LUMEFANTRINE, (+)-

Details

Stereochemistry	UNKNOWN
Molecular Formula	C30H32Cl3NO
Molecular Weight	528.94
Optical Activity	( + )
Defined Stereocenters	0 / 1
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCCCN(CCCC)CC(O)C1=CC(Cl)=CC2=C1C3=CC=C(Cl)C=C3\C2=C\C4=CC=C(Cl)C=C4

InChI

InChIKey=DYLGFOYVTXJFJP-MYYYXRDXSA-N

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-

HIDE SMILES / InChI

Molecular Formula	C30H32Cl3NO
Molecular Weight	528.94
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	1
Optical Activity	( + / - )

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022268s012lbl.pdf
Curator's Comment: description was created based on several sources, including: http://www.drugbank.ca/drugs/DB06708 https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=7866ec19-dfac-47d4-a53f-511a12643cbf

Lumefantrine is an antimalarial agent used to treat acute uncomplicated malaria. It is administered in combination with artemether for improved efficacy (Coartem tablets). Lumefantrine is a blood schizonticide active against erythrocytic stages of Plasmodium falciparum. The exact mechanism by which lumefantrine exerts its antimalarial effect is unknown. The most common adverse reactions of Coartem in adults are headache, anorexia, dizziness, asthenia, arthralgia and myalgia.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Hemin 3 Target ID: Hemin Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022268s012lbl.pdf	Binding Agent 1064

Conditions

Condition	Modality	Targets	Highest Phase	Product
Malaria 95 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022268s012lbl.pdf	Curative		Approved 8429	COARTEM Approved Use Coartem (artemether/lumefantrine) Tablets are indicated for treatment of acute, uncomplicated malaria infections due to Plasmodium falciparum in patients of 5 kg bodyweight and above. Coartem Tablets have been shown to be effective in geographical regions where resistance to chloroquine has been reported [see Clinical Studies (14.1) Launch Date 2009

C_max

Value	Dose	Co-administered	Analyte	Population
6.2 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10681341/	480 mg 1 times / day multiple, oral dose: 480 mg route of administration: Oral experiment type: MULTIPLE co-administered:		LUMEFANTRINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Co-administered	Analyte	Population
356 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10681341/	480 mg 1 times / day multiple, oral dose: 480 mg route of administration: Oral experiment type: MULTIPLE co-administered:		LUMEFANTRINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Co-administered	Analyte	Population
6.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10681341/	480 mg 1 times / day multiple, oral dose: 480 mg route of administration: Oral experiment type: MULTIPLE co-administered:		LUMEFANTRINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
0.3% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10681341/	480 mg 1 times / day multiple, oral dose: 480 mg route of administration: Oral experiment type: MULTIPLE co-administered:		LUMEFANTRINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

Doses

Dose	Population	Adverse events
240 mg 3 times / day multiple, oral Recommended Dose: 240 mg, 3 times / day Route: oral Route: multiple Dose: 240 mg, 3 times / day Co-administed with:: artemether(40 mg; PO; 4D1+2D2) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: A2403	unhealthy, 2 n = 310 Health Status: unhealthy Condition: malaria Age Group: 2 Sex: M+F Population Size: 310 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: A2403	Disc. AE: Urticaria... AEs leading to discontinuation/dose reduction: Urticaria (grade 3-4) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: A2403
480 mg 3 times / day multiple, oral Recommended Dose: 480 mg, 3 times / day Route: oral Route: multiple Dose: 480 mg, 3 times / day Co-administed with:: artemether(80 mg; PO; 4D1+2D2) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: A028	unhealthy, 25 n = 115 Health Status: unhealthy Condition: malaria Age Group: 25 Sex: M+F Population Size: 115 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: A028	Disc. AE: Abdominal pain... Other AEs: Dyspnea, Pulmonary edema... AEs leading to discontinuation/dose reduction: Abdominal pain (grade 1-2, uncommon) Other AEs: Dyspnea (grade 3-4, uncommon) Pulmonary edema (grade 3-4, uncommon) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: A028
240 mg 3 times / day multiple, oral Recommended Dose: 240 mg, 3 times / day Route: oral Route: multiple Dose: 240 mg, 3 times / day Co-administed with:: artemether(40 mg; PO; 4D1+2D2) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: B2303	unhealthy, 3 n = 447 Health Status: unhealthy Condition: malaria Age Group: 3 Sex: M+F Population Size: 447 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: B2303	Disc. AE: Vomiting, Urticaria... AEs leading to discontinuation/dose reduction: Vomiting (grade 3-4, most common) Urticaria (grade 3-4) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: B2303

