Epoetin Alfa
Recombinant human erythropoietin for anemia treatment in chronic kidney disease and chemotherapy.
Chemical Identity
| Property | Value |
|---|---|
| Molecular Weight | ~30.4 kDa |
| CAS Number | 113427-24-0 |
| Peptide Class | Recombinant Glycoprotein |
| Sequence | Identical to human EPO |
| Route | IV, SC |
Structure
Epoetin alfa (Epogen, Procrit) is recombinant human erythropoietin produced in Chinese hamster ovary (CHO) cells. It has the same 165-amino acid sequence as endogenous EPO with similar glycosylation, though glycan patterns may differ slightly from endogenous EPO.
Mechanism of Action
Epoetin alfa binds EPOR on erythroid progenitor cells, activating JAK2/STAT5 signaling to promote survival, proliferation, and differentiation of red blood cell precursors. Increases reticulocyte count within 10 days and hemoglobin within 2-6 weeks.
Clinical Applications
- CKD anemia: First-line ESA therapy
- Chemotherapy-induced anemia: When hemoglobin <10 g/dL
- HIV/Zidovudine anemia: When endogenous EPO <500 mU/mL
- Surgical blood conservation: Reducing allogeneic transfusion
- Anemia of prematurity: In premature infants
Pharmacokinetics
- Half-life: 4-13 hours (IV), 24 hours (SC)
- Bioavailability: 21% (SC)
- Onset: Reticulocyte increase in 10 days
- Peak Hgb: 2-6 weeks
- Route: IV, SC (SC preferred for longer half-life)
Safety and Side Effects
Hypertension (24%), headache, arthralgias, nausea, edema, seizures (with rapid Hgb rise), and pure red cell aplasia (rare, antibody-mediated). Boxed warning for increased mortality and cardiovascular events when targeting Hgb >11 g/dL.
References
- Eschbach, J.W., et al. (1987). Recombinant human erythropoietin in anemic patients with CKD. New England Journal of Medicine, 316, 73-78.
- Singh, A.K., et al. (2006). Normal hematocrit trial. New England Journal of Medicine, 355, 2085-2098.
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