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IC50: 9.8 to 217.3 nM for P. falciparum isolates

Piperaquine, an antimalarial drug, is first synthesised in the 1960s and extensively used as prophylaxis and treatment during the next 20 years.

In vitro: In 280 P. falciparum isolates, the IC50 for piperaquine ranged from 9.8 nM to 217.3 nM and a significant but low correlation was observed between the IC50 values for piperaquine and chloroquine. However, the coefficient of determination indicated that only 2.1% of the variation in the response to piperaquine was explained by the variation in the response to chloroquine. Moreover, the mean value for piperaquine was 74.0 nM in the Pfcrt K76 wild-type group and 87.7 nM in the 76T mutant group and such difference was not significant [1].

In vivo: Male SD rats were orally administered piperaquine or as a short-term i.v. infusion. Results showed that piperaquine disposition was best described by a 3-compartment model with a rapid initial distribution phase after i.v. administration. The PK of piperaquine was characterized by a low clearance, a large volume of distribution and a long terminal half-life [2].

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