AEs

AE	Significance	Dose	Population
Urticaria	grade 3-4 Disc. AE	240 mg 3 times / day multiple, oral Recommended Dose: 240 mg, 3 times / day Route: oral Route: multiple Dose: 240 mg, 3 times / day Co-administed with:: artemether(40 mg; PO; 4D1+2D2) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: A2403	unhealthy, 2 n = 310 Health Status: unhealthy Condition: malaria Age Group: 2 Sex: M+F Population Size: 310 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: A2403
Abdominal pain	grade 1-2, uncommon Disc. AE	480 mg 3 times / day multiple, oral Recommended Dose: 480 mg, 3 times / day Route: oral Route: multiple Dose: 480 mg, 3 times / day Co-administed with:: artemether(80 mg; PO; 4D1+2D2) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: A028	unhealthy, 25 n = 115 Health Status: unhealthy Condition: malaria Age Group: 25 Sex: M+F Population Size: 115 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: A028
Dyspnea	grade 3-4, uncommon	480 mg 3 times / day multiple, oral Recommended Dose: 480 mg, 3 times / day Route: oral Route: multiple Dose: 480 mg, 3 times / day Co-administed with:: artemether(80 mg; PO; 4D1+2D2) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: A028	unhealthy, 25 n = 115 Health Status: unhealthy Condition: malaria Age Group: 25 Sex: M+F Population Size: 115 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: A028
Pulmonary edema	grade 3-4, uncommon	480 mg 3 times / day multiple, oral Recommended Dose: 480 mg, 3 times / day Route: oral Route: multiple Dose: 480 mg, 3 times / day Co-administed with:: artemether(80 mg; PO; 4D1+2D2) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: A028	unhealthy, 25 n = 115 Health Status: unhealthy Condition: malaria Age Group: 25 Sex: M+F Population Size: 115 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: A028
Vomiting	grade 3-4, most common Disc. AE	240 mg 3 times / day multiple, oral Recommended Dose: 240 mg, 3 times / day Route: oral Route: multiple Dose: 240 mg, 3 times / day Co-administed with:: artemether(40 mg; PO; 4D1+2D2) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: B2303	unhealthy, 3 n = 447 Health Status: unhealthy Condition: malaria Age Group: 3 Sex: M+F Population Size: 447 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: B2303
Urticaria	grade 3-4 Disc. AE	240 mg 3 times / day multiple, oral Recommended Dose: 240 mg, 3 times / day Route: oral Route: multiple Dose: 240 mg, 3 times / day Co-administed with:: artemether(40 mg; PO; 4D1+2D2) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: B2303	unhealthy, 3 n = 447 Health Status: unhealthy Condition: malaria Age Group: 3 Sex: M+F Population Size: 447 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_MedR_P2.pdf Page: B2303

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737	inhibitor 1767 inducer 389	inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1524 CYP2A6 707 CYP2C19 1478 CYP2E1 882 CYP3A4/5 278 CYP4A9/11 37		CYP1A2 701 CYP2B6 547 CYP2C8 168 CYP2C19 293 CYP3A 129 CYP1A1 108

