Page last updated: 2024-11-06

halofantrine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Halofantrine is an antimalarial drug that was developed in the 1980s. It is a synthetic compound with a complex chemical structure. It is a potent inhibitor of the parasite's heme polymerization, which is a crucial step in the parasite's life cycle. This effect is thought to contribute to its antimalarial activity. Halofantrine is effective against chloroquine-resistant strains of Plasmodium falciparum, the most dangerous species of malaria parasite. However, it has a number of potential side effects, including cardiac arrhythmias, which can be life-threatening. Due to these concerns, halofantrine is no longer widely used in many countries, but it remains an important treatment option in some regions where chloroquine resistance is high. Ongoing research is being conducted to develop safer and more effective antimalarial drugs. The study of halofantrine provides insight into the mechanisms of malaria parasite resistance and the development of new antimalarial drugs.'

halofantrine: used in treatment of mild to moderate acute malaria [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID37393
CHEMBL ID1107
CHEBI ID94392
SCHEMBL ID43795
MeSH IDM0081385

Synonyms (72)

Synonym
AC-481
CHEMBL1107
dl-wr-171669
BSPBIO_001241
PRESTWICK3_001031
NCI60_002593
3-(dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl]propan-1-ol
PRESTWICK2_001031
1,3-dichloro-alpha-(2-(dibutylamino)ethyl)-6-(trifluoromethyl)-9-phenanthrenemetnaol
3-(dibutylamino)-1-(1,3-dichlor-6-(trifluormethyl)-9-phenanthryl)propanol
halofantrine [usan]
halofantrina [inn-spanish]
halofantrinum [inn-latin]
9-phenanthrenemethanol, 1,3-dihydro-alpha-(2-(dibutylamino)ethyl)-6-(trifluoromethyl)-
BPBIO1_001366
NCGC00179250-01
3-(dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)-9-phenanthryl]propan-1-ol
(1)-halofantrine
9-phenanthrenemethanol, 1,3-dichloro-.alpha.-[2-(dibutylamino)ethyl]-6-(trifluoromethyl)-(1)
1,3-dichloro-.alpha.-[2-(dibutylamino)ethyl]-6- (trifluoromethyl)-9-phenathrenemethanol
AB00514703
halofantrine
C07634
69756-53-2
DB01218
PRESTWICK0_001031
SPBIO_003092
PRESTWICK1_001031
D08033
halofantrine (inn)
q2os4303hz ,
halofantrine [usan:inn:ban]
unii-q2os4303hz
FT-0601579
NCGC00179250-04
AKOS015907678
halofantrine [vandf]
halofantrine [who-dd]
9-phenanthrenemethanol, 1,3-dichloro-.alpha.-(2-(dibutylamino)ethyl)-6-(trifluoromethyl)-
1,3-dichloro-.alpha.-(2-(dibutylamino)ethyl)-6-(trifluoromethyl)-9-phenanthrenemethanol
(+/-)-halofantrine
halofantrine [mi]
halofantrine [inn]
MLS006010152
smr004701269
SCHEMBL43795
3-(dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)-9-phenanthrenyl]-1-propanol;hydrochloride
cid_37392
3-(dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)-9-phenanthryl]propan-1-ol;hydrochloride
1-[1,3-bis(chloranyl)-6-(trifluoromethyl)phenanthren-9-yl]-3-(dibutylamino)propan-1-ol;hydrochloride
bdbm79214
1-[-1,3-dichloro-6-trifluoromethyl-9-phenanthryl]-3-di(n-butyl)aminopropanol
9-phenanthrenemethanol, 1,3-dichloro-.alpha.-[2-(dibutylamino)ethyl]-6-(trifluoromethyl)-
1,3-dichloro-.alpha.-[2-(dibutylamino)ethyl]-6-(trifluoromethyl)-9-phenanthrene-methanol
3-(dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)-9-phenanthryl]-1-propanol #
3-(dibutylamino)-1-(1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl)propan-1-ol
DTXSID0023119
3-(dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)-9-phenanthrenyl]-1-propanol
CHEBI:94392
unii-r7ads21fsn
9-phenanthrenemethanol, 1,3-dichloro-alpha-(2-(dibutylamino)ethyl)-6-(trifluoromethyl)-, (-)-
66051-76-1
halofantrine, (-)-
gtpl10019
AS-14162
BCP13777
Q947595
9-phenanthrenemethanol, 1,3-dichloro-alpha-(2-(dibutylamino)ethyl)-6-(trifluoromethyl)-, (+)-
unii-4646b297u7
HY-A0148
CS-0017473
EN300-226522

Research Excerpts

Overview

Halofantrine (Hf) is a chiral, lipophilic phenanthrene methanol antimalarial which exhibits both enantioselective plasma pharmacokinetics and extensive lymphatic absorption when administered postprandially. It is a poor inhibitor of calmodulin-dependent myosin light chain kinase (MLCK) and wheat embryo Ca(2+)-dependent protein kinases.

ExcerptReferenceRelevance
"Halofantrine is a newly developed antimalarial drug used for the treatment of Plasmodium falciparum malaria. "( Is halofantrine ototoxic? Experimental study on guinea pig cochlea model.
Ahmed, MR; Iskander, NM; Mohamed, AA; Youssef, TF, 2010
)
2.42
"Halofantrine (Hf) is a chiral, lipophilic phenanthrene methanol antimalarial which exhibits both enantioselective plasma pharmacokinetics and extensive lymphatic absorption when administered postprandially. "( Does stereoselective lymphatic absorption contribute to the enantioselective pharmacokinetics of halofantrine In Vivo?
Charman, WN; Porter, CJ; Shackleford, DM, 2003
)
1.98
"Halofantrine is an antimalarial drug developed as a treatment of P. "( Block of wild-type and inactivation-deficient human ether-a-go-go-related gene K+ channels by halofantrine.
Navarro-Polanco, RA; Sánchez-Chapula, JA; Sanguinetti, MC, 2004
)
1.99
"Halofantrine (HF) is a poorly water-soluble antimalarial drug with low bioavailability. "( Dissolution properties and characterization of halofantrine-2-hydroxypropyl-beta-cyclodextrin binary systems.
Oladimeji, FA; Omoruyi, SI; Onyeji, CO, 2007
)
2.04
"Halofantrine is a poor inhibitor of calmodulin-dependent myosin light chain kinase (MLCK) and wheat embryo Ca(2+)-dependent protein kinase (CDPK) and does not inhibit rat brain Ca(2+)- and phospholipid-dependent protein kinase C (PKC)."( Specific inhibition of cyclic AMP-dependent protein kinase by the antimalarial halofantrine and by related phenanthrenes.
Polya, GM; Ternai, B; Wang, BH, 1994
)
1.24
"Halofantrine is an antimalarial drug widely prescribed for chloroquine-resistant strains of Plasmodium falciparum. "( [Halofantrine: for new rules of prescription].
Fourcade, L; Mojon, M; Peyron, F; Touze, JE, 1995
)
2.64
"Halofantrine is a phenanthrenemethanol antimalarial that is effective against asexual forms of multidrug-resistant Plasmodium falciparum malaria. "( Clinical pharmacokinetics of halofantrine.
Karbwang, J; Na Bangchang, K, 1994
)
2.02
"Halofantrine is a viable drug in the treatment of uncomplicated P."( Efficacy of halofantrine in the treatment of uncomplicated falciparum malaria.
Chunge, C; Luta, M; Mbori-Ngacha, DA; Muga, RO; Oloo, AJ; Onyango, FE, 1995
)
1.39
"Halofantrine hydrochloride is an important, highly lipophilic anti-malarial agent. "( Lymphatic transport of halofantrine in the triple-cannulated anesthetized rat model: effect of lipid vehicle dispersion.
Charman, SA; Charman, WN; Porter, CJ, 1996
)
2.05
"Halofantrine (Hf) is a highly lipophilic antimalarial which significantly associates with triglyceride (TG) rich plasma lipoproteins, and this is likely manifest as a decrease in the free fraction of drug. "( Effect of altered serum lipid concentrations on the IC50 of halofantrine against Plasmodium falciparum.
Charman, WN; Cowman, AF; Horton, J; Humberstone, AJ, 1998
)
1.99
"Halofantrine is an antimalarial drug which is widely prescribed for the treatment of infections with chloroquine-resistant strains of Plasmodium falciparum. "( Is halofantrine still advisable in malaria attacks?
Deharo, JC; Fourcade, L; Heno, P; Peyron, F; Touze, JE, 1997
)
2.36
"Halofantrine (Hf) is a highly lipophilic antimalarial with poor and erratic absorption. "( Metabolism of halofantrine to its equipotent metabolite, desbutylhalofantrine, is decreased when orally administered with ketoconazole.
Charman, WN; Edwards, GA; Khoo, SM; Porter, JH, 1998
)
2.1
"Halofantrine is a newer antimalarial drug which has not been approved for clinical use in Papua New Guinea. "( In vitro susceptibility of Plasmodium falciparum isolates to halofantrine in the Central Province of Papua New Guinea.
Hombhanje, FW; Kereu, RK, 1998
)
1.98
"Halofantrine is a newer antimalarial drug which has not been approved for clinical use in Papua New Guinea. "( In vitro susceptibility of Plasmodium falciparum isolates to halofantrine in the Central Province of Papua New Guinea.
Hombhanje, FW; Kereu, RK, 1998
)
1.98
"Halofantrine is a widely used antimalarial agent which has been associated with prolongation of the 'QT interval' of the electrocardiogram (ECG), torsades de pointes and sudden death. "( Inhibition of HERG potassium channels by the antimalarial agent halofantrine.
Breit, SN; Bursill, JA; Campbell, TJ; Singleton, CB; Tie, H; Valenzuela, SM; Walker, BD; Wyse, KR, 2000
)
1.99
"Halofantrine (HF) is a chiral antimalarial drug known to cause cardiac arrhythmias in susceptible patients. "( Stereoselective halofantrine and desbutylhalofantrine disposition in the rat: cardiac and plasma concentrations and plasma protein binding.
Brocks, DR, 2002
)
2.1
"Halofantrine is an orally administered blood schizontocide which is active against both chloroquine-sensitive and chloroquine-resistant plasmodia. "( Halofantrine. A review of its antimalarial activity, pharmacokinetic properties and therapeutic potential.
Bryson, HM; Goa, KL, 1992
)
3.17
"Halofantrine is a new blood schizontocidal drug used for the treatment of multidrug-resistant falciparum malaria. "( Pharmacokinetics of halofantrine and n-desbutylhalofantrine in patients with falciparum malaria following a multiple dose regimen of halofantrine.
Edstein, MD; Kere, N; Parkinson, AD; Rieckmann, KH; Veenendaal, JR, 1991
)
2.05
"Halofantrine is a new precious alternative for the treatment of malaria in regions with extensive multi-drug resistant strains of Plasmodium."( [Halofantrine hydrochloride in the treatment of Plasmodium falciparum malaria in a region of resistance. Analysis of 54 pediatric cases].
Kayembe, N; Kingway, MP; Mashako, MN, 1990
)
1.91
"Halofantrine hydrochloride is an efficient antimalarial drug in semi-immune patients."( [Halofantrine in the treatment of malaria. Clinical trial in a semi-rural zone of Cameroon].
Bouloumie, J; Lambert, MT; Macaigne, F; Raccurt, CP; Ribou, G; Ripert, C, 1989
)
1.91
"Halofantrine (WR 171.669) is a phenanthrene methanol derivative effective against the multidrug resistant strains of Plasmodium falciparum. "( [Efficacy of halofantrine in Plasmodium falciparum or Plasmodium vivax malaria in a resistance area (French Guiana)].
Carles, G; John, M; Joly, F; Maisonneuve, H; Rossignol, JF, 1988
)
2.09
"Halofantrine is a 9-phenanthrenemethanol which is effective against multi-drug resistant strains of Plasmodium falciparum. "( Treatment of imported cases of falciparum malaria in France with halofantrine.
Coulaud, JP; Le Bras, J; Matheron, S; Moriniere, B; Rossignol, JF; Saimot, AG, 1986
)
1.95
"Halofantrine is a 9-phenanthrene-methanol effective against multiresistant strains of Plasmodium falciparum. "( [Treatment with halofantrine of Plasmodium falciparum malaria imported into France].
Coulaud, JP; Le Bras, J; Matheron, S; Morinière, B; Rossignol, JF; Saimot, AG, 1985
)
2.06

