> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/lumefantrine-5a02c559-879a-4fc5-808f-895181937743
> Record changed: 2026-10-13

# Lumefantrine

Highest phase reached

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL38827)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL38827)

First approval year

2009

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL38827)

## Development status

**First approval year**

2009

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL38827)

**Listing at source**

Listed

**Highest phase reached**

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL38827)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL38827)

**Drug name**

Lumefantrine

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL38827)

**Molecular weight**

528.95

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL38827)

**Structure (SMILES)**

CCCCN(CCCC)CC(O)c1cc(Cl)cc2c1-c1ccc(Cl)cc1/C2=C/c1ccc(Cl)cc1

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL38827)

### Brand names (2)

- lumefantrine component of coartem
- Lumefantrine component of coartem

### Other names (23)

- artemeter lumefantrine combination therapy
- Artemeter-Lumefantrine (combination therapy)
- arthemeter lumefantrine
- Arthemeter-lumefantrine
- benflumelol
- Benflumelol
- benflumetol
- Benflumetol
- cpg 56695
- CPG-56695
- d benflumelol
- D-BENFLUMELOL
- dl benflumelol
- Dl-benflumelol
- gnf pf 1971
- GNF-PF-1971
- lumefantrina
- Lumefantrina
- lumefantrine
- Lumefantrine
- LUMEFANTRINE, (+)-
- lumefantrinum
- Lumefantrinum

## Identifiers

**ChEMBL ID**

CHEMBL38827

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL38827)

**InChIKey**

DYLGFOYVTXJFJP-MYYYXRDXSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL38827)

