Disease relevance of dl-Benflumelol

• Efficacy of six doses of artemether-lumefantrine (benflumetol) in multidrug-resistant Plasmodium falciparum malaria [1].
• Benflumetol AUC is associated with cure and the effect of benflumetol when coadministered with artemether is to prevent recrudescence [2].
• After 28 days of follow-up, there were 2/61 (3.2%) recurrent parasitemias in the Coartem group and 4/64 (6.2%) in the ASAQ group (P = 0.72), all classified as re-infections after PCR genotyping (cure rate = 100% [95%CI: 94-100] in both groups) [3].

High impact information on dl-Benflumelol

• The 50% inhibitory concentration (IC50s) of benflumetol (range, 12.5 to 240 nM; mean, 55.1 nM) for 158 Senegalese isolates were evaluated [4].
• In April 2004, 137 children 6-59 months of age with uncomplicated Plasmodium falciparum (Pf) malaria (Caala, Central Angola) were randomized to receive either artemether-lumefantrine (Coartem) or artesunate + amodiaquine (ASAQ) [3].
• In vitro sensitivity of Plasmodium falciparum and clinical response to lumefantrine (benflumetol) and artemether [5].
• Population pharmacokinetics and therapeutic response of CGP 56697 (artemether + benflumetol) in malaria patients [2].
• The variability in bioavailability of artemether and dihydroartemisinin was large both between doses and between patients, but was less pronounced for benflumetol [2].

Chemical compound and disease context of dl-Benflumelol

• A randomized, double-blind, comparative trial of a new oral combination of artemether and benflumetol (CGP 56697) with mefloquine in the treatment of acute Plasmodium falciparum malaria in Thailand [6].
• METHODS AND FINDINGS: In a randomised controlled trial, 497 children with uncomplicated falciparum malaria were treated with CQ and SP (three doses and one dose respectively; n = 91), or six doses of artemether in fixed combination with lumefantrine (co-artemether [Coartem, Riamet]) (n = 406) [7].

Biological context of dl-Benflumelol

• Higher benflumetol AUC was found to significantly increase the chance of cure [2].
• Due to its molecular structure benflumetol occurs in the dextrorotatory and the laevorotatory form [8].

Anatomical context of dl-Benflumelol

• Determination of a new antimalarial drug, benflumetol, in blood plasma by high-performance liquid chromatography [9].

Analytical, diagnostic and therapeutic context of dl-Benflumelol

• Patient data from eight clinical trials were pooled and analyzed to study the efficacy and safety of the six-dose versus four-dose regimen of artemether-lumefantrine (coartemether; Coartem) in children weighing 5-25 kg [10].
• Determination of benflumetol in human plasma by reversed-phase high-performance liquid chromatography with ultraviolet detection [11].
• Plasma concentration-time profiles in healthy volunteer adults were measured after a single-dose oral administration of 500 mg of benflumetol [11].
• In patients on regimens A and B who showed a sensitive response, plasma concentrations of benflumetol were significantly higher than in those with treatment failure [12].

References