Lumefantrine

Summary

Lumefantrine (CHEMBL38827) is an approved small-molecule antimalarial; indicated across 6 conditions including malaria and plasmodium falciparum malaria.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Indications: 6 conditions
• Clinical trials: 36
• Chemistry: 528.9 Da · C30H32Cl3NO

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL38827
Name	Lumefantrine
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	6437380
ChEBI	CHEBI:156095
Molecular formula	C30H32Cl3NO
Molecular weight	528.9
InChIKey	DYLGFOYVTXJFJP-MYYYXRDXSA-N

SMILES: CCCCN(CCCC)CC(C1=CC(=CC\2=C1C3=C(/C2=C/C4=CC=C(C=C4)Cl)C=C(C=C3)Cl)Cl)O

IUPAC name: 2-(dibutylamino)-1-[(9Z)-2,7-dichloro-9-[(4-chlorophenyl)methylidene]fluoren-4-yl]ethanol

ChEBI definition: A member of the class of fluorenes that is 9-(p-chlorobenzylidene)-9H-fluorene which is substitutec by chlorine at positions 2 and 7, and by a 2-(dibutylamino)-1-hydroxyethyl group at position 4. An antimalarial drug used in combination with artemether for the treatment of multi-drug resistant strains of falciparum malaria.

Pharmacological roles (ChEBI): antimalarial.

Also known as: Benflumelol, Benflumetol, CPG-56695, Dl-benflumelol, GNF-PF-1971, Lumefantrina, Lumefantrine, Lumefantrine component of coartem, Lumefantrinum, GNF-Pf-1971, lumefantrine, SID50112743

Patent coverage: 1,034 distinct patent families (3,479 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: Nuclear receptor ROR-gamma, 4’-phosphopantetheinyl transferase ffp, Voltage-gated inwardly rectifying potassium channel KCNH2.

Bioactivity

ChEMBL activities: 5 potent at pChembl ≥ 5 of 8 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
KCNH2	6.42	IC50	377	nM	CHEMBL_ACT_18062973
KCNH2	6.42	IC50	380	nM	CHEMBL_ACT_24959575
KCNH2	6.42	IC50	380	nM	CHEMBL_ACT_29118758
KCNH2	5.09	IC50	8100	nM	CHEMBL_ACT_1449659
KCNH2	5.09	IC50	8128	nM	CHEMBL_ACT_5218922

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

6 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
malaria	4	MONDO:0005136	EFO:0001068
Plasmodium falciparum malaria	3	MONDO:0005920	EFO:0007444
Plasmodium vivax malaria	3	MONDO:0005921	EFO:0007445
urinary schistosomiasis	2	MONDO:0006001	EFO:0007530
HIV infectious disease	1	MONDO:0005109	EFO:0000764

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 36.

