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Trade names | Mircera |
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Routes of administration | Intravenous, subcutaneous |
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Methoxy polyethylene glycol-epoetin beta, sold under the brand name Mircera, is a long-acting erythropoietin receptor activator (CERA) used for the treatment of anaemia associated with chronic kidney disease. [4] It is the first approved, chemically modified erythropoiesis-stimulating agent (ESA).[ citation needed ]
It is on the World Health Organization's List of Essential Medicines. [6] It was approved for medical use in the European Union, [5] Switzerland,[ citation needed ] and the United States in 2007. [4]
Methoxy polyethylene glycol-epoetin beta is made from erythropoietin by chemically linking the N-terminal amino group or the ε-amino group of any lysine present in the protein with methoxy polyethylene glycol butanoic acid.[ citation needed ] The average molecular weight is approximately 60 kDa. [7] The drug stimulates erythropoiesis by interacting with the erythropoietin receptor on progenitor cells in the bone marrow. [7] It has a reduced receptor binding activity compared to other ESAs and but retains in vivo activity due to an extended serum half-life.[ medical citation needed ] It has an in vivo half-life of around 135 hours (5.6 days) as compared to darbepoetin alfa which has a half life of around 21 to 70 hours, the half life of which is three times that of the naturally occurring erthropoietin in the body.[ medical citation needed ]
A U.S. Federal Appeals Court ruled in September 2009, that Mircera infringed a patent held by Amgen Inc. The court refused to lift an injunction entered in the fall of 2008 which barred Roche from selling Mircera in the United States. [8] The injunction has since expired and Mircera has been available on the U.S. market since 2015. [9]
Mircera can reportedly replace traditional erythropoietin drugs as a blood doping agent in endurance sports. The drug appears to fall under section S2 of the list of substances officially prohibited - in competition and out of competition - in France and by the World Anti-Doping Agency. [10]
In July 2008, Italian bicycle racer Riccardo Riccò was disqualified from the Tour de France after reports that a urine sample tested positive for Mircera. [11] [12] There had not previously been any public acknowledgment that a test for the new drug was being administered, or had even been developed yet. The Tour de France testing was done under the auspices of the French Cycling Federation and the French Anti-Doping Agency, not the Union Cycliste Internationale. [13] [14]
Darbepoetin alfa (INN) is a re-engineered form of erythropoietin containing 5 amino acid changes resulting in the creation of 2 new sites for N-linked carbohydrate addition. It has a 3-fold longer serum half-life compared to epoetin alpha and epoetin beta. It stimulates erythropoiesis by the same mechanism as rHuEpo and is used to treat anemia, commonly associated with chronic kidney failure and cancer chemotherapy. Darbepoetin is marketed by Amgen under the trade name Aranesp.
Erythropoietin, also known as erythropoetin, haematopoietin, or haemopoietin, is a glycoprotein cytokine secreted mainly by the kidneys in response to cellular hypoxia; it stimulates red blood cell production (erythropoiesis) in the bone marrow. Low levels of EPO are constantly secreted in sufficient quantities to compensate for normal red blood cell turnover. Common causes of cellular hypoxia resulting in elevated levels of EPO include any anemia, and hypoxemia due to chronic lung disease and mouth disease.
ATC code B03Antianemic preparations is a therapeutic subgroup of the Anatomical Therapeutic Chemical Classification System, a system of alphanumeric codes developed by the World Health Organization (WHO) for the classification of drugs and other medical products. Subgroup B03 is part of the anatomical group B Blood and blood forming organs.
Anemia of chronic disease (ACD) or anemia of chronic inflammation is a form of anemia seen in chronic infection, chronic immune activation, and malignancy. These conditions all produce elevation of interleukin-6, which stimulates hepcidin production and release from the liver. Hepcidin production and release shuts down ferroportin, a protein that controls export of iron from the gut and from iron storing cells. As a consequence, circulating iron levels are reduced. Other mechanisms may also play a role, such as reduced erythropoiesis. It is also known as anemia of inflammation, or anemia of inflammatory response.
