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1. Alfa Hexal, Epoetin
2. Alfa, Epoetin
3. Binocrit
4. Compound, Hx575
5. Epoetin Alfa
6. Epoetin Alfa Hexal
7. Epogen
8. Eprex
9. Heberitro
10. Hexal, Epoetin Alfa
11. Hx575
12. Hx575 Compound
13. Procrit
14. Recombinant 1 165 Erythropoietin, Glycoform Alpha
15. Recombinant 1-165 Erythropoietin, Glycoform Alpha
1. Epoetin Alfa
2. 113427-24-0
3. (4r,5s,6s,7r,9r,10r,11e,13e,16r)-10-[(2r,4r,5s,6s)-4,5-dihydroxy-4,6-dimethyloxan-2-yl]oxy-6-[(2s,3r,4r,5s,6r)-5-[(2r,4r,5s,6s)-4,5-dihydroxy-4,6-dimethyloxan-2-yl]oxy-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-4-hydroxy-7-(2-hydroxyethyl)-5-methoxy-9,16-dimethyl-1-oxacyclohexadeca-11,13-dien-2-one
4. Zinc263583856
| Molecular Weight | 848.0 g/mol |
|---|---|
| Molecular Formula | C42H73NO16 |
| XLogP3 | 0.8 |
| Hydrogen Bond Donor Count | 7 |
| Hydrogen Bond Acceptor Count | 17 |
| Rotatable Bond Count | 10 |
| Exact Mass | 847.49293524 g/mol |
| Monoisotopic Mass | 847.49293524 g/mol |
| Topological Polar Surface Area | 236 Ų |
| Heavy Atom Count | 59 |
| Formal Charge | 0 |
| Complexity | 1370 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 20 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 2 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently Bonded Unit Count | 1 |
Hematinics
National Library of Medicine's Medical Subject Headings online file (MeSH, 1999)
Epoetin is indicated for the treatment of anemia associated with chronic renal failure in adults and children. It is used for adults and children who do not require dialysis as well as adults and children receiving dialysis (continuous peritoneal dialysis, high-flux short-time hemodialysis, or conventional hemodialysis). However, in patients not receiving dialysis, use of epoetin should be limited to individuals having hemoglobin less than 10 g per dL. /Included in US product label/
Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2007., p. 1248
Epoetin is indicated for the treatment of severe anemia associated with zidovudine therapy in HIV-infected adults and children. Epoetin is not indicated for the treatment of anemia in HIV-infected patients due to other factors. Epoetin is effective in decreasing the transfusion requirement and increasing the red blood cell level of anemic, HIV-infected patients treated with zidovudine, when the endogenous serum erythropoietin level is less than or equal to 500 mUnits per mL and when patients are receiving a dose of zidovudine less than or equal to 4200 mg per week. /Included in US product label/
Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2007., p. 1248
Epoetin is indicated for the treatment of anemia in adults and children with nonmyeloid malignancies in which the anemia is due to the effect of concomitantly administered chemotherapy. Epoetin is indicated to decrease the need for transfusions in patients who will be receiving concomitant chemotherapy for a minimum of 2 months. Epoetin is not indicated for the treatment of anemia in cancer patients due to other factors such as iron or folate deficiencies, hemolysis, or gastrointestinal bleeding, which should be managed appropriately. /Included in US product label/
Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2007., p. 1248
For more Therapeutic Uses (Complete) data for EPOETIN ALFA (12 total), please visit the HSDB record page.
FDA notified healthcare professionals of new safety information for erythropoiesis-stimulating agents (ESAs) darbepoetin alfa (Aranesp), epoetin alfa (Epogen and Procrit). Four new studies in patients with cancer found a higher chance of serious and life-threatening side effects or death with the use of ESAs. These research studies were evaluating an unapproved dosing regimen, a patient population for which ESAs are not approved, or a new unapproved ESA. FDA believes these new concerns apply to all ESAs and is re-evaluating how to safely use this product class. FDA and Amgen, the manufacturer of Aranesp, Epogen and Procrit, have changed the full prescribing information for these drugs to include a new boxed warning, updated warnings, and a change to the dosage and administration sections for all ESAs.
McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007.
FDA notified healthcare professionals of the results from a large clinical trial evaluating use of an erythropoiesis-stimulating agent (ESA) to treat anemia in cancer patients not receiving chemotherapy. In this study, patients received either darbepoetin alfa (Aranesp), an ESA, according to the approved dosing regimen or placebo. Patients treated with darbepoetin alfa had a higher death rate and no reduction in the need for transfusions compared to those treated with placebo. The findings in the darbepoetin alfa study may apply to other ESAs. Additionally, the findings show that treating anemic cancer patients not currently on chemotherapy with an ESA may offer no benefit and may cause serious harm.
McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007.
On November 8, 2007, FDA approved new labeling strengthening the Boxed Warning and Warnings sections of the labeling for Epogen/Procrit and Aranesp and summarizing the results of six studies showing decreased survival and/or tumor progression in patients with cancer receiving an ESA. This communication provides you with the findings from two additional clinical studies (PREPARE and GOG-191 studies) showing an increase in mortality and shorter time to tumor progression in patients with cancer receiving an ESA. This new information further underscores the safety concerns regarding the use of ESAs in patients with cancer addressed in previous communications. ... Both the PREPARE study in breast cancer and the GOG-191 study in cervical cancer showed higher rates of death and or tumor progression in patients who received an ESA compared to patients who did not receive an ESA.
FDA; Center for Drug Evaluation and Research; Communication about an Ongoing Safety Review: Erythropoiesis-Stimulating Agents (ESAs) Epoetin alfa (marketed as Procrit, Epogen) Darbepoetin alfa (marketed as Aranesp) (Last updated January 3, 2008). Available from, as of March 10, 2008: https://www.fda.gov/cder/drug/early_comm/ESA.htm
FDA is issuing this alert to provide new safety information for erythropoiesis-stimulating agents (ESAs) [Aranesp (darbepoetin alfa), Epogen (epoetin alfa), and Procrit (epoetin alfa)]. Analyses of four new studies in patients with cancer found a higher chance of serious and life-threatening side effects and/or death with the use of ESAs. These research studies were evaluating an unapproved dosing regimen, a patient population for which ESAs are not approved, or a new unapproved ESA. In another study, patients scheduled for orthopedic surgery had a higher rate of deep venous thrombosis when treated with Procrit at the approved dose. This new information is consistent with risks found in two clinical studies in patients with chronic renal failure treated with an unapproved regimen of an ESA that were reported in November 2006 ... All ESAs have the same mechanism of action. As a result, FDA believes these new concerns apply to all ESAs and is re-evaluating how to safely use this product class. FDA and Amgen, the manufacturer of Aranesp, Epogen and Procrit, have changed the full prescribing information for these drugs. The new product labeling includes a new boxed warning, updated warnings, and a change to the dosage and administration sections for all ESAs. ...[FDA; Center for Drug Evaluation and Research; Information for Healthcare Professionals Erythropoiesis Stimulating Agents (ESA)
Aranesp (darbepoetin), Epogen (epoetin alfa), and Procrit (epoetin alfa)] (Last updated March 9, 2007). Available from, as of March 10, 2008: https://www.fda.gov/cder/drug/InfoSheets/HCP/RHE2007HCP.htm
For more Drug Warnings (Complete) data for EPOETIN ALFA (55 total), please visit the HSDB record page.
Hematinics
Agents which improve the quality of the blood, increasing the hemoglobin level and the number of erythrocytes. They are used in the treatment of anemias. (See all compounds classified as Hematinics.)