Effects

Halofantrine has mild to moderate pathological effects on cochlea histology, and can be considered an ototoxic drug. It has been shown to be effective against multidrug resistant Plasmodium falciparum.

ExcerptReferenceRelevance
"Halofantrine has an elimination half-life of between 1.3 and 6.6 days."( [Pharmacokinetics of antimalarials: quinine and mefloquine, halofantrine, qinghaosu, amino-4-quinolines].
Blayo, MC; Pussard, E; Verdier, F,
)
1.09
"Halofantrine has mild to moderate pathological effects on cochlea histology, and can be considered an ototoxic drug."( Is halofantrine ototoxic? Experimental study on guinea pig cochlea model.
Ahmed, MR; Iskander, NM; Mohamed, AA; Youssef, TF, 2010
)
2.42
"Halofantrine efficacy has been poorly assessed in non-immune children."( Halofantrine efficacy in non-immune children with imported acute Plasmodium falciparum malaria Infection.
Aberrane, S; Cohen, R; De la Rocque, F; Delacourt, C; Hau, I; Ovetchkine, P; Reinert, P; Seringe, S, 2004
)
2.49
"Halofantrine has been observed to cause QT interval prolongation in susceptible patients and the effect has most commonly been observed after post-prandial administration. "( Evaluation of the impact of altered lipoprotein binding conditions on halofantrine induced QTc interval prolongation in an anaesthetized rabbit model.
Batey, AJ; Charman, WN; Coker, SJ; McIntosh, MP; Porter, CJ, 2004
)
2
"Halofantrine has been shown to be very effective against multiple drug resistant falciparum malaria. "( [Long QTc interval complicating halofantrine therapy in 2 children with Plasmodium falciparum malaria].
Jacqz-Aigrain, E; Olivier, C; Rizk, C; Zhang, D, 1999
)
2.03
"Halofantrine has been shown to be effective against multidrug resistant Plasmodium falciparum."( Clinical trial of halofantrine with modified doses for treatment of malaria in the hospital for tropical diseases.
Chalermrut, K; Horton, J; Kaivipakbanyai, W; Krudsood, S; Kyle, D; Looareesuwan, S; Phophak, N; Silachamroon, U; Singhasivanon, P; Treeprasertsuk, S, 2001
)
1.37
"Halofantrine has been given to 14 children and 15 adults suffering from an acute attack of P. "( [Trial of halofantrine in the treatment of malaria attacks by Plasmodium falciparum in Dakar (Senegal)].
Bah, IB; Diallo, S; Dieng, T; Faye, O; Gaye, O; Konate, L; Legros, C; Trape, JF, 1991
)
2.13
"Halofantrine has an elimination half-life of between 1.3 and 6.6 days."( [Pharmacokinetics of antimalarials: quinine and mefloquine, halofantrine, qinghaosu, amino-4-quinolines].
Blayo, MC; Pussard, E; Verdier, F,
)
1.09

Actions

Halofantrine can cause a prolongation of the cardiac QT interval, leading to serious ventricular arrhythmias.

ExcerptReferenceRelevance
"Halofantrine was chosen because its behaviour in lipid-based formulations has been widely investigated and because of its close structural relationship to lumefantrine, an antimalarial drug of current interest for the treatment of paediatric malaria."( The impact of digestion is essential to the understanding of milk as a drug delivery system for poorly water soluble drugs.
Boyd, BJ; Clulow, AJ; Hawley, A; Pham, AC; Ramirez, G; Salim, M, 2018
)
1.2
"Halofantrine can cause a prolongation of the cardiac QT interval, leading to serious ventricular arrhythmias. "( Effect of experimental hyperlipidaemia on the electrocardiographic effects of repeated doses of halofantrine in rats.
Brocks, DR; Patel, JP, 2010
)
2.02

Treatment

Halofantrine was successful in all but one case which required combined chemotherapy using quinine and doxycycline. Treatment by halofantrin with a single cure was followed by five relapses.

