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. 2020 Mar 29;25(7):1571. doi: 10.3390/molecules25071571

Table 1.

Inhibition of β-haematin formation and parasite activity in CQ-sensitive (PfNF54) and multidrug-resistant (PfK1) strains of P. falciparum of top-ranked USFDA approved drugs selected on the basis of their ranking in a previously published Bayesian model [15].

Bayesian
Rank
Drug β-haematin IC50 (μM) PfNF54
IC50 (µM)
PfK1
IC50 (µM)
RI 2
1 Lapatinib 5.43 ± 0.03 0.26 ± 0.07 0.85 ± 0.02 3.3
2 Amodiaquine 21 4 NT 3 0.0086 5 -
3 Imatinib 99 ± 5 3.9 ± 0.1 NT 3 -
4 Nafarelin 48 ± 5 NA 1 NT 3 -
5 Nilotinib 7 ± 1 0.28 ± 0.02 0.38 ± 0.06 1.4
6 Antrafenine NT 3 NT 3 NT 3 -
7 Vapreotide 48 ± 7 NA 1 NT 3 -
8 Gefitinib 20.4 ± 0.8 11.5 ± 0.4 NT 3 -
13 Thiabendazole > 500 NA 1 NT 3 -
14 Erlotinib 17.6 ± 0.2 13.3 ± 0.4 NT 3 -
19 Lomitapide 68.2 ± 0.9 0.56 ± 0.10 0.69 ± 0.14 1.2
21 Chloroquine 26 ± 0.3 0.015 ± 0.001 0.272 ± 0.005 18
1505 Dantrolene >500 NT 3 NT 3 -
1506 Nitrendipine >500 NT 3 NT 3 -
1508 Nimodipine >500 NT 3 NT 3 -
1510 Acenocumarol >500 NT 3 NT 3 -

1 not active at tested concentration of 10 µg/mL; 2 Resistance Index (RI) = PfK1-IC50/Pf NF54-IC50. 3 Not tested. 4 Data from Sandlin et al. [16]. 5 Data from Guglielmo et al. [17].