Page last updated: 2024-11-06

lorcainide

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

Lorcainide is an antiarrhythmic drug that was developed in the 1970s and marketed in the 1980s. It is a class Ic antiarrhythmic agent, meaning it blocks sodium channels in the heart, slowing down the conduction of electrical impulses and reducing the risk of arrhythmias. It was initially studied for its potential to treat a variety of cardiac arrhythmias, including ventricular tachycardia and atrial fibrillation. However, it was later withdrawn from the market in several countries due to concerns about its potential for proarrhythmic effects, meaning that it could actually increase the risk of arrhythmias in some patients. Despite its withdrawal, lorcainide remains an important compound for research, as it provides insights into the mechanisms of action of antiarrhythmic drugs and the potential for drug-induced arrhythmias.'

Cross-References

ID SourceID
PubMed CID42884
CHEMBL ID87543
CHEBI ID135568
SCHEMBL ID364045
MeSH IDM0065647

Synonyms (46)

Synonym
ro-13-1042
CHEMBL87543
benzeneacetamide, n-(4-chlorophenyl)-n-[1-(1-methylethyl)-4-piperidinyl]-
lorcainide
n-(4-chlorophenyl)-n-[1-(1-methylethyl)piperidin-4-yl]-2-phenylacetamide
59729-31-6
SPECTRUM_001714
brn 0497568
lorcainida [inn-spanish]
lorcainide [inn:ban]
lorcainid
n-(4-chlorophenyl)-n-(1-(1-methylethyl)-4-piperidinyl)benzeneacetamide
benzeneacetamide, n-(4-chlorophenyl)-n-(1-(1-methylethyl)-4-piperidinyl)-
lorcainidum [inn-latin]
4'-chloro-n-(1-isopropyl-4-piperidyl)-2-phenylacetanilide
lorcainide hydrochloride (usan)
KBIOSS_002194
KBIO2_004762
KBIO2_002194
KBIO2_007330
CHEBI:135568
n-(4-chlorophenyl)-2-phenyl-n-(1-propan-2-ylpiperidin-4-yl)acetamide
lorcainide (inn)
D08020
lorcainida
lorcainidum
5-22-08-00059 (beilstein handbook reference)
kgj2t0n7iq ,
unii-kgj2t0n7iq
lorcainide [who-dd]
lorcainide [inn]
lorcainide [mi]
SCHEMBL364045
XHOJAWVAWFHGHL-UHFFFAOYSA-N
4'-chloro-n-(1-isopropyl-4-piperidinyl)-2-phenylacetanilide
n-(4-chlorophenyl)-n-(1-isopropyl-4-piperidinyl)-2-phenylacetamide #
bdbm50237589
DTXSID2023226
n-(4-chlorophenyl)-2-phenyl-n-[1-(propan-2-yl)piperidin-4-yl]acetamide
AKOS027327571
n-(4-chlorophenyl)-n-(1-isopropylpiperidin-4-yl)-2-phenylacetamide
A857054
FT-0758616
DB13653
Q6678811
NCGC00487358-02

Research Excerpts

Overview

Lorcainide is an antiarrhythmic drug with unusual pharmacokinetics and an active metabolite, norlorcainide, which complicate oral drug loading. The drug is well absorbed orally, with bioavailability increasing with both dose and continued administration.

