NEW PREPARATION FOR COMBINED CHEMOTHERAPY OF ONCOLOGICAL DISEASES
 

alt♦ The nitroxyl complex of Pt(IV), namely, [e-ammin-c/-(4-amino-2,2,6,6-tetramethylpiperidin-l-oxyl)-a,/-bis(acetato)-b.t-dichloroplatinum(IV)] (BC118) has been synthesized and tested as a cytostatic agent.
 

 


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♦ A comparative analysis of BC118strong> and cisplatin activity on leukaemia P388 has revealed that though both preparations show close chemotherapeutic sensitivity, toxicity of BC118strong> for mice is almost four times lower than that of cisplatin. Additionally to high toxicity, cisplatin is characterized by quickly developing resistivity to it.

♦ The experimental data obtained for laboratory mice allowed the combined use of cisplatin and BC118 to be proposed. As a result, a well-pronounced synergistic effect was observed, namely, an essentially stronger effect of cisplatin and a slower development of resistivity to it in combination with complex BC118strong>. The combined use of lower doses of preparations provides 100 % survival of laboratory animals.

♦ The rate of the development of resisitivity to combined therapy with small doses of cisplatin and BC118strong> is almost two times lower than that at cisplatin monotherapy. Low therapeutic doses allow total high toxicity of preparations to be avoided, with an extremely high anti-tumor effect observed.

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Comparative activity of cisplatin and BC118 on leukaemia P388 of mice Synergism of combined effect of cisplatin and complex BC118 on leukaemia P388 of mice