Arterolane (RBx 11160) maleate is a new, fully synthetic 1,2,4-trioxolane with a peroxidic pharmacophore and is a rapidly acting oral antimalarial drug. Therefore, there is an urgent need for development of novel synthetic antimalarial drugs with similar antimalarial activity. Artemisinins are used in combination with different partner drugs however, because they are plant derived, there is potential for mismatch in demand and supply.
The new “artemisinin-derived treatments,” now adopted by 77 countries as first-line therapy, provide rapid parasitological responses, clinical cure, and life-saving benefits for patients with severe malaria. Plasmodium falciparum is the main cause of disease (250 million cases) and death (nearly 1 million deaths) due to malaria, and the development of resistance to existing antimalarial drugs has severely compromised the treatment and control of the disease. Arterolane at daily doses of 100 and 200 mg is a rapidly acting, effective, and safe synthetic antimalarial drug, which may potentially represent an alternative to artemisinin derivatives in antimalarial combination therapy. Biochemistry and hematological analyses did not show any sign of drug toxicity in any patient.Ĭonclusion.
Mild complaints were reported in <10% of the patients and were similar in the 3 groups. No patient died or experienced any serious adverse event. The polymerase chain reaction- corrected adequate clinical and parasitological responses on day 28 were 63%, 71%, and 72% for the groups receiving the 50-mg, 100-mg, and 200-mg doses, respectively, by intention-to-treat analysis (odds ratio, 1.55 95% confidence interval, 0.78–3.06, for comparison of the 200-mg and 50-mg dose groups). The median PC 90 was longer in the group receiving the 50-mg dose (19.4 h), compared with the groups receiving the 100-mg dose (12.8 h) and 200-mg dose (12.6 h) ( P <. The median time to 90% parasite clearance (PC 90) was evaluated. Patients (aged 13–65 years) with asexual parasite density of 1000–100,000 parasites/mL were included and were followed up for 28 days. In this randomized, double-blind, multicenter, parallel-group, dose-finding, phase II trial, 230 patients from 4 centers in Thailand, India, and Tanzania (mainland and Zanzibar) received either 50 mg ( n = 78), 100 mg ( n = 76), or 200 mg ( n = 76) of arterolane once daily for 7 days. The present study assessed the efficacy and safety of 3 dose levels of arterolane (RBx 11160), a synthetic trioxolane, for treatment of acute uncomplicated falciparum malaria. Drug-resistant Plasmodium falciparum malaria necessitates development of novel drugs for treatment.
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