ExcerptReferenceRelevance
"Halofantrine effectively treated uncomplicated P."( Short report: in vivo sensitivity of Plasmodium falciparum to halofantrine in southern central Vietnam.
Baird, JK; Doan, HN; Fryauff, DJ; Gómez-Saladín, E; Le, DC; Nguyen, DT; Susanti, I; Taylor, WR; Tran, TU, 2003
)
1.28
"Treatment with halofantrine was followed by a significant increase in QTc dispersion at 9 hours (P < 0.0001) and 24 hours (P < 0.01)."( The effects of antimalarial drugs on ventricular repolarization.
Bohan, S; Buguet, A; Deharo, JC; Fourcade, L; Heno, P; Kouassi, E; Paule, P; Riviere, P; Thomas, G; Touze, JE, 2002
)
0.65
"Treatment with halofantrine was successful after he developed cerebral malaria with recovery."( Recrudescence of Plasmodium falciparum malaria contracted in Lombok, Indonesia after quinine/doxycycline and mefloquine: case report.
Pillans, PI; Tish, KN, 1997
)
0.64
"Treatment with halofantrine was successful in all but one case which required combined chemotherapy using quinine and doxycycline."( [Health assessments of a military company stationed on the Maroni River in French Guiana].
Lial, JP, 1999
)
0.64
"Treatment by halofantrine with a single cure was followed by five relapses."( [Imported malaria in children in 1999. Study of the Armand-Trousseau Hospital in Paris].
Adam, M; Bégué, P; Delée, S; Favier, R; Grimprel, E; Parez, N; Quinet, B, 2002
)
0.67

Toxicity

ExcerptReferenceRelevance
" Mild adverse reactions of abdominal pain in one patient and vomiting in one patient were encountered which did not require any treatment."( Efficacy and safety of halofantrine in acute malaria.
Kamalakar, KV; Rao, KS, 1993
)
0.6
" Abdominal pain was the commonest adverse event reported (22 cases)."( Evaluation of the safety and efficacy of micronized halofantrine in the treatment of semi-immune patients with acute, Plasmodium falciparum malaria.
Gillespie, SH; Kennedy, N; Msaki, EP; Ngowi, FI; Ramsay, AR, 1996
)
0.54
" The pharmacokinetic data, however, showed that they are of similar profile, except in adverse features and contraindications, and values like their half-life (t1/2) where the long (t1/2) in drugs like sulphadoxine-pyrimethamine endows them with suppressive-cure feature, especially against recrudescent strains."( Comparative efficacy and safety of chloroquine and alternative antimalarial drugs: a meta-analysis from six African countries.
Makonnen, E; Mengesha, T, 1999
)
0.3
" Pharmacokinetic profile demonstrates that all these drugs have similar therapeutic effects, but differ in their adverse reactions, contraindications, and half-life."( Comparative efficacy and safety of chloroquine and alternative antimalarial drugs: a meta-analysis from six African countries.
Makonnen, E; Mengesha, T, 1999
)
0.3
"Although it is difficult to ascertain causality and to estimate overall incidence, a significant number of adverse events related to the cardiovascular system were reported, including QT interval prolongation, life-threatening arrhythmias, and sudden death."( Mechanism of cardiotoxicity of halofantrine.
Schuster, BG; Wang, WX; Wesche, DL; Woosley, RL, 2000
)
0.59
"The clinical potential of mefloquine has been compromised by reports of adverse neurological effects."( The antimalarial potential of 4-quinolinecarbinolamines may be limited due to neurotoxicity and cross-resistance in mefloquine-resistant Plasmodium falciparum strains.
Bhattacharjee, AK; Dow, GS; Gerena, L; Hudson, TH; Koenig, ML; Lopez-Sanchez, M; Wolf, L, 2004
)
0.32
" Eleven point eight percent (12/102) of patients reported adverse events, of which abdominal pain, reported by one subject, was considered to be probably related to the drug and required corrective therapy."( Efficacy and safety of halofantrine in Pakistani children and adults with malaria caused by P. falciparum and P. vivax.
Ahmed, TM; Gilal, N; Isani, Z; Khan, MZ; Maqbool, S; Mehmood, K; Srinivasa, KB; Yazdani, I; Zafar, AB, 2006
)
0.64
"Halofantrine (HF) was considered an effective and safe treatment for multi-drug resistant falciparum malaria until 1993, when the first case of drug-associated death was reported."( Fatal cardiotoxicity related to halofantrine: a review based on a worldwide safety data base.
Bouchaud, O; Danis, M; Dodoo, AN; Imbert, P; Legros, F; Touze, JE, 2009
)
2.08

Pharmacokinetics

Halofantrine elimination half-life was significantly shorter in patients with malaria than healthy control subjects. Poor and erratic absorption could be just as likely to explain therapeutic failure as resistance of the parasite to effects of this drug.

ExcerptReferenceRelevance
" For Hfm, in the dose range 250-500 mg, AUC but not Cmax increased in proportion in the increase in dose size."( Pharmacokinetics of halofantrine in man: effects of food and dose size.
Breckenridge, AM; Edwards, G; Milton, KA; Orme, ML; Ward, SA, 1989
)
0.6
" Parameters such as half-life distribution volume, clearance and bioavailability, are defined."( [Pharmacokinetics of antimalarials: quinine and mefloquine, halofantrine, qinghaosu, amino-4-quinolines].
Blayo, MC; Pussard, E; Verdier, F,
)
0.37
"For the past 300 years antimalarial dosage regimens have not been based on pharmacokinetic information."( Clinical pharmacokinetics of antimalarial drugs.
White, NJ,
)
0.13
" Halofantrine elimination half-life was significantly shorter in patients with malaria than healthy control subjects (9."( Pharmacokinetics of an extended-dose halofantrine regimen in patients with malaria and in healthy volunteers.
Fleckenstein, L; Keeratithakul, D; Loesuttiviboon, L; Ohrt, C; Schuster, B; Teja-Isavadharm, P; Watt, G; Webster, HK, 1995
)
1.47
" Bioavailability is not dose-proportional for doses over 500mg, but there is a dose-proportional increase in Cmax and area under the plasma concentration-time curve (AUC) for doses between 250 and 500mg."( Clinical pharmacokinetics of halofantrine.
Karbwang, J; Na Bangchang, K, 1994
)
0.58
" Similarly, evaluation of the pharmacokinetic properties of halofantrine has led to the demonstration that poor and erratic absorption could be just as likely to explain therapeutic failure as resistance of the parasite to effects of this drug."( Clinical pharmacokinetics in the treatment of tropical diseases. Some applications and limitations.
Edwards, G; Ward, SA; Winstanley, PA, 1994
)
0.53
" Pharmacokinetic studies suggested that the micronized formulation of halofantrine hydrochloride may not increase drug absorption considerably."( Clinical efficacy and pharmacokinetics of micronized halofantrine for the treatment of acute uncomplicated falciparum malaria in nonimmune patients.
Basco, LK; Bouchaud, O; Bouvet, E; Coulaud, JP; Farinotti, R; Genissel, B; Gillotin, C; Gimenez, F; Le Bras, J; Ramiliarisoa, O, 1994
)
0.77
" In theory, short half-life compounds reduce the selective pressure for resistance, which may be a major determinant of the useful therapeutic life of an antimalarial drug."( Pharmacology and pharmacokinetics of new antimalarials.
Watkins, WM, 1995
)
0.29
" This study confirms that the clearance of Hf is influenced by plasma lipoprotein profiles, and the findings have implications for the design and interpretation of fed/fasted bioavailability studies of lipophilic drugs and determination of their intrinsic pharmacokinetic parameters in subjects or patients with dyslipidemic profiles."( Association of halofantrine with postprandially derived plasma lipoproteins decreases its clearance relative to administration in the fasted state.
Charman, WN; Edwards, GA; Humberstone, AJ; Porter, CJ, 1998
)
0.65
" In order to define the pharmacokinetic properties of halofantrine enantiomers in the rat, male Sprague-Dawley rats (264-311 g) were given halofantrine HCl orally (n = 5; 14 mg/kg) or intravenously (i."( Pharmacokinetics of halofantrine in the rat: stereoselectivity and interspecies comparisons.
Brocks, DR; Toni, JW, 1999
)
0.88
"05) in the maximum plasma concentration (C(max)), total area under the concentration-time curve (AUC), and terminal elimination half-life (t(1/2,z)), compared with halofantrine alone."( Effects of tetracycline on the pharmacokinetics of halofantrine in healthy volunteers.
Bassi, PU; Onyeji, CO; Ukponmwan, OE, 2004
)
0.77
" The method was successfully applied for the pharmacokinetic study in rats."( Determination of lumefantrine in rat plasma by liquid-liquid extraction using LC-MS/MS with electrospray ionization: assay development, validation and application to a pharmacokinetic study.
Jain, GK; Singh, SP, 2009
)
0.35
"The pharmacokinetic properties of HF in patients with malaria are affected by several demographic variables as well as other relevant covariates."( Population pharmacokinetics of halofantrine in healthy volunteers and patients with symptomatic falciparum malaria.
Aarons, L; Edstein, MD; Klein, K; Nosten, F; Teja-Isavadharm, P; Ter Kuile, FO; White, NJ, 2012
)
0.66
"The pharmacokinetic compatibility of short-acting CDRI candidate antimalarial trioxane derivative, 99-411, was tested with long-acting prescription antimalarials, lumefantrine and piperaquine."( Assessment of pharmacokinetic compatibility of short acting CDRI candidate trioxane derivative, 99-411, with long acting prescription antimalarials, lumefantrine and piperaquine.
Raju, KS; Singh, SP; Taneja, I; Wahajuddin, M, 2015
)
0.42

Compound-Compound Interactions

ExcerptReferenceRelevance
" falciparum in a high-throughput in vitro assay and to protect mice against lethal cerebral malaria caused by Plasmodium berghei ANKA when used alone or in combination with established antimalarial drugs."( Treatment of murine cerebral malaria by artemisone in combination with conventional antimalarial drugs: antiplasmodial effects and immune responses.
Clark, J; Golenser, J; Guiguemde, WA; Guo, J; Guy, RK; Haynes, RK; Hunt, NH; Marciano, A, 2014
)
0.4

Bioavailability

The bioavailability of the poorly soluble model drug halofantrine, dosed in a soy bean oil solution or in a self-nanoemulsifying drug delivery system (SNEDDS), at two levels of lipid, was assessed in rats. The more compound, the more PS80 was needed to prevent precipitation.

