New avenues of exploration for erythropoietin.
The study demonstrated that erythropoietin (EPO) has significant cytoprotective roles in neuronal and vascular systems, with potential applications in various disorders.
EPO · Epoetin · Procrit · Epogen
Erythropoietin (Epo) is a glycoprotein hormone primarily produced in the kidneys, with additional production occurring in the liver. Researchers primarily study Epo for its critical role in stimulating the production of red blood cells (RBCs), which enhances tissue oxygenation and is particularly relevant in conditions such as anemia. Key findings indicate that Epo secretion is stimulated by hypoxia, and its receptor is expressed in various tissues, including the central nervous system, where it may exert neuroprotective effects. Clinical evidence suggests that recombinant forms of Epo have been misused in sports for performance enhancement, leading to ongoing challenges in doping control. Current research continues to explore Epo's broader physiological roles and its potential applications in various medical conditions, underscoring its significance in both hematology and neurology.
Erythropoietin (EPO) is an endogenous glycoprotein hormone primarily produced in the kidneys, with the liver serving as an extra-renal site of production. It is composed of 165 amino acids and is characterized by three N-glycosylation and one O-glycosylation sites. EPO is also available in synthetic forms, such as recombinant human erythropoietin (rHuEPO) and its analogs, including epoetin and darbepoetin. Researchers have found that EPO plays a crucial role in erythropoiesis, stimulating the proliferation and differentiation of erythrocyte precursors, thereby increasing red blood cell mass and enhancing tissue oxygenation. This hormone has been extensively studied for its potential neuroprotective effects, particularly in the context of hypoxia-ischemia in the central nervous system. EPO exerts its effects by binding to the erythropoietin receptor (Epo-R), a multimeric protein that initiates intracellular signaling pathways leading to erythropoiesis and neurogenesis. The receptor is expressed in various tissues, including the CNS, where it influences neural progenitor cells, neurons, and other cell types. Pharmacokinetic studies have shown that the bioavailability of subcutaneously administered epoetin is about 20-30%, with a plasma half-life of over 24 hours, while darbepoetin has a longer half-life of approximately 48 hours. Clinically, EPO is used to treat anemia, particularly in patients with renal disease or chemotherapy-induced anemia. It is banned in sports due to its performance-enhancing effects. Regulatory agencies such as the World Anti-Doping Agency monitor its use in athletics. In medical practice, its use is guided by established clinical guidelines to minimize adverse effects such as hypertension and thrombotic complications.
| Formel | C42H73NO16 |
| Molekulargewicht | 848g/mol |
| CAS-Nummer | 113427-24-0 |
| PubChem CID | 92043599 |
Erythropoietin acts primarily on the erythropoietin receptor (Epo-R), which is expressed on erythroid progenitor cells. Upon binding, it activates intracellular signaling pathways that promote erythrocyte proliferation and differentiation, enhancing oxygen delivery to tissues.
Erythropoietin (Epo) exerts its effects primarily through the erythropoietin receptor (Epo-R), a multimeric protein that activates the JAK2/STAT5 signaling pathway upon Epo binding. This activation promotes the proliferation and differentiation of erythroid progenitor cells in the bone marrow, enhancing erythropoiesis and subsequently increasing red blood cell production. While the primary mechanism is well-characterized, aspects of Epo-R structure and additional signaling pathways remain incompletely understood.
Circulating half-life ~5-9 hours
Bioavailability ~20-30%, half-life >24 hours
Half-life ~4-13 hours
Poor bioavailability due to first-pass metabolism
Darbepoetin has a longer half-life (~48 hours) compared to epoetin.
Temperature
Refrigerate at 2-8C
Light
Protect from light
Form
Aqueous solution: use within specified period after opening
Notes
Do not freeze; discard if frozen.
Erythropoietin is soluble in water, facilitating its formulation as an injectable solution.
🇩🇪DE
Verschreibungspflichtig (prescription only); not a controlled substance under BtMG.
