Table 2.
Summary of key antimalarials, front-runner and development compounds as well as investigative hits with in vitro activity (< 5 µM) against P. falciparum mature gametocytes.
| Compound | IC50 (nM) Stg V | Target | Ref |
|---|---|---|---|
| Mefloquine (+RS) | 158 | 80S ribosome | (Plouffe et al., 2016) |
| ELQ-300 | 72 | Cytochrome bc1(Qi) | (Nilsen et al., 2013) |
| Cipargamin (KAE609) | 100* | PfATP4 / Na2+ homeostasis | (Van Pelt-Koops et al., 2012) |
| KAF246 | 2 | (Rottmann et al., 2010; Plouffe et al., 2016) | |
| M5717 (DDD498) | 9 | PfEF2 / protein synthesis | (Rottmann et al., 2010; Plouffe et al., 2016) |
| MMV390048 | 140 | PfPI4K | (Paquet et al., 2017) |
| AZD-0156 | 236 | (Reader et al., 2021) | |
| KDU691 | 150 | (Mcnamara et al., 2013) | |
| ML324 | 77 | Pfjmj3 | (Reader et al., 2021) |
| JIB-04 | 3630 | (Matthews et al., 2020) | |
| Methylene blue | 258 | Glutathione reductase | (Buchholz et al., 2008; Plouffe et al., 2016) |
| GNF179 | 3 | Protein secretory pathway | (Plouffe et al., 2016) |
| Birinapant | 135 | Unknown (caspase 3 inhibitor) | (Reader et al., 2021) |
| MMV1581558 | 130 | Unknown (Adenosine A3 receptor) | |
| MMV1580843 | 108 | Unknown | |
| SQ109 | 104 | Unknown (MmpL3 in Mtb) | |
| Epoxomicin | 6.6 | β2 and 5 proteasome subunits | (D'Alessandro et al., 2016) |
*% inhibition of gametocyte viability 500 nM.