Identification

Name
Ranolazine
Accession Number
DB00243  (APRD01300)
Type
Small Molecule
Groups
Approved, Investigational
Description

Ranolazine is an antianginal medication. On January 31, 2006, ranolazine was approved for use in the United States by the FDA for the treatment of chronic angina. [Wikipedia]

Structure
Thumb
Synonyms
Not Available
External IDs
CVT-303 / RS-43285-003
Product Ingredients
IngredientUNIICASInChI Key
Ranolazine hydrochlorideF71253DJUN95635-56-6RJNSNFZXAZXOFX-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
RanexaTablet, film coated, extended release1000 mg/1OralGilead Palo Alto, Inc.2007-02-122011-05-31Us
RanexaTablet, film coated, extended release500 mg/1OralGilead Sciences2006-01-27Not applicableUs61958 100120180907 15195 1vtc5i
RanexaTablet, film coated, extended release500 mg/1OralCardinal Health2006-01-272015-12-31Us61958 1003 01 nlmimage10 a83ed476
RanexaTablet, film coated, extended release500 mg/1OralGilead Sciences2006-01-27Not applicableUs61958 100320180907 15195 18u0tsx
RanexaTablet, film coated, extended release500 mg/1OralGilead Palo Alto, Inc.2006-01-272013-03-31Us
RanexaTablet, film coated, extended release500 mg/1OralAphena Pharma Solutions Tennessee, Inc.2006-01-27Not applicableUs
RanexaTablet, film coated, extended release500 mg/1OralCarilion Materials Management2006-01-27Not applicableUs68151 500420180907 15195 f63t8y
RanexaTablet, film coated, extended release1000 mg/1OralGilead Sciences2007-02-12Not applicableUs
RanexaTablet, film coated, extended release500 mg/1OralCardinal Health2007-02-122013-03-31Us61958 1001 01 nlmimage10 e31c7193
RanexaTablet, film coated, extended release1000 mg/1OralGilead Sciences2007-02-12Not applicableUs61958 1004 01 nlmimage10 32431978
Categories
UNII
A6IEZ5M406
CAS number
95635-55-5
Weight
Average: 427.5365
Monoisotopic: 427.247106559
Chemical Formula
C24H33N3O4
InChI Key
XKLMZUWKNUAPSZ-UHFFFAOYSA-N
InChI
InChI=1S/C24H33N3O4/c1-18-7-6-8-19(2)24(18)25-23(29)16-27-13-11-26(12-14-27)15-20(28)17-31-22-10-5-4-9-21(22)30-3/h4-10,20,28H,11-17H2,1-3H3,(H,25,29)
IUPAC Name
N-(2,6-dimethylphenyl)-2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetamide
SMILES
COC1=CC=CC=C1OCC(O)CN1CCN(CC(=O)NC2=C(C)C=CC=C2C)CC1

Pharmacology

Indication

For the treatment of chronic angina. It should be used in combination with amlodipine, beta-blockers or nitrates.

Associated Conditions
Pharmacodynamics

Ranolazine has antianginal and anti-ischemic effects that do not depend upon reductions in heart rate or blood pressure. It is the first new anti-anginal developed in over 20 years.

Mechanism of action

The mechanism of action of ranolazine is unknown. It does not increase the rate-pressure product, a measure of myocardial work, at maximal exercise. In vitro studies suggest that ranolazine is a P-gp inhibitor. Ranolazine is believed to have its effects via altering the trans-cellular late sodium current. It is by altering the intracellular sodium level that ranolazine affects the sodium-dependent calcium channels during myocardial ischemia. Thus, ranolazine indirectly prevents the calcium overload that causes cardiac ischemia.

TargetActionsOrganism
ASodium channel protein type 5 subunit alpha
inhibitor
Human
USodium channel protein type 9 subunit alpha
inhibitor
Human
Absorption

Absorption is highly variable. After oral administration of ranolazine as a solution, 73% of the dose is systemically available as ranolazine or metabolites. The bioavailability of oral ranolazine relative to that from a solution is 76%.