ExcerptReferenceRelevance
" We suggest that the large intersubject variability in plasma drug concentrations may relate in part to its poor and inconsistent bioavailability and this rather than true resistance might be responsible for some of the treatment failures."( Pharmacokinetics of halofantrine in Thai patients with acute uncomplicated falciparum malaria.
Bunnag, D; Edwards, G; Karbwang, J; Milton, KA; Na Bangchang, K; Ward, SA, 1991
)
0.6
" Oral HF may be appropriate for some cases of uncomplicated falciparum malaria in Africa, but in patients with severe malaria, the bioavailability of HF and HFm may be inadequate."( Halofantrine pharmacokinetics in Kenyan children with non-severe and severe malaria.
Forster, D; Kokwaro, G; Marsh, K; Mberu, EK; Murphy, SA; Mwangi, I; Newton, CJ; Watkins, WM; Winstanley, PA, 1995
)
1.73
" Halofantrine peak plasma concentrations and bioavailability on the first day of treatment were significantly lower in patients with malaria than in healthy volunteers."( Pharmacokinetics of an extended-dose halofantrine regimen in patients with malaria and in healthy volunteers.
Fleckenstein, L; Keeratithakul, D; Loesuttiviboon, L; Ohrt, C; Schuster, B; Teja-Isavadharm, P; Watt, G; Webster, HK, 1995
)
1.47
" Bioavailability is not dose-proportional for doses over 500mg, but there is a dose-proportional increase in Cmax and area under the plasma concentration-time curve (AUC) for doses between 250 and 500mg."( Clinical pharmacokinetics of halofantrine.
Karbwang, J; Na Bangchang, K, 1994
)
0.58
" Food increases the oral bioavailability of Hf in humans approximately 3-5-fold, although neither the absolute bioavailability nor the basis for the food effect has been fully defined."( A physicochemical basis for the effect of food on the absolute oral bioavailability of halofantrine.
Charman, WN; Humberstone, AJ; Porter, CJ, 1996
)
0.52
" Lymphatic transport was a major contributor to bioavailability as demonstrated by the recovery of up to approximately 20% of the administered dose in the intestinal lymph."( Lymphatic transport of halofantrine in the triple-cannulated anesthetized rat model: effect of lipid vehicle dispersion.
Charman, SA; Charman, WN; Porter, CJ, 1996
)
0.6
"The oral bioavailability of halofantrine (Hf), a highly lipophilic phenanthrenemethanol antimalarial, is significantly enhanced when ingested with food."( Association of halofantrine with postprandially derived plasma lipoproteins decreases its clearance relative to administration in the fasted state.
Charman, WN; Edwards, GA; Humberstone, AJ; Porter, CJ, 1998
)
0.95
" The effect of magnesium carbonate on the bioavailability of Hf was evaluated in seven healthy volunteers."( Altered pharmacokinetics of halofantrine by an antacid, magnesium carbonate.
Aideloje, SO; Onyeji, CO; Ugwu, NC, 1998
)
0.59
" The bioavailability of the enantiomers after oral administration was less than 27%."( Pharmacokinetics of halofantrine in the rat: stereoselectivity and interspecies comparisons.
Brocks, DR; Toni, JW, 1999
)
0.63
"The contribution of lymphatic transport and absorption directly into the portal blood to the overall oral bioavailability of a model lipophilic drug, halofantrine (Hf), was determined in lymph-cannulated, conscious, unrestrained rats after administration in lipidic vehicles with different fatty acid chain lengths."( Effect of short-, medium-, and long-chain fatty acid-based vehicles on the absolute oral bioavailability and intestinal lymphatic transport of halofantrine and assessment of mass balance in lymph-cannulated and non-cannulated rats.
Caliph, SM; Charman, WN; Porter, CJ, 2000
)
0.71
"A non-solubilizing solid dispersion formulation (polyethylene glycol 6000) and two solubilizing solid dispersions (Vitamin E TPGS and a Gelucire 44/14/Vitamin E TPGS blend) containing the antimalarial, Halofantrine (Hf), were formulated for bioavailability assessment in fasted beagles to determine if the oral absorption of Hf can be enhanced by these delivery systems."( The formulation of Halofantrine as either non-solubilizing PEG 6000 or solubilizing lipid based solid dispersions: physical stability and absolute bioavailability assessment.
Charman, WN; Khoo, SM; Porter, CJ, 2000
)
0.82
" The statistically analysis of the mean total bioavailability therefore shows that the absorption of halofantrine was largely independent on triglyceride unsaturation."( Comparison of total oral bioavailability and the lymphatic transport of halofantrine from three different unsaturated triglycerides in lymph-cannulated conscious rats.
Christensen, E; Holm, R; Høy, CE; Kristensen, HG; Müllertz, A, 2001
)
0.76
"The low aqueous solubility of halofantrine (HF) and its low bioavailability from commercially available tablets (Halfan) suggested the formulation of solid dispersions (SDs) of HF to reduce its particle size and improve its wettability and aqueous solubility."( Preparation and in vitro evaluation of solid dispersions of halofantrine.
Abdul-Fattah, AM; Bhargava, HN, 2002
)
0.85
" Because lipids may affect clearance of drugs that bind to lipoproteins, in determining bioavailability of such drugs in food-effect studies, reference intravenous groups should be included to separate true increase in bioavailability from the effects of decreased clearance."( The influence of lipids on stereoselective pharmacokinetics of halofantrine: Important implications in food-effect studies involving drugs that bind to lipoproteins.
Brocks, DR; Wasan, KM, 2002
)
0.55
"In this study, we evaluated the ability of a coated, encapsulated formulation to increase the oral bioavailability of (+/-)-halofantrine (HF) enantiomers, a drug with low and erratic oral bioavailability."( Enhanced oral absorption of halofantrine enantiomers after encapsulation in a proliposomal formulation.
Betageri, GV; Brocks, DR, 2002
)
0.82
" Grapefruit juice increases the bioavailability of several orally administered CYP3A4 substrates by inhibiting CYP3A4 at the enterocyte level and could therefore increase the risk of halofantrine-induced QT interval prolongation."( Pharmacokinetic and pharmacodynamic interaction between grapefruit juice and halofantrine.
Becquemont, L; Charbit, B; Funck-Brentano, C; Lepère, B; Peytavin, G, 2002
)
0.74
"Grapefruit juice increases halofantrine bioavailability and halofantrine-induced QT interval prolongation."( Pharmacokinetic and pharmacodynamic interaction between grapefruit juice and halofantrine.
Becquemont, L; Charbit, B; Funck-Brentano, C; Lepère, B; Peytavin, G, 2002
)
0.84
" A previously optimised SMEDDS formulation for halofantrine, comprising of triglyceride, Cremophor EL, Maisine 35-1 and ethanol was selected for bioavailability assessment."( Examination of oral absorption and lymphatic transport of halofantrine in a triple-cannulated canine model after administration in self-microemulsifying drug delivery systems (SMEDDS) containing structured triglycerides.
Charman, WN; Edwards, GA; Holm, R; Kristensen, HG; Müllertz, A; Porter, CJ, 2003
)
0.82
"Recent studies in a conscious dog model demonstrated intestinal lymphatic transport to be a significant contributor to the bioavailability of the highly lipid-soluble free-base of halofantrine (Hf), and surprisingly, also the poorly lipid-soluble hydrochloride salt (Hf."( Partitioning of halofantrine hydrochloride between water, micellar solutions, and soybean oil: Effects on its apparent ionization constant.
