Table 1. Properties and status of some current drugs and some drugs under development.
| Drug | Elimination half-life | Efficacy | Advantages/ disadvantages | Status |
|---|---|---|---|---|
| Chloroquine | 3–14 days | Major resistance; some efficacy in partially immune patients | Cheap Readily available | Not recommended Still widely used for treatment |
| Sulphadoxine/ pyrimethamine (Fansidar®) | 6–9 day for sulphadoxine; 3–4 days for pyrimethamine | Major resistance; some efficacy in partially immune patients | Cheap Readily available | Only recommended in areas of low-grade resistance Still widely used for treatment |
| Mefloquine | 2–3 weeks | High, except in some regions of South-East Asia | Can produce neurological side effects Expensive | Has been used in ACT |
| Quinine | 10–20 h | High | Tinnitus, giddiness, hypoglycemia Hemolysis in G6PD-deficient patients | Use limited by toxicity and compliance issues Used to treat severe malaria |
| Malarone | 12–15 h for proguanil; 2–3 days for atovaquone | Good prophylaxis efficacy Few studies of efficacy as treatment | Expensive | Use limited by cost and potential for development of resistance |
| Lumefantrine | 4–6 days | High | Expensive Must be taken with food | Component (with artemether) of the only GMP-registered ACT now available |
| Piperaquine | 3–4 weeks | High | Inexpensive Increasingly available | Combination with dihydroartemisinin under development |
| Isoquine | Under investigation Slowly eliminated active metabolites | High, even against chloroquine-resistant strains | Readily synthesized. No amodoaquine-like side effects | Under development by MMV/GSK |
| Artemether | ∼1 h | High Rapid action Problems with recrudescence | Oil-soluble Can be used orally or as an i.m. injection | Used in combination with mefloquine in South-East Asia |
| Dihydroartemisinin | ∼1 h | High Rapid action Problems with recrudescence | Oil-soluble Can be used orally or rectally | Combinations with piperaquine under development |
| Artesunate | ∼1 h | High Rapid action Problems with recrudescence | Water soluble Fastest acting artemisinin derivative Can be used parenterally, rectally or orally | Combinations with pyronaridine, amodiaquine, mefloquine and chlorproguanil–dapsone under development |
| Artemisone | ∼1 h | High | Increased water solubility Potential neurological side effects less likely than other artemisinin drugs | Some stability problems Development under review |
| OZ277 | ∼2 h | High | Fully synthetic | Trials underway |
| Fosmidomycin | 1–5 h | Early trials are promising | Targets a novel pathway in the apicoplast | Under development in combination with clindamycin |
| Clindamycin | 2–4 h | Moderate to high | Inhibits protein synthesis | Under development in combination with fosmidomycin |
ACT: Artemisinin combination therapy; G6PD: Glucose-6-phosphate dehydrogenase; GMP: Good manufacturing practice; GSK: GlaxoSmithKline; i.m.: Intramuscular; MMV: Medicines for Malaria Venture.