Levamlodipine

Identification

Summary

Levamlodipine is a calcium channel blocker used to treat hypertension.

Brand Names
Conjupri
Generic Name
Levamlodipine
DrugBank Accession Number
DB09237
Background

Levamlodipine, also known as S-amlodipine, is a pharmacologically active enantiomer of amlodipine, an antihypertensive medication.8 Levamlodipine belongs to the dihydropyridine group of calcium channel blockers.8 This medication was first marketed in Russia and India before being granted FDA approval.9 The names S-amlodipine and levamlodipine may be used interchangeably as both substances are the same, however.8 As a racemic mixture, amlodipine contains (R) and (S)-amlodipine isomers, but only (S)-amlodipine as the active moiety possesses therapeutic activity.7

Levamlodipine was granted FDA approval on 19 December 2019.8

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 408.88
Monoisotopic: 408.1451996
Chemical Formula
C20H25ClN2O5
Synonyms
  • Levamlodipine
  • Levoamlodipine
  • S-amlodipine

Pharmacology

Indication

Levamlodipine is indicated alone or in combination to treat hypertension in adults and children.8

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Used in combination to treatHigh blood pressure (hypertension)•••••••••••••••••• •••••••••••••••
Treatment ofHigh blood pressure (hypertension)•••••••••••••••••• •••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Levamlodipine inhibits L-type calcium channels in vascular smooth muscle, reducing peripheral vascular resistance and blood pressure.8 It is given once daily in doses of 1.25-2.5mg in children and 2.5-5mg in adults.8 Patients should be counselled regarding the risk of symptomatic hypotension, worsening angina, and myocardial infarction.8

Mechanism of action

Levamlodipine blocks the transmembrane influx of calcium through L-type calcium channels into the vascular and cardiac smooth muscles resulting in vasodilation and a subsequent decrease in blood pressure.4,8 Levamlodipine inhibits calcium influx in vascular smooth muscle to a greater degree than in cardiac muscle, leading to decreased peripheral vascular resistance and lowered blood pressure.8 In vitro studies have shown a negative inotropic effect but this is unlikely to be clinically relevant.8

TargetActionsOrganism
UVoltage-dependent L-type calcium channel subunit alpha-1C
antagonist
Humans
UVoltage-dependent L-type calcium channel subunit alpha-1D
antagonist
Humans
UNitric oxide synthase, endothelial
agonist
Humans
UNitric oxide synthase, inducible
agonist
Humans
Absorption

Oral levamlodipine has a Tmax of 6-12h and a bioavailability of 64-90%.8 Absorption of levamlodipine is not significantly affected by food.8

20mg or oral s-amlodipine besylate reaches a Cmax of 6.13±1.29ng/mL with a Tmax of 8.4±3.6h and an AUC of 351±72h*ng/mL.3 20mg or oral s-amlodipine maleate reaches a Cmax of 5.07±1.09ng/mL with a Tmax of 10.7±3.4h and an AUC of 330±88h*ng/mL.3

Volume of distribution

The volume of distribution of levamlodipine is similar to amlodipine.3 The volume of distribution of amlodipine is 21L/kg.5,6

Protein binding

Levamlodipine is 93% protein bound in plasma,8 largely to human serum albumin.2

Metabolism

Levamlodipine is 90% metabolized to inactive metabolites.8 Incubation with liver microsomes has shown that this metabolism is primarily mediated by CYP3A4.1 Levamlodipine's dehydrogenation to a pyridine metabolite (M9) is the most important metabolic pathway in human liver microsomes.1 This derivative can be further oxidatively deaminated or O-dealkylated, but does not appear to undergo O-demethylation like racemic amlodipine.1

Hover over products below to view reaction partners

Route of elimination

Levamlodipine is 60% eliminated in urine with 10% eliminated as the unmetabolized drug.8

Half-life

Levamlodipine has a half life of 30-50h.8

Clearance

The oral clearance of S-amlodipine besylate is 6.9±1.6mL/min/kg and the oral clearance of S-amlodipine maleate is 7.3±2.1mL/min/kg.3