Charman, WN; Galland, A; Perry, CS; Prankerd, RJ; Taillardat-Bertschinger, A, 2003
)
0.86
"The relative oral bioavailability (BA) of halofantrine base (Hf) was assessed in male beagle dogs after administration of a medium chain triglyceride (MCT), a long chain triglyceride (LCT), and a blended LCT/MCT lipid solution formulation of Hf (Study 1) and after administration of suspensions of Hf base and Hf."( Use of in vitro lipid digestion data to explain the in vivo performance of triglyceride-based oral lipid formulations of poorly water-soluble drugs: studies with halofantrine.
Boyd, BJ; Charman, WN; Edwards, GA; Kaukonen, AM; O'Connor, JM; Porter, CJ; Taillardat-Bertschinger, A, 2004
)
0.78
" The fraction of halofantrine transported to the lymphatic system was determined as the difference between the bioavailability in saline-pretreated rats and cycloheximide-pretreated rats."( Intestinal lymphatic transport of halofantrine in rats assessed using a chylomicron flow blocking approach: the influence of polysorbate 60 and 80.
Holm, R; Jacobsen, J; Lind, ML; Müllertz, A, 2008
)
0.96
"The contribution of lymphatic transport to the oral bioavailability of methylnortestosterone (M) after oral administration of the lipophilic prodrug methylnortestosterone undecanoate (MU) has been evaluated, and the sensitivity of lymphatic MU transport to lymphatic lipid transport has been investigated."( Lymphatic transport of Methylnortestosterone undecanoate (MU) and the bioavailability of methylnortestosterone are highly sensitive to the mass of coadministered lipid after oral administration of MU.
Charman, WN; Edwards, GA; Faassen, WA; Nguyen, G; Porter, CJ; White, KL, 2009
)
0.35
"The aim of this study was to examine the effects of formulations of polysorbate 80 (PS 80) and polyethylene glycol 400 (PEG 400) on the precipitation and oral bioavailability of the hydrophobic drug halofantrine."( Effects of polysorbate 80 on the in-vitro precipitation and oral bioavailability of halofantrine from polyethylene glycol 400 formulations in rats.
Bisgaard, J; Holm, R; Jacobsen, J; Müllertz, A; Tønsberg, H, 2010
)
0.77
" The animals dosed with the PEG 400 formulation had significant lower bioavailability than the PS 80-PEG 400 co-mixtures, possibly due to halofantrine precipitation in the gastrointestinal tract."( Effects of polysorbate 80 on the in-vitro precipitation and oral bioavailability of halofantrine from polyethylene glycol 400 formulations in rats.
Bisgaard, J; Holm, R; Jacobsen, J; Müllertz, A; Tønsberg, H, 2010
)
0.79
"Addition of PS80 to the formulation increased the bioavailability of halofantrine and the more compound, the more PS80 was needed to prevent precipitation."( Effects of polysorbate 80 on the in-vitro precipitation and oral bioavailability of halofantrine from polyethylene glycol 400 formulations in rats.
Bisgaard, J; Holm, R; Jacobsen, J; Müllertz, A; Tønsberg, H, 2010
)
0.82
" However, in vivo bioavailability studies in rats showed the same plasma concentration-time profiles when dosing 10mg/kg halofantrine at two dose levels of F6H8, MCT or F6H8:MCT (1:1) (AUC ranged from 3058 to 3447hng/ml, T(max)∼6."( A novel excipient, 1-perfluorohexyloctane shows limited utility for the oral delivery of poorly water-soluble drugs.
Harborg, M; Holm, P; Holm, R; Jacobsen, J; Jørgensen, EB; Larsen, R; Müllertz, A, 2011
)
0.58
"The bioavailability of halofantrine was significantly lower in BDC rats when dosed with 0-5% PS 80 in PEG 400 compared with BDC rats dosed with >15% PS 80."( Effect of bile on the oral absorption of halofantrine in polyethylene glycol 400 and polysorbate 80 formulations dosed to bile duct cannulated rats.
Boll, JB; Holm, R; Jacobsen, J; Mu, H; Müllertz, A; Tønsberg, H, 2011
)
0.95
" Adjusting the level of surfactant in drug formulations could therefore be used to minimise variability in the bioavailability from co-solvent systems based upon differences in bile concentration between individuals."( Effect of bile on the oral absorption of halofantrine in polyethylene glycol 400 and polysorbate 80 formulations dosed to bile duct cannulated rats.
Boll, JB; Holm, R; Jacobsen, J; Mu, H; Müllertz, A; Tønsberg, H, 2011
)
0.64
"The bioavailability of the poorly soluble model drug halofantrine, dosed in a soy bean oil solution or in a self-nanoemulsifying drug delivery system (SNEDDS), at two levels of lipid, was assessed in rats."( Influence of bile on the absorption of halofantrine from lipid-based formulations.
Abedinpour, P; Farsad, S; Holm, R; Jørgensen, EB; Müllertz, A; Tønsberg, H, 2012
)
0.9
" Because temporal changes to plasma lipid levels occur as a result of the absorption of formulation or food-derived lipids and the infusion of intravenous lipid emulsions, the current data suggest that a mismatch in plasma lipid levels after intravenous and oral administrations may lead to differences in drug Cl and errors in bioavailability assessment."( Intravenous dosing conditions may affect systemic clearance for highly lipophilic drugs: implications for lymphatic transport and absolute bioavailability studies.
Caliph, SM; Charman, WN; Porter, CJ; Trevaskis, NL, 2012
)
0.38
" For bioavailability calculation, animals were intravenuosly administered halofantrine."( A mouse model to evaluate the impact of species, sex, and lipid load on lymphatic drug transport.
Caliph, SM; Charman, WN; Nguyen, G; Porter, CJ; Trevaskis, NL; Tso, P, 2013
)
0.62
" Lower bioavailability appeared responsible for some species differences in halofantrine lymphatic transport; however other systematic differences were involved."( A mouse model to evaluate the impact of species, sex, and lipid load on lymphatic drug transport.
Caliph, SM; Charman, WN; Nguyen, G; Porter, CJ; Trevaskis, NL; Tso, P, 2013
)
0.62
" Upon coadministration of 97-78, the relative bioavailability of lumefantrine significantly decreased to 64."( Simultaneous quantification of proposed anti-malarial combination comprising of lumefantrine and CDRI 97-78 in rat plasma using the HPLC-ESI-MS/MS method: application to drug interaction study.
Gayen, JR; Raju, KS; Siddiqui, HH; Singh, SK; Singh, SP; Taneja, I; Wahajuddin, M, 2015
)
0.42
"A super-saturated self-nanoemulsifying drug delivery system (super-SNEDDS), containing the poorly water-soluble drug halofantrine (Hf) at 150% of equilibrium solubility (S eq), was compared in vitro and in vivo with a conventional SNEDDS (75% of S eq) with respect to bioavailability and digestibility."( The Effect of Digestion and Drug Load on Halofantrine Absorption from Self-nanoemulsifying Drug Delivery System (SNEDDS).
Michaelsen, MH; Müllertz, A; Rades, T; Sivak, O; Wasan, KM, 2016
)
0.91
" For cinnarizine and danazol the oral bioavailability in rats after chase dosing or dosing the compound dissolved in Labrafil M21515CS was similar and significantly higher than for the aqueous suspension."( Solution or suspension - Does it matter for lipid based systems? In vivo studies of chase dosing lipid vehicles with aqueous suspensions of a poorly soluble drug.
Holm, R; Larsen, AT; Müllertz, A, 2017
)
0.46
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

