A phase I clinical and pharmacology study using amifostine as a radioprotector in dose-escalated whole liver radiation therapy

Int J Radiat Oncol Biol Phys. 2012 Aug 1;83(5):1441-7. doi: 10.1016/j.ijrobp.2011.10.020. Epub 2012 Mar 21.

Abstract

Purpose: Diffuse intrahepatic tumors are difficult to control. Whole-liver radiotherapy has been limited by toxicity, most notably radiation-induced liver disease. Amifostine is a prodrug free-radical scavenger that selectively protects normal tissues and, in a preclinical model of intrahepatic cancer, systemic amifostine reduced normal liver radiation damage without compromising tumor effect. We hypothesized that amifostine would permit escalation of whole-liver radiation dose to potentially control microscopic disease. We also aimed to characterize the pharmacokinetics of amifostine and its active metabolite WR-1065 to optimize timing of radiotherapy.

Methods and materials: We conducted a radiation dose-escalation trial for patients with diffuse, intrahepatic cancer treated with whole-liver radiation and intravenous amifostine. Radiation dose was assigned using the time-to-event continual reassessment method. A companion pharmacokinetic study was performed.

Results: Twenty-three patients were treated, with a maximum dose of 40 Gy. Using a logistical regression model, compared with our previously treated patients, amifostine increased liver tolerance by 3.3 ± 1.1 Gy (p = 0.007) (approximately 10%) with similar response rates. Peak concentrations of WR-1065 were 25 μM with an elimination half-life of 1.5 h; these levels are consistent with radioprotective effects of amifostine in patients.

Conclusion: These findings demonstrate for the first time that amifostine is a normal liver radioprotector. They further suggest that it may be useful to combine amifostine with fractionated or stereotactic body radiation therapy for patients with focal intrahepatic cancer.

Publication types

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

MeSH terms

  • Adult
  • Aged
  • Amifostine / pharmacokinetics
  • Amifostine / therapeutic use*
  • Bile Duct Neoplasms / metabolism
  • Bile Duct Neoplasms / radiotherapy*
  • Bile Ducts, Intrahepatic
  • Carcinoma, Hepatocellular / metabolism
  • Carcinoma, Hepatocellular / radiotherapy*
  • Cholangiocarcinoma / metabolism
  • Cholangiocarcinoma / radiotherapy*
  • Female
  • Humans
  • Liver / drug effects
  • Liver / metabolism
  • Liver / radiation effects*
  • Liver Neoplasms / metabolism
  • Liver Neoplasms / radiotherapy*
  • Liver Neoplasms / secondary
  • Logistic Models
  • Male
  • Maximum Tolerated Dose
  • Mercaptoethylamines / pharmacokinetics
  • Middle Aged
  • Organs at Risk / radiation effects
  • Prospective Studies
  • Radiation Dosage
  • Radiation Injuries / prevention & control
  • Radiation Tolerance / drug effects
  • Radiation-Protective Agents / pharmacokinetics
  • Radiation-Protective Agents / therapeutic use*
  • Radiotherapy Planning, Computer-Assisted
  • Radiotherapy, Conformal

Substances

  • Mercaptoethylamines
  • Radiation-Protective Agents
  • N-(2-mercaptoethyl)-1,3-diaminopropane
  • Amifostine