A phase 2 study to assess the pharmacokinetics and pharmacodynamics of CPX-351 and its effects on cardiac repolarization in patients with acute leukemias

Cancer Chemother Pharmacol. 2019 Jul;84(1):163-173. doi: 10.1007/s00280-019-03856-9. Epub 2019 May 16.

Abstract

Purpose: Daunorubicin can induce left ventricular dysfunction and QT interval prolongation. This study assessed the effects of CPX-351, a liposomal encapsulation of cytarabine and daunorubicin, on cardiac repolarization.

Methods: Twenty-six adults with acute leukemia were treated with CPX-351 for 1-2 induction cycles and ≤ 4 consolidation cycles. The primary endpoint was mean change in QTcF from baseline.

Results: Mean QTcF changes were < 10 ms at all time points. No clinically meaningful effects on heart rate, QRS interval, PR interval, or QTcB were observed. Estimated mean half-lives for total cytarabine and daunorubicin were > 30 h. Thirteen (50%) patients achieved remission. The most common adverse events were febrile neutropenia, fatigue, and nausea.

Conclusions: The cytarabine and daunorubicin in CPX-351 liposomes were metabolized and excreted similarly to conventional formulation; however, plasma pharmacokinetics were altered. CPX-351 did not prolong the QT interval, suggesting that CPX-351 may induce less cardiotoxicity than previously reported for conventional daunorubicin.

Trial registration: Clinicaltrials.gov identifier: NCT02238925.

Keywords: Acute lymphoblastic leukemia; Acute myeloid leukemia; Cardiac repolarization; Pharmacodynamics; Pharmacokinetics.

Publication types

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

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Antineoplastic Combined Chemotherapy Protocols / administration & dosage*
  • Antineoplastic Combined Chemotherapy Protocols / adverse effects
  • Antineoplastic Combined Chemotherapy Protocols / pharmacokinetics
  • Cytarabine / administration & dosage*
  • Cytarabine / adverse effects
  • Cytarabine / pharmacokinetics
  • Daunorubicin / administration & dosage*
  • Daunorubicin / adverse effects
  • Daunorubicin / pharmacokinetics
  • Drug Combinations
  • Female
  • Half-Life
  • Humans
  • Leukemia, Myeloid, Acute / drug therapy*
  • Liposomes
  • Male
  • Middle Aged
  • Treatment Outcome

Substances

  • CPX-351
  • Drug Combinations
  • Liposomes
  • Cytarabine
  • Daunorubicin

Associated data

  • ClinicalTrials.gov/NCT02238925