The enhanced dissolution of the amorphous halofantrine was also reflected in vivo since two capsules of conventional SNEDDS were needed to achieve similar AUC and C(max) as obtained after dosing of a single capsule of super-SNEDDS. At the 2 dosage levels tested halofanrine proved highly effective in the treatment of malaria caused by resistant and sensitive strains to P.

ExcerptRelevanceReference
" Validation studies with artemisinin demonstrated the need for revising the protocol for the production of the dosing solutions."( In vitro sensitivity of multiresistant Plasmodium falciparum to new candidate antimalarial drugs in western Thailand.
Rooney, W; Schildbach, S; Suebsaeng, L; Wernsdorfer, WH, 1990
)
0.28
"1 mM) or on the rate of N-demethylation of aminopyrine or O-dealkylation of Ec in microsomes produced from rats dosed chronically with Hf (200 mg/kg) for 4 days."( Lack of effect of halofantrine on hepatic drug metabolism in the rat in vivo and in vitro.
Edwards, G; Hoaksey, PE; Milton, KA; Ward, SA, 1990
)
0.61
" Time to reach peak concentrations for Hf and Hfm and the elimination half-life of Hf remained unchanged across the dosage range."( Pharmacokinetics of halofantrine in man: effects of food and dose size.
Breckenridge, AM; Edwards, G; Milton, KA; Orme, ML; Ward, SA, 1989
)
0.6
" For prophylaxis, it has been suggested that the dosage of 10 mg/kg/wk should be spread over the week (3."( [Pharmacokinetics of antimalarials: quinine and mefloquine, halofantrine, qinghaosu, amino-4-quinolines].
Blayo, MC; Pussard, E; Verdier, F,
)
0.37
" This dosage should be repeated after 14 days to obtain the same cure rate in non-immune patients."( Treatment of imported cases of falciparum malaria in France with halofantrine.
Coulaud, JP; Le Bras, J; Matheron, S; Moriniere, B; Rossignol, JF; Saimot, AG, 1986
)
0.51
"For the past 300 years antimalarial dosage regimens have not been based on pharmacokinetic information."( Clinical pharmacokinetics of antimalarial drugs.
White, NJ,
)
0.13
" This dosage could be repeated after 14 days in order to obtain the same cure rate in non-immune patients."( [Treatment with halofantrine of Plasmodium falciparum malaria imported into France].
Coulaud, JP; Le Bras, J; Matheron, S; Morinière, B; Rossignol, JF; Saimot, AG, 1985
)
0.62
" This dosing regimen was effective and well tolerated, with mild transient diarrhea during the first few days of treatment in both groups."( Pharmacokinetics of an extended-dose halofantrine regimen in patients with malaria and in healthy volunteers.
Fleckenstein, L; Keeratithakul, D; Loesuttiviboon, L; Ohrt, C; Schuster, B; Teja-Isavadharm, P; Watt, G; Webster, HK, 1995
)
0.56
"In recent years major advances have been made in the clinical pharmacology of many drugs used for the treatment of tropical diseases, particularly in the design and development of dosage regimens for the treatment of severe malaria."( Clinical pharmacokinetics in the treatment of tropical diseases. Some applications and limitations.
Edwards, G; Ward, SA; Winstanley, PA, 1994
)
0.29
" Halofantrine was administered on two separate days at a total oral dosage of 24 mg/kg/day in three doses over a 12-hr period."( Electrocardiographic changes and halofantrine plasma level during acute falciparum malaria.
Bernard, J; Chaudet, H; Doury, JC; Imbert, P; Keundjian, A; Touze, JE; Viguier, A, 1996
)
1.49
" Dose-response studies showed that expression of wild-type pfmdr1 causes cellular resistance to quinine, quinacrine, mefloquine, and halofantrine in yeast cells."( The pfmdr1 gene of Plasmodium falciparum confers cellular resistance to antimalarial drugs in yeast cells.
Brault, M; Delling, U; Gros, P; Ruetz, S; Schurr, E, 1996
)
0.5
" Considering the different lymphatic transport profiles of Hf base in the anesthetized and conscious rat models, it is proposed that the lipid vehicle effects observed in the intraduodenally dosed anesthetized model most likely reflects the lack of gastric processing by preduodenal lipase and the shear action of the stomach otherwise present in the conscious rat model."( Lymphatic transport of halofantrine in the conscious rat when administered as either the free base or the hydrochloride salt: effect of lipid class and lipid vehicle dispersion.
Charman, SA; Charman, WN; Humberstone, AJ; Porter, CJ, 1996
)
0.6
" A new dosage of halofantrine is proposed for the second injection due to cardiac toxicity."( [Malaria in expatriates in Africa. 154 cases. Clinical problems and therapeutic difficulties].
Gorge, O; Nicolas, F; Nicolas, X; Perret, JL; Touze, JE, 1997
)
0.64
" After dosing by both routes of administration the (+) enantiomer was found to have significantly higher AUC, and higher Cmax after oral dosing."( Pharmacokinetics of halofantrine in the rat: stereoselectivity and interspecies comparisons.
Brocks, DR; Toni, JW, 1999
)
0.63
" CGP 56697 is an effective, well-tolerated treatment for uncomplicated falciparum malaria but for this dosing regimen the recrudescence rate is unacceptablyhigh (18%)."( The comparative efficacy and tolerability of CGP 56697 (artemether + lumefantrine) versus halofantrine in the treatment of uncomplicated falciparum malaria in travellers returning from the Tropics to The Netherlands and France.
Barette, S; Bernard, J; Bouchaud, O; Danis, M; Delmont, J; Gathmann, I; Gras, C; Malvy, D; Mull, R; Touze, JE; van Agtmael, M, 1999
)
0.52
" For optimal efficacy, treatment regimens must be adjusted with regard to dosage of primaquine and association with halofantrine, mefloquine or other new antimalarial agents."( [Epidemiological and therapeutic aspects of plasmodial infection from Plasmodium vivax].
Granier, H; Klotz, F; Martin, J; Nicolas, X, 2000
)
0.52
" In terms of rank order effects, the plasma concentrations of halofantrine were highest for the rats dosed C18:2 followed by C18:3 and C18:1."( Comparison of the lymphatic transport of halofantrine administered in disperse systems containing three different unsaturated fatty acids.
Holm, R; Kristensen, HG; Müllertz, A; Pedersen, GP, 2001
)
0.82
" Electrocardiograms (ECGs) were recorded from 48 hours before dosing until 48 hours thereafter."( Comparison of the cardiac effects of the antimalarials co-artemether and halofantrine in healthy participants.
Bindschedler, M; Degen, P; Lefèvre, G; Sioufi, A, 2002
)
0.55
" The four drivers had been treated with chloroquine and proguanil but the dosage may have been insufficient with regard to their body weight (average weight = 110 kg)."( [A collective malarial infestation during a humanitarian mission in west Africa].
Beytout, J; Caumon, L; Chouaki, M; Cueto, T; Delort, P; Dufraise, S; Monchard, F; Philippe, JM; Rimeize, H, 2002
)
0.31
"Conscious, lymph cannulated and nonlymph cannulated rats were dosed orally with three structurally different triglycerides; sunflower oil, and two structured triglycerides containing different proportion and position of medium-(M) and long-chain (L) fatty acids on the glycerol backbone."( Structured triglyceride vehicles for oral delivery of halofantrine: examination of intestinal lymphatic transport and bioavailability in conscious rats.
Charman, WN; Holm, R; Kristensen, HG; Müllertz, A; Porter, CJ, 2002
)
0.56
" The estimated total absorption of halofantrine in the lymph cannulated animals was higher than in the nonlymph cannulated animals, and this was most pronounced for the animals dosed with the structured triglycerides."( Structured triglyceride vehicles for oral delivery of halofantrine: examination of intestinal lymphatic transport and bioavailability in conscious rats.
Charman, WN; Holm, R; Kristensen, HG; Müllertz, A; Porter, CJ, 2002
)
0.84
" In order to determine whether enantioselective lymphatic absorption contributes to the previously reported enantioselective pharmacokinetics of Hf, lymph samples collected from thoracic duct-cannulated dogs dosed with racemic Hf (100 mg, administered postprandially) were assayed with a chiral HPLC method capable of quantifying the relative amounts of (+)- and (-)-Hf."( Does stereoselective lymphatic absorption contribute to the enantioselective pharmacokinetics of halofantrine In Vivo?
