Avatrombopag

DB11995ApprovedInvestigationalSmall moleculeThrombopoietin Receptor Agonist

Avatrombopag is a thrombopoietin receptor agonist used pre-operatively to treat thrombocytopenia in patients with chronic liver disease and in patients with chronic refractory thrombocytopenia. Avatrombopag (Doptelet), is an orally administered, small molecule thrombopoietin receptor (c-Mpl) agonist that increases platelet number without increasing platelet activation, thereby decreasing the need for blood transfusions.

Mechanism: Avatrombopag is an orally bioavailable, small molecule thrombopoietin (TPO) receptor agonist that stimulates proliferation and differentiation of megakaryocytes from bone marrow progenitor cells resulting in an increased production of platelets. Avatrombopag is not competitive with thrombopoietin for binding to the TPO receptor and has an additive pharmacological effect with TPO on platelet production.
Avatrombopag is a thrombopoietin receptor (TPOR; MPL) agonist, with possible megakaryopoiesis stimulating activity. After administration, avatrombopag binds to and stimulates the platelet thrombopoeitin receptor (TPOR), which can lead to the proliferation and differentiation of megakaryocytes from bone marrow progenitor cells. This process increases the production of platelets and may serve to prevent chemotherapy-induced thrombocytopenia (CIT). TPOR is classified as a cytokine receptor and as a member of the hematopoietin receptor superfamily.
Curator reviewed · 2 references
Primary indication: Indicated for the treatment of thrombocytopenia in pediatric patients 1 year and older with persistent or chronic immune thrombocytopenia who have had an insufficient response to a previous treatment.Curator reviewed · 4 structured indications
Formula / weight: C₂₉H₃₄Cl₂N₆O₃S₂ · 649.65 g/mol (avg)
First approval: Canada, 2023 · United States, 2018 · European Union, 2020
Code names: E5501 · YM-477
Brand names: Doptelet
Doptelet 60 Mg Daily Dose Carton