**PubChem compound IDs**

- 6437380

**RxNorm IDs (RxCUI)**

- 847728

**FDA ingredient codes (UNII)**

- ZUV4B00D9P

### CAS registry numbers (2)

- 82186-77-4
- 120583-70-2

## Regulatory information

### United States

**Applicant**

NOVARTIS

**Approval date**

7 Apr 2009

**Application number**

NDA022268

### Other regulatory facts

**First in class**

No

**Orphan designation**

No

**Availability**

Prescription only

## Pharmacology

### Drug classification

**Pharmacology name**

lumefantrine

**Type**

Synthetic organic

**Approval recorded by Guide to Pharmacology**

Yes

#### Administration routes

- Oral

### Mechanisms of action

- **Mechanism**  
Ferriprotoporphyrin IX inhibitor

**Action type**  
Inhibitor

**Target**  
Ferriprotoporphyrin IX

### Investigated indications (6)

- **Condition**  
HIV Infections

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0000764

**Subject identifier**  
D015658
- **Condition**  
Malaria

**Highest recorded phase**  
4

**Condition identifier**  
EFO:0001068

**Subject identifier**  
D008288
- **Condition**  
Malaria, Falciparum

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0007444

**Subject identifier**  
D016778
- **Condition**  
Malaria, Vivax

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0007445

**Subject identifier**  
D016780
- **Condition**  
Schistosomiasis haematobia

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0007530

**Subject identifier**  
D012553
- **Condition**  
Fever

**Highest recorded phase**  
3

**Condition identifier**  
HP:0001945

**Subject identifier**  
D005334

### Open Targets indications (10)

- **Condition identifier**  
EFO\_0000764

**Highest recorded phase**  
1
- **Condition identifier**  
EFO\_0001068
- **Condition identifier**  
EFO\_0007444

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0007445

**Highest recorded phase**  
3
- **Condition identifier**  
HP\_0001945

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0005136

**Highest recorded phase**  
4
- **Condition identifier**  
MONDO\_0005249
- **Condition identifier**  
MONDO\_0005920

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0005921

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0100096

**Highest recorded phase**  
3

### Reported adverse events (28)

- **Event**  
asthenia

**Reports**  
16

**Reporting signal score**

12.1523
- **Event**  
blood bilirubin increased

**Reports**  
5

**Reporting signal score**

7.89423
- **Event**  
blood smear test abnormal

**Reports**  
1

**Reporting signal score**

5.96703
- **Event**  
cerebral malaria

**Reports**  
2

**Reporting signal score**

15.2513
- **Event**  
chromaturia

**Reports**  
4

**Reporting signal score**

7.86631
- **Event**  
congenital hair disorder

**Reports**  
1

**Reporting signal score**

5.96703
- **Event**  
conjunctival hyperaemia

**Reports**  
2

**Reporting signal score**

6.4222
- **Event**  
coombs negative haemolytic anaemia

**Reports**  
3

**Reporting signal score**

17.2882
- **Event**  
coombs positive haemolytic anaemia

**Reports**  
5

**Reporting signal score**

26.6647
- **Event**  
coombs test negative

**Reports**  
1

**Reporting signal score**

7.03527
- **Event**  
eye discharge

**Reports**  
2

**Reporting signal score**

5.86802
- **Event**  
haemolysis

**Reports**  
5

**Reporting signal score**

15.0213
- **Event**  
haemolytic anaemia

**Reports**  
38

**Reporting signal score**

173.71
- **Event**  
haptoglobin decreased

**Reports**  
2

**Reporting signal score**

8.71365
- **Event**  
hepatocellular injury

**Reports**  
6

**Reporting signal score**

11.2572
- **Event**  
hookworm infection

**Reports**  
1

**Reporting signal score**

6.83467
- **Event**  
infection protozoal

**Reports**  
1

**Reporting signal score**

6.83467
- **Event**  
jaundice acholuric

**Reports**  
2

**Reporting signal score**

12.5823
- **Event**  
labia enlarged

**Reports**  
1

**Reporting signal score**

6.5544
- **Event**  
malaria

**Reports**  
2

**Reporting signal score**

8.61798
- **Event**  
malaria antibody test positive

**Reports**  
1

**Reporting signal score**

8.13366
- **Event**  
nematodiasis

**Reports**  
1

**Reporting signal score**

7.84602
- **Event**  
plasmodium falciparum infection

**Reports**  
6

**Reporting signal score**

43.2563
- **Event**  
pyrexia

**Reports**  
17

**Reporting signal score**

11.7206
- **Event**  
skin swelling

**Reports**  
2

**Reporting signal score**

6.24236

And 3 more, listed on the interactive page.

### Trial references (86)

- NCT00118794  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00118794)
- NCT00123552  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00123552)
- NCT00140361  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00140361)
- NCT00297882  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00297882)
- NCT00336375  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00336375)
- NCT00386750  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00386750)
- NCT00386763  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00386763)
- NCT00393679  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00393679)
- NCT00406146  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00406146)
- NCT00444106  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00444106)
- NCT00451139  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00451139)
- NCT00452907  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00452907)
- NCT00454961  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00454961)
- NCT00495508  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00495508)
- NCT00540202  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00540202)
- NCT00541385  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00541385)
- NCT00694694  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00694694)
- NCT00808951  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00808951)
- NCT01038063  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01038063)
- NCT01075945  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01075945)
- NCT01082731  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01082731)
- NCT01150344  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01150344)
- NCT01152931  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01152931)
- NCT01374581  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01374581)
- NCT01445938  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01445938)

And 61 more, listed on the interactive page.

## Dosing

**Dose**

4 tablets for adults 35 kg and above; 1-4 tablets based on bodyweight for children

**Route**

Oral

**How often**

3 days (initial dose, after 8 hours, then twice daily for 2 days)

### Conditions of use (2)

- Crush and mix with water if necessary
- Take with food

## Chemical properties

**Hydrogen bond acceptors**

2

**Hydrogen bond donors**

1

**Polar surface area**

23.47

**Calculated partition coefficient (ALogP)**

9.15

**Calculated partition coefficient (XLogP)**

8.7

**Prodrug**

No

**Chirality**

Achiral

**Inorganic**

No

**Rule-of-five violations**

2

**Rotatable bonds**

10

**Heavy atoms**

35

**Molecular formula**

C30H32Cl3NO

**Monoisotopic mass**

527.154948

**Natural product**

Yes

## Evidence counts

**Recorded assays**

873

**Active assays**

206

### Active assay types (3)

- Confirmatory
- Other
- Summary

## Pharmacologic actions

- Antimalarials  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D000962.html)