🇺🇸US
FDA approved for specific indications; prescription required.
🇦🇺AU
TGA Schedule 4 (prescription only medicine).
🇬🇧UK
Prescription only medicine (POM) under MHRA regulations.
Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.
Current evidence is limited regarding the long-term effects and safety profiles of various erythropoietin analogs, particularly in specific populations such as cancer patients and premature infants. Further research is needed to clarify the mechanisms underlying the neuroprotective effects of erythropoietin in the central nervous system, as well as to identify the accessory chains of the erythropoietin receptor that remain elusive. Additionally, larger randomized controlled trials are necessary to evaluate the efficacy and safety of different administration routes and dosing regimens in diverse patient populations, particularly those at high risk for thromboembolic events.
3,621
Total Citations
8
Human/RCT
4.3
Avg. Influence
2019
Latest
The study demonstrated that erythropoietin (EPO) has significant cytoprotective roles in neuronal and vascular systems, with potential applications in various disorders.
Researchers observed that erythropoietin (EPO) has diverse biological effects in non-haematopoietic tissues, indicating its potential as a therapeutic agent in neurological and cardiovascular diseases.
The study demonstrated that the magnitude of increase in red blood cell concentration in response to recombinant human erythropoietin is primarily controlled by the duration of EPO concentration maintenance rather than its level.
Researchers observed that erythropoietin plays a significant role in brain development and neuroprotection, with potential therapeutic implications for brain ischemia and trauma.
The study demonstrated that erythropoietin is essential for erythropoiesis and has potential cytoprotective effects outside the bone marrow, particularly in chronic kidney disease.
The study demonstrated that erythropoietin's actions extend beyond erythropoiesis, influencing multiple tissues and metabolic responses, particularly during ischemic stress.
Researchers observed that multiple factors, including iron deficiency and inflammation, contribute to hyporesponsiveness to recombinant human erythropoietin (rh-Epo) in patients with renal failure.
Researchers observed that the pharmacokinetics of epoetin vary with administration routes, with subcutaneous delivery showing prolonged serum concentrations compared to intravenous administration.
Researchers observed that erythropoietin exhibits angiogenic activity in various tissues, suggesting its potential role in both protective and pathological processes.
The study demonstrated that erythropoietin gene expression is regulated by various transcription factors, and novel compounds are being explored to stimulate endogenous EPO production.
41
Total Trials
11,257
Total Enrolled
Hospital Authority, Hong Kong
66
2001
endothelial function and atherosclerosis
Penang Hospital, Malaysia
44
2015
Mean change in haemoglobin levels
University of Aarhus
35
2011
Changes in serum protein isoforms measured by proteomics
University of Copenhagen
12
2022
Changes in CD71 expression
Hillerod Hospital, Denmark
11
2008
Cognitive function
Ortho Pharmaceuticals
Hoffmann-La Roche
102
2010
Mean time taken to achieve target hemoglobin (Hb) levels range (10-12 g/dL) During Efficacy Evaluation Period (EEP)
Hoffmann-La Roche
90
Hb level, decline in renal function, 24h proteinuria, creatinine clearance.
Germans Trias i Pujol Hospital
74
2005
Percentage of patients with undetectable RNA-HCV
Hoffmann-La Roche
1
2007
Change in Hb concentration between baseline and efficacy evaluation period (EEP).
Amgen
Subject preference
GlaxoSmithKline
3,872
2016
Time to First Occurrence of Adjudicated Major Adverse Cardiovascular Event (MACE) During Cardiovascular (CV) Events Follow-up Time Period (Non-inferiority Analysis)
Amgen
2,549
2009
Overall Survival (OS)
Giovanni FM Strippoli, MD
656
2009
TSAT (transferrin saturation), serum albumin, serum ferritin, serum transferrin, serum C reactive protein
Amgen
420
2005
Ratio of weekly dose at the evaluation period to the weekly dose at baseline
Johnson & Johnson Pharmaceutical Research & Development, L.L.C.