Adverse Effects
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Toxicity

Patients experiencing an overdose may present with hypotension and reflex tachycardia.8 Treat overdose with cardiac and respiratory monitoring, frequent blood pressure measurement, elevation of extremities to treat hypotension, and possible administration of vasopressors.8 Hemodialysis is not expected to be useful as levamlodipine is highly protein bound.8

Pathways
Not Available
Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbaloparatideAbaloparatide may increase the hypotensive activities of Levamlodipine.
AbametapirThe serum concentration of Levamlodipine can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Levamlodipine can be increased when combined with Abatacept.
AcalabrutinibThe serum concentration of Levamlodipine can be increased when it is combined with Acalabrutinib.
AcarboseThe risk or severity of hypoglycemia can be increased when Levamlodipine is combined with Acarbose.
Food Interactions
  • Take with or without food. Co-administration with food does not affect bioavailability.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Levamlodipine maleate12WW9T2ITA135969-53-8TZNOWAJJWCGILX-HNUXRKMMSA-N
International/Other Brands
Asomex (Emcure Pharmaceutical Ltd) / Conjupri / EsCordi Cor (Actavis Pharma) / Eslo (Zuventus Healthcare Ltd.) / Espin (Intas Pharmaceuticals Ltd)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
ConjupriTablet5 mg/1OralBurke Therapeutics, LLC2020-09-012022-08-11US flag
ConjupriTablet5 mg/5mgOralCSPC Ouyi Pharmaceutical Co. Ltd2020-12-19Not applicableUS flag
ConjupriTablet2.5 mg/1OralWraser Llc2021-08-15Not applicableUS flag
ConjupriTablet2.5 mg/1OralBurke Therapeutics, LLC2020-09-012022-08-11US flag
ConjupriTablet2.5 mg/2.5mgOralCSPC Ouyi Pharmaceutical Co. Ltd2021-10-08Not applicableUS flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
LevamlodipineTablet5 mg/1OralXspire Pharma, Llc2021-08-15Not applicableUS flag
LevamlodipineTablet2.5 mg/1OralXspire Pharma, Llc2021-08-15Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
ALENCAL IRBE® 2.5/150 MG TABLETAS RECUBIERTASLevamlodipine (2.5 mg) + Irbesartan (150 mg)Tablet, coatedOralCLARIPACK S.A2014-02-25Not applicableColombia flag
ALENCAL VALS 2.5/160MG TABLETAS RECUBIERTASLevamlodipine (2.5 mg) + Valsartan (160 mg)Tablet, coatedOralCLARIPACK S.A.2015-01-232020-08-05Colombia flag
ALENCAL VALS 2.5/320 MG TABLETAS RECUBIERTASLevamlodipine (2.5 mg) + Valsartan (320 mg)Tablet, coatedOralCOLOMPACK S.A.2017-03-16Not applicableColombia flag
VOLTRAMOS 2.5 MG/160 MG FILM KAPLI TABLET, 28 ADETLevamlodipine (2.5 mg) + Valsartan (160 mg)Tablet, coatedOralPOLPHARMA SAĞLIK ÜRÜNLERİ SAN. VE TİC. A.Ş.2020-08-142017-11-14Turkey flag
VOLTRAMOS 5 MG/160 MG FILM KAPLI TABLET, 28 ADETLevamlodipine (5 mg) + Valsartan (160 mg)Tablet, coatedOralPOLPHARMA SAĞLIK ÜRÜNLERİ SAN. VE TİC. A.Ş.2020-08-142017-11-14Turkey flag

Categories

ATC Codes
C08CA17 — Levamlodipine
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as dihydropyridinecarboxylic acids and derivatives. These are compounds containing a dihydropyridine moiety bearing a carboxylic acid group.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Pyridines and derivatives
Sub Class
Hydropyridines
Direct Parent
Dihydropyridinecarboxylic acids and derivatives
Alternative Parents
Chlorobenzenes / Aryl chlorides / Dicarboxylic acids and derivatives / Vinylogous amides / Methyl esters / Enoate esters / Amino acids and derivatives / Azacyclic compounds / Dialkyl ethers / Dialkylamines
show 7 more
Substituents
Alpha,beta-unsaturated carboxylic ester / Amine / Amino acid or derivatives / Aromatic heteromonocyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzenoid / Carbonyl group / Carboxylic acid derivative
show 25 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
amlodipine (CHEBI:53796)
Affected organisms
  • Humans

