eltrombopag

Ligand id: 6961

Name: eltrombopag

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 7
Hydrogen bond donors 3
Rotatable bonds 5
Topological polar surface area 114.59
Molecular weight 442.16
XLogP 7.39
No. Lipinski's rules broken 1

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Used to stimulate platelet production in the bone marrow, in patients with chronic immune (idiopathic) thrombocytopenia (ITP, a rare blood disorder) or in patients with chronic hepatitis C who have low blood platelet counts. In August 2014, the US FDA granted approval for the additional indication, severe aplastic anemia (SAA). In June 2015, eltrombopag was granted approval from the US FDA for the treatment of children (≥ 6 yrs) with ITP.
Eltrombopag is being evaluated in clinical trials for additional indications such as myelodysplastic syndromes (Phase III) and acute myeloid leukaemia (AML, Phase II).
Mechanism Of Action and Pharmacodynamic Effects
Eltrombopag activates the JAK-STAT pathway via interaction with the transmembrane domain of the thrombopoeitin receptor, leading to increased platelet production in the bone marrow (by increasing megakaryocytopoiesis).