Volume of distribution
Not Available
Protein binding

62%

Metabolism

Hepatic, metabolized mainly by CYP3A and to a lesser extent by CYP2D6. The pharmacologic activity of the metabolites has not been well characterized.

Route of elimination

Ranolazine is metabolized rapidly and extensively in the liver and intestine; less than 5% is excreted unchanged in urine and feces.

Half life

7 hours

Clearance
Not Available
Toxicity

In the event of overdose, the expected symptoms would be dizziness, nausea/vomiting, diplopia, paresthesia, and confusion. Syncope with prolonged loss of consciousness may develop.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Ranolazine.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Ranolazine.
16-BromoepiandrosteroneThe metabolism of 16-Bromoepiandrosterone can be decreased when combined with Ranolazine.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Ranolazine.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Ranolazine.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Ranolazine.
6-Deoxyerythronolide BThe metabolism of Ranolazine can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when combined with Ranolazine.
AbemaciclibThe serum concentration of Ranolazine can be increased when it is combined with Abemaciclib.
AbexinostatThe risk or severity of QTc prolongation can be increased when Ranolazine is combined with Abexinostat.
Food Interactions
  • Grapefruit and grapefruit juice should be avoided throughout treatment.
  • Take without regard to meals.

References

Synthesis Reference

Raghupathi Reddy Anumula, Goverdhan Gilla, Sampath Aalla, Lokeswara Rao Madivada, Prabhaker Macherla, Srinivas Kurella, Kavitha Charagondla, Ramamurthy Kasula, Rajagopala Rao Mandadapu, Krishaniah Charagondla, Malati Vakamulla, Durga Prasad Janaki Bhavanipurapu, "PREPARATION OF RANOLAZINE." U.S. Patent US20110151258, issued June 23, 2011.

