Table 1 Relevant activity parameters of SC81458 and SC83288.

From: SC83288 is a clinical development candidate for the treatment of severe malaria

 

SC81458

SC83288

IC50, IC90, IC99 (nM)

8, 18, 50

3, 8, 20

In vitro PCT99.9% (h)

37±4 (4)

51±6 (4)

In vitro logPRR

3.4±0.4 (4)

3.0±0.5 (4)

In vitro lag phase (h)

<5

<5

In vivo PCT99.9% (h)*

<48

48

In vivo logPRR*

5.3 (W2), 3.2 (3D7)

3.0

  1. IC50/90/99, inhibitory concentration of 50, 90 or 99% of the maximal effect; PCT99.9%, clearance time of 99.9% of the original parasite population; PRR, parasite reduction ratio.
  2. For the in vitro PCT99.9% and the in vitro logPRR the means±s.e. of the means of (n) independent determinations are shown.
  3. *Obtained in the P. falciparum-infected humanized NSG mouse model system.
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