Drug as perpetrator

Target	Modality	Activity
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_ClinPharmR.pdf#page=30, https://www.pmda.go.jp/drugs/2016/P20161222001/300242000_22800AMX00727_I100_1.pdf#page=249 Page: (ClinPharm) 30, (PMDA_I100_1 in Japanese) 38	no [IC50 >2.0 uM]
CYP2A6 739	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_ClinPharmR.pdf#page=30, https://www.pmda.go.jp/drugs/2016/P20161222001/300242000_22800AMX00727_I100_1.pdf#page=249 Page: (ClinPharm) 30, (PMDA_I100_1 in Japanese) 38	no [IC50 >2.0 uM]
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_ClinPharmR.pdf#page=30, https://www.pmda.go.jp/drugs/2016/P20161222001/300242000_22800AMX00727_I100_1.pdf#page=249 Page: (ClinPharm) 30, (PMDA_I100_1 in Japanese) 38	no [IC50 >2.0 uM]
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_ClinPharmR.pdf#page=30, https://www.pmda.go.jp/drugs/2016/P20161222001/300242000_22800AMX00727_I100_1.pdf#page=249 Page: (ClinPharm) 30, (PMDA_I100_1 in Japanese) 38	no [IC50 >2.0 uM]
CYP2E1 970	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_ClinPharmR.pdf#page=30, https://www.pmda.go.jp/drugs/2016/P20161222001/300242000_22800AMX00727_I100_1.pdf#page=249 Page: (ClinPharm) 30, (PMDA_I100_1 in Japanese) 38	no [IC50 >2.0 uM]
CYP3A4/5 335	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_ClinPharmR.pdf#page=30, https://www.pmda.go.jp/drugs/2016/P20161222001/300242000_22800AMX00727_I100_1.pdf#page=249 Page: (ClinPharm) 30, (PMDA_I100_1 in Japanese) 38	no [IC50 >2.0 uM]
CYP4A9/11 37	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_ClinPharmR.pdf#page=30, https://www.pmda.go.jp/drugs/2016/P20161222001/300242000_22800AMX00727_I100_1.pdf#page=249 Page: (ClinPharm) 30, (PMDA_I100_1 in Japanese) 38	no [IC50 >2.0 uM]
CYP1A1 218	inducer 1573 Sources: https://www.pmda.go.jp/drugs/2016/P20161222001/300242000_22800AMX00727_I100_1.pdf#page=250 Page: (PMDA_I100_1 in Japanese) 250	no
CYP1A2 1692	inducer 1573 Sources: https://www.pmda.go.jp/drugs/2016/P20161222001/300242000_22800AMX00727_I100_1.pdf#page=250 Page: (PMDA_I100_1 in Japanese) 38, 250	no
CYP2B6 1001	inducer 1573 Sources: https://www.pmda.go.jp/drugs/2016/P20161222001/300242000_22800AMX00727_I100_1.pdf#page=250 Page: (PMDA_I100_1 in Japanese) 38, 250	no
CYP2C19 1553	inducer 1573 Sources: https://www.pmda.go.jp/drugs/2016/P20161222001/300242000_22800AMX00727_I100_1.pdf#page=250 Page: (PMDA_I100_1 in Japanese) 38, 250	no
CYP2C8 965	inducer 1573 Sources: https://www.pmda.go.jp/drugs/2016/P20161222001/300242000_22800AMX00727_I100_1.pdf#page=250 Page: (PMDA_I100_1 in Japanese) 38, 250	no
CYP2C9 1819	inducer 1573 Sources: https://www.pmda.go.jp/drugs/2016/P20161222001/300242000_22800AMX00727_I100_1.pdf#page=250 Page: (PMDA_I100_1 in Japanese) 38, 250	no
CYP3A 298	inducer 1573 Sources: https://www.pmda.go.jp/drugs/2016/P20161222001/300242000_22800AMX00727_I100_1.pdf#page=250 Page: (PMDA_I100_1 in Japanese) 38, 250	no
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_ClinPharmR.pdf#page=11, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_ClinPharmR.pdf#page=30, https://www.pmda.go.jp/drugs/2016/P20161222001/300242000_22800AMX00727_I100_1.pdf#page=249 Page: (ClinPharm) 2, 11, 30, (PMDA_I100_1 in Japanese) 38, 248-249	yes [IC50 0.997 uM]

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_ClinPharmR.pdf#page=9, https://www.pmda.go.jp/drugs/2016/P20161222001/300242000_22800AMX00727_K100_1.pdf#page=61 Page: (ClinPharm) 7, 9, 11, 21, (PMDA_K100_1 in Japanese) 61	major		yes (co-administration study) Comment: Human liver microsomes, Recombinant CYP3A4; Modest changes (<2.5-fold increase) in systemic exposure were observed with inhibitors or substrates of CYP3A4 including ketoconazole, mefloquine or quinine. The concentrations seen in the ketoconazole drug interaction study were within the range of systemic concentrations of Coartem seen in malaria patients in Phase III efficacy and safety studies. The concurrent oral administration of ketoconazole (400 mg on Day 1 followed by 200 mg on days 2,3, 4 and 5) with co-artemether (single dose of 4 tablets of 20 mg artemether/120 mg lumefantrine) led to a modest increase in lumefantrine (1.3-fold (Cmax), 1.6-fold (AUClast)) exposure in healthy subjects. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_ClinPharmR.pdf#page=9, https://www.pmda.go.jp/drugs/2016/P20161222001/300242000_22800AMX00727_K100_1.pdf#page=61 Page: (ClinPharm) 7, 9, 11, 21, (PMDA_K100_1 in Japanese) 61

