Phase I study of liposomal annamycin

Daniel J. Booser, Roman Perez-Soler, Paul Cossum, Laura Esparza-Guerra, Qing Ping Wu, Yiyu Zou, Waldemar Priebe, Gabriel N. Hortobagyi

Research output: Contribution to journalArticlepeer-review

14 Scopus citations


Annamycin is a highly lipophilic anthracycline with the ability to bypass the MDR-1 mechanism of cellular drug resistance. In this phase I study, annamycin entrapped in liposomes was administered by a 1- to 2-h intravenous infusion at 3-week intervals. Thirty-six patients with relapsed solid tumors were treated and 109 courses were administered at doses ranging from 3 to 240 mg/m2. The dose-limiting toxicity was thrombocytopenia. Five patients had a probable allergic reaction, requiring discontinuation of treatment in one. Treatment was well tolerated otherwise. No cardiac toxicity was seen on endomyocardial biopsy of four patients studied. There was limited gastrointestinal toxicity and no alopecia. No objective tumor responses were observed. Pharmacokinetic studies at 24, 120 and 240 mg/m2 showed a biexponential plasma concentration-versus-time profile. There was a linear relationship between the dose and the maximal plasma concentration with relatively constant plasma clearance values. The maximum tolerated dose (MTD) for liposomal annamycin defined in this study is 210 mg/m2. Because of a subsequent change in the formulation of the drug, future studies will use 190 mg/m2 as the MTD.

Original languageEnglish (US)
Pages (from-to)427-432
Number of pages6
JournalCancer Chemotherapy and Pharmacology
Issue number5
StatePublished - 2000
Externally publishedYes


  • Anthracycline
  • Pharmacokinetics
  • Phase I study

ASJC Scopus subject areas

  • Oncology
  • Toxicology
  • Pharmacology
  • Cancer Research
  • Pharmacology (medical)


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