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Blood, 1 June 2007, Vol. 109, No. 11, pp. 4739-4741.
Prepublished online as a Blood First Edition Paper on February 27, 2007; DOI 10.1182/blood-2006-11-057968.
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Submitted November 14, 2006
Accepted January 29, 2007
Phase I clinical study of eltrombopag, an oral, non-
peptide thrombopoietin receptor agonist
Julian M Jenkins*, Daphne Williams, Yanli Deng, Joanne Uhl, Valerie Kitchen, David Collins, and Connie L Erickson-Miller
GlaxoSmithKline, Collegeville, PA, United States
* Corresponding author; email: julian.m.jenkins{at}gsk.com.
Eltrombopag (SB-497115) is a first in class, oral, small molecule, non-peptide agonist of the thrombopoietin receptor (TpoR), being developed as a treatment for thrombocytopenia of various etiologies. In this phase I placebo-controlled clinical trial in 73 healthy male subjects, eltrombopag was administered as once daily oral capsules for 10 days at doses of 5, 10, 25, 30, 50 and 75mg. The pharmacokinetics of eltrombopag were dose dependent and linear, and eltrombopag increased platelet counts in a dose dependent manner. There were no apparent differences in the incidence or severity of adverse events in subjects receiving active or placebo study medication. These observations indicate that eltrombopag is a once daily, oral TpoR agonist with demonstrated thrombopoietic activity in human subjects, encouraging further studies in patients with thrombocytopenia.
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