Eltrombopag (SB-497115) is a thrombopoietin (TPO) receptor agonist developed for certain conditions that lead to thrombocytopenia. In preclinical studies, the compound was shown to interact selectively with the thrombopoeitin receptor, leading to activation of the JAK-STAT signaling pathway and increased proliferation and differentiation of megakaryocytes. Animal studies confirmed that administration could increase platelet counts. In addition, eltrombopag (SB-497115) decreased proliferation of all cancer cell lines.
Molecular Weight | 442.47 |
Formula | C25H22N4O4 |
CAS Number | 496775-61-2 |
Solubility (25°C) | DMSO 27 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Phillip Scheinberg. Activity of eltrombopag in severe aplastic anemia
[3] Taylor Olmsted Kim, et al. Eltrombopag for use in children with immune thrombocytopenia
[5] Danielle M Townsley, et al. Eltrombopag Added to Standard Immunosuppression for Aplastic Anemia
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