(E/Z)-Eltrombopag 13C4 ((E/Z)-SB-497115 13C4) is a mixture complex of E-Eltrombopag and Z-Eltrombopag, with 13C labeled. Z-Eltrombopag is a thrombopoietin (TPO) receptor agonist developed for certain conditions that lead to thrombocytopenia.
Avatrombopag hydrochloride (AKR-501) is an orally active, nonpeptide agonist of the thrombopoietin (TPO) receptor with an EC 50 of 3.3 nM. It effectively mimics the biological activities of TPO, stimulating platelet production by activating the intracellular signaling system and facilitating the generation of platelets and megakaryocytes from hemopoietic precursor cells. Additionally, Avatrombopag hydrochloride serves as a substrate for cytochrome P450 (CYP) 2C9 and CYP3A.
Totrombopag, also known LGD-4665, GSK2285921 and SB559448, is an oral thromobopoietin receptor agonist, is being developed as a new generation small molecule thrombopoietin (TPO) mimetic. It is a highly selective and potent agonist of the TPO receptor and therefore induces differentiation and proliferation of megakaryocytes. The pharmacologic characteristics indicate potential therapeutic use in thrombocytopenic patients with a variety of clinical etiologies.
Avatrombopag, also known as AKR-501, YM477, AS 1670542 or E5501, is a novel orally-active thrombopoietin (TPO) receptor agonist. AKR-501 specifically targeted the TPO receptor and stimulated megakaryocytopoiesis throughout the development and maturation of megakaryocytes just as rhTPO did. AKR-501 may be useful in the treatment of patients with thrombocytopenia. Avatrombopag was first approved in 2018.