Safety of recombinant human factor XIII in a cynomolgus monkey model of extracorporeal blood circulation

Toxicol Pathol. 2005;33(6):702-10. doi: 10.1080/15459620500330625.

Abstract

Factor XIII (FXIII) is a thrombin-activated plasma coagulation factor critical for blood clot stabilization and longevity. Administration of exogenous FXIII to replenish depleted stores after major surgery, including cardiopulmonary bypass, may reduce bleeding complications and transfusion requirements. Thus, a model of extracorporeal circulation (ECC) was developed in adult male cynomolgus monkeys (Macaca fascicularis) to evaluate the nonclinical safety of recombinant human FXIII (rFXIII). The hematological and coagulation profile in study animals during and after 2 h of ECC was similar to that reported for humans during and after cardiopulmonary bypass, including observations of anemia, thrombocytopenia, and activation of coagulation and platelets. Intravenous slow bolus injection of 300 U/kg (2.1 mg/kg) or 1000 U/kg (7 mg/kg) rFXIII after 2 h of ECC was well tolerated in study animals, and was associated with a dose-dependent increase in FXIII activity. No clinically significant effects in respiration, ECG, heart rate, blood pressure, body temperature, clinical chemistry, hematology (including platelet counts), or indicators of thrombosis (thrombin:anti-thrombin complex and D-Dimer) or platelet activation (platelet factor 4 and beta-thromboglobulin) were related to rFXIII administration. Specific examination of brain, heart, lung, liver, and kidney from rFXIII-treated animals provided no evidence of histopathological alterations suggestive of subclinical hemorrhage or thrombosis. Taken as a whole, the results demonstrate the ECC model suitably replicated the clinical presentation reported for humans during and after cardiopulmonary bypass surgery, and do not suggest significant concerns regarding use of rFXIII in replacement therapy after extracorporeal circulation.

MeSH terms

  • Animals
  • Blood Coagulation / drug effects
  • Blood Coagulation Disorders / blood
  • Blood Coagulation Disorders / drug therapy*
  • Cardiopulmonary Bypass*
  • Coagulants / administration & dosage
  • Coagulants / therapeutic use*
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Drug Evaluation, Preclinical
  • Extracorporeal Circulation*
  • Factor XIII / administration & dosage
  • Factor XIII / therapeutic use*
  • Humans
  • Macaca fascicularis
  • Male
  • Pilot Projects
  • Platelet Activation / drug effects
  • Postoperative Care
  • Postoperative Complications / blood
  • Postoperative Complications / drug therapy*
  • Recombinant Proteins / therapeutic use
  • Time Factors

Substances

  • Coagulants
  • Recombinant Proteins
  • Factor XIII