Chemical Identifiers

UNII
0P6NLP6806
CAS number
103129-82-4
InChI Key
HTIQEAQVCYTUBX-KRWDZBQOSA-N
InChI
InChI=1S/C20H25ClN2O5/c1-4-28-20(25)18-15(11-27-10-9-22)23-12(2)16(19(24)26-3)17(18)13-7-5-6-8-14(13)21/h5-8,17,23H,4,9-11,22H2,1-3H3/t17-/m0/s1
IUPAC Name
3-ethyl 5-methyl (4S)-2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
SMILES
CCOC(=O)C1=C(COCCN)NC(C)=C([C@@H]1C1=CC=CC=C1Cl)C(=O)OC

References

General References
  1. Zhu Y, Wang F, Li Q, Zhu M, Du A, Tang W, Chen W: Amlodipine metabolism in human liver microsomes and roles of CYP3A4/5 in the dihydropyridine dehydrogenation. Drug Metab Dispos. 2014 Feb;42(2):245-9. doi: 10.1124/dmd.113.055400. Epub 2013 Dec 3. [Article]
  2. Liu Z, Zheng X, Yang X, Wang E, Wang J: Affinity and specificity of levamlodipine-human serum albumin interactions: insights into its carrier function. Biophys J. 2009 May 20;96(10):3917-25. doi: 10.1016/j.bpj.2008.12.3965. [Article]
  3. Laufen H, Leitold M: Enantioselective disposition of oral amlodipine in healthy volunteers. Chirality. 1994;6(7):531-6. doi: 10.1002/chir.530060704. [Article]
  4. Striessnig J, Ortner NJ, Pinggera A: Pharmacology of L-type Calcium Channels: Novel Drugs for Old Targets? Curr Mol Pharmacol. 2015;8(2):110-22. [Article]
  5. Meredith PA, Elliott HL: Clinical pharmacokinetics of amlodipine. Clin Pharmacokinet. 1992 Jan;22(1):22-31. doi: 10.2165/00003088-199222010-00003. [Article]
  6. Faulkner JK, McGibney D, Chasseaud LF, Perry JL, Taylor IW: The pharmacokinetics of amlodipine in healthy volunteers after single intravenous and oral doses and after 14 repeated oral doses given once daily. Br J Clin Pharmacol. 1986 Jul;22(1):21-5. [Article]
  7. Liu F, Qiu M, Zhai SD: Tolerability and effectiveness of (S)-amlodipine compared with racemic amlodipine in hypertension: a systematic review and meta-analysis. Curr Ther Res Clin Exp. 2010 Feb;71(1):1-29. doi: 10.1016/j.curtheres.2010.02.005. [Article]
  8. FDA Approved Drug Products: Conjupri Levamlodipine Oral Tablets [Link]
  9. S-Amlodipine [Link]
PubChem Compound
9822750
PubChem Substance
310265141
ChemSpider
7998499
RxNav
2376944
ChEBI
53796
ChEMBL
CHEMBL2111097
ZINC
ZINC000100001964
PDBe Ligand
6UB
Wikipedia
Levamlodipine
PDB Entries
5kmd / 6ke5 / 7jpx / 8we8
FDA label
Download (350 KB)