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_PharmR.pdf#page=77, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_ClinPharmR.pdf#page=16 Page: 77, (ClinPharm) 16
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022268s000_PharmR.pdf#page=77 Page: 77.0		DESBUYL-BENFLUMETOL 3

Sourcing

Vendor/Aggregator	ID	URL
3B Scientific (Wuhan) Corp	3B2-6299	http://www.3bsc.com/index/pro_info.php?id=116861
AA Blocks	AA0036I3	https://www.aablocks.com/goods/Goods/detail?id=AA0036I3
AK Scientific, Inc. (AKSCI)	65683	http://www.aksci.com/item_detail.php?cat=65683
Aaron Chemicals	AR00379V	http://www.aaronchem.com/82186-77-4
Achemo Scientific Limited	AC-74186	http://www.achemo.com/search/?Keyword= 82186-77-4
Achemtek	0104-019643	http://www.achemtek.com/82186-77-4
Acorn PharmaTech	ACN-048710	http://www.acornpharmatech.com/
Alfa Chemistry	AP82186774	https://reagents.alfa-chemistry.com/product/lumefantrine-cas-82186-77-4-16977.html
Alsachim	1354	http://www.alsachim.com/product-C1742-glo.bal-view.html
AstaTech, Inc.	24538	http://www.astatechinc.com/CPSResult.php?CRNO=27834
Aurum Pharmatech LLC	S-4170	http://www.Aurumpharmatech.com/Product/ProductDetails/S_4170
AvaChem Scientific	2433	http://www.avachem.com/productSearch.asp?2433
Avantor Inc	TCL0256-25G	https://us.vwr.com/store/product/16813025/lumefantrine-98-0-by-hplc-titration-analysis
Avantor Inc	TCL0256-5G	https://us.vwr.com/store/product/16813025/lumefantrine-98-0-by-hplc-titration-analysis
BLD Pharm	BD220185	http://www.bldpharm.com/products/204133-10-8.html
BLD Pharm	BD115323	http://www.bldpharm.com/products/82186-77-4.html
Boerchem	BC682501	http://www.boerchem.com/?product_40130.html
CSNpharm	CSN10394	https://www.csnpharm.com/products/lumefantrine.html
Chem Scene	CS-5130	http://www.chemscene.com/82186-77-4.html
ChemMol	30110287	http://www.chemmol.com/chemmol/30110287.html
ChemMol	44011083	http://www.chemmol.com/chemmol/44011083.html
ChemMol	49400258	http://www.chemmol.com/chemmol/49400258.html
ChemMol	99172515	http://www.chemmol.com/chemmol/99172515.html
Chemenu	CM110477	http://www.chemenu.com/products/CM110477
Chemspace	CSSB00016988937	https://chem-space.com/CSSB00016988937
Glentham Life Sciences	GP5101	http://www.glentham.com/products/product/GP5101/
Hairui	HR126098	http://www.hairuichem.com/en/product/82186-77-4.html
Lab Network	LN00175760	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN00175760
Matrix Scientific	76072	https://www.matrixscientific.com/076072.html
MedChem Express	HY-B0803	https://www.medchemexpress.com/Lumefantrine.html
MuseChem	I004976	https://www.musechem.com/product/I004976.html
OChem	10386	http://www.ocheminc.com/index.php?act=psearch&pid=186L774
Oakwood	79421	http://www.oakwoodchemical.com/ProductsList.aspx?CategoryID=-2&txtSearch=64595&ExtHyperLink=1
Parchem	29326	http://www.parchem.com/chemical-supplier-distributor/Lumefantrine-019326.aspx
Renno Tech	RL05134	http://www.rennotech.com/product_show.asp?id=5383
Selleck Chemicals	S3746	http://www.selleckchem.com/products/lumefantrine.html
Sigma-Aldrich	L5420_SIGMA	https://www.sigmaaldrich.com/catalog/product/sigma/l5420?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich	1370746_USP	https://www.sigmaaldrich.com/catalog/product/usp/1370746?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Smolecule	S533785	http://www.smolecule.com/products/s533785
Smolecule	S533786	http://www.smolecule.com/products/s533786
TCI (Tokyo Chemical Industry)	L0256	http://www.tcichemicals.com/eshop/en/us/commodity/L0256/index.html
THE BioTek	bt-274421	https://www.thebiotek.com/product/inhibitors/bt-274421
THE BioTek	bt-274423	https://www.thebiotek.com/product/inhibitors/bt-274423
VladaChem	VL279049-25G	https://www.vladachem.com/product.php?products=82186-77-4
Yuhao Chemical	SY0308	http://www.chemyuhao.com/82186-77-4.html
abcr GmbH	AB436173	http://www.abcr.com/shop/en/AB436173
eNovation Chemicals	D506030	https://www.enovationchem.com/ProductDetails.asp?ProductID=D506030
eNovation Chemicals	D674512	https://www.enovationchem.com/ProductDetails.asp?ProductID=D674512
eNovation Chemicals	D767145	https://www.enovationchem.com/ProductDetails.asp?ProductID=D767145

