Identification
- Generic Name
- Lumefantrine co-artemether
- DrugBank Accession Number
- DB13085
- 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.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Lumefantrine co-artemether (DB13085)
- Weight
- Average: 6116.74
Monoisotopic: 6096.8824492 - Chemical Formula
- C346H378Cl33N11O16
- Synonyms
- Artemether/lumefantrine
- Lumefantrine co-artemether
- External IDs
- CPG-56697
Pharmacology
- Indication
Not Available
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Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Not Available
- Mechanism of action
- Not Available
- Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.Not Available
- Food Interactions
- Not Available
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- International/Other Brands
- Coartem / Riamet
Categories
- Drug Categories
- Not Available
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 5T2U51A0MW
- CAS number
- 141204-94-6
- InChI Key
- VZQXHIJHMCHBNW-UFIXNTOBSA-N
- InChI
- InChI=1S/6C30H32Cl3NO.C16H26O5/c6*1-3-5-13-34(14-6-4-2)19-29(35)28-18-23(33)17-27-25(15-20-7-9-21(31)10-8-20)26-16-22(32)11-12-24(26)30(27)28;1-9-5-6-12-10(2)13(17-4)18-14-16(12)11(9)7-8-15(3,19-14)20-21-16/h6*7-12,15-18,29,35H,3-6,13-14,19H2,1-2H3;9-14H,5-8H2,1-4H3/b6*25-15-;/t;;;;;;9-,10-,11+,12+,13+,14-,15-,16-/m......1/s1
- IUPAC Name
- SMILES
- [H][C@@]12CC[C@@H](C)[C@]3([H])CC[C@]4(C)OO[C@@]13[C@]([H])(O[C@H](OC)[C@@H]2C)O4.CCCCN(CCCC)CC(O)C1=CC(Cl)=CC2=C1C1=CC=C(Cl)C=C1\C2=C\C1=CC=C(Cl)C=C1.CCCCN(CCCC)CC(O)C1=CC(Cl)=CC2=C1C1=CC=C(Cl)C=C1\C2=C\C1=CC=C(Cl)C=C1.CCCCN(CCCC)CC(O)C1=CC(Cl)=CC2=C1C1=CC=C(Cl)C=C1\C2=C\C1=CC=C(Cl)C=C1.CCCCN(CCCC)CC(O)C1=CC(Cl)=CC2=C1C1=CC=C(Cl)C=C1\C2=C\C1=CC=C(Cl)C=C1.CCCCN(CCCC)CC(O)C1=CC(Cl)=CC2=C1C1=CC=C(Cl)C=C1\C2=C\C1=CC=C(Cl)C=C1.CCCCN(CCCC)CC(O)C1=CC(Cl)=CC2=C1C1=CC=C(Cl)C=C1\C2=C\C1=CC=C(Cl)C=C1
References
- General References
- Not Available
- External Links
- PubChem Substance
- 347911423
- Wikipedia
- Artemether/lumefantrine
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Malaria 1 4 Active Not Recruiting Treatment Uncomplicated Malaria caused by Plasmodium falciparum 1 4 Completed Basic Science Drug Drug Interaction (DDI) 1 4 Completed Basic Science Human Immunodeficiency Virus (HIV) Infections 1 4 Completed Basic Science Plasmodium Falciparum Clinical Episode / Plasmodium Falciparum Infection / Plasmodium Vivax Clinical Episode / Plasmodium Vivax Infection 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Not Available
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 3.09e-05 mg/mL ALOGPS logP 8.34 ALOGPS logS -7.2 ALOGPS Rule of Five No Chemaxon Ghose Filter No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Drug created at October 21, 2016 02:50 / Updated at May 22, 2021 06:01