ExcerptReferenceRelevance
"Lorcainide is an antiarrhythmic drug with unusual pharmacokinetics and an active metabolite, norlorcainide, which complicate oral drug loading. "( Pharmacodynamics of the initiation of antiarrhythmic therapy with lorcainide.
Kates, RE; Keefe, DL; Rodriguez, I; Winkle, RA, 1984
)
1.95
"Lorcainide is a type I antiarrhythmic drug of the local anesthetic type. "( Lorcainide. A preliminary review of its pharmacodynamic properties and therapeutic efficacy.
Brogden, RN; Eiriksson, Ce, 1984
)
3.15
"Lorcainide is a new type 1 antiarrhythmic drug that is well absorbed orally, with bioavailability increasing with both dose and continued administration. "( Pharmacology of lorcainide.
Keefe, DL, 1984
)
2.06
"Lorcainide is a new antiarrhythmic drug undergoing clinical investigation for management of patients with ventricular arrhythmias. "( Lorcainide kinetics and protein binding in patients with end-stage renal disease.
Gupta, RK; King, P; Shapiro, RS; Simon, V; Somani, P; Stockard, H, 1984
)
3.15
"Lorcainide appears to be a promising new antiarrhythmic agent in patients with the Wolff-Parkinson-White syndrome."( Electrophysiologic effects of lorcainide on the accessory pathway in the Wolff-Parkinson-White syndrome.
Jähnchen, E; Kasper, W; Meinertz, T; Pop, T; Treese, N, 1983
)
1.28
"Lorcainide is an effective antiarrhythmic agent against ventricular arrhythmias otherwise difficult to treat."( Antiarrhythmic effect of lorcainide during chronic treatment.
Bechtold, H; Jähnchen, E; Just, H; Kasper, W; Kersting, F; Meinertz, T, 1980
)
1.29
"Lorcainide seems to be a useful addition to the available anti-arrhythmic agents, and should form part of the armamentarium against ventricular ectopic activity."( Lorcainide -- an anti-arrhythmic agent for ventricular arrhythmias.
Goldman, AP; Myburgh, DP; Schamroth, JM, 1980
)
2.43
"Lorcainide was shown to be an effective anti-arrhythmic agent."( The effect of lorcainide on arrhythmias and survival in patients with acute myocardial infarction: an example of publication bias.
Cowley, AJ; Hampton, JR; Skene, A; Stainer, K, 1993
)
1.37
"Lorcainide is a new antiarrhythmic agent which effectively suppresses ventricular premature contractions. "( Electrophysiological actions of lorcainide in patients with cardiac disease.
Just, H; Kasper, W; Kersting, F; Lang, K; Löllgen, H; Meinertz, T,
)
1.86
"Lorcainide is a promising antiarrhythmic agent that belongs to the class of local anesthetics. "( Initial clinical experience of lorcainide (Ro 13-1042), a new antiarrhythmic agent.
Cocco, G; Strozzi, C, 1978
)
1.99
"Lorcainide is an antiarrhythmic of the local anaesthetic type."( Antiarrhythmic, electrophysiologic and hemodynamic effects of lorcainide.
Carmeliet, E; Janssen, PA; Marsboom, R; Van Nueten, JM; Xhonneux, R, 1978
)
1.22

Effects

Lorcainide has a very promising antiarrhythmic effect in the suppression of tachyarrhythmias with accessory pathway conduction, too. Because of its side-effects it should be used only in special circumstances.

Lorcainide has a very promising antiarrhythmic effect in the suppression of tachyarrhythmias with accessory pathway conduction, too. Because of its side-effects, it should be used only in special circumstances.

ExcerptReferenceRelevance
"Lorcainide thus has a good anti-arrhythmic effect but, because of its side-effects, it should be used only in special circumstances."( [Lorcainide in stable ventricular extrasystole. A double-blind study with 48-hour continuous ECG recording].
Buss, J; Geiger, S; Gores, D; Heene, DL; Stegaru, B, 1984
)
1.9
"Lorcainide has a very promising antiarrhythmic effect in the suppression of tachyarrhythmias with accessory pathway conduction, too."( Electrophysiological characteristics of lorcainide, a new antiarrhythmic drug.
Czakó, E; Solti, F; Szatmáry, L, 1986
)
1.26
"Lorcainide thus has a good anti-arrhythmic effect but, because of its side-effects, it should be used only in special circumstances."( [Lorcainide in stable ventricular extrasystole. A double-blind study with 48-hour continuous ECG recording].
Buss, J; Geiger, S; Gores, D; Heene, DL; Stegaru, B, 1984
)
1.9
"Lorcainide has only negligible depressant effects on important haemodynamic parameters and its toxicity is minimal."( Lorcainide (R 15 889), a first review.
Amery, WK; Gough, DA; Heykants, JJ; Janssen, PA; Oettel, P; Towse, G; Xhonneux, R, 1981
)
2.43
"Lorcainide has been shown to be as effective as lignocaine in suppressing ventricular ectopy."( Evaluation of lorcainide, a new anti-arrhythmic agent.
Commerford, PJ; Lloyd, EA; Mabin, TA; Workman, LJ, 1981
)
1.34
"Lorcainide has a very promising antiarrhythmic effect in the suppression of tachyarrhythmias with accessory pathway conduction, too."( Electrophysiological characteristics of lorcainide, a new antiarrhythmic drug.
Czakó, E; Solti, F; Szatmáry, L, 1986
)
1.26

