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Anagrelide is an inhibitor of phosphodiesterase 3 (PDE3; IC50 = 36 nM for the human platelet enzyme).1 It inhibits thrombopoietin-induced megakaryocytopoiesis of isolated human CD34+ progenitor cells (IC50 = 26 nM).2 Anagrelide reduces platelet aggregation induced by ADP, collagen, thrombin, or arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) in isolated rabbit platelet rich-plasma (EC50s = 0.31, 0.08, 0.18, and 0.1 µg/ml, respectively).3 It inhibits platelet thrombus formation in a dog model of electrically induced carotid artery thrombosis when administered at doses ranging from 0.5 to 5 mg/kg.4 Formulations containing anagrelide have been used in the treatment of thrombocythemia.
WARNING This product is not for human or veterinary use.
1. Comparison of the biological activities of anagrelide and its major metabolites in haematopoietic cell cultures. Br. J. Pharmacol. 146(3), 324-332 (2005).
2. Comparison between anagrelide and hydroxycarbamide in their activities against haematopoietic progenitor cell growth and differentiation: Selectivity of anagrelide for the megakaryocytic lineage. Leukemia 20(6), 1117-1122 (2006).
3. A potent new inhibitor of platelet aggregation and experimental thrombosis, anagrelide (BL-
4. Anagrelide. New drugs annual: Cardiovascular drugs 277-294 (1983).