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Eltrombopag (rINN
International Nonproprietary Name

An International Nonproprietary Name is the official non-proprietary or generic name given to a pharmaceutical substance, as designated by the World Health Organization ....
, codenamed SB-497115-GR) is a medication
Medication

A pharmaceutical drug, also referred to as medicine or medicament, can be loosely defined as any substance intended for use in the diagnosis, cure, mitigation, treatment, or prevention of disease....
 that has been developed for conditions that lead to thrombocytopenia
Thrombocytopenia

Thrombocytopenia is the presence of relatively few platelets in blood.Generally speaking, in humans, a normal platelet count ranges from 150,000 and 450,000 per mm3....
 (abnormally low platelet
Platelet

Platelets, or Thrombocyte, are small, irregularly shaped anuclear cells, 2-4?m in diameter, which are derived from fragmentation of precursor megakaryocytes....
 counts). It is a small molecule agonist
Agonist

An agonist is a term used to describe a type of Ligand or drug that binds and alters the activity of a Receptor . The ability to alter the activity of a receptor, also known as the agonist's efficacy is a property that distinguishes it from receptor antagonist, a type of receptor ligand which also binds a receptor but which does not alter t...
 of the c-mpl (TpoR) receptor
Receptor (biochemistry)

In biochemistry, a receptor is a protein molecule, embedded in either the plasma membrane or cytoplasm of a cell, to which a mobile signaling molecule may attach....
, which is the physiological target of the hormone
Hormone

Hormones are chemicals released by cells that affect cells in other parts of the body. Only a small amount of hormone is required to alter cell metabolism....
 thrombopoietin
Thrombopoietin

Thrombopoietin , also known as THPO, is a glycoprotein hormone produced mainly by the liver and the kidney that regulates the production of platelets by the bone marrow....
. Designated an orphan drug
Orphan drug

The term orphan drug refers to a medication that has been developed specifically to treat a rare medical condition, the condition itself being referred to as an rare disease....
 in the USA and European Union
European Union

The European Union is an economic and political union of 27 European Union member state, located primarily in Europe. It was established by the Treaty of Maastricht on 1 November 1993 upon the foundations of the pre-existing European Economic Community....
, it is being manufactured and marketed by GlaxoSmithKline
GlaxoSmithKline

GlaxoSmithKline plc is a United Kingdom-based pharmaceutical industry, biological, and healthcare company. GSK is the world's second largest pharmaceutical company and a research-based company with a wide portfolio of pharmaceutical products covering anti-infectives, central nervous system, respiratory, gastro-intestinal/metabolic,...
 and Ligand Pharmaceuticals,, under the trade names Promacta in the USA and Revolade in the EU.






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Eltrombopag (rINN
International Nonproprietary Name

An International Nonproprietary Name is the official non-proprietary or generic name given to a pharmaceutical substance, as designated by the World Health Organization ....
, codenamed SB-497115-GR) is a medication
Medication

A pharmaceutical drug, also referred to as medicine or medicament, can be loosely defined as any substance intended for use in the diagnosis, cure, mitigation, treatment, or prevention of disease....
 that has been developed for conditions that lead to thrombocytopenia
Thrombocytopenia

Thrombocytopenia is the presence of relatively few platelets in blood.Generally speaking, in humans, a normal platelet count ranges from 150,000 and 450,000 per mm3....
 (abnormally low platelet
Platelet

Platelets, or Thrombocyte, are small, irregularly shaped anuclear cells, 2-4?m in diameter, which are derived from fragmentation of precursor megakaryocytes....
 counts). It is a small molecule agonist
Agonist

An agonist is a term used to describe a type of Ligand or drug that binds and alters the activity of a Receptor . The ability to alter the activity of a receptor, also known as the agonist's efficacy is a property that distinguishes it from receptor antagonist, a type of receptor ligand which also binds a receptor but which does not alter t...
 of the c-mpl (TpoR) receptor
Receptor (biochemistry)

In biochemistry, a receptor is a protein molecule, embedded in either the plasma membrane or cytoplasm of a cell, to which a mobile signaling molecule may attach....
, which is the physiological target of the hormone
Hormone

Hormones are chemicals released by cells that affect cells in other parts of the body. Only a small amount of hormone is required to alter cell metabolism....
 thrombopoietin
Thrombopoietin

Thrombopoietin , also known as THPO, is a glycoprotein hormone produced mainly by the liver and the kidney that regulates the production of platelets by the bone marrow....
. Designated an orphan drug
Orphan drug

The term orphan drug refers to a medication that has been developed specifically to treat a rare medical condition, the condition itself being referred to as an rare disease....
 in the USA and European Union
European Union

The European Union is an economic and political union of 27 European Union member state, located primarily in Europe. It was established by the Treaty of Maastricht on 1 November 1993 upon the foundations of the pre-existing European Economic Community....
, it is being manufactured and marketed by GlaxoSmithKline
GlaxoSmithKline

GlaxoSmithKline plc is a United Kingdom-based pharmaceutical industry, biological, and healthcare company. GSK is the world's second largest pharmaceutical company and a research-based company with a wide portfolio of pharmaceutical products covering anti-infectives, central nervous system, respiratory, gastro-intestinal/metabolic,...
 and Ligand Pharmaceuticals,, under the trade names Promacta in the USA and Revolade in the EU. Eltrombopag was approved by the U.S. Food and Drug Administration on November 20, 2008.

Development

In preclinical studies, the compound was shown to interact selectively with the thrombopoeitin receptor, leading to activation of the JAK-STAT signaling pathway
JAK-STAT signaling pathway

The JAK-STAT signaling pathway takes part in the regulation of cellular responses to cytokines and growth factors. Employing Janus kinases and STAT protein , the pathway transduces the signal carried by these extracellular polypeptides to the cell nucleus, where activated STAT proteins modify gene expression....
 and increased proliferation and differentiation of megakaryocyte
Megakaryocyte

The megakaryocyte is a bone marrow cell responsible for the production of blood thrombocytes , which are necessary for normal blood clotting....
s. Animal studies confirmed that administration could increase platelet counts. In 73 healthy volunteers, higher doses of eltrombopag caused larger increases in the number of circulating platelets without tolerability problems.

Clinical trials

Eltrombopag has been studied, and shown to be effective, in two major clinical syndromes: idiopathic thrombocytopenic purpura
Idiopathic thrombocytopenic purpura

Idiopathic thrombocytopenic purpura is the condition of having a low platelet platelet count of no known cause . As most causes appear to be related to antibody against platelets, it is also known as immune thrombocytopenic purpura or immune-mediated thrombocytopenic purpura....
 and cirrhosis
Cirrhosis

Cirrhosis is a consequence of chronic liver disease characterized by replacement of liver Tissue by fibrous scar tissue as well as regenerative Nodule , leading to progressive loss of liver function....
 due to hepatitis C
Hepatitis C

Hepatitis C is a Blood-borne disease infectious disease that is caused by the hepatitis C virus , affecting the liver. The infection is often asymptomatic, but once established, chronic infection can cause inflammation of the liver ....
 (in which low platelet counts may be a contraindication for interferon
Interferon

Interferons are natural proteins produced by the cells of the immune system of most vertebrates in response to challenges by foreign agents such as viruses, parasites and tumor cells....
 treatment).