Charman, WN; Porter, CJ; Shackleford, DM, 2003
)
0.54
" 5 These data provide the basis for the design of improved dosing regimens for the use of parenteral halofantrine in malaria."( Pharmacokinetics, efficacy and toxicity of parenteral halofantrine in uncomplicated malaria.
Krishna, S; Kyle, D; Pukrittayakamee, S; Supanaranond, W; Teja-Isavadharm, P; ter Kuile, F; White, NJ, 1993
)
0.75
"9% of the dose for the animals dosed with the MLM SMEDDS and 27."( Examination of oral absorption and lymphatic transport of halofantrine in a triple-cannulated canine model after administration in self-microemulsifying drug delivery systems (SMEDDS) containing structured triglycerides.
Charman, WN; Edwards, GA; Holm, R; Kristensen, HG; Müllertz, A; Porter, CJ, 2003
)
0.56
"Lymph cannulated rats were orally dosed with Hf in a TG solution or in o/w-emulsions dispersed by lecithin or Cremophor RH40."( Influence of the type of surfactant and the degree of dispersion on the lymphatic transport of halofantrine in conscious rats.
Holm, R; Karpf, DM; Kristensen, HG; Müllertz, A, 2004
)
0.54
"05) higher level of Hf was found in the intestinal lymph when dosed in one of the emulsions (22."( Influence of the type of surfactant and the degree of dispersion on the lymphatic transport of halofantrine in conscious rats.
Holm, R; Karpf, DM; Kristensen, HG; Müllertz, A, 2004
)
0.54
" Plasma, adipose, and highly perfused tissues heart, lung, liver, kidney, spleen and brain were harvested for up to 48 h after dosing animals with 2 mg/kg (+/-)-HF intravenously by tail vein."( The effect of experimental hyperlipidemia on the stereoselective tissue distribution, lipoprotein association and microsomal metabolism of (+/-)-halofantrine.
Brocks, DR; Fleischer, JG; Patel, JP; Wasan, KM, 2009
)
0.55
" M and MU were administered intravenously and orally to greyhound dogs to determine absolute bioavailability after oral dosing of MU."( Lymphatic transport of Methylnortestosterone undecanoate (MU) and the bioavailability of methylnortestosterone are highly sensitive to the mass of coadministered lipid after oral administration of MU.
Charman, WN; Edwards, GA; Faassen, WA; Nguyen, G; Porter, CJ; White, KL, 2009
)
0.35
" The animals dosed with the PEG 400 formulation had significant lower bioavailability than the PS 80-PEG 400 co-mixtures, possibly due to halofantrine precipitation in the gastrointestinal tract."( Effects of polysorbate 80 on the in-vitro precipitation and oral bioavailability of halofantrine from polyethylene glycol 400 formulations in rats.
Bisgaard, J; Holm, R; Jacobsen, J; Müllertz, A; Tønsberg, H, 2010
)
0.79
" However, in vivo bioavailability studies in rats showed the same plasma concentration-time profiles when dosing 10mg/kg halofantrine at two dose levels of F6H8, MCT or F6H8:MCT (1:1) (AUC ranged from 3058 to 3447hng/ml, T(max)∼6."( A novel excipient, 1-perfluorohexyloctane shows limited utility for the oral delivery of poorly water-soluble drugs.
Harborg, M; Holm, P; Holm, R; Jacobsen, J; Jørgensen, EB; Larsen, R; Müllertz, A, 2011
)
0.58
"The bioavailability of halofantrine was significantly lower in BDC rats when dosed with 0-5% PS 80 in PEG 400 compared with BDC rats dosed with >15% PS 80."( Effect of bile on the oral absorption of halofantrine in polyethylene glycol 400 and polysorbate 80 formulations dosed to bile duct cannulated rats.
Boll, JB; Holm, R; Jacobsen, J; Mu, H; Müllertz, A; Tønsberg, H, 2011
)
0.95
" In vitro release result obtained revealed sustained and controlled drug release from the lipid microspheres compared with the tablet dosage form."( In vitro properties of surface-modified solid lipid microspheres containing an antimalarial drug: halofantrine.
Attama, AA; Igbonekwu, CN, 2011
)
0.59
" The enhanced dissolution of the amorphous halofantrine was also reflected in vivo since two capsules of conventional SNEDDS were needed to achieve similar AUC and C(max) as obtained after dosing of a single capsule of super-SNEDDS."( In vitro and in vivo performance of novel supersaturated self-nanoemulsifying drug delivery systems (super-SNEDDS).
Holm, R; Müllertz, A; Rades, T; Thomas, N, 2012
)
0.64
"The bioavailability of the poorly soluble model drug halofantrine, dosed in a soy bean oil solution or in a self-nanoemulsifying drug delivery system (SNEDDS), at two levels of lipid, was assessed in rats."( Influence of bile on the absorption of halofantrine from lipid-based formulations.
Abedinpour, P; Farsad, S; Holm, R; Jørgensen, EB; Müllertz, A; Tønsberg, H, 2012
)
0.9
" Ideally, synergistic combinations can provide 1) increased efficacy of the therapeutic effect 2) reduced toxicity as a result of decreased dosage providing equivalent or increased efficacy 3) the avoidance or delayed onset of drug resistance."( CDA: combinatorial drug discovery using transcriptional response modules.
Bae, TJ; Jang, Y; Kim, BC; Kim, DG; Kim, JT; Kim, S; Lee, JH; Lee, JJ; Park, KM; Rho, K, 2012
)
0.38
" Ultimately, careful control of dosing conditions (formulation, prandial state), and thus the extent of lymphatic transport, may be important in assuring reproducible efficacy and toxicity for lymphatically transported drugs."( The impact of lymphatic transport on the systemic disposition of lipophilic drugs.
Bulitta, JB; Caliph, SM; Cao, E; Han, S; Hu, L; Porter, CJ; Trevaskis, NL, 2013
)
0.39
" The bioavailability of Hf dosed in super-SNEDDS (32."( The Effect of Digestion and Drug Load on Halofantrine Absorption from Self-nanoemulsifying Drug Delivery System (SNEDDS).
Michaelsen, MH; Müllertz, A; Rades, T; Sivak, O; Wasan, KM, 2016
)
0.7
"A 3D printer was used to realise compartmental dosage forms containing multiple active pharmaceutical ingredient (API) formulations."( Analysis of 3D Prints by X-ray Computed Microtomography and Terahertz Pulsed Imaging.
Bøtker, J; Markl, D; Michaelsen, MH; Müllertz, A; Rades, T; Rantanen, J; Rasch, C; Zeitler, JA, 2017
)
0.46
" The microstructural information extracted by XμCT and TPI will assist to gain a better understanding about the performance of 3D printed dosage forms."( Analysis of 3D Prints by X-ray Computed Microtomography and Terahertz Pulsed Imaging.
Bøtker, J; Markl, D; Michaelsen, MH; Müllertz, A; Rades, T; Rantanen, J; Rasch, C; Zeitler, JA, 2017
)
0.46
" For cinnarizine and danazol the oral bioavailability in rats after chase dosing or dosing the compound dissolved in Labrafil M21515CS was similar and significantly higher than for the aqueous suspension."( Solution or suspension - Does it matter for lipid based systems? In vivo studies of chase dosing lipid vehicles with aqueous suspensions of a poorly soluble drug.
Holm, R; Larsen, AT; Müllertz, A, 2017
)
0.46
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
phenanthrenesAny benzenoid aromatic compound that consists of a phenanthrene skeleton and its substituted derivatives thereof.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fumarate hydrataseHomo sapiens (human)Potency37.22120.00308.794948.0869AID1347053
EWS/FLI fusion proteinHomo sapiens (human)Potency6.21620.001310.157742.8575AID1259253; AID1259256
polyproteinZika virusPotency37.22120.00308.794948.0869AID1347053
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC50 (µMol)1.90000.00032.63119.0000AID1207743
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC50 (µMol)1.90000.00032.59559.0000AID1207743
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)0.16220.00091.901410.0000AID1445968; AID161281; AID1915901; AID240820; AID243151; AID243188; AID346849; AID408340; AID420668; AID576612; AID82353
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki7.50000.00211.840710.0000AID1059571
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC50 (µMol)1.90000.00032.63119.0000AID1207743
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC50 (µMol)1.90000.00032.25459.6000AID1207743
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (62)

