Lumefantrine
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2009
- First approval year
- 2009
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Lumefantrine
- Molecular weight
- 528.95
- Structure (SMILES)
- CCCCN(CCCC)CC(O)c1cc(Cl)cc2c1-c1ccc(Cl)cc1/C2=C/c1ccc(Cl)cc1
- lumefantrine component of coartem
- Lumefantrine component of coartem
- 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
- ChEMBL ID
- CHEMBL38827
- InChIKey
- DYLGFOYVTXJFJP-MYYYXRDXSA-N
- PubChem compound IDs
- 6437380
- RxNorm IDs (RxCUI)
- 847728
- FDA ingredient codes (UNII)
- ZUV4B00D9P
- 82186-77-4
- 120583-70-2
- Applicant
- NOVARTIS
- Approval date
- 7 Apr 2009
- Application number
- NDA022268
- First in class
- No
- Orphan designation
- No
- Availability
- Prescription only
- 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
- 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
- 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
- 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.
- NCT00118794
- NCT00123552
- NCT00140361
- NCT00297882
- NCT00336375
- NCT00386750
- NCT00386763
- NCT00393679
- NCT00406146
- NCT00444106
- NCT00451139
- NCT00452907
- NCT00454961
- NCT00495508
- NCT00540202
- NCT00541385
- NCT00694694
- NCT00808951
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And 61 more, listed on the interactive page.
- 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)
- Crush and mix with water if necessary
- Take with food
- 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
- Recorded assays
- 873
- Active assays
- 206
- Confirmatory
- Other
- Summary
- Antimalarials
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
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Approved for (1)
In development for (4)
- HIV infectious disease Phase 1
- Plasmodium falciparum malaria Phase 3
- Plasmodium vivax malaria Phase 3
- Urinary schistosomiasis Phase 2