Actions

ExcerptReferenceRelevance
"Lorcainide did not suppress group mean PVDs per hour, pairs, or ventricular tachycardia."( Antiarrhythmic effect of lorcainide in patients taking digoxin.
Giardina, EG; Louie-Chu, M; Raby, K; Saroff, AL,
)
1.16

Pharmacokinetics

Lorcainide, a new antiarrhythmic agent currently undergoing clinical trial, has been pentadeuterated. The usefulness of this labelled compound in pharmacokinetic and metabolism studies has been investigated in dogs.

ExcerptReferenceRelevance
"This work deals with the pharmacodynamic problem of relating a drug effect E(t) to an observable pharmacokinetic (PK) predictor variable r(t), which may be a venous and/or arterial drug level, some other PK variable, or a drug infusion scheme."( Pharmacodynamic system analysis of the biophase level predictor and the transduction function.
Modi, NB; Veng-Pedersen, P, 1992
)
0.28
"Lorcainide, a new antiarrhythmic agent currently undergoing clinical trial, has been pentadeuterated and the usefulness of this labelled compound in pharmacokinetic and metabolism studies has been investigated in dogs."( The use and limitations of deuterated lorcainide in metabolism and pharmacokinetic studies.
Gelijkens, CF; Heykants, J; Knaeps, A; Lenoir, H; Van Peer, A; Woestenborghs, R, 1985
)
1.98
"The influence of cardiac function as measured by the left ventricular ejection fraction on the pharmacokinetic variables of a new antiarrhythmic drug, lorcainide, was investigated in 20 cardiac patients."( Pharmacokinetic implications of lorcainide therapy in patients with normal and depressed cardiac function.
Fraker, TD; Somani, P; Temesy-Armos, PN, 1987
)
0.76
" It can be given either intravenously or orally, and its pharmacokinetic properties allow relatively long (12 hours) dosing intervals with oral administration."( Lorcainide. A preliminary review of its pharmacodynamic properties and therapeutic efficacy.
Brogden, RN; Eiriksson, Ce, 1984
)
1.71
"This article reviews clinical pharmacokinetic data on 8 new antiarrhythmic agents."( Clinical pharmacokinetics of the newer antiarrhythmic agents.
Gillis, AM; Kates, RE,
)
0.13
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35

Bioavailability

Lorcainide is a new type 1 antiarrhythmic drug that is well absorbed orally, with bioavailability increasing with both dose and continued administration. In control rats, the total blood clearance of lorcianide was 30 ml/kg/min and the bioavailability was 14%.

