Methoxy polyethylene glycol-epoetin beta, sold under the brand name Mircera, is a long-acting

erythropoietin receptor The erythropoietin receptor (EpoR) is a protein that in humans is encoded by the ''EPOR'' gene. EpoR is a 52 kDa peptide with a single carbohydrate chain resulting in an approximately 56–57 kDa protein found on the surface of EPO res ...

activator (CERA) used for the treatment of

anaemia Anemia (also spelt anaemia in British English) is a blood disorder in which the blood has a reduced ability to carry oxygen. This can be due to a lower than normal number of red blood cells, a reduction in the amount of hemoglobin availab ...

associated with chronic kidney disease. It is the first approved, chemically modified

erythropoiesis-stimulating agent 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 t ...

(ESA). It is on the

World Health Organization's List of Essential Medicines The WHO Model List of Essential Medicines (aka Essential Medicines List or EML), published by the World Health Organization (WHO), contains the medications considered to be most effective and safe to meet the most important needs in a health s ...

. It was approved for medical use in the European Union, Switzerland, and the United States in 2007. Methoxy polyethylene glycol-epoetin beta is made from

erythropoietin Erythropoietin (; EPO), 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 th ...

by chemically linking the N-terminal amino group or the ε-amino group of any

lysine Lysine (symbol Lys or K) is an α-amino acid that is a precursor to many proteins. Lysine contains an α-amino group (which is in the protonated form when the lysine is dissolved in water at physiological pH), an α-carboxylic acid group ( ...

present in the protein with methoxy polyethylene glycol butanoic acid. The average

molecular weight A molecule is a group of two or more atoms that are held together by Force, attractive forces known as chemical bonds; depending on context, the term may or may not include ions that satisfy this criterion. In quantum physics, organic chemi ...

is approximately 60 kDa. The drug stimulates

erythropoiesis Erythropoiesis (from Greek ''erythro'', meaning ''red'' and ''poiesis'', meaning ''to make'') is the process which produces red blood cells (erythrocytes), which is the development from erythropoietic stem cell to mature red blood cell. It is s ...

by interacting with the erythropoietin receptor on progenitor cells in the

bone marrow Bone marrow is a semi-solid biological tissue, tissue found within the Spongy bone, spongy (also known as cancellous) portions of bones. In birds and mammals, bone marrow is the primary site of new blood cell production (or haematopoiesis). It i ...

. It has a reduced receptor binding activity compared to other ESAs and but retains in vivo activity due to an extended serum half-life. 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.

Society and culture

Legal status

Patent infringement claims

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 An injunction is an equitable remedy in the form of a special court order compelling a party to do or refrain from doing certain acts. It was developed by the English courts of equity but its origins go back to Roman law and the equitable rem ...

entered in the fall of 2008 which barred Roche from selling Mircera in the United States. The injunction has since expired and Mircera has been available on the U.S. market since 2015.

Controversies

Use in sports

Mircera can reportedly replace traditional

drugs as a

blood doping Blood doping is a form of Doping in sport, doping in which the number of red blood cells in the bloodstream is boosted in order to enhance athletic performance. Because such blood cells carry oxygen from the lungs to the muscles, a higher concentr ...

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 The World Anti-Doping Agency (WADA; , AMA) is an international organization co-founded by the governments of over 140 nations along with the International Olympic Committee based in Canada to promote, coordinate, and monitor the fight against d ...

. In July 2008, Italian bicycle racer

Riccardo Riccò Riccardo Riccò (born 1 September 1983) is an Italian professional road bicycle racer, who was suspended from all competition until 2024. He was previously ejected from the 2008 Tour de France for doping violations and suspended. Riccò returned ...

was disqualified from the

Tour de France The Tour de France () is an annual men's multiple-stage cycle sport, bicycle race held primarily in France. It is the oldest and most prestigious of the three Grand Tour (cycling), Grand Tours, which include the Giro d'Italia and the Vuelta a ...

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 The Fédération Française de Cyclisme (''FFC'') or French Cycling Federation is the national governing body of cycle racing in France. The FFC is a member of the UCI and the UEC. In February 2009, David Lappartient was elected for a four-ye ...

and the

French Anti-Doping Agency The French Anti-Doping Agency (, AFLD) is an independent public authority formed in 2006 and charged with ensuring that participants in sports in France do not violate rules regarding doping. As a national anti-doping organization ( NADO), the ...

, not the

Union Cycliste Internationale The Union Cycliste Internationale (; UCI; ) is the world governing body for sports cycling and oversees international competitive cycling events. The UCI is based in Aigle, Switzerland. The UCI issues racing licenses to riders and enforces di ...

References

{{Portal bar , Medicine Antianemic preparations Erythropoiesis-stimulating agents World Anti-Doping Agency prohibited substances Drugs developed by Hoffmann-La Roche