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Bifendate (DDB) is a synthetic intermediate of Schisandrin C with anti-HBV efficacy in research of chronic hepatitis B[1].

[1]. Cui S, et al. [Anti-HBV efficacy of bifendate in treatment of chronic hepatitis B, a primary study]. Zhonghua Yi Xue Za Zhi. 2002 Apr 25;82(8):538-40.

Buparvaquone is a hydroxynaphthoquinone antiprotozoal drug related to parvaquone and atovaquone.

In 4-day proliferation assays, buparvaquone efficiently inhibits N. caninum tachyzoite replication(IC50=4.9 nM; IC100=100 nM)[1]. Buparvaquone is significantly selective against L. (L.) infantum chagasi intracellular amastigotes, with an IC50 value of 1.5 μM. Other cutaneous species are also susceptible to buparvaquone, with IC50 values in the range 1-4 μM[2].

Treatment of N. caninum infected mice with buparvaquone (100 mg/kg) either by intraperitoneal injection or gavage prevents neosporosis symptoms in 4 out of 6 mice in the intraperitoneally treated group, and in 6 out of 7 mice in the group receiving oral treatment[1]. Both a hydrous gel and water-in-oil emulsion of buparvaquone significantly reduce cutaneous parasite burden and lesion size, compared with the untreated control[3].

Clinical trial: Up to now, BTZ043 is still in the preclinical development stage.

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