Methoxy polyethylene glycol-epoetin beta
Encyclopedia
Methoxy polyethylene glycol-epoetin beta is the active ingredient of a drug marketed by Hoffmann-La Roche
under the brand name Mircera. Mircera is a long-acting erythropoietin receptor
activator (CERA) indicated for the treatment of patients with anaemia associated with chronic kidney disease. It is the first approved, chemically-modified erythropoiesis-stimulating agent
(ESA). Mircera is supplied as a solution in pre-filled syringes for intravenous or subcutaneous administration. Mircera was approved for use in Europe in July 2007 by the European Commission, in September 2007 by the Swissmedic
, and in November 2007 by the U.S. Food and Drug Administration for use in the United States
.
Methoxy polyethylene glycol-epoetin beta is made from erythropoietin
by chemically linking the N-terminal amino group or the Є-amino group of any lysine present in the protein with methoxy polyethylene glycol butanoic acid. The average molecular weight is approximately 60kDa. The drug stimulates erythropoiesis
by interacting with the erythropoietin receptor on progenitor cells in the bone marrow
.
ruled 15 September 2009 that Mircera infringes 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.
drugs as 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
.
On July 17, 2008, Italian bicycle racer Riccardo Riccò
was kicked out of the Tour de France
after reports that a urine sample tested positive for Mircera. 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
.
Hoffmann-La Roche
F. Hoffmann-La Roche Ltd. is a Swiss global health-care company that operates worldwide under two divisions: Pharmaceuticals and Diagnostics. Its holding company, Roche Holding AG, has shares listed on the SIX Swiss Exchange....
under the brand name Mircera. Mircera is a long-acting erythropoietin receptor
Erythropoietin receptor
The erythropoietin receptor is a protein that in humans is encoded by the EPOR gene. EpoR is a 59 kDa peptide and is a member of the cytokine receptor family. EpoR pre-exists as dimers...
activator (CERA) indicated for the treatment of patients with anaemia associated with chronic kidney disease. It is the first approved, chemically-modified erythropoiesis-stimulating agent
Erythropoiesis-stimulating agent
Erythropoiesis-stimulating agent, commonly abbreviated ESA, an agent similar to the cytokine that stimulates red blood cell production...
(ESA). Mircera is supplied as a solution in pre-filled syringes for intravenous or subcutaneous administration. Mircera was approved for use in Europe in July 2007 by the European Commission, in September 2007 by the Swissmedic
Swissmedic
Swissmedic, the Swiss Agency for Therapeutic Products, is the Swiss surveillance authority for medicines and medical devices, registered in Berne. It started operations on 1 January 2002 as successor of Interkantonale Kontrollstelle für Heilmittel , which was itself the successor of Schweizerische...
, and in November 2007 by the U.S. Food and Drug Administration for use in the United States
United States
The United States of America is a federal constitutional republic comprising fifty states and a federal district...
.
Methoxy polyethylene glycol-epoetin beta is made from erythropoietin
Erythropoietin
Erythropoietin, or its alternatives erythropoetin or erthropoyetin or EPO, is a glycoprotein hormone that controls erythropoiesis, or red blood cell production...
by chemically linking the N-terminal amino group or the Є-amino group of any lysine present in the protein with methoxy polyethylene glycol butanoic acid. The average molecular weight is approximately 60kDa. The drug stimulates erythropoiesis
Erythropoiesis
Erythropoiesis is the process by which red blood cells are produced. It is stimulated by decreased O2 in circulation, which is detected by the kidneys, which then secrete the hormone erythropoietin...
by interacting with the erythropoietin receptor on progenitor cells in the bone marrow
Bone marrow
Bone marrow is the flexible tissue found in the interior of bones. In humans, bone marrow in large bones produces new blood cells. On average, bone marrow constitutes 4% of the total body mass of humans; in adults weighing 65 kg , bone marrow accounts for approximately 2.6 kg...
.
Patent infringement claims
A U.S. Federal Appeals CourtUnited States courts of appeals
The United States courts of appeals are the intermediate appellate courts of the United States federal court system...
ruled 15 September 2009 that Mircera infringes a patent
Patent infringement
Patent infringement is the commission of a prohibited act with respect to a patented invention without permission from the patent holder. Permission may typically be granted in the form of a license. The definition of patent infringement may vary by jurisdiction, but it typically includes using or...
held by Amgen Inc.. The court refused to lift an injunction
Injunction
An injunction is an equitable remedy in the form of a court order that requires a party to do or refrain from doing certain acts. A party that fails to comply with an injunction faces criminal or civil penalties and may have to pay damages or accept sanctions...
entered in the fall of 2008 which barred Roche from selling Mircera in the United States.
Use in sports
Mircera can reportedly replace traditional EPOErythropoietin
Erythropoietin, or its alternatives erythropoetin or erthropoyetin or EPO, is a glycoprotein hormone that controls erythropoiesis, or red blood cell production...
drugs as blood doping
Blood doping
Blood doping is the practice of boosting the number of red blood cells in the bloodstream in order to enhance athletic performance. Because such blood cells carry oxygen from the lungs to the muscles, a higher concentration in the blood can improve an athlete’s aerobic capacity and...
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
France
The French Republic , The French Republic , The French Republic , (commonly known as France , is a unitary semi-presidential republic in Western Europe with several overseas territories and islands located on other continents and in the Indian, Pacific, and Atlantic oceans. Metropolitan France...
and by the World Anti-Doping Agency
World Anti-Doping Agency
The World Anti-Doping Agency , , is an independent foundation created through a collective initiative led by the International Olympic Committee . It was set up on November 10, 1999 in Lausanne, Switzerland, as a result of what was called the "Declaration of Lausanne", to promote, coordinate and...
.
On July 17, 2008, Italian bicycle racer Riccardo Riccò
Riccardo Riccò
Riccardo Riccò is a professional road bicycle racer from Italy, currently under contract to UCI Continental team Meridiana-Kamen, and suspended from competition. He was ejected from the 2008 Tour de France for doping violations and suspended...
was kicked out of the Tour de France
Tour de France
The Tour de France is an annual bicycle race held in France and nearby countries. First staged in 1903, the race covers more than and lasts three weeks. As the best known and most prestigious of cycling's three "Grand Tours", the Tour de France attracts riders and teams from around the world. The...
after reports that a urine sample tested positive for Mircera. 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
Union Cycliste Internationale
Union Cycliste Internationale is the world governing body for sports cycling and oversees international competitive cycling events. The UCI is based in Aigle, Switzerland....
.