A Phase I study of bortezomib plus irinotecan in patients with advanced solid tumors

Cancer. 2006 Dec 1;107(11):2688-97. doi: 10.1002/cncr.22280.

Abstract

Background: The authors conducted a Phase I dose-finding trial to study the use of combined bortezomib plus irinotecan in patients with advanced solid tumors.

Methods: Patients who had received >/=1 prior chemotherapy regimen were eligible. Patients received bortezomib (1.0 mg/m(2), 1.3 mg/m(2), or 1.5 mg/m(2)) on Days 1, 4, 8, and 11 and received irinotecan (from 50 mg/m(2) to 125 mg/m(2)) on Days 1 and 8 of each 21-day cycle for a maximum of 8 cycles. Bortezomib followed irinotecan on coadministration days in Cycle 1 and Cycles 3 through 8 but preceded irinotecan in Cycle 2 to assess the effect of administration sequence on bortezomib pharmacodynamics.

Results: Fifty-one enrolled patients with malignancies, including colorectal cancer (n = 23 patients), lung cancer (n = 6 patients), gastroesophageal cancer (n = 6 patients), and pancreatic cancer (n = 3 patients), received >/=1 dose of study drug. Nausea, vomiting, and diarrhea were the principal dose-limiting toxicities and led to the maximum tolerated doses of 1.3 mg/m(2) bortezomib and 125 mg/m(2) irinotecan. The most common grade >/=3 bortezomib-related nonhematologic adverse events were fatigue (n = 5 episodes), diarrhea (n = 4 episodes), and nausea (n = 4 episodes). grade >/=3 bortezomib-related hematologic adverse events included neutropenia (n = 6 episodes) and thrombocytopenia (n = 4 episodes) and rarely were dose limiting. Of 34 evaluable patients, no objective responses according to the Response Evaluation Criteria in Solid Tumors were seen; 10 patients achieved stable disease. The degree of proteasome inhibition in whole blood indicated that the biologic activity of bortezomib was unaffected by irinotecan coadministration.

Conclusions: The results of this Phase I study in patients with solid tumors indicated that bortezomib at a dose of 1.3 mg/m(2) on Days 1, 4, 8, and 11 plus irinotecan at a dose of 125 mg/m(2) on Days 1 and 8 every 21 days were the recommended Phase II doses.

Publication types

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

MeSH terms

  • Adult
  • Aged
  • Antineoplastic Combined Chemotherapy Protocols / adverse effects*
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use*
  • Boronic Acids / administration & dosage
  • Boronic Acids / adverse effects
  • Bortezomib
  • Camptothecin / administration & dosage
  • Camptothecin / adverse effects
  • Camptothecin / analogs & derivatives
  • Female
  • Humans
  • Irinotecan
  • Male
  • Middle Aged
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology
  • Proteasome Inhibitors
  • Pyrazines / administration & dosage
  • Pyrazines / adverse effects

Substances

  • Boronic Acids
  • Proteasome Inhibitors
  • Pyrazines
  • Bortezomib
  • Irinotecan
  • Camptothecin