Thrombopoietin receptor agonists

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}}intro}} The thrombopoietin receptor agonists mimic the action of thrombopoietin on its receptor and stimulate the activation, proliferation and maturation of megakaryocytes, resulting in an increase in circulating platelet counts.

Mechanism of action of Thrombopoietin receptor agonists

Thrombopoietin itself acts in this manner, but when recombinant thrombopoietins were used clinically, they were found to cause rebound thrombocytopenia, probably due to induction of anti-thrombopoietin antibodies. For this reason, direct administration of thrombopoietin was abandoned as an approach to treating thrombocytopenia and other approaches to activating the thrombopoietin receptor were sought.

List of Thrombopoietin receptor agonists

Several thrombopoietin receptor agonists were subsequently developed and are now in clinical use for chronic idiopathic thrombocytopenic purpura (ITP) and for raising platelet counts in persons with thrombocytopenia undergoing surgical procedures or other thrombocytopenic conditions.

Eltrombopag, lusutrombopag and avatrombopag are peptide-like, small molecular weight agonists of the thrombopoietin receptor. These agents are given by mouth and result in significant increases in platelet counts in normal persons as well as patients with thrombocytopenia due to hematologic and liver diseases. Romiplostim, in contrast, is a recombinant polypeptide that binds to and activates the thrombopoietin receptor despite having no amino acid homology to native thrombopoietin. It also increases platelet counts in normal subjects as well as patients with chronic ITP but has not been associated with induction of anti-thrombopoietin antibodies.

ELTROMBOPAG

Eltrombopag (el trom' boe pag) is a small molecular weight peptide-like molecule that binds to the transmembrane domain of the thrombopoietin receptor and causes its activation and the proliferation and differentiation of megakaryocytes, with a resultant increase in synthesis and release of platelets. In multiple clinical trials, eltrombopag was shown to raise the platelet count in patients with idiopathic thrombocytopenic purpura (ITP), aplastic anemia and cirrhosis due to chronic hepatitis C during interferon therapy.

FDA approval information for Thrombopoietin receptor agonists

Eltrombopag was the first oral thrombopoietin receptor agonist approved for use in the United States, initially for treatment of ITP iin 2008.

Clinical use of Thrombopoietin receptor agonists

The indications have subsequently been expanded to other thrombocytopenic conditions.

Dosage and administration for Thrombopoietin receptor agonists

Eltrombopag is available as tablets of 12.5, 25, 50, 75 and 100 mg under the brand name Promacta. The typical dose is 25 to 50 mg once daily by mouth.

Side effects of Thrombopoietin receptor agonists

The most common side effects include nausea, diarrhea, fatigue, muscle aches, headaches and dizziness. Rare, but potentially serious adverse reactions include vascular occlusions, stroke and myocardial infarction. Hematologic Agents Eculizumab, Emapalumab, Emicizumab, Lanadelumab, Ravulizumab

Hematologic Growth Factors

  • Granulocyte-Macrophage Colony Stimulating Factors

Thrombopoietin receptor agonists and Thrombopoiesis Stimulators

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