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LGD-4665

LGD-4665, an oral thromobopoietin receptor agonist, is being developed as a new generation small molecule thrombopoietin (TPO) mimetic. It is a highly selective and potent agonist of the TPO receptor and therefore induces differentiation and proliferation of megakaryocytes. The pharmacologic characteristics indicate potential therapeutic use in thrombocytopenic patients with a variety of clinical etiologies.

Research demonstrated that LGD-4665 was well-tolerated with an excellent safety profile. Multiple phase-II studies in thrombocytopenic patients due to ITP, Hep-C and MDS with daily and weekly dosing regimens, as well as additional Phase-I pharmacology studies in healthy volunteers are underway.

Current developer:  Ligand Pharmaceuticals

1. Fox, Norma E.; Lim, Jihyang; Chen, Rose; Geddis, Amy E. F104S c-Mpl responds to a transmembrane domain-binding thrombopoietin receptor agonist: Proof of concept that selected receptor mutations in congenital amegakaryocytic thrombocytopenia can be stimulated with alternative thrombopoietic agents. Experimental Hematology (New York, NY, United States) (2010), 38(5), 384-391.

2. Rice, Lawrence. Treatment of immune thrombocytopenic purpura: focus on eltrombopag. Biologics: Targets & Therapy (2009), 3 151-157.

3. Tomillero A; Moral M A Gateways to clinical trials. Methods and findings in experimental and clinical pharmacology (2008), 30(7), 543-88.

4. Bayes M; Rabasseda X Gateways to clinical trials. Methods and findings in experimental and clinical pharmacology (2008), 30(1), 67-99.