US20110151258
General References
  1. Hale SL, Kloner RA: Ranolazine, an inhibitor of the late sodium channel current, reduces postischemic myocardial dysfunction in the rabbit. J Cardiovasc Pharmacol Ther. 2006 Dec;11(4):249-55. [PubMed:17220471]
  2. Fraser H, Belardinelli L, Wang L, Light PE, McVeigh JJ, Clanachan AS: Ranolazine decreases diastolic calcium accumulation caused by ATX-II or ischemia in rat hearts. J Mol Cell Cardiol. 2006 Dec;41(6):1031-8. Epub 2006 Oct 5. [PubMed:17027025]
  3. Stone PH, Gratsiansky NA, Blokhin A, Huang IZ, Meng L: Antianginal efficacy of ranolazine when added to treatment with amlodipine: the ERICA (Efficacy of Ranolazine in Chronic Angina) trial. J Am Coll Cardiol. 2006 Aug 1;48(3):566-75. Epub 2006 Jun 15. [PubMed:16875985]
  4. Chaitman BR, Pepine CJ, Parker JO, Skopal J, Chumakova G, Kuch J, Wang W, Skettino SL, Wolff AA: Effects of ranolazine with atenolol, amlodipine, or diltiazem on exercise tolerance and angina frequency in patients with severe chronic angina: a randomized controlled trial. JAMA. 2004 Jan 21;291(3):309-16. [PubMed:14734593]
  5. Morrow DA, Scirica BM, Karwatowska-Prokopczuk E, Murphy SA, Budaj A, Varshavsky S, Wolff AA, Skene A, McCabe CH, Braunwald E: Effects of ranolazine on recurrent cardiovascular events in patients with non-ST-elevation acute coronary syndromes: the MERLIN-TIMI 36 randomized trial. JAMA. 2007 Apr 25;297(16):1775-83. [PubMed:17456819]
External Links
Human Metabolome Database
HMDB0014388
PubChem Compound
56959
PubChem Substance
46505145
ChemSpider
51354
ChEBI
87690
ChEMBL
CHEMBL1404
Therapeutic Targets Database
DAP000875
PharmGKB
PA164746007
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Ranolazine
ATC Codes
C01EB18 — Ranolazine
FDA label
Download (203 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableType 2 Diabetes Mellitus2
1CompletedOtherDrug-induced QT Interval Prolongation / Pharmacodynamics / Pharmacokinetics1
1CompletedTreatmentDrug-induced Surface ECG Changes1
1CompletedTreatmentPulmonary Arterial Hypertension (PAH)1
1CompletedTreatmentType 2 Diabetes Mellitus1
1RecruitingTreatmentHealthy Male Individuals1
1TerminatedTreatmentSevere Renal Impairment1
2CompletedNot AvailableDiastolic Heart Failure1
2CompletedTreatmentAnginal Pain1
2CompletedTreatmentMicrovascular Angina1
2CompletedTreatmentMyocardial Ischemia1
2CompletedTreatmentMyotonia Congenita / Myotonia Congenita (Enrollment Complete) / Myotonic Dystrophy 1 / Paramyotonia Congenita1
2CompletedTreatmentNonvalvular Atrial Fibrillation1
2CompletedTreatmentPersistent Atrial Fibrillation1
2CompletedTreatmentType 2 Diabetes Mellitus1
2RecruitingPreventionLong QT Syndrome Type 31
2RecruitingTreatmentAmyotrophic Lateral Sclerosis (ALS)1
2RecruitingTreatmentLong qt Syndrome1
2RecruitingTreatmentMyocardial Ischemia / Ventricular Premature Complexes1
2TerminatedNot AvailableAtherosclerotic Coronary Vascular Disease1
2TerminatedPreventionAcute Coronary Syndromes (ACS)1
2TerminatedTreatmentAnginal Pain1
2TerminatedTreatmentHeart Failure, Unspecified / Nonvalvular Atrial Fibrillation1
2Unknown StatusTreatmentCongestive Cardiomyopathy1
2, 3CompletedTreatmentAcute Myocardial Ischemia / Coronary Artery Disease1
2, 3TerminatedTreatmentDiarrhoea Predominant Irritable Bowel Syndrome1
3CompletedNot AvailableAnginal Pain / Coronary Artery Disease / Type 2 Diabetes Mellitus / Type I Diabetes1
3CompletedTreatmentAngina Pectoris / Coronary Artery Disease1
3CompletedTreatmentAnginal Pain1
3CompletedTreatmentAnginal Pain / Pulmonary Arterial Hypertension (PAH)1
3CompletedTreatmentHeart Failure, Unspecified / Ischaemic Cardiomyopathy / Nonischemic Cardiomyopathy1
3CompletedTreatmentMyocardial Ischemia1
3CompletedTreatmentSudden Cardiac Death / Ventricular Arrythmias1
3CompletedTreatmentType 2 Diabetes Mellitus3
3Not Yet RecruitingPreventionCoronary Artery Disease1
3TerminatedTreatmentHeart; Dysfunction Postoperative, Cardiac Surgery1
3Unknown StatusTreatmentNonvalvular Atrial Fibrillation1
4CompletedNot AvailableChronic Angina1
4CompletedSupportive CareHypertrophic Cardiomyopathy1
4CompletedTreatmentAngina Pectoris / Coronary Artery Disease / Type 2 Diabetes Mellitus1
4CompletedTreatmentCardiovascular Disease (CVD) / End-Stage Renal Disease (ESRD)1
4CompletedTreatmentChronic Stable Angina Pectoris1
4CompletedTreatmentDiastolic Left Ventricular Dysfunction / Pulmonary Hypertension (PH)1
4CompletedTreatmentDyspnea / Prophylaxis of cardiomyopathy / Thoracic Pain1
4CompletedTreatmentMicrovascular Angina1
4CompletedTreatmentMyocardial Ischemia / Myocardial Perfusion Imaging1
4Not Yet RecruitingPreventionMyocardial Stunning1
4Not Yet RecruitingTreatmentCoronary Artery Disease1
4RecruitingTreatmentAnginal Pain1
4RecruitingTreatmentMetabolic Syndromes / Stable Angina (SA)1
4TerminatedTreatmentCoronary Artery Disease / Pain / Peripheral Nervous System Diseases / Polyneuropathies1
4TerminatedTreatmentDiabetic Peripheral Neuropathic Pain1
4Unknown StatusDiagnosticCoronary Artery Disease1
4Unknown StatusSupportive CareIschemic Mitral Regurgitation1
4Unknown StatusTreatmentAnginal Pain / Coronary Artery Disease / Metabolic Syndromes1
4Unknown StatusTreatmentChronic Stable Angina Pectoris / Coronary Artery Disease / Nonvalvular Atrial Fibrillation / Ventricular Tachycardia (VT)1
4Unknown StatusTreatmentIschaemic Heart Diseases1
4Unknown StatusTreatmentPremature Ventricular Beats1
4WithdrawnTreatmentAngina Pectoris / Coronary Artery Disease / Type 2 Diabetes Mellitus1
4WithdrawnTreatmentAnginal Pain / Peripheral Arterial Disease (PAD)1
4WithdrawnTreatmentArteriosclerosis / Chronic Stable Angina Pectoris / Coronary Artery Disease / Myocardial Ischemia1
Not AvailableActive Not RecruitingTreatmentPulmonary Hypertension (PH)1
Not AvailableCompletedDiagnosticAdenocarcinoma of the Prostate / Bone Metastases / Soft Tissue Metastases / Stage IIA Prostate Cancer / Stage IIB Prostate Cancer / Stage III Prostate Cancer / Stage IV Prostate Cancer1
Not AvailableCompletedPreventionAtrial Fibrillation New Onset / Hemorrhage / Medical Care; Complications, Late Effect of Complications / Prolonged QTc Interval / Ventricular Tachycardia (VT)1
Not AvailableCompletedTreatmentMicrovascular Coronary Dysfunction (MCD)1
Not AvailableCompletedTreatmentPeripheral Arterial Disease (PAD)1
Not AvailableNot Yet RecruitingTreatmentAnginal Pain1
Not AvailableRecruitingTreatmentCoronary Artery Disease / Coronary Microcirculation / Myocardial Diseases / Transient ischemia attacks1
Not AvailableRecruitingTreatmentPulmonary Hypertension (PH)1
Not AvailableTerminatedSupportive CareProphylaxis of cardiomyopathy1
Not AvailableUnknown StatusNot AvailableAnginal Pain / Heart Diseases1
Not AvailableUnknown StatusTreatmentDiastolic Heart Failure / Echocardiography / Ranolazine / Tissue Doppler Ultrasound1
Not AvailableUnknown StatusTreatmentHeart Failure With Preserved Ejection Fraction (HFpEF)1
Not AvailableWithdrawnNot AvailableIschaemic Myocardial Dysfunction / Severe Coronary Artery Disease1
Not AvailableWithdrawnOtherSilent Myocardial Ischemia / Type 2 Diabetes Mellitus1