ExcerptReferenceRelevance
" Comparison of the area under the curves during steady state (ss) indicated a complete bioavailability of multiple oral doses."( Disposition and antiarrhythmic effect of lorcainide.
Heimburg, P; Klotz, U; Müller-Seydlitz, P, 1979
)
0.53
" In 4 of the healthy volunteers, the bioavailability of a single 100mg(n = 2) and 150mg (n = 2) oral dose was determined."( Pharmacokinetics of lorcainide in man: a new antiarrhythmic agent.
Heimburg, P; Klotz, U; Müller-Seydlitz, P,
)
0.45
" According to these findings in the dog, the use of deuterated lorcainide in human bioavailability and metabolism studies is probably of limited value."( The use and limitations of deuterated lorcainide in metabolism and pharmacokinetic studies.
Gelijkens, CF; Heykants, J; Knaeps, A; Lenoir, H; Van Peer, A; Woestenborghs, R, 1985
)
0.78
" Flecainide pharmacokinetics are suitable for oral use but encainide disposition is complex with variable bioavailability and active metabolites that contribute substantially to activity."( Clinical profiles of newer class I antiarrhythmic agents--tocainide, mexiletine, encainide, flecainide and lorcainide.
Pottage, A, 1983
)
0.48
" Lorcainide is also a class Ic antiarrhythmic drug, the bioavailability of which is nonlinear."( Clinical pharmacokinetics of the newer antiarrhythmic agents.
Gillis, AM; Kates, RE,
)
1.04
"Lorcainide is a new type 1 antiarrhythmic drug that is well absorbed orally, with bioavailability increasing with both dose and continued administration."( Pharmacology of lorcainide.
Keefe, DL, 1984
)
2.06
" In control rats, the total blood clearance of lorcainide was 30 ml/kg/min and the bioavailability was 14%."( Effect of enzyme induction on the disposition of lorcainide in rats following intravenous and oral administration.
Jähnchen, E; Plänitz, V, 1984
)
0.78
" The drug is well absorbed by the oral route and its elimination half-life is long when compared with other substances."( Lorcainide (R 15 889), a first review.
Amery, WK; Gough, DA; Heykants, JJ; Janssen, PA; Oettel, P; Towse, G; Xhonneux, R, 1981
)
1.71
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36

Dosage Studied

In a randomized double-blind cross-over trial, the effectiveness of lorcainide at a dosage of three times 100 mg/d by mouth was compared with that of a placebo for the treatment of subjectively disturbing stable ventricular extrasystoles (VES) Twenty-five adult patients were given 100 mg lorcianide tablets according to one of 3 different dosage schedules.

ExcerptRelevanceReference
" After the single intravenous dose total plasma clearance (Cl) ranged from 570 to 1670 ml/min (988 +/- 425 ml/min) while after multiple dosing Cl decreased to 666 +/- 27 ml/min."( Disposition and antiarrhythmic effect of lorcainide.
Heimburg, P; Klotz, U; Müller-Seydlitz, P, 1979
)
0.53
" Serious adverse reactions necessitate a change in antiarrhythmic therapy, as opposed to lowering drug dosage to an ineffective level."( Antiarrhythmic drug therapy. Recent advances and current status.
Somberg, J, 1985
)
0.27
" If side effects intervene that may cause continued therapy to be intolerable, changing the antiarrhythmic agent, as opposed to decreasing the dosage to an ineffective range, may be appropriate."( New directions in antiarrhythmic drug therapy.
Somberg, JC, 1984
)
0.27
"In a randomized double-blind cross-over trial, the effectiveness of lorcainide at a dosage of three times 100 mg/d by mouth was compared with that of a placebo for the treatment of subjectively disturbing stable ventricular extrasystoles (VES), using 48-hour continuous ECG monitoring."( [Lorcainide in stable ventricular extrasystole. A double-blind study with 48-hour continuous ECG recording].
Buss, J; Geiger, S; Gores, D; Heene, DL; Stegaru, B, 1984
)
1.41
" It can be given either intravenously or orally, and its pharmacokinetic properties allow relatively long (12 hours) dosing intervals with oral administration."( Lorcainide. A preliminary review of its pharmacodynamic properties and therapeutic efficacy.
Brogden, RN; Eiriksson, Ce, 1984
)
1.71
"Measurement of drug levels is becoming increasingly popular to optimise the dosage of various drugs."( Reliability of antiarrhythmic drug plasma concentration monitoring.
Follath, F; Ganzinger, U; Schuetz, E,
)
0.13
" It is metabolized through the liver, and patients with significant liver disease will require dosage reduction."( Pharmacology of lorcainide.
Keefe, DL, 1984
)
0.61
" Only minor quantitative differences were observed between intravenously and orally dosed animals, and between male and female rats."( Excretion and metabolism of lorcainide in rats, dogs and man.
Hendrickx, J; Heykants, J; Hurkmans, R; Lauwers, W; Meuldermans, W; Swysen, E; Thijssen, J,
)
0.43
" These data suggest that renal disease should not alter either the dose or the dosing interval of lorcainide."( Lorcainide kinetics and protein binding in patients with end-stage renal disease.
Gupta, RK; King, P; Shapiro, RS; Simon, V; Somani, P; Stockard, H, 1984
)
1.93
" 3 On a dosage basis, encainide was seven times, lorcainide fourteen times and ORG 6001 twice as potent as lignocaine in raising VFT."( Antifibrillatory efficacy of encainide, loracainide and ORG 6001 compared with lignocaine in isolated hearts of rabbits and guinea-pigs.
Almotrefi, AA; Baker, JB, 1981
)
0.52
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
acetamidesCompounds with the general formula RNHC(=O)CH3.
[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 (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)134.00000.11007.190310.0000AID1443980; AID1473738
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (41)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (35)