## Biological measurements

### Observed measurements

#### Cardiac potassium channel inhibition

**Median**

380

**Mean**

3,473.06

**Minimum**

377

**Maximum**

8,128.31

**Unit**

nM

**Assays**

5

**Standard deviation**

4,236.73

**Summary method**

median

**Censored results excluded**

0

**Other units excluded**

0

**Unknown units excluded**

0

#### Measurement types

- IC50

## Related records

### Trials (128)

- A Combination Product of Sumatriptan and Naproxen Sodium Versus Single-entity Oral Triptans: An Analysis of Real World Data
- A Combination Therapy Including Anti-PD-1 Immunotherapy in MSS Rectal Cancer With Resectable Distal Metastasis
- A Combination Therapy Including Anti-PD-1 Immunotherapy in Rectal Cancer With Refractory Distal Metastasis
- A Preliminary Study on the Efficacy of Danggui Shaoyao San and Cuscuta Chinensis in Patients with Primary Dysmenorrhea
- A Registry to Capture Patient Outcomes With KRAS G12R Altered Advanced Pancreatic Ductal Adenocarcinoma Treated With MEK Inhibitor-based Combination Therapy
- A Registry-based Randomized Controlled Trial in Type 2 Diabetes With Cardiovascular Risk Factors (REMATCH)
- A Single Dose Phase I Exploratory Study in Healthy Volunteers With GSK2894512 Cream
- A Single-Arm Phase II Clinical Study of Docetaxel Combined With Nimotuzumab and Pucotenlimab as Second-Line and Beyond Therapy for Recurrent/Metastatic Head and Neck Squamous Cell Carcinoma
- A Study of JS009 Monotherapy and JS009 as a Triple Combination Therapy in Patients With Advanced Malignancies
- A Study of Patients With Primary Open Angle Glaucoma or Ocular Hypertension Who Were Insufficiently Responsive to Monotherapy
- A Study of PY314 in Subjects With Advanced Solid Tumors
- A Study of RC148 As a Single Agent and Combination Therapy in Patients with Locally Advanced Unresectable or Metastatic Malignant Solid Tumors
- A Study of Trifluridine/Tipiracil Combined With Anlotinib as Second-line Treatment for Recurrent and Metastatic Esophageal Squamous Cell Carcinoma
- A Study to Evaluate Antimalarial Activity and Safety of MK-7602 in Healthy Adults (MK-7602-003)
- A Study to Evaluate the Pharmacokinetics of a Single Dose of Tafenoquine Co-administered With Either Artemether + Lumefantrine or Dihydroartemisinin + Piperaquine Tetraphosphate
- A Therapeutic Protocol in Previous Failed ART Patients With High Total NK Cells
- Acetazolamide and Spironolactone to Increase Natriuresis in Congestive Heart Failure
- ACT MALI: Treatment of Malaria Based on Combination Therapies
- Adebrelimab Plus Full-course Neoadjuvant Therapy for Resectable Locally Advanced ESCC (Phase 2)
- Adolescent Type 1 Diabetes Cardio-Renal Intervention Trial

### Approved for (1)

- [Malaria](https://trialight.com/data/condition/malaria-54828cac-9b96-5833-93e2-e012d4505853.md)

### In development for (4)

- [HIV infectious disease](https://trialight.com/data/condition/hiv-infectious-disease-1260f28c-d667-55f9-b221-15d5017fde05.md) Phase 1
- [Plasmodium falciparum malaria](https://trialight.com/data/condition/plasmodium-falciparum-malaria-5e0103dd-4e60-581d-924b-3435883b51f8.md) Phase 3
- Plasmodium vivax malaria Phase 3
- Urinary schistosomiasis Phase 2

---

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