Drug intelligence / Profile preview

eltrombopag + romiplostim

Development stage
Unknown
Lead developer
Amgen
Modality
Small Molecules
Administration
Oral, Subcutaneous
01

Overview

Eltrombopag and romiplostim are thrombopoietin receptor agonists (TPO-RAs) used primarily for the treatment of chronic immune (idiopathic) thrombocytopenia (ITP) in patients who have had an insufficient response to corticosteroids, immunoglobulins, or splenectomy. Both drugs act by stimulating the thrombopoietin receptor (c-Mpl/CD110), leading to increased platelet production. Romiplostim is a peptibody that binds directly and competitively at the TPO binding site on the receptor, while eltrombopag is a small molecule that binds at a transmembrane site on the same receptor. Activation of these receptors leads to downstream signaling via JAK2/STAT5 and other pathways, resulting in proliferation of megakaryocyte progenitors and increased platelet counts. Eltrombopag is also indicated for severe aplastic anemia and hepatitis C-associated thrombocytopenia; romiplostim’s primary indication remains ITP[1][2][3][6][8].

Brand names
PromactaRevoladeNplate
Other names
TPO-RAsThrombopoietin receptor agonists
02

Targets

TPOR (Thrombopoietin receptor)

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