Because of its protein nature, epoetin alfa is destroyed in the GI tract and must be administered parenterally (e.g., via IV infusion, subcutaneous injection, intraperitoneal instillation). Systemic absorption of epoetin alfa is delayed and incomplete following subcutaneous injection or intraperitoneal instillation. However, while serum concentrations peak sooner and are substantially higher with iv than subcutaneous injection of epoetin alfa, they are less sustained, and the iv route of administration generally offers no clinical advantage over the subcutaneous route except in patients with existing accessible iv sites (e.g., hemodialysis patients). In fact, limited evidence suggests that subcutaneous injection of epoetin alfa 3 times weekly can produce a hemoglobin response similar to that with iv administration but at lower dosages; other evidence indicates that dosages of epoetin alfa required for maintenance therapy generally are lower with subcutaneous than iv injection. The decreased and variable systemic absorption of subcutaneously administered epoetin alfa relative to iv administration may result from the lipophilicity and/or relatively large size of the molecule; degradation by peptidases in the skin also may be responsible. With usual epoetin alfa dosages of 50-300 units/kg 3 times weekly given either subcutaneously or iv, detectable serum concentrations of erythropoietin are maintained for at least 24 hours.
McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007., p. 1528
Serum erythropoietin concentrations exhibit considerable interindividual variation with a given epoetin alfa dose and route of administration. Peak serum erythropoietin concentrations following iv administration of 80, 120, or 150 units/kg of epoetin alfa reportedly range from 1200-1800, 3200-4700, or 3000-5000 mU/mL, respectively, in patients with chronic renal failure; in healthy adults, peak serum concentrations following iv administration of 150 or 300 units/kg of the drug average 3500 or 7300 mU/mL, respectively. Peak serum erythropoietin concentrations after subcutaneous injection of 50, 150, or 300 units/kg of epoetin alfa in healthy individuals averaged 36 (corrected for endogenous serum erythropoietin concentration), 144-226, or 285-288 mU/mL. Peak serum erythropoietin concentrations are achieved within 4-24 hours following subcutaneous injection of usual therapeutic doses of epoetin alfa, and serum erythropoietin concentrations generally remain above baseline for 2-4 days. Following iv doses of 50-300 units/kg of exogenous erythropoietin, serum erythropoietin concentrations generally decline to baseline levels within 1-3 days.
McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007., p. 1528
Serum erythropoietin concentrations peak sooner but are substantially lower following intraperitoneal instillation compared with subcutaneous injection, at least when the drug is administered via a dialysis solution. In addition, systemic absorption following intraperitoneal administration via a dialysis solution is substantially lower than that following iv administration. The bioavailability of epoetin alfa following subcutaneous or intraperitoneal (via a dialysis solution) administration reportedly ranges from 10-49 or 2.5-14%, respectively. Although such data suggest that intraperitoneal administration of epoetin alfa would be impractical, limited evidence in animals and humans suggests that systemic bioavailability following intraperitoneal instillation can be increased substantially (e.g., to 40%) by administering the drug into an empty peritoneal cavity; additional study is needed to determine the clinical feasibility of administering the drug by this method. In a study in patients undergoing continuous ambulatory peritoneal dialysis (CAPD), peak serum drug concentrations following a single IV or subcutaneous dose of 300 units/kg of epoetin alfa averaged 7688 or 484 mU/mL, respectively, and 108 or 170 mU/mL with intraperitoneal instillation (via a dialysis solution) for 4 or 12 hours (dwell time), respectively. Peak serum erythropoietin concentrations in these CAPD patients were achieved within 24-36 or 8-12 hours after subcutaneous or intraperitoneal administration, respectively. Systemic absorption (as determined by area under the serum concentration-time curve [AUC]) during the first 24 hours after intraperitoneal dosing was approximately 25-33% of that after subcutaneous injection.
McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007., p. 1529
Peak serum drug concentrations following subcutaneous injection of epoetin alfa appear to be reduced (by up to 40-70% compared with the first-dose peak) with multiple-dose administration of the drug. Limited evidence suggests that bioavailability of the drug following subcutaneous administration into the thigh is increased compared with subcutaneous administration into the arm or abdomen.
McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007., p. 1529
For more Absorption, Distribution and Excretion (Complete) data for EPOETIN ALFA (12 total), please visit the HSDB record page.
The metabolic fate of endogenous erythropoietin and the recombinant hormone (i.e., epoetin alfa) is poorly understood. Although some in vitro and animal data suggest that the kidney may be involved in erythropoietin metabolism, limited evidence in humans suggests otherwise. It also has been suggested that the physicochemical characteristics of the glycoprotein would impede access to potential sites of renal metabolism, thus limiting any contribution of the kidney in the degradation of the endogenous and recombinant hormones. Current evidence from studies in animals suggests that hepatic metabolism contributes only minimally to elimination of the intact hormone, but desialylated epoetin alfa (i.e., terminal sialic acid groups removed) appears to undergo substantial hepatic clearance via metabolic pathways and/or binding. Desialylation and/or removal of the oligosaccharide side chains of erythropoietin appear to occur principally in the liver; bone marrow also may have a role in catabolism of the hormone. Elimination of desialylated drug by the kidneys, bone marrow, and spleen also may occur; results of animal studies suggest that proximal renal tubular secretion may be involved in renal elimination.
McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007., p. 1529
Elimination /half-life/ may average 4 to 13 hours following intravenous or subcutaneous administration. The elimination half-life is generally higher after the first few doses (> 7.5 hours) than after 2 or more weeks treatment (6.2 hours after 7 doses; 4.6 hours after 24 doses).
Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2007., p. 1248
The elimination half-life of epoetin alfa following iv administration in healthy individuals and in adults and children with chronic renal failure ranges from 4-16 hours. There is some evidence that the elimination half-life of epoetin alfa may increase with increasing dosage, but a reduction in half-life during continuous dosing also has been reported. The half-life of epoetin alfa is similar in adults older or younger than 65 years of age. In patients with impaired renal function, a prolongation in elimination half-life relative to that in patients with normal renal function may occur; however, the elimination half-life does not appear to be affected by hemodialysis.
McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007., p. 1529
With continuous dosing at iv doses of 15-500 units/kg administered up to 3 times weekly, the elimination half-life of epoetin alfa may decrease over time. In patients undergoing hemodialysis, mean elimination half-life was reduced by 20-40% after several weeks to months of such dosing; no further reductions generally were observed beyond 3-4 months of continued therapy. Similar reductions in half-life with multiple dosing have been observed in predialysis patients; the mean half-life of the drug decreased by 40% after 8 weeks of therapy in one study. Although it has been suggested that this decrease in half-life may be related to increased clearance of the drug as more erythroid precursors are formed and increased numbers of erythropoietin receptors are made available, other studies have not found reductions in elimination half-life after continuous dosing.
McEvoy, G.K. (ed.). American Hospital Formulary Service. AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda, MD. 2007., p. 1529
Epoetin alfa is a glycoprotein, produced by recombinant DNA technology, that contains 165 amino acids in a sequence identical to that of endogenous human erythropoietin. Recombinant epoetin has the same biological activity as the endogenous hormone, which induces erythropoiesis by stimulating the division and differentiation of committed erythroid progenitor cells, including burst-forming units-erythroid, colony-forming units- erythroid, erythroblasts, and reticulocytes, in bone marrow. Erythropoietin also induces the release of reticulocytes from the bone marrow into the blood stream, where they mature into erythrocytes.
Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2007., p. 1248
Endogenous erythropoietin is produced primarily in the kidney. The anemia associated with chronic renal failure is caused primarily by inadequate production of the hormone. Administration of epoetin corrects the erythropoietin deficiency in patients with chronic renal failure. Epoetin also stimulates red blood cell production in patients who do not have a documented erythropoietin deficiency, i.e., patients with normal or slightly elevated concentrations of endogenous erythropoietin. However, it may not be effective in patients who are anemic despite having significantly elevated concentrations of erythropoietin.
Thomson/Micromedex. Drug Information for the Health Care Professional. Volume 1, Greenwood Village, CO. 2007., p. 1248
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