Pharmacoeconomics

Manufacturers
  • Gilead sciences inc
Packagers
  • Atlantic Biologicals Corporation
  • DSM Corp.
  • Gilead Sciences Inc.
Dosage forms
FormRouteStrength
Tablet, film coated, extended releaseOral1000 mg/1
Tablet, film coated, extended releaseOral500 mg/1
Prices
Unit descriptionCostUnit
Ranexa 1000 mg 12 Hour tablet6.89USD tablet
Ranexa 1000 mg tablet6.63USD tablet
Ranexa 500 mg 12 Hour tablet4.06USD tablet
Ranexa 500 mg tablet4.04USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6303607No1999-05-272019-05-27Us
US6479496No1999-05-272019-05-27Us
US6525057No1999-05-272019-05-27Us
US6562826No1999-05-272019-05-27Us
US6620814No1999-05-272019-05-27Us
US6852724No1999-05-272019-05-27Us
US6864258No1999-05-272019-05-27Us
US6617328No1999-05-272019-05-27Us
US6369062No1999-05-272019-05-27Us
US6503911No1999-05-272019-05-27Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityVery slightly solubleNot Available
logP1.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.11 mg/mLALOGPS
logP2.08ALOGPS
logP2.83ChemAxon
logS-3.6ALOGPS
pKa (Strongest Acidic)13.6ChemAxon
pKa (Strongest Basic)7.17ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area74.27 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity123.46 m3·mol-1ChemAxon
Polarizability47.22 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.7425
Blood Brain Barrier-0.5334
Caco-2 permeable-0.5853
P-glycoprotein substrateSubstrate0.8667
P-glycoprotein inhibitor IInhibitor0.7566
P-glycoprotein inhibitor IIInhibitor0.7524
Renal organic cation transporterNon-inhibitor0.7648
CYP450 2C9 substrateNon-substrate0.7965
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7456
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorNon-inhibitor0.8287
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8155
Ames testNon AMES toxic0.8529
CarcinogenicityNon-carcinogens0.9128
BiodegradationNot ready biodegradable0.9936
Rat acute toxicity2.3256 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8753
hERG inhibition (predictor II)Inhibitor0.8775
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0udi-0010900000-41c6c10d624710416f8e
MS/MS Spectrum - , positiveLC-MS/MSsplash10-004i-1321900000-58e490b47155b2267ecc
MS/MS Spectrum - , positiveLC-MS/MSsplash10-004i-1320900000-9a6cdfcd606e98d38452
MS/MS Spectrum - , positiveLC-MS/MSsplash10-004i-0320900000-ab04122e7d0d6e7c3690
MS/MS Spectrum - , positiveLC-MS/MSsplash10-004i-5951300000-885e790d3cd4d8746c02

