MedPath

Lumefantrine co-artemether

Generic Name
Lumefantrine co-artemether
Drug Type
Small Molecule
Chemical Formula
C346H378Cl33N11O16
CAS Number
141204-94-6
Unique Ingredient Identifier
5T2U51A0MW
Background

Lumefantrine Co-Artemether (Riamet) has been investigated for the treatment of Malaria, Malaria, Falciparum, Malaria in Pregnancy, Uncomplicated Malaria, and Uncomplicated Knowlesi Malaria. Lumefantrine Co-Artemether is a tablet formulation of artemether and lumefantrine, a well-tolerated, fast-acting and effective blood schizontocidal drug that serves primarily in the treatment of uncomplicated falciparum malaria that is resistant to other antimalarials. Artemether, an artemisinin derivative, has several proposed mechanisms of action, including interference with plasmodial transport proteins, interference with mitochondrial electron transport, and the production of free radicals to reduce blood antioxidants and glutathione. While artemether results in rapid defervescence, parasite clearance, and clinical improvement, it also has a relatively high recrudescence rate when used as monotherapy. The exact mechanism of action of lumefantrine is not well defined, but it is thought to inhibit -hematin formation, an important detoxification pathway for the parasite. Unlike artemether, lumefantrine has a slower onset of action, resulting in clearance of residual parasites and a decrease in recrudescence rate. The combination is an effective and well-tolerated malaria treatment, providing high cure rates even in areas of multi-drug resistance.

Novartis and MMV Advance Novel Malaria Drug Combination into Phase 3 Trials

• Novartis and Medicines for Malaria Venture (MMV) are progressing a new drug combination of ganaplacide and lumefantrine into Phase 3 trials to combat resistant malaria infections. • The novel non-artemisinin regimen aims to treat uncomplicated Plasmodium falciparum malaria with a once-daily solid dispersion formulation (SDF). • Phase 2 results showed the new combination was as effective as Coartem, potentially clearing artemisinin-resistant strains and blocking malaria parasite transmission. • A large Phase 3 trial will compare ganaplacide/lumefantrine with artemether/lumefantrine across multiple sites in sub-Saharan Africa.

Artefenomel-Piperaquine Combination Shows Synergistic Effects Against Malaria in Human Study

• A randomized, open-label trial assessed the interaction of artefenomel and piperaquine against malaria using the induced blood-stage malaria (IBSM) model. • The study found that the combination of artefenomel and piperaquine exhibits synergistic effects in killing Plasmodium falciparum parasites. • Pharmacokinetic/pharmacodynamic modeling was used to predict the efficacy of the drug combination, showing consistency with phase 2b trial results. • The findings support the potential of artefenomel-piperaquine as an effective treatment for malaria, warranting further clinical development.

Artemisinin Resistance Emerges in Ugandan Children with Severe Malaria

• A study in Uganda found that some children with severe malaria show partial resistance to artemisinin, a key antimalarial drug. • The resistance is linked to the A675V mutation in the _Plasmodium falciparum_ parasite's _Pfkelch13_ gene, causing slower parasite clearance. • Children with the mutation had significantly longer parasite clearance times, with 37.5% exceeding five hours. • Experts emphasize the urgent need for trials to assess the impact of artemisinin resistance on the efficacy of artesunate in treating severe malaria.

Novartis and MMV Develop Novel Malaria Treatment for Infants Under 5kg, Addressing Critical Treatment Gap

• Novartis and Medicines for Malaria Venture (MMV) have announced positive results from the CALINA study for a new formulation of Coartem® specifically designed for babies weighing less than 5kg with malaria. • The novel formulation uses a new ratio and dose of artemether-lumefantrine to account for metabolic differences in infants, addressing a significant treatment gap as no evidence-based malaria treatment currently exists for this vulnerable population. • If approved, Coartem <5kg Baby would be the first antimalarial specifically developed for the smallest infants, potentially saving countless lives in malaria-endemic regions where current treatments risk overdose and toxicity in this age group.
© Copyright 2025. All Rights Reserved by MedPath