Phase I trial of zoledronic acid + imatinib mesylate (Gleevec) in patients with bone metastases

Am J Clin Oncol. 2010 Feb;33(1):75-8. doi: 10.1097/COC.0b013e31819cccdc.

Abstract

Objectives and methods: Patients with bone metastases suffer from long-term skeletal morbidity and a reduction in quality of life. Treatment consists of radiation or surgery to prevent or repair fractures and bisphosphonates to delay skeletal-related events (SRE). Platelet-derived growth factor released from metastatic cancer cells may influence the development and progression of bone metastases. Imatinib mesylate (Gleevec) inhibits platelet-derived growth factor-receptor tyrosine kinase signaling, increases apoptosis, reduces proliferation, and lowers microvessel density in human tumors. This phase I study assessed the effects of the combination of zoledronic acid (a bisphosphonate used to delay SRE) and Gleevec on 15 evaluable patients with osteolytic or osteoblastic bone metastases.

Results: Although 6 of 9 patients noted an improvement in pain and 1 patient was stable, the quality of life improved in only 3 patients. Dose limiting toxicity was observed in 0 of 5 (400 mg Gleevec), 2 of 5 (600 mg), and 4 of 5 (800 mg) patients. Although no patient required radiation and only 2 SRE occurred during the study, disease progression in bone and/or extraskeletal sites occurred in most patients.

Conclusion: The combination of zoledronic acid + Gleevec is not recommended in patients with bone metastases because of toxicity and limited clinical efficacy.

Publication types

  • Clinical Trial, Phase I
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aged
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use*
  • Benzamides
  • Bone Neoplasms / drug therapy*
  • Bone Neoplasms / secondary
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / pathology
  • Diphosphonates / administration & dosage
  • Female
  • Humans
  • Imatinib Mesylate
  • Imidazoles / administration & dosage
  • Kidney Neoplasms / drug therapy*
  • Kidney Neoplasms / pathology
  • Male
  • Maximum Tolerated Dose
  • Neoplasm Staging
  • Piperazines / administration & dosage
  • Prognosis
  • Prostatic Neoplasms / drug therapy*
  • Prostatic Neoplasms / pathology
  • Pyrimidines / administration & dosage
  • Sarcoma / drug therapy*
  • Sarcoma / secondary
  • Survival Rate
  • Treatment Outcome
  • Zoledronic Acid

Substances

  • Benzamides
  • Diphosphonates
  • Imidazoles
  • Piperazines
  • Pyrimidines
  • Zoledronic Acid
  • Imatinib Mesylate