Overview
Benflumetol, also known as lumefantrine in its combination form, is a synthetic aryl amino alcohol compound developed as an antimalarial agent. It is primarily used in combination with artemether (as Coartem) to enhance efficacy and reduce resistance development in Plasmodium falciparum malaria treatment. The drug was developed in the late 20th century to address the growing resistance to traditional antimalarial medications like chloroquine. Its mechanism involves inhibiting heme polymerization in malaria parasites, leading to toxic heme accumulation and parasite death.
Physical and Chemical Properties
Benflumetol is a yellow crystalline powder with a molecular weight of 528.94 g/mol. It is highly lipophilic (logP ~7.5), contributing to its long half-life in the body. The compound melts at 128-132°C and is practically insoluble in water but dissolves well in organic solvents like ethanol and DMSO. Its stability is maintained under standard storage conditions, though it should be protected from light and moisture to prevent degradation. The CAS number 82186-77-4 uniquely identifies its chemical structure, which includes a trifluoromethyl group and a biphenyl moiety critical to its antimalarial activity.
Main Applications
The primary application of benflumetol is in fixed-dose combination therapy with artemether for treating uncomplicated Plasmodium falciparum malaria. The combination is marketed as Coartem and is on the WHO Model List of Essential Medicines. Outside malaria treatment, research has explored its potential against other parasitic infections and even certain cancers, though these applications remain investigational. Its long half-life makes it particularly useful in ensuring clinical efficacy after artemether’s rapid action phase.
Safety and Storage
Benflumetol should be handled in accordance with pharmaceutical safety protocols. While it has low acute toxicity, prolonged exposure may cause irritation to skin, eyes, or respiratory tract. Always use PPE, including gloves and goggles, in laboratory settings. Storage requires protection from light and moisture at room temperature (15-30°C). Bulk quantities should be sealed in airtight containers with desiccants to maintain stability. Disposal must follow local regulations for pharmaceutical compounds.
B2B Procurement Guide
When procuring benflumetol for pharmaceutical use, prioritize suppliers with GMP certification and documented quality control processes. Key considerations include batch-specific certificates of analysis (CoA), impurity profiles, and stability data under ICH guidelines. Pricing varies by purity (typically 98-99.5%) and order volume. For reference, bulk purchases (100+ kg) may reduce costs to approximately $200/kg. Audit supplier facilities to verify compliance with regulatory standards like USFDA or EMA, especially for API (Active Pharmaceutical Ingredient) production.
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