Epotiv Mechanism of Action

epoetin alfa


LG Chem Life Sciences




LG Chem Life Sciences
Full Prescribing Info
Pharmacology: Pharmacodynamics: Epotiv Prefilled Inj. is a glycoprotein that stimulates RBC production. It is produced mainly in the kidney and stimulates the division and differentiation of committed erythroid progenitors in the bone marrow. Epotiv Prefilled Inj. consists of a single 165 amino acid peptide chain with a total molecular weight of approximately 30,400 daltons when fully glycosylated. Epotiv Prefilled lnj. is produced by mammalian cells into which the human erythropoietin gene has been introduced. As a product of this recombinant DNA technology, Epotiv Prefilled lnj. has the same amino acid sequence as the naturally occurring hormone, and is functionally and immunologically similar to the endogenous form.
Mechanism of action: Epotiv Prefilled Inj. stimulates the proliferation, maturation, and differentiation of erythroid precursor cells in the bone marrow. The most primitive erythroid progenitor that responds to erythropoietin is called the burst-forming unit-erythroid (BFU-E) because it produces multiclustered colonies of Hb-synthesizing cells in response to increased concentrations of erythropoietin. The colony-forming unit-erythroid (CFU-E) has a lower proliferative potential than the BFU-E, and is absolutely dependent on erythropoietin for its ability to proliferate and differentiate. As differentiation of the erythroid cell line proceeds, erythropoietin dependence declines – a response associated with a loss of erythropoietin receptors.
The maturation time for red blood cell formation is approximately 7 days. During the first 4 days, cell proliferation and differentiation occur. During the remaining 3 days, maturation, including completion of Hb synthesis and nuclear extrusion, occurs. Erythropoietin production in the kidney is controlled by the oxygen-mediated feedback loop. The feedback loop is triggered by a reduction in erythrocyte-carried oxygen, and suppressed by restoration of adequate tissue oxygenation.
Pharmacokinetics: rhEPO is administered by IV or SC injection. Intravenously administered rhEPO is eliminated at a rate consistent with first order kinetics with a circulating half-life ranging from approximately 4 to 13 hours in patients with chronic renal failure (CRF). Within the therapeutic dose range, detectable levels of plasma erythropoietin are maintained for at least for 24 hours. After subcutaneous administration of rhEPO to patients with CRF, peak serum levels are achieved within 5-24 hours after administration and decline slowly thereafter. There is no apparent difference in half-life between patients not on dialysis whose serum creatinine levels were greater than 3, and patients maintained on dialysis. In normal volunteers, the half-life of intravenously administered rhEPO is approximately 20% shorter than the half-life in CRF patients. The pharmacokinetics of rhEPO has not been studied in HIV-infected patients.
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