PHARMACOKINETICS AND METABOLISM OF PIRARUBICIN IN HUMANS - CORRELATION WITH PHARMACODYNAMICS

The pharmacokinetic monitoring of anthracycline-containing regimens is warranted because of the important toxicity of these drugs and becaus e pharmacokinetic-pharmacodynamic relationships have been clearly esta blished. We studied the pharmacokinetics of the new anthracycline pira rubicin in 80 courses of treatment performed in 27 patients, using a l imited sampling protocol we had previously validated. We observed (for 47 of these courses) a significant correlation between the leucocyte cell kill and the pirarubicin area under the time x concentration curv e, but the most significant correlation was obtained using the plasma concentration of doxorubicin, a metabolite of pirarubicin, at the end of the infusion. On the basis of this value, it is possible to predict for pirarubicin haematological toxicity in a way that can help the cl inician in identifying patients at risk for toxicity.