Heparanase inhibitor PI-88 as adjuvant therapy for hepatocellular carcinoma after curative resection: a randomized phase II trial for safety and optimal dosage

J Hepatol. 2009 May;50(5):958-68. doi: 10.1016/j.jhep.2008.12.023. Epub 2009 Feb 15.

Abstract

Background/aims: Hepatocellular carcinoma recurrence after curative treatment adversely influences clinical outcome. It is important to explore adjuvant therapies. This phase II/stage 1 multi-center, randomized trial investigated the safety, optimal dosage and preliminary efficacy of PI-88, a novel heparanase inhibitor, in the setting of post-operative recurrence of HCC according to a Simon's 2-stage design.

Methods: Three groups were included: one untreated arm (Group A) and two PI-88 arms (Group B: 160 mg/day; Group C: 250 mg/day). Treatment groups received PI-88 over nine 4-week treatment cycles, followed by a 12-week treatment-free period. Safety and optimal dosage were assessed.

Results: Overall, 172 patients were randomized and 168 were included in the intention-to-treat (ITT) population. Treatment-related adverse effects included cytopenia, injection site hemorrhage, PT prolongation, etc. Four serious adverse events were possibly related to PI-88 treatment. One (1.8%) group B patients and six (10.5%) group C had hepatotoxicity-related withdrawals. Among the ITT population, 29 patients (50%) in Group A, 35 (63%) in Group B, and 22 (41%) in Group C remained recurrence-free at completion. Calculated T(1) value suggested 160 mg/day treatment satisfied the criteria for the next stage of the trial.

Conclusions: PI-88 at 160 mg/day is optimal and safe, and shows preliminary efficacy as an adjunct therapy for post-operative HCC.

Trial registration: ClinicalTrials.gov NCT00247728.

Publication types

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

MeSH terms

  • Adult
  • Aged
  • Carcinoma, Hepatocellular / drug therapy*
  • Carcinoma, Hepatocellular / surgery*
  • Chemotherapy, Adjuvant
  • Combined Modality Therapy
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / adverse effects
  • Enzyme Inhibitors / therapeutic use*
  • Female
  • Glucuronidase / antagonists & inhibitors*
  • Humans
  • Liver Neoplasms / drug therapy*
  • Liver Neoplasms / surgery*
  • Male
  • Middle Aged
  • Neoplasm Recurrence, Local / prevention & control
  • Oligosaccharides / adverse effects
  • Oligosaccharides / therapeutic use*
  • Treatment Outcome

Substances

  • Enzyme Inhibitors
  • Oligosaccharides
  • phosphomannopentaose sulfate
  • heparanase
  • Glucuronidase

Associated data

  • ClinicalTrials.gov/NCT00247728