Epoetin alfa is a human erythropoietin produced in cell culture using recombinant DNA technology. Authorised by the European Medicines Agency on 28 August 2007, it stimulates erythropoiesis and is used to treat anemia, commonly associated with chronic kidney failure and cancer chemotherapy.
The 2008 Tour de France was the 95th running of the race. The event took place from 5 to 27 July. Starting in the French city of Brest, the tour entered Italy on the 15th stage and returned to France during the 16th, heading for Paris, its regular final destination, which was reached in the 21st stage. The race was won by Carlos Sastre.
Riccardo Riccò is an Italian professional road bicycle racer, who is suspended from all competition until 2024. He was previously ejected from the 2008 Tour de France for doping violations and suspended. Riccò returned to competition in late 2010, but in February 2011 he was fired by his team, Vacansoleil–DCM, after he became seriously ill allegedly through a self-administered autologous blood transfusion. He then signed to UCI Continental team Meridiana–Kamen.
PEGylation is the process of both covalent and non-covalent attachment or amalgamation of polyethylene glycol polymer chains to molecules and macrostructures, such as a drug, therapeutic protein or vesicle, which is then described as PEGylated. PEGylation affects the resulting derivatives or aggregates interactions, which typically slows down their coalescence and degradation as well as elimination in vivo.
The Festina affair was a series of doping scandals within the sport of professional cycling that occurred during and after the 1998 Tour de France. The affair began when a large haul of doping products was found in a support car belonging to the Festina cycling team just before the start of the race. A resulting investigation revealed systematic doping involving many teams in the Tour de France. Hotels where teams were staying were raided and searched by police, confessions were made by several retired and current riders, and team personnel were arrested or detained. Several teams withdrew completely from the race.
Macrogol, also known as polyethylene glycol (PEG), is used as a medication to treat constipation in children and adults. It is taken by mouth. Benefits usually occur within three days. Generally it is only recommended for up to two weeks. It is also used as an excipient. It is also used to clear the bowels before a colonoscopy, when the onset of the laxative effect is more rapid, typically within an hour.
Erythropoiesis-stimulating agents (ESA) are medications which stimulate the bone marrow to make red blood cells. They are used to treat anemia due to end stage kidney disease, chemotherapy, major surgery, or certain treatments in HIV/AIDS. In these situations they decrease the need for blood transfusions. The different agents are more or less equivalent. They are given by injection.
Epoetin beta (INN), sold under the brand name Neorecormon among others, is a synthetic, recombinant form of erythropoietin, a protein that promotes the production of red blood cells. It is an erythropoiesis-stimulating agent (ESA) that is used to treat anemia, commonly associated with chronic kidney failure and cancer chemotherapy.
The 2008 Giro d'Italia was the 91st running of the Giro d'Italia, one of cycling's Grand Tours. It began in Palermo on 10 May and ended in Milan on 1 June. Twenty-two teams entered the race, which was won by Spaniard Alberto Contador of the Astana cycling team. Second and third respectively were Italians Riccardo Riccò and Marzio Bruseghin.
Matteo Priamo is an Italian professional road bicycle racer, previously of UCI Professional Continental team CSF Group–Navigare.
Continuous erythropoietin receptor activator (CERA) is the generic term for drugs in a new class of third-generation erythropoiesis-stimulating agents (ESAs). In the media, these agents are commonly referred to as 'EPO', short for erythropoietin. CERAs have an extended half-life and a mechanism of action that promotes increased stimulation of erythropoietin receptors compared with other ESAs.
Peginesatide, developed by Affymax and Takeda, is an erythropoietic agent, a functional analog of erythropoietin.
CSL Vifor is a global specialty pharmaceuticals company in the treatment areas of iron deficiency, dialysis, nephrology & rare disease. It is headquartered in Switzerland and consists of CSL Vifor, Vifor Fresenius Medical Care Renal Pharma (VFMCRP) and Sanifit Therapeutics.
Daprodustat, sold under the brand name Duvroq among others, is a medication that is used for the treatment of anemia due to chronic kidney disease. It is a hypoxia-inducible factor prolyl hydroxylase inhibitor. It is taken by mouth.