Preparation, Characterization, And Pharmacodynamics Of A Novel Anti-tumor Drug, Ga(III)-EDTMP

This paper centered on the parts of preclinical studies of a novel anti-tumor drug,gallium ethylenediaminetetramethylene phosphonate[Ga(III)-EDTMP].The aim of this work is to study a novel and effective therapeutic preparation which issupposed to be not only able to prevent or treat bone metastases resulted frommalignant tumors such as lung, prostate, liver cancers, but also inhibit thereproduction of malignances or even solicit tumor cells necrosis. As a result, thepromising drug should improve the life quality of seriously cancer-bearing patients orsurvive their life time. Like other effective phosphonates, Ga(III)-EDTMP is expectedto prevent or treat the osteoporosis of postmenopausal women to some extent.The detailed study basically involved three parts: pharmacy, pharmacology, andkinetic binding assay. In the chapter of pharmacy study, we have performed suchworks as preparation of the intermediate, EDTMP (ethylenediaminetetramethylenephosphonic acid), and the pharmaceutical, Ga(III)-EDTMP;structure conformation ofthe metal chelate via element analysis, IR, NMR, HPLC, and potentiometric titration;determination of its stability constants, pharmaceutical, and prescription, and study ofpharmaceutical stability. In the following chapter, we tested the effects of the drug invivo, as well as giving some theoretical explanation. Finally, the kinetics of binding tohydroxyapatite crystals was measured in vitro.Results of this preliminary study, although incomplete, strongly indicated that thedrug can clinically treat the bone metastases and primary malignances. Accordingly,we succeed in testing a novel drug for bone metastases that is designed under theconnection of target and synergy.