Clinical efficacy and safety of first-line nilotinib therapy and evaluation of the clinical utility of the FRET-based drug sensitivity test

Int J Hematol. 2019 Oct;110(4):482-489. doi: 10.1007/s12185-019-02696-w. Epub 2019 Jun 25.

Abstract

Nilotinib is widely used for primary treatment of patients with chronic myelogenous leukemia (CML). We previously reported that use of an FRET-based drug sensitivity test at diagnosis efficiently predicts the response to treatment with imatinib or dasatinib. Here, we conducted a phase-II study to evaluate the efficacy and safety of nilotinib treatment and identify useful biomarkers, including results of the FRET-based drug sensitivity test, for predicting treatment response. Data from 42 patients were used in the analysis. Major molecular response (MMR), MR4, and MR4.5 rates at 12 months were 64.3, 42.9, and 28.6%, respectively. Grade 3/4 non-hematologic adverse events occurred in 11 patients (26.2%). The dose intensity of nilotinib (> 76.44%) and halving time (HT, < 13.312 days) were identified as significant factors for MMR at 12 months. However, when we focused on patients whose dose intensity of nilotinib was > 76.44%, the FRET-based drug sensitivity test became a predictive factor of MR4 achievement at 12 months. Our study reconfirmed the efficacy and safety of nilotinib treatment in CML patients. Moreover, our results suggest that the FRET-based drug sensitivity test is an independent predictor for achievement of MR4 in patients treated with a sufficient dose intensity of nilotinib.

Keywords: BCR-ABL; Chronic myeloid leukemia (CML); Drug sensitivity test; Förster resonance energy transfer (FRET); Tyrosine kinase inhibitor.

Publication types

  • Clinical Trial, Phase II

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Aged, 80 and over
  • Antineoplastic Agents / administration & dosage*
  • Antineoplastic Agents / pharmacology*
  • Dose-Response Relationship, Drug
  • Drug Resistance, Neoplasm*
  • Drug Screening Assays, Antitumor / methods
  • Female
  • Fluorescence Resonance Energy Transfer / methods*
  • Humans
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive / diagnosis
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive / drug therapy*
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive / pathology*
  • Male
  • Middle Aged
  • Predictive Value of Tests
  • Pyrimidines / administration & dosage*
  • Pyrimidines / pharmacology*
  • Time Factors
  • Young Adult

Substances

  • Antineoplastic Agents
  • Pyrimidines
  • nilotinib