Taxonomy

Description
This compound belongs to the class of organic compounds known as anisoles. These are organic compounds containing a methoxybenzene or a derivative thereof.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Phenol ethers
Sub Class
Anisoles
Direct Parent
Anisoles
Alternative Parents
m-Xylenes / Phenoxy compounds / Methoxybenzenes / N-alkylpiperazines / Alkyl aryl ethers / Trialkylamines / Secondary alcohols / 1,2-aminoalcohols / Propargyl-type 1,3-dipolar organic compounds / Carboximidic acids
show 3 more
Substituents
Phenoxy compound / Anisole / M-xylene / Xylene / Methoxybenzene / Alkyl aryl ether / N-alkylpiperazine / Monocyclic benzene moiety / 1,4-diazinane / Piperazine
show 20 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
monocarboxylic acid amide, secondary alcohol, aromatic amide, N-alkylpiperazine, monomethoxybenzene (CHEBI:87690)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated sodium channel activity involved in sa node cell action potential
Specific Function
This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the pr...
Gene Name
SCN5A
Uniprot ID
Q14524
Uniprot Name
Sodium channel protein type 5 subunit alpha
Molecular Weight
226937.475 Da
References
  1. Hale SL, Kloner RA: Ranolazine, an inhibitor of the late sodium channel current, reduces postischemic myocardial dysfunction in the rabbit. J Cardiovasc Pharmacol Ther. 2006 Dec;11(4):249-55. [PubMed:17220471]
  2. Rajamani S, Shryock JC, Belardinelli L: Block of tetrodotoxin-sensitive, Na(V)1.7 and tetrodotoxin-resistant, Na(V)1.8, Na+ channels by ranolazine. Channels (Austin). 2008 Nov-Dec;2(6):449-60. Epub 2008 Nov 7. [PubMed:19077543]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Voltage-gated sodium channel activity
Specific Function
Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a...
Gene Name
SCN9A
Uniprot ID
Q15858
Uniprot Name
Sodium channel protein type 9 subunit alpha
Molecular Weight
226370.175 Da
References
  1. Rajamani S, Shryock JC, Belardinelli L: Block of tetrodotoxin-sensitive, Na(V)1.7 and tetrodotoxin-resistant, Na(V)1.8, Na+ channels by ranolazine. Channels (Austin). 2008 Nov-Dec;2(6):449-60. Epub 2008 Nov 7. [PubMed:19077543]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Transporter activity
Specific Function
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name
ABCB11
Uniprot ID
O95342
Uniprot Name
Bile salt export pump
Molecular Weight
146405.83 Da
References
  1. Pedersen JM, Matsson P, Bergstrom CA, Hoogstraate J, Noren A, LeCluyse EL, Artursson P: Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. Epub 2013 Sep 6. [PubMed:24014644]

Drug created on June 13, 2005 07:24 / Updated on August 26, 2018 01:48