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
PhaseStatusPurposeConditionsCount
4CompletedTreatmentHypertension2
4Unknown StatusTreatmentHypertension1
4Unknown StatusTreatmentHypertension, Essential Hypertension1
3CompletedTreatmentHypertension3
3Unknown StatusTreatmentHypertension2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
TabletOral2.5 mg
TabletOral250000 mg
Tablet, coatedOral5 mg
TabletOral1.25 mg/1
TabletOral1.25 mg/1.25mg
TabletOral2.5 mg/2.5mg
TabletOral2.5 mg/1
TabletOral5 mg/5mg
TabletOral5 mg/1
Tablet, coatedOral
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)138https://comptox.epa.gov/dashboard/dsstoxdb/results?formula=1&isotopes=1&search=C24H31ClN2O10
boiling point (°C)413https://comptox.epa.gov/dashboard/dsstoxdb/results?formula=1&isotopes=1&search=C24H31ClN2O10
water solubility81 mg/mLhttp://www.selleckchem.com/products/levamlodipine.html
logP3.30https://comptox.epa.gov/dashboard/dsstoxdb/results?formula=1&isotopes=1&search=C24H31ClN2O10
pKa8.6FDA Label
Predicted Properties
PropertyValueSource
Water Solubility0.0074 mg/mLALOGPS
logP2.22ALOGPS
logP1.64Chemaxon
logS-4.7ALOGPS
pKa (Strongest Acidic)19.12Chemaxon
pKa (Strongest Basic)9.45Chemaxon
Physiological Charge1Chemaxon
Hydrogen Acceptor Count5Chemaxon
Hydrogen Donor Count2Chemaxon
Polar Surface Area99.88 Å2Chemaxon
Rotatable Bond Count10Chemaxon
Refractivity108.64 m3·mol-1Chemaxon
Polarizability42.11 Å3Chemaxon
Number of Rings2Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-07fs-0009100000-9b57943551fbdd06a2b2
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-066r-0009200000-01d7ac102a78a1193f78
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0pxs-0019200000-afac5bbded5eaac7522a
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-014i-0009000000-f69bd27017aa8c548520
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-00ei-2093000000-ed19c8ab0979143df9b2
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0ug0-3159000000-c0dfd6c3948e96bf6eb3
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-201.61644
predicted
DeepCCS 1.0 (2019)
[M+H]+203.97444
predicted
DeepCCS 1.0 (2019)
[M+Na]+210.40398
predicted
DeepCCS 1.0 (2019)

Targets

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Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Voltage-gated calcium channel activity
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1C
Uniprot ID
Q13936
Uniprot Name
Voltage-dependent L-type calcium channel subunit alpha-1C
Molecular Weight
248974.1 Da
References
  1. Striessnig J, Ortner NJ, Pinggera A: Pharmacology of L-type Calcium Channels: Novel Drugs for Old Targets? Curr Mol Pharmacol. 2015;8(2):110-22. [Article]
  2. Johnson R, Dludla P, Mabhida S, Benjeddou M, Louw J, February F: Pharmacogenomics of amlodipine and hydrochlorothiazide therapy and the quest for improved control of hypertension: a mini review. Heart Fail Rev. 2019 May;24(3):343-357. doi: 10.1007/s10741-018-09765-y. [Article]
  3. FDA Approved Drug Products: Conjupri Levamlodipine Oral Tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Voltage-gated calcium channel activity involved sa node cell action potential
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1D
Uniprot ID
Q01668
Uniprot Name
Voltage-dependent L-type calcium channel subunit alpha-1D
Molecular Weight
245138.75 Da
References
  1. Johnson R, Dludla P, Mabhida S, Benjeddou M, Louw J, February F: Pharmacogenomics of amlodipine and hydrochlorothiazide therapy and the quest for improved control of hypertension: a mini review. Heart Fail Rev. 2019 May;24(3):343-357. doi: 10.1007/s10741-018-09765-y. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Tetrahydrobiopterin binding
Specific Function
Produces nitric oxide (NO) which is implicated in vascular smooth muscle relaxation through a cGMP-mediated signal transduction pathway. NO mediates vascular endothelial growth factor (VEGF)-induce...
Gene Name
NOS3
Uniprot ID
P29474
Uniprot Name
Nitric oxide synthase, endothelial
Molecular Weight
133287.62 Da
References
  1. He Y, Si D, Yang C, Ni L, Li B, Ding M, Yang P: The effects of amlodipine and S(-)-amlodipine on vascular endothelial function in patients with hypertension. Am J Hypertens. 2014 Jan;27(1):27-31. doi: 10.1093/ajh/hpt138. Epub 2013 Aug 19. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Tetrahydrobiopterin binding
Specific Function
Produces nitric oxide (NO) which is a messenger molecule with diverse functions throughout the body. In macrophages, NO mediates tumoricidal and bactericidal actions. Also has nitrosylase activity ...
Gene Name
NOS2
Uniprot ID
P35228
Uniprot Name
Nitric oxide synthase, inducible
Molecular Weight
131116.3 Da
References
  1. He Y, Si D, Yang C, Ni L, Li B, Ding M, Yang P: The effects of amlodipine and S(-)-amlodipine on vascular endothelial function in patients with hypertension. Am J Hypertens. 2014 Jan;27(1):27-31. doi: 10.1093/ajh/hpt138. Epub 2013 Aug 19. [Article]

