First-in-human, phase I/IIa dose-escalation and safety study of balugrastim in breast cancer patients receiving myelosuppressive chemotherapy

Cancer Chemother Pharmacol. 2015 May;75(5):929-39. doi: 10.1007/s00280-015-2703-1. Epub 2015 Mar 5.

Abstract

Purpose: To evaluate safety of balugrastim, a recombinant human serum albumin and granulocyte colony-stimulating factor (G-CSF), administered over a range of therapeutic doses in women with breast cancer receiving doxorubicin plus docetaxel chemotherapy.

Methods: The phase I, sequential dose-escalation first segment compared subcutaneous balugrastim 50, 150, 300, and 450 µg/kg during chemotherapy cycles 0-2. The randomized (2:2:1), open-label, phase IIa second segment compared balugrastim 300 or 450 µg/kg with pegfilgrastim 6 mg during chemotherapy cycles 1 and 2.

Results: In the phase I segment, balugrastim was escalated to 450 µg/kg in 13 patients without dose-limiting toxicity. Three (9.7 %) of the 31 adverse events (AEs) reported in nine patients were grade 3 (agranulocytosis, vomiting, hypertension); none was grade 4. In the open-label phase IIa segment (N = 51), the majority of the 64 AEs reported in 31 (75.6 %) balugrastim-treated patients were grade 1 (59.4 %), with 39.1 % grade 2, 1.6 % grade 3 (one AE of vomiting), and none grade 4. Of the 16 AEs reported in seven (70.0 %) pegfilgrastim-treated patients, 87.5 % were grade 1, 6.3 % were grade 2, 6.3 % were grade 3 (one AE of thrombocytopenia), and none were grade 4. Overall, there were six bone pain AEs reported, one in the balugrastim 300 µg/kg group and five in the balugrastim 450 µg/kg group. No AEs in either study necessitated treatment interruption/discontinuation. The incidence and duration of grade 3-4 neutropenia were similar between balugrastim- and pegfilgrastim-treated patients.

Conclusions: Balugrastim was well tolerated in this small population of breast cancer patients.

Publication types

  • Clinical Trial, Phase I
  • Clinical Trial, Phase II
  • Multicenter Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Antineoplastic Combined Chemotherapy Protocols / adverse effects
  • Antineoplastic Combined Chemotherapy Protocols / pharmacokinetics
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use*
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / metabolism
  • Docetaxel
  • Dose-Response Relationship, Drug
  • Doxorubicin / administration & dosage
  • Doxorubicin / adverse effects
  • Doxorubicin / pharmacokinetics
  • Female
  • Filgrastim
  • Granulocyte Colony-Stimulating Factor / adverse effects
  • Granulocyte Colony-Stimulating Factor / pharmacokinetics
  • Granulocyte Colony-Stimulating Factor / therapeutic use*
  • Humans
  • Middle Aged
  • Polyethylene Glycols
  • Recombinant Fusion Proteins / adverse effects
  • Recombinant Fusion Proteins / pharmacokinetics
  • Recombinant Fusion Proteins / therapeutic use*
  • Recombinant Proteins / adverse effects
  • Recombinant Proteins / pharmacokinetics
  • Recombinant Proteins / therapeutic use
  • Serum Albumin / adverse effects
  • Serum Albumin / pharmacokinetics
  • Serum Albumin / therapeutic use*
  • Serum Albumin, Human
  • Taxoids / administration & dosage
  • Taxoids / adverse effects
  • Taxoids / pharmacokinetics

Substances

  • Recombinant Fusion Proteins
  • Recombinant Proteins
  • Serum Albumin
  • Taxoids
  • Granulocyte Colony-Stimulating Factor
  • Docetaxel
  • pegfilgrastim
  • Polyethylene Glycols
  • Doxorubicin
  • Filgrastim
  • balugrastim
  • Serum Albumin, Human