Phase I trial of the polyamine analog N1,N14-diethylhomospermine (DEHSPM) in patients with advanced solid tumors

Invest New Drugs. 2004 Apr;22(2):131-8. doi: 10.1023/B:DRUG.0000011789.79368.ae.

Abstract

Background: This phase I study was conducted to determine maximal tolerated dose (MTD) and dose-limiting toxicities (DLT) in patients with advanced solid tumors treated with the polyamine analog N1, N14-diethylhomospermine (DEHSPM).

Methods: Patients were treated with DEHSPM administered as a subcutaneous (SC) injection daily for five consecutive days repeated every 4 weeks. Three dose levels were examined starting at 12.5 mg/m2/day, escalating to 37.5 mg/m2/day.

Results: A total of 15 patients were enrolled. Dose limiting toxicities (grade 3 or 4) included nausea, vomiting, constipation, ileus, elevations of aspartate aminotransferase (AST) and alkaline phosphatase, hyperbilirubinemia, and ventricular bigeminy.

Conclusion: DEHSPM given as a SC injection is overall well tolerated at lower doses, but significant toxicities were observed at the 37.5mg/m2/day dose level. MTD was established at 25 mg/m2/day but further investigation with this study drug is not recommended secondary to the potential for neurotoxicities and hepatic damage as a result of cumulative doses.

Publication types

  • Clinical Trial
  • Clinical Trial, Phase I
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Aged
  • Dose-Response Relationship, Drug
  • Drug Administration Schedule
  • Female
  • Gastrointestinal Diseases / blood
  • Gastrointestinal Diseases / chemically induced
  • Humans
  • Male
  • Middle Aged
  • Neoplasms / blood
  • Neoplasms / drug therapy*
  • Polyamines / blood
  • Polyamines / chemistry
  • Polyamines / therapeutic use
  • Spermine / adverse effects
  • Spermine / analogs & derivatives*
  • Spermine / blood
  • Spermine / therapeutic use*

Substances

  • Polyamines
  • N(1),N(14)-bis(ethyl)homospermine
  • Spermine