316
1993
Proportion of patients in each treatment group, overall, and within each baseline hemoglobin group requiring blood transfusion following major orthopedic surgery
Astellas Pharma Inc
303
2016
Change from baseline in the average hemoglobin (Hb)
Deutsches Herzzentrum Muenchen
138
2006
Left ventricular ejection fraction measured by magnetic resonance imaging
Hoffmann-La Roche
111
2007
Percentage of Patients Able to Maintain Hemoglobin (Hb) Within 10-12 g/dL
University Eye Hospital, Freiburg
108
2014
Global retinal nerve fibre layer thickness (RNFLT-G)
Azidus Brasil
92
2013
Change of hemoglobin levels at correction phase (baseline vs end of treatment)
The First Affiliated Hospital of Soochow University
76
2023
The treatment response
Hoffmann-La Roche
61
2003
Percentage of Participants With Response to Treatment
Johnson & Johnson Pharmaceutical Research & Development, L.L.C.
60
2001
Number of red blood cell transfusions
Johnson & Johnson Pharmaceutical Research & Development, L.L.C.
51
2005
Percent of patients that achieved a hematopoietic response, defined as a Hb increase >= 2 g/dL and/or Hb = 12 g/dL during the study independent of transfusion within 28 days
Ain Shams University
18
2024
Clinical Scoring
Sheri Kashmir Institute of Medical Sciences
100
2012
Death or moderate or severe disability at 18-22 months of age
University Medical Center Groningen
529
2007
Left ventricular ejection fraction 6 weeks after primary PCI, measured with planar radionuclide ventriculography
Amgen
300
2001
Proportion of subjects whose baseline score on the subjective FCST correctly estimates the baseline MHST score
Amgen
300
2002
Exercise tolerance
Johnson & Johnson Pharmaceutical Research & Development, L.L.C.
235
2006
Hemoglobin (Hb) Change From Baseline to Study Week 7
Imperial College London
150
2021
Primary outcome measure (Mean (SD) of thalamic NAA level)
Groupe Francophone des Myelodysplasies
99
2004
To evaluate the efficacy of association of Erythropoetin and ATRA in patients with low risk myelodysplastic syndromes
Shenyang Sunshine Pharmaceutical Co., LTD.
80
2025
Incidence and severity of adverse events (AEs) and serious adverse events (SAEs) Events (NCI-CTCAE V5.0).
GlaxoSmithKline
80
2012
Modeled Hemoglobin (Hgb) Change From Baseline (Pre-dose on Day 1) at 4 Weeks of Treatment
Johnson & Johnson Pharmaceutical Research & Development, L.L.C.
32
2006
The Number of Patients Who Developed Peripheral Sensory Neuropathy (National Cancer Institute Common Toxicity Criteria (NCI CTC) Score >= 1) at Week 12.
Johnson & Johnson Pharmaceutical Research & Development, L.L.C.
29
2004
To assess changes in fatigue in patients at least 18 years old with chronic rheumatoid arthritis (RA) and chronic anemia (Hb < 11.0 g/dL) due to ACD receiving weekly s.c. doses of PROCRIT versus placebo.
Johnson & Johnson Pharmaceutical Research & Development, L.L.C.
11
2005
The primary endpoint is the hemoglobin response rate, defined as the proportion of subjects who achieve at least a 1 gram per deciliter hemoglobin increase from baseline by Week 17.
Johnson & Johnson Pharmaceutical Research & Development, L.L.C.
9
2004
To assess the change in physical function from baseline to end of study as measured by the Short Physical Performance Battery (SPPB) summary score.
Amgen
2002
Anemia correction
Ajou University School of Medicine
37
2010
Functional status of the participants after 6 months of procedure assessed by modified Rankin Scale.
Log cycles, set reminders and visualize serum levels.
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