Epoetin

Information about Epoetin

Epoetin is a recombinant form of erythropoietin, a hematologic growth factor that induces proliferation and maturation of red blood cells and is used in the treatment of anemia caused by renal disease, myelodysplasia, cancer chemotherapy and hematopoietic cell transplantation.

Liver safety of Epoetin

Epoetin and its various derivatives have not been associated with serum enzyme elevations during therapy or with instances of clinically apparent liver injury.

Epoetin

Epoetin (e poe' e tin) is a recombinant form of erythropoietin, a 165 amino acid glycoprotein that induces red blood cell production from their progenitors in the bone marrow.

Erythropoietin is normally made in the kidneys and acts on progenitor erythroblasts through the erythropoietin receptor to cause proliferation and maturation of red cells. The major stimulus to erythropoietin synthesis is tissue hypoxia, but other factors can modulate the response. Deficiency of erythropoietin synthesis is common in end stage renal disease and may also be present in premature infants and in patients with malignancies, chronic inflammation and cancer chemotherapy. Recombinant forms of erythropoietin became available in the 1980’s and were shown to raise hemoglobin and hematocrit levels in patients with end stage renal disease on hemodialysis, as well as in patients receiving cancer chemotherapy and patients with AIDS on drugs that cause anemia.

FDA approval information for Epoetin

Epoetin alfa was approved for use to treat anemia in patients with renal disease and receiving cancer chemotherapy in 1989 and is now widely used. Indications have broadened to include reduction of allogeneic red cell transfusion in patients undergoing elective surgery and it is used off-label for other forms of anemia associated with relative erythropoietin deficiency. The target hemoglobin level is usually between 11 and 12 g/dL. Epoetin alfa is available as a liquid solution for subcutaneous administration in vials and prefilled syringes under the brands name Epogen and Procrit, the dose and regimen varying by indication and initial response, being given by subcutaneous or intravenous injection at intervals varying from daily, several times weekly, weekly or as needed to achieve a target hemoglobin.

Darbepoetin

Longer acting formulations are also available including darbepoetin (Aranesp: 2001) and peginesatide (Omontys, 2012, now withdrawn). Darbepoetin alfa (dar” be poe’ e tin) is a modified (hyperglycosylated) recombinant erythropoietin that has an extended half-life and can be administered every one to three weeks.

Dosage and administration for Epoetin

Darbepoetin is available in single dose vials and prefilled syringes of varying concentrations and is administered intravenously or subcutaneously. Peginesatide (peg” in es’ a tide) is a novel synthetic pegylated dipeptide that mimics the effects of erythropoietin on red cell progenitors, despite having no amino acid homology to the native growth factor. Peginesatide was typically given either subcutaneously or intravenously at 4 week intervals, but was withdrawn from the market in 2013 because of reports of severe hypersensitivity reactions. Epoetin, darbepoetin and peginesatide are collectively referred to as erythropoiesis-stimulating agents (ESA). Dosages and dose regimens (daily, three times weekly, weekly, and every two to four weeks) vary by formulation, indications and initial response.

Side effects of Epoetin

Common side effects include hypertension (particularly in patients with renal disease), muscle and joint aches, fever, dizziness, headache, depression, cough and injection site reactions. Potentially serious, but rare side effects include hypersensitivity reactions, vascular occlusions, stroke and myocardial infarction.

Hematologic Agents Eculizumab, Emapalumab, Emicizumab, Lanadelumab, Ravulizumab

Hematologic Growth Factors

• Granulocyte colony stimulating factors
  • Filgrastim, Pegfilgrastim

• Granulocyte-Macrophage Colony Stimulating Factors
  • Sargramostim

• Erythropoiesis stimulating agents
  • Epoetin, Darbepoetin, Peginesatide

Thrombopoietin receptor agonists and Thrombopoiesis Stimulators

• • Avatrombopag, Eltrombopag, Fostamatinib, Lusutrombopag, Romiplostim, Oprelvekin (IL-11)

• Dailymed label info on Epoetin
• FDA Epoetin

Epoetin Resources
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