Assessment of Sunitinib-Induced Toxicities and Clinical Outcomes Based on Therapeutic Drug Monitoring of Sunitinib for Patients With Renal Cell Carcinoma

Clin Genitourin Cancer. 2015 Aug;13(4):350-358. doi: 10.1016/j.clgc.2015.01.007. Epub 2015 Jan 21.

Abstract

Background: Sunitinib has been approved for the treatment of metastatic renal cell carcinoma (RCC). Sunitinib pharmacokinetics shows a large interpatient variability.

Patients and methods: A retrospective, observational clinical study of 21 patients with RCC was performed. Sunitinib was administered for 4 weeks of a 6-week cycle for the first cycle. We evaluated the association of sunitinib-induced toxicities and clinical outcomes with the trough total sunitinib concentration in a steady state during the first cycle.

Results: The median total sunitinib concentration was 91.8 ng/mL (range, 49.8-205 ng/mL). There was an association between total sunitinib concentration and the severity of thrombocytopenia, anorexia, and fatigue. Patients with ≥ 100 ng/mL total sunitinib (n = 8), compared with patients with < 100 ng/mL (n = 13), had a greater incidence of Grade ≥ 3 toxicities (6 patients [75.0%] vs. 3 patients [23.1%]). Patients with < 100 ng/mL total sunitinib had significantly longer time to treatment failure (TTF) and progression-free survival (PFS) time than patients with ≥ 100 ng/mL (median TTF, 590 vs. 71 days; P = .04; median PFS, 748 vs. 238 days; P = .02).

Conclusion: Results of this study suggest that therapeutic drug monitoring of sunitinib could be useful for avoiding severe toxicities. Dose reduction might be needed, especially when the total sunitinib concentration is ≥ 100 ng/mL, to avoid unnecessary early discontinuation of treatment.

Keywords: Individualized pharmacotherpy; Kidney cancer; Pharmacokinetics; Tolerability; Tyrosine kinase inhibitor.

Publication types

  • Clinical Study
  • Multicenter Study
  • Observational Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aged
  • Aged, 80 and over
  • Angiogenesis Inhibitors / adverse effects*
  • Angiogenesis Inhibitors / pharmacokinetics
  • Angiogenesis Inhibitors / therapeutic use
  • Carcinoma, Renal Cell / drug therapy*
  • Carcinoma, Renal Cell / genetics
  • Carcinoma, Renal Cell / mortality
  • Disease-Free Survival
  • Female
  • Gene Frequency
  • Humans
  • Indoles / adverse effects*
  • Indoles / pharmacokinetics
  • Indoles / therapeutic use
  • Kaplan-Meier Estimate
  • Kidney Neoplasms / drug therapy*
  • Kidney Neoplasms / genetics
  • Kidney Neoplasms / mortality
  • Male
  • Middle Aged
  • Polymorphism, Single Nucleotide
  • Pyrroles / adverse effects*
  • Pyrroles / pharmacokinetics
  • Pyrroles / therapeutic use
  • Retrospective Studies
  • Sunitinib
  • Treatment Outcome

Substances

  • Angiogenesis Inhibitors
  • Indoles
  • Pyrroles
  • Sunitinib