PubMed

Title	Date	PubMed
Antimalarial drugs: QT prolongation and cardiac arrhythmias.	2005 May	15934850
In vitro sensitivities of Plasmodium falciparum to different antimalarial drugs in Uganda.	2010 Mar	20065051
In vitro activity of antiretroviral drugs against Plasmodium falciparum.	2011 Nov	21876053
Synthesis of novel 6-phenyl-2,4-disubstituted pyrimidine-5-carbonitriles as potential antimicrobial agents.	2011 Sep	21849221
A SYBR Green 1-based in vitro test of susceptibility of Ghanaian Plasmodium falciparum clinical isolates to a panel of anti-malarial drugs.	2013 Dec 17	24341604
Ex vivo responses of Plasmodium falciparum clinical isolates to conventional and new antimalarial drugs in Niger.	2013 Jul	23612203
Synthesis and antimalarial efficacy of two-carbon-linked, artemisinin-derived trioxane dimers in combination with known antimalarial drugs.	2013 Mar 28	23425037
Breakdown of phosphatidylserine asymmetry following treatment of erythrocytes with lumefantrine.	2014 Feb 20	24561477
In vitro and in vivo combination of cepharanthine with anti-malarial drugs.	2014 Mar 12	24618129

Patents

Sample Use Guides

In Vivo Use Guide

Tablets should be administered over 3 days for a total of 6 doses: an initial dose, second dose after 8 hours and then twice-daily (morning and evening) for the following 2 days. The adult dosage for patients with bodyweight of 35 kg and above is 4 tablets per dose for a total of 6 doses. Tablets are scored and contain 20 mg rtemether and 120 mg lumefantrine.

Route of Administration: Oral

In Vitro Use Guide

IC90 is higher in Plasmodium falciparum strain T-996 compared with strain LS-21: for Lumefantrine 293.03 and 95.61 nmol/L (154.69 and 50.47 ng/ml of EMM).

Substance Class	Chemical Created by `admin` on `Sat Dec 16 09:52:42 GMT 2023` Edited by `admin` on `Sat Dec 16 09:52:42 GMT 2023`
Record UNII	ZUV4B00D9P
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

LUMEFANTRINE, (+)-

Common Name

English

9H-FLUORENE-4-METHANOL, 2,7-DICHLORO-9-((4-CHLOROPHENYL)METHYLENE)-.ALPHA.-((DIBUTYLAMINO)METHYL)-, (Z)-(+)-

Systematic Name

English

D-BENFLUMELOL

Common Name

English

9H-FLUORENE-4-METHANOL, 2,7-DICHLORO-9-((4-CHLOROPHENYL)METHYLENE)-.ALPHA.-((DIBUTYLAMINO)METHYL)-, (9Z)-(+)-

Systematic Name

English

Code System Code Type Description

CAS

120583-70-2

Created by admin on Sat Dec 16 09:52:42 GMT 2023 , Edited by admin on Sat Dec 16 09:52:42 GMT 2023

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FDA UNII

ZUV4B00D9P

Created by admin on Sat Dec 16 09:52:42 GMT 2023 , Edited by admin on Sat Dec 16 09:52:42 GMT 2023

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PUBCHEM

6437380

Created by admin on Sat Dec 16 09:52:42 GMT 2023 , Edited by admin on Sat Dec 16 09:52:42 GMT 2023

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Related Record Type Details


					F38R0JR742

LUMEFANTRINE

RACEMATE -> ENANTIOMER


					01NP22J3SV

LUMEFANTRINE, (-)-

ENANTIOMER -> ENANTIOMER

Amount:

Details

SMILES

InChI

Originator

Approval Year

Targets

Conditions

Approved Use

Launch Date

Cmax

AUC

T1/2

Funbound

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

Tox targets

Sourcing

PubMed

Patents

Sample Use Guides

C_max

T_1/2

F_unbound

Drug as perpetrator