Lumefantrine

Lumefantrine
Systematic (IUPAC) name

2-(dibutylamino)-1-[(9Z)-2,7-dichloro-9-(4-chlorobenzylidene)-9H-fluoren-4-yl]ethanol
Clinical data
AHFS/Drugs.com	International Drug Names
MedlinePlus	a609024
Legal status
Legal status	US: C
Identifiers
CAS Number	82186-77-4^N
ATC code	P01BF01 (WHO) (combination with artemether)
PubChem	CID 6437380
DrugBank	DB06708^Y
ChemSpider	4941944^Y
UNII	F38R0JR742^Y
KEGG	D03821^Y
ChEBI	CHEBI:156095^Y
ChEMBL	CHEMBL38827^Y
Chemical data
Formula	C₃₀H₃₂Cl₃NO
Molar mass	528.939 g/mol
SMILES Clc1ccc(cc1)\C=C3\c4c(c2c(cc(Cl)cc23)C(O)CN(CCCC)CCCC)ccc(Cl)c4
InChI InChI=1S/C30H32Cl3NO/c1-3-5-13-34(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/h7-12,15-18,29,35H,3-6,13-14,19H2,1-2H3/b25-15-^Y Key:DYLGFOYVTXJFJP-MYYYXRDXSA-N^Y
^NY (what is this?) (verify)

Lumefantrine (or benflumetol) is an antimalarial drug. It is only used in combination with artemether. The term "co-artemether" is sometimes used to describe this combination.^[1] Lumefantrine has a much longer half life compared to artemether and so is therefore thought to clear any residual parasites that remain after combination treatment.^[2]

Lumefantrine, along with pyronaridine and naphtoquine, were synthesized in course of the Project 523 antimalaria drug research initiated in 1967; these compounds are all used in combination antimalaria therapies.^[3]^[4]^[5]

References

↑ Toovey S, Jamieson A, Nettleton G (2003). "Successful co-artemether (artemether-lumefantrine) clearance of falciparum malaria in a patient with severe cholera in Mozambique". Travel medicine and infectious disease 1 (3): 177–9. doi:10.1016/j.tmaid.2003.09.002. PMID 17291911.
↑ White, Nicholas J.; van Vugt, Michele; Ezzet, Farkad (1999). "Clinical Pharmacokinetics and Pharmacodynamics of Artemether-Lumefantrine". Clinical Pharmacokinetics 37 (2): 105–125. doi:10.2165/00003088-199937020-00002. ISSN 0312-5963.
↑ Cui, Liwang; Su, Xin-zhuan (2009). "Discovery, mechanisms of action and combination therapy of artemisinin". Expert Review of Anti-infective Therapy 7 (8): 999–1013. doi:10.1586/eri.09.68. PMC 2778258. PMID 19803708.
↑ http://aac.asm.org/content/56/5/2465.full
↑ http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4280121/

Antiparasitics – antiprotozoal agents – Chromalveolate antiparasitics (P01)

Alveo-
late

Apicom-
plexa

Conoidasida/
(Coccidiostats)

Cryptosporidiosis	thiazolide (nitazoxanide)

Isosporiasis	trimethoprim/sulfamethoxazole^#

Toxoplasmosis	pyrimethamine sulfadiazine

Aconoidasida

Malaria

Individual
agents

Hemozoin
inhibitors

aminoquinolines	(4-): amodiaquine^# chloroquine^# Tafenoquine (8-): primaquine^# pamaquine

4-methanolquinolines	mefloquine^# quinine^# quinidine

Other	lumefantrine combined with artemether halofantrine

Antifolates

DHFR inhibitors (antifols)	pyrimethamine proguanil^# chlorproguanil biguanides

Sulfonamides	sulfadoxine sulfamethoxypyrazine

Coformulation	sulfadoxine/pyrimethamine (SP)^#

Sesquiterpene
lactones

Other

Combi-
nations

Fixed-dose (coformulated) ACTs	artemether/lumefantrine^# artesunate/amodiaquine (ASAQ) artesunate/mefloquine (ASMQ) dihydroartemisinin/piperaquine artesunate/pyronaridine arterolane/piperaquine

Other combinations (not co-formulated)	artesunate/SP artesunate/mefloquine quinine/tetracycline quinine/doxycycline quinine/clindamycin

Babesiosis

clindamycin

Cilio-
phora

Balantidiasis: Tetracycline

Hetero-
kont

Blastocystosis: Metronidazole

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

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