Assay IDTitleYearJournalArticle
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
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.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID660334Half life in human liver microsomes assessed as CYP2C8-mediated parent compound depletion at 1 uM2011ACS medicinal chemistry letters, Aug-11, Volume: 2, Issue:8
Metabolism of 4-Aminopiperidine Drugs by Cytochrome P450s: Molecular and Quantum Mechanical Insights into Drug Design.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID22293Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID660331Half life in human liver microsomes assessed as CYP3A4-mediated parent compound depletion at 1 uM2011ACS medicinal chemistry letters, Aug-11, Volume: 2, Issue:8
Metabolism of 4-Aminopiperidine Drugs by Cytochrome P450s: Molecular and Quantum Mechanical Insights into Drug Design.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID660336Half life in human liver microsomes assessed as CYP2C19-mediated parent compound depletion at 1 uM2011ACS medicinal chemistry letters, Aug-11, Volume: 2, Issue:8
Metabolism of 4-Aminopiperidine Drugs by Cytochrome P450s: Molecular and Quantum Mechanical Insights into Drug Design.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID660332Half life in human liver microsomes assessed as CYP2D6-mediated parent compound depletion at 1 uM2011ACS medicinal chemistry letters, Aug-11, Volume: 2, Issue:8
Metabolism of 4-Aminopiperidine Drugs by Cytochrome P450s: Molecular and Quantum Mechanical Insights into Drug Design.
AID660337Half life in human liver microsomes assessed as CYP1A2-mediated parent compound depletion at 1 uM2011ACS medicinal chemistry letters, Aug-11, Volume: 2, Issue:8
Metabolism of 4-Aminopiperidine Drugs by Cytochrome P450s: Molecular and Quantum Mechanical Insights into Drug Design.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID660333Half life in human liver microsomes assessed as CYP2B6-mediated parent compound depletion at 1 uM2011ACS medicinal chemistry letters, Aug-11, Volume: 2, Issue:8
Metabolism of 4-Aminopiperidine Drugs by Cytochrome P450s: Molecular and Quantum Mechanical Insights into Drug Design.
AID660338Clearance in human liver microsomes at 1 uM2011ACS medicinal chemistry letters, Aug-11, Volume: 2, Issue:8
Metabolism of 4-Aminopiperidine Drugs by Cytochrome P450s: Molecular and Quantum Mechanical Insights into Drug Design.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID660335Half life in human liver microsomes assessed as CYP2C9-mediated parent compound depletion at 1 uM2011ACS medicinal chemistry letters, Aug-11, Volume: 2, Issue:8
Metabolism of 4-Aminopiperidine Drugs by Cytochrome P450s: Molecular and Quantum Mechanical Insights into Drug Design.
AID26304Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
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 (146)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990121 (82.88)18.7374
1990's12 (8.22)18.2507
2000's5 (3.42)29.6817
2010's7 (4.79)24.3611
2020's1 (0.68)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 33.59

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index33.59 (24.57)
Research Supply Index5.19 (2.92)
Research Growth Index4.26 (4.65)
Search Engine Demand Index45.27 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (33.59)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials22 (14.10%)5.53%
Reviews23 (14.74%)6.00%
Case Studies8 (5.13%)4.05%
Observational0 (0.00%)0.25%
Other103 (66.03%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]