NAV

Lumefantrine co-artemether

This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

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
Similar Structures
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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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
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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

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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
PubChem Substance
347911423
Wikipedia
Artemether/lumefantrine

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedBasic ScienceDrug Drug Interaction (DDI)1
4CompletedBasic ScienceHuman Immunodeficiency Virus (HIV) Infections1
4CompletedBasic SciencePlasmodium Falciparum Clinical Episode / Plasmodium Falciparum Infection / Plasmodium Vivax Clinical Episode / Plasmodium Vivax Infection1
4CompletedHealth Services ResearchAnemia / Plasmodium Infections / Pregnancy1
4CompletedOtherPlasmodium Infections1
4CompletedScreeningPlasmodium Falciparum, Malaria1
4CompletedTreatmentEffectiveness / Plasmodium Infections1
4CompletedTreatmentFalciparum / Plasmodium Infections1
4CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Plasmodium Infections1
4CompletedTreatmentInstantaneous Clearance1

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
PropertyValueSource
Water Solubility3.09e-05 mg/mLALOGPS
logP8.34ALOGPS
logS-7.2ALOGPS
Rule of FiveNoChemaxon
Ghose FilterNoChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Drug created at October 21, 2016 02:50 / Updated at May 22, 2021 06:01