For Health Care Professionals Outside the US

REVOLADE complements, rather than competes with, endogenous thrombopoietin (TPO)1,2

  • REVOLADE uniquely binds to the transmembrane domain of TPO receptors, while endogenous TPO binds to the extracellular domain1,2
    • By not competing with endogenous TPO, REVOLADE can work together with endogenous TPO to promote platelet production2
  • As a small molecule, REVOLADE enters the bone marrow more effectively than endogenous TPO2,3

EPO, erythropoietin; G-CSF, granulocyte colony-stimulating factor.

REVOLADE may improve the function of CD4+ regulatory T cells (Tregs)9,11

  • REVOLADE may improve Tregs activity and reduce effector T helper functions9,11
  • This immunomodulatory activity may restore immune tolerance in ITP9-11

REVOLADE may help restore the natural balance of FΓ receptors (FcγR) that link antibody-mediated immunity and phagocytic activity9

  • REVOLADE may downregulate activating FcγRI and upregulate inhibitory FcγRIIb9
  • This rebalancing activity may reduce the platelet-targeted phagocytic activity of monocytes in ITP9,10

References:

1. REVOLADE Summary of Product Characteristics. February 2019. 2. Lum SH, Grainger JD. Eltrombopag for the treatment of aplastic anemia: current perspectives. Drug Des Devel Ther. 2016;10:2833-2843. 3. Bussel JB, Provan D, Shamsi T, et al. Effect of eltrombopag on platelet counts and bleeding during treatment of chronic idiopathic thrombocytopenic purpura: a randomised, double-blind, placebo-controlled trial. Lancet. 2009;373(9664):641-648. 4. Kuter DJ. The biology of thrombopoietin and thrombopoietin receptor agonists. Int J Hematol. 2013;98(1):10-23. 5. Cheng G. Eltrombopag, a thrombopoietin-receptor agonist in the treatment of adult chronic immune thrombocytopenia: a review of the efficacy and safety profile. Ther Adv Hematol. 2012;3(3):155-164. 6. McCrae K. Immune thrombocytopenia: no longer ‘idiopathic’. Cleve Clin J Med. 2011;78(6):358-373. 7. Desmond R, Townsley DM, Dumitriu B, et al. Eltrombopag restores trilineage hematopoiesis in refractory severe aplastic anemia that can be sustained on discontinuation of drug. Blood. 2014;123(12):1818-1825. 8. Camitta BM, Thomas ED, Nathan DG, et al. Severe aplastic anemia: a prospective study of the effect of early marrow transplantation on acute mortality. Blood. 1976;48(1):63-70. 9. Liu X, Liu S, Feng Q, et al. Thrombopoietin receptor agonists shift the balance of Fcγ receptors toward inhibitory receptor IIb on monocytes in ITP. Blood. 2016;128(6):852-861. 10. Ghadaki B, Nazi I, Kelton JG, Arnold DM. Sustained remissions of immune thrombocytopenia associated with the use of thrombopoietin receptor agonists. Transfusion. 2013;53(11):2807-2812. 11. Bao W, Bussel JB, Heck S, et al. Improved regulatory T-cell activity in patients with chronic immune thrombocytopenia treated with thrombopoietic agents. Blood. 2010;116(22):4639-4645.