is a recombinant fusion toxin in which the native diphtheria toxin-receptor binding-domain has been replaced with human interleukin-2 (IL-2). This molecule is specifically cytotoxic in vitro within 30 minutes for cells that express the high-affinity IL-2 receptor (IL-2R).

Methods: This was a Phase I/II study of DAB486IL-2 as a brief infusion in 15 patients with refractory lymphoid malignancies. Five patients per cohort received DAB486IL-2 as a 30-60 minute intravenous infusion at dose levels of 0.075, 0.115, and 0.2 mg/kg daily for 5 days.

Results: The maximal tolerated dose (MTD) of DAB486IL-2 was determined to be 0.2 mg/kg daily on the basis of hypersensitivity-like symptoms and reversible hepatic transaminase elevations. Other adverse effects included mild creatinine elevations, proteinuria, and hypoalbuminemia. The presence of antibodies to diphtheria toxin or DAB486IL-2 was correlated with hypersensitivity-like effects but did not prevent an antitumor effect. One complete response was observed in a patient with Hodgkin's disease in relapse with bilateral pulmonary nodules after autologous bone marrow transplantation. He remains free of disease more than 2 years after completion of therapy.

Conclusions: The dramatic antitumor response seen in one patient and the relative tolerability of DAB486IL-2 indicates the potential utility of this targeted agent in IL-2-expressing hematologic malignancies.

Publication types

  • Clinical Trial
  • Clinical Trial, Phase I
  • Clinical Trial, Phase II
  • Controlled Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Antineoplastic Agents / pharmacokinetics
  • Antineoplastic Agents / therapeutic use*
  • Biomarkers / blood
  • Diphtheria Toxin / administration & dosage
  • Diphtheria Toxin / adverse effects
  • Diphtheria Toxin / pharmacokinetics
  • Diphtheria Toxin / therapeutic use*
  • Drug Administration Schedule
  • Female
  • Hodgkin Disease / drug therapy*
  • Hodgkin Disease / immunology
  • Humans
  • Immune System / drug effects
  • Interleukin-2 / administration & dosage
  • Interleukin-2 / adverse effects
  • Interleukin-2 / pharmacokinetics
  • Interleukin-2 / therapeutic use*
  • Male
  • Middle Aged
  • Recombinant Fusion Proteins / pharmacokinetics
  • Recombinant Fusion Proteins / therapeutic use*
  • Remission Induction

Substances

  • Antineoplastic Agents
  • Biomarkers
  • DAB(486)-interleukin 2
  • Diphtheria Toxin
  • Interleukin-2
  • Recombinant Fusion Proteins