Phase distribution

Phase	Trials
PHASE4	15
PHASE1	8
PHASE3	6
Not specified	3
PHASE2	2
PHASE2/PHASE3	1
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07403643	PHASE4	NOT_YET_RECRUITING	Investigating the Pharmacology of Tafenoquine in Papua New Guinean Children With Uncomplicated Malaria
NCT00451139	PHASE4	COMPLETED	Ototoxicity of Artemether / Lumefantrine (Coartem) and Other Antimalarials
NCT00452907	PHASE4	COMPLETED	ACT MALI: Treatment of Malaria Based on Combination Therapies
NCT00495508	PHASE4	COMPLETED	Quinine vs. Artemether/Lumefantrine in Uncomplicated Malaria During Pregnancy
NCT00529867	PHASE4	COMPLETED	Randomised Efficacy Study of Two Artemether-Lumefantrine Oral Formulations for the Treatment of Uncomplicated P. Falciparum Malaria
NCT00790881	PHASE4	COMPLETED	Artemether/Lumefantrine and Nevirapine Interaction Study in HIV-infected Adults
NCT00869700	PHASE4	COMPLETED	Pharmacokinetic Interaction Between the Antimalarial Combination Artemether/Lumefantrine and Combination Antiretroviral Therapy Including Lopinavir/Ritonavir in HIV-infected Adults
NCT01075945	PHASE4	UNKNOWN	Dihydroartemisinin- Piperaquine Versus Artemether- Lumefantrine in the Treatment Uncomplicated Plasmodium Falciparum Malaria in Sudan
NCT01906788	PHASE4	UNKNOWN	The Optimal Timing Of Primaquine To Prevent Malaria Transmission After Artemisinin-Combination Therapy
NCT01976780	PHASE4	COMPLETED	In Vivo and In Vitro Efficacy of Artemisinin Combination Therapy
NCT01998295	PHASE4	COMPLETED	Parasite Clearance Time and Time to Recurrent Infection Following Treatment With Artemether/Lumefantrine
NCT02143934	PHASE4	COMPLETED	Effect of Liver and Blood-stage Treatment on Subsequent Plasmodium Reinfection and Morbidity
NCT02742285	PHASE4	COMPLETED	Lumefantrine in Venous Plasma Versus Dried Capillary Blood Spot
NCT04767191	PHASE4	COMPLETED	Malaria Therapeutic Efficacy Study (TES) Kenya
NCT05605925	PHASE4	UNKNOWN	Ivermectin-artemisinin Combination Therapy for Eradication of Malaria
NCT00123552	PHASE3	COMPLETED	Longitudinal Antimalarial Combinations in Uganda
NCT00541385	PHASE3	COMPLETED	Pyronaridine Artesunate 3:1 Granule Formulation vs. Coartem© Crushed Tablets in P. Falciparum Malaria Pediatric Patients
NCT01152931	PHASE3	COMPLETED	Antioxidant Micronutrients in Malaria
NCT01374581	PHASE3	COMPLETED	Impact of Artemisinin-based Combination Therapy and Quinine on Treatment Failure and Resistance in Uncomplicated Malaria
NCT01625871	PHASE3	COMPLETED	Artemether/Lumefantrine and Vivax Malaria
NCT01899820	PHASE3	UNKNOWN	Evaluation of the Efficacy of Artemisinin Combination Therapy in Kenya
NCT05192265	PHASE2/PHASE3	COMPLETED	Efficacy and Safety of Pyronaridine-Artesunate Versus Artemether-Lumefantrine
NCT07559370	PHASE2	RECRUITING	Safety and Efficacy of Imatinib in Combination With Artemether-Lumefantrine for Uncomplicated Malaria
NCT04280692	PHASE1/PHASE2	SUSPENDED	Controlled Human Malaria Infection Transmission Model - Phase A
NCT04661579	PHASE2	COMPLETED	Study of Malaria Vaccine RTS,S/AS01E in Plasmodium Falciparum-infected and Uninfected Adults Pre-treated With Anti-malarial Therapy
NCT00266058	PHASE1	COMPLETED	Drug Interaction Study Between Antimalarial and Anti-HIV Medications
NCT00697892	PHASE1	COMPLETED	Pharmacokinetic Interactions Between Antiretroviral Agents and Antimalarial Drug Combinations
NCT01876966	PHASE1	COMPLETED	Interaction Between Etravirine or Darunavir/Ritonavir and Artemether / Lumefantrine
NCT02184637	PHASE1	COMPLETED	A Study to Evaluate the Pharmacokinetics of a Single Dose of Tafenoquine Co-administered With Either Artemether + Lumefantrine or Dihydroartemisinin + Piperaquine Tetraphosphate
NCT05084651	PHASE1	COMPLETED	Drug-drug Interaction Study of Ganaplacide and Lumefantrine With Itraconazole
NCT05236530	PHASE1	COMPLETED	Drug-drug Interaction Study of Ganaplacide and Lumefantrine With Midazolam, Repaglinide, Dextromethorphan, Metformin, Rosuvastatin and Dolutegravir
NCT05330273	PHASE1	COMPLETED	Drug-drug Interaction Study of Ganaplacide and Lumefantrine With Efavirenz
NCT06294912	PHASE1	COMPLETED	A Study to Evaluate Antimalarial Activity and Safety of MK-7602 in Healthy Adults (MK-7602-003)
NCT02213211	Not specified	COMPLETED	School-based Programme of Malaria Diagnosis and Treatment in Southern Malawi
NCT04666350	Not specified	COMPLETED	Clinical Investigation Study to Evaluate the Consistency and Reproducibility of Two Consecutive Mosquito Feeding Assays
NCT07362498	Not specified	COMPLETED	Health Systems Implementation and Molecular Surveillance of Multiple First-Line Treatments for Uncomplicated Malaria in Western Kenya

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 4 clinical and 18 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).