Processvia Protein(s)Taxonomy
visual perceptionVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
detection of light stimulus involved in visual perceptionVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
sensory perception of soundVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
positive regulation of calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion importVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
membrane depolarization during SA node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of potassium ion transmembrane transporter activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of potassium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
skeletal system developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
extraocular skeletal muscle developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
striated muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
endoplasmic reticulum organizationVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
myoblast fusionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
neuromuscular junction developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
skeletal muscle adaptationVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
skeletal muscle fiber developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
release of sequestered calcium ion into cytosolVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
cellular response to caffeineVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
immune system developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
heart developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
embryonic forelimb morphogenesisVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
camera-type eye developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transport into cytosolVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transport via high voltage-gated calcium channelVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cell communication by electrical coupling involved in cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of ventricular cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

Processvia Protein(s)Taxonomy
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
ankyrin bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activity involved SA node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
small molecule bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
molecular function activator activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (18)

Processvia Protein(s)Taxonomy
photoreceptor outer segmentVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
sarcoplasmic reticulumVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
T-tubuleVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
I bandVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic densityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
dendriteVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic density membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (99)

Assay IDTitleYearJournalArticle
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1207743Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits2013Scientific reports, , Volume: 3MICE models: superior to the HERG model in predicting Torsade de Pointes.
AID161281Inhibition of human Potassium channel HERG expressed in mammalian cells2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID420669Lipophilicity, log D at pH 7.02009European journal of medicinal chemistry, May, Volume: 44, Issue:5
GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID243151Inhibitory concentration against potassium channel HERG2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors.
AID1136694Antimalarial activity against Plasmodium berghei infected in mouse assessed as change in mean survival time at 20 mg/kg (Rvb = 6.2 +/- 0.5 days)1978Journal of medicinal chemistry, Apr, Volume: 21, Issue:4
Resolution of antimalarial agents via complex formation with alpha-(2,4,5,7-tetranitro-9-fluorenylideneaminooxy) propionic acid.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID519975Antimalarial activity against early trophozoite-stage Plasmodium falciparum 3D7 infected in erythrocyte assessed as reduction in parasite hemoglobin content at 5 times IC50 after 8 hrs in presence of 40 uM protease inhibitor ALLN2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Differential effects of quinoline antimalarials on endocytosis in Plasmodium falciparum.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1136696Antimalarial activity against Plasmodium berghei infected in mouse assessed as change in mean survival time at 80 mg/kg (Rvb = 6.2 +/- 0.5 days)1978Journal of medicinal chemistry, Apr, Volume: 21, Issue:4
Resolution of antimalarial agents via complex formation with alpha-(2,4,5,7-tetranitro-9-fluorenylideneaminooxy) propionic acid.
AID264203Antimalarial activity against multidrug-resistant Plasmodium yoelii nigeriensis in mice (Mus musculus) at 30 mg/kg/day peroral dose after 4 days2006Journal of medicinal chemistry, May-04, Volume: 49, Issue:9
Orally active 1,2,4-trioxanes: synthesis and antimalarial assessment of a new series of 9-functionalized 3-(1-arylvinyl)-1,2,5-trioxaspiro[5.5]undecanes against multi-drug-resistant plasmodium yoelii nigeriensis in mice.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1136693Antimalarial activity against Plasmodium berghei infected in mouse assessed as change in mean survival time at 10 mg/kg (Rvb = 6.2 +/- 0.5 days)1978Journal of medicinal chemistry, Apr, Volume: 21, Issue:4
Resolution of antimalarial agents via complex formation with alpha-(2,4,5,7-tetranitro-9-fluorenylideneaminooxy) propionic acid.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1136691Antimalarial activity against Plasmodium berghei infected in mouse assessed as change in mean survival time at 2.5 mg/kg (Rvb = 6.2 +/- 0.5 days)1978Journal of medicinal chemistry, Apr, Volume: 21, Issue:4
Resolution of antimalarial agents via complex formation with alpha-(2,4,5,7-tetranitro-9-fluorenylideneaminooxy) propionic acid.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1136690Antimalarial activity against Plasmodium berghei infected in mouse assessed as change in mean survival time at 1.25 mg/kg (Rvb = 6.2 +/- 0.5 days)1978Journal of medicinal chemistry, Apr, Volume: 21, Issue:4
Resolution of antimalarial agents via complex formation with alpha-(2,4,5,7-tetranitro-9-fluorenylideneaminooxy) propionic acid.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID240820Inhibitory concentration against IKr potassium channel2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
The pharmacophore hypotheses of I(Kr) potassium channel blockers: novel class III antiarrhythmic agents.
AID1915901Inhibition of hERG by fluorescence polarization assay
AID1136692Antimalarial activity against Plasmodium berghei infected in mouse assessed as change in mean survival time at 5 mg/kg (Rvb = 6.2 +/- 0.5 days)1978Journal of medicinal chemistry, Apr, Volume: 21, Issue:4
Resolution of antimalarial agents via complex formation with alpha-(2,4,5,7-tetranitro-9-fluorenylideneaminooxy) propionic acid.
AID1915900Protein binding in human plasma at 1 uM incubated for 5 hrs by LC-MS/MS analysis
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID519978Antimalarial activity against Plasmodium falciparum 3D7 infected in erythrocyte assessed as reduction in endocytic vesicle content after 8 hrs by immunofluorescence microscopy2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Differential effects of quinoline antimalarials on endocytosis in Plasmodium falciparum.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1136695Antimalarial activity against Plasmodium berghei infected in mouse assessed as change in mean survival time at 40 mg/kg (Rvb = 6.2 +/- 0.5 days)1978Journal of medicinal chemistry, Apr, Volume: 21, Issue:4
Resolution of antimalarial agents via complex formation with alpha-(2,4,5,7-tetranitro-9-fluorenylideneaminooxy) propionic acid.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1123507Antimalarial activity against Plasmodium berghei1979Journal of medicinal chemistry, Apr, Volume: 22, Issue:4
Quantitative structure-activity relationships in 1-aryl-2-(alkylamino)ethanol antimalarials.
AID1445968Inhibition of human ERG by fluorescence polarization assay2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
3-Hydroxy-N'-arylidenepropanehydrazonamides with Halo-Substituted Phenanthrene Scaffolds Cure P. berghei Infected Mice When Administered Perorally.
AID420668Inhibition of human ERG in MCF7 cells2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID346849Inhibition of human cloned ERG2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
AID519976Antimalarial activity against early trophozoite-stage Plasmodium falciparum 3D7 infected in erythrocyte assessed as reduction in parasite hemoglobin content at 5 times IC50 after 8 hrs in presence of 40 uM protease inhibitor E642008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Differential effects of quinoline antimalarials on endocytosis in Plasmodium falciparum.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID408340Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Support vector machines classification of hERG liabilities based on atom types.
AID264204Antimalarial activity against multidrug-resistant Plasmodium yoelii nigeriensis in mice (Mus musculus) at 100 mg/kg/day peroral dose after 4 days2006Journal of medicinal chemistry, May-04, Volume: 49, Issue:9
Orally active 1,2,4-trioxanes: synthesis and antimalarial assessment of a new series of 9-functionalized 3-(1-arylvinyl)-1,2,5-trioxaspiro[5.5]undecanes against multi-drug-resistant plasmodium yoelii nigeriensis in mice.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID519974Antimalarial activity against early trophozoite-stage Plasmodium falciparum 3D7 infected in erythrocyte assessed as reduction in parasite hemoglobin content at 5 times IC50 after 8 hrs2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Differential effects of quinoline antimalarials on endocytosis in Plasmodium falciparum.
AID576612Inhibition of human ERG2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model.
AID347271Toxicity in monkey assessed as increase in QTc interval2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID562110Antiplasmodial activity against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID243188Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state2005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
A two-state homology model of the hERG K+ channel: application to ligand binding.
AID158849Inhibitory activity against Plasmodium falciparum Dd2 in erythrocytes2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Structure-activity relationships of novel anti-malarial agents. Part 2: cinnamic acid derivatives.
AID82353K+ channel blocking activity in Chinese hamster ovary cells expressing HERG Kv11.12002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID519977Antimalarial activity against schizont-stage Plasmodium falciparum 3D7 infected in erythrocyte assessed as inhibition of horseradish peroxidase(HRP) uptake after 10 hrs by colorimetric peroxidase assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Differential effects of quinoline antimalarials on endocytosis in Plasmodium falciparum.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1059571Inhibition of human ERG expressed in CHO cells2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Identification and optimization of an aminoalcohol-carbazole series with antimalarial properties.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1202799Inhibition of human ERG expressed in CHL cells assessed as tail current at 10 uM after 7 mins by patch clamp assay relative to control2015Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
Antimalarial activity of 4-amidinoquinoline and 10-amidinobenzonaphthyridine derivatives.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (441)

TimeframeStudies, This Drug (%)All Drugs %
pre-199035 (7.94)18.7374
1990's225 (51.02)18.2507
2000's120 (27.21)29.6817
2010's50 (11.34)24.3611
2020's11 (2.49)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 44.29

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index44.29 (24.57)
Research Supply Index6.32 (2.92)
Research Growth Index5.08 (4.65)
Search Engine Demand Index69.24 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (44.29)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials68 (13.99%)5.53%
Reviews24 (4.94%)6.00%
Case Studies45 (9.26%)4.05%
Observational0 (0.00%)0.25%
Other349 (71.81%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Relative Bioavailability Study Between the Formulations: Paroxetine 25 mg Tablets With Controlled Release Manufactured by GSK Mississauga and Paroxetine 25 mg Tablets With Controlled Release Manufactured by SmithKline Beecham (Cidra), Fed Administration i [NCT01339247]Phase 160 participants (Actual)Interventional2009-10-20Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01339247 (3) [back to overview]AUC_ss
NCT01339247 (3) [back to overview]Cmax_ss
NCT01339247 (3) [back to overview]Cmin_ss

AUC_ss

The area under the plot of plasma concentration of drug against time after drug administration is defined as the area under the curve (AUC). The AUC_ss is the area under the curve during the steady-state period. The AUC_ss is of particular use in estimating the bioavailability of drugs, by measuring the extent of absorption. ng, nanograms; h, hour; ml, milliliter; ng.h/ml, nanograms per hour per milliliter. (NCT01339247)
Timeframe: Days 14 to 17 (period 1) and Days 23 to 24 (Period 2)

Interventionng.h/ml (Mean)
Test Product672.9221
Reference Product645.5407

[back to top]

Cmax_ss

"Cmax_ss is defined as the maximum or peak concentration of a drug observed after its administration, in steady-state. Cmax_ss is one of the parameters of particular use in estimating the bioavailability of drugs, by measuring the total amount of drug absorbed." (NCT01339247)
Timeframe: Days 14 to 17 (period 1) and Days 23 to 24 (Period 2)

Interventionng/ml (Mean)
Test Product36.7235
Reference Product36.6630

[back to top]

Cmin_ss

Cmin_ss is defined as the minimum concentration of a drug observed after its administration, in steady-state. Cmin_ss is one of the parameters of particular use in estimating the bioavailability of drugs, for studies employing multiple doses. (NCT01339247)
Timeframe: Days 14 to 17 (period 1) and Days 23 to 24 (Period 2)

Interventionng/ml (Mean)
Test Product19.4468
Reference Product18.9010

[back to top]