Between-course targeting of methotrexate exposure using pharmacokinetically guided dosage adjustments

Cancer Chemother Pharmacol. 2013 Aug;72(2):369-78. doi: 10.1007/s00280-013-2206-x. Epub 2013 Jun 13.

Abstract

Purpose: It is advantageous to individualize high-dose methotrexate (HDMTX) to maintain adequate exposure while minimizing toxicities. Previously, we accomplished this through within-course dose adjustments.

Methods: In this study, we evaluated a strategy to individualize HDMTX based on clearance of each individual's previous course of HDMTX in 485 patients with newly diagnosed acute lymphoblastic leukemia. Doses were individualized to achieve a steady-state plasma concentration (Cpss) of 33 or 65 μM (approximately 2.5 or 5 g/m(2)/day) for low- and standard-/high-risk patients, respectively.

Results: Individualized doses resulted in 70 and 63 % of courses being within 20 % of the targeted Cpss in the low- and standard-/high-risk arms, respectively, compared to 60 % (p < 0.001) and 61 % (p = 0.43) with conventionally dosed therapy. Only 1.3 % of the individualized courses in the standard-/high-risk arm had a Cpss greater than 50 % above the target compared to 7.3 % (p < 0.001) in conventionally dosed therapy. We observed a low rate (8.5 % of courses) of grade 3-4 toxicities. The odds of gastrointestinal toxicity were related to methotrexate plasma concentrations in both the low (p = 0.021)- and standard-/high-risk groups (p = 0.003).

Conclusions: Individualizing HDMTX based on the clearance from the prior course resulted in fewer extreme Cpss values and less delayed excretion compared to conventional dosing.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Algorithms
  • Antidotes / administration & dosage
  • Antidotes / therapeutic use
  • Antimetabolites / administration & dosage*
  • Antimetabolites / pharmacokinetics*
  • Antimetabolites / therapeutic use
  • Dose-Response Relationship, Drug
  • Drug Delivery Systems
  • Fluorescence Polarization Immunoassay
  • Gastrointestinal Diseases / chemically induced
  • Humans
  • Injections, Spinal
  • Leucovorin / administration & dosage
  • Leucovorin / therapeutic use
  • Methotrexate / administration & dosage*
  • Methotrexate / pharmacokinetics*
  • Methotrexate / therapeutic use
  • Models, Biological
  • Precision Medicine
  • Precursor Cell Lymphoblastic Leukemia-Lymphoma / drug therapy*

Substances

  • Antidotes
  • Antimetabolites
  • Leucovorin
  • Methotrexate