Enzymes

Kind
Protein
Organism
Humans
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
References
  1. Zhu Y, Wang F, Li Q, Zhu M, Du A, Tang W, Chen W: Amlodipine metabolism in human liver microsomes and roles of CYP3A4/5 in the dihydropyridine dehydrogenation. Drug Metab Dispos. 2014 Feb;42(2):245-9. doi: 10.1124/dmd.113.055400. Epub 2013 Dec 3. [Article]
  2. Amlodipine Metabolism in Human Liver Microsomes and Roles of CYP3A4/5 in the Dihydropyridine Dehydrogenation [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Tetrahydrobiopterin binding
Specific Function
Produces nitric oxide (NO) which is a messenger molecule with diverse functions throughout the body. In macrophages, NO mediates tumoricidal and bactericidal actions. Also has nitrosylase activity ...
Gene Name
NOS2
Uniprot ID
P35228
Uniprot Name
Nitric oxide synthase, inducible
Molecular Weight
131116.3 Da
References
  1. He Y, Si D, Yang C, Ni L, Li B, Ding M, Yang P: The effects of amlodipine and S(-)-amlodipine on vascular endothelial function in patients with hypertension. Am J Hypertens. 2014 Jan;27(1):27-31. doi: 10.1093/ajh/hpt138. Epub 2013 Aug 19. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Tetrahydrobiopterin binding
Specific Function
Produces nitric oxide (NO) which is implicated in vascular smooth muscle relaxation through a cGMP-mediated signal transduction pathway. NO mediates vascular endothelial growth factor (VEGF)-induce...
Gene Name
NOS3
Uniprot ID
P29474
Uniprot Name
Nitric oxide synthase, endothelial
Molecular Weight
133287.62 Da
References
  1. He Y, Si D, Yang C, Ni L, Li B, Ding M, Yang P: The effects of amlodipine and S(-)-amlodipine on vascular endothelial function in patients with hypertension. Am J Hypertens. 2014 Jan;27(1):27-31. doi: 10.1093/ajh/hpt138. Epub 2013 Aug 19. [Article]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Liu Z, Zheng X, Yang X, Wang E, Wang J: Affinity and specificity of levamlodipine-human serum albumin interactions: insights into its carrier function. Biophys J. 2009 May 20;96(10):3917-25. doi: 10.1016/j.bpj.2008.12.3965. [Article]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Johnson R, Dludla P, Mabhida S, Benjeddou M, Louw J, February F: Pharmacogenomics of amlodipine and hydrochlorothiazide therapy and the quest for improved control of hypertension: a mini review. Heart Fail Rev. 2019 May;24(3):343-357. doi: 10.1007/s10741-018-09765-y. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Bile acid:sodium symporter activity
Specific Function
Plays a critical role in the sodium-dependent reabsorption of bile acids from the lumen of the small intestine. Plays a key role in cholesterol metabolism.
Gene Name
SLC10A2
Uniprot ID
Q12908
Uniprot Name
Ileal sodium/bile acid cotransporter
Molecular Weight
37713.405 Da
References
  1. Zheng X, Diao L, Ekins S, Polli JE: Why we should be vigilant: drug cytotoxicity observed with in vitro transporter inhibition studies. Biochem Pharmacol. 2010 Oct 1;80(7):1087-92. doi: 10.1016/j.bcp.2010.06.012. Epub 2010 Jun 23. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Symporter activity
Specific Function
Sodium-ion dependent, high affinity carnitine transporter. Involved in the active cellular uptake of carnitine. Transports one sodium ion with one molecule of carnitine. Also transports organic cat...
Gene Name
SLC22A5
Uniprot ID
O76082
Uniprot Name
Solute carrier family 22 member 5
Molecular Weight
62751.08 Da
References
  1. Zheng X, Diao L, Ekins S, Polli JE: Why we should be vigilant: drug cytotoxicity observed with in vitro transporter inhibition studies. Biochem Pharmacol. 2010 Oct 1;80(7):1087-92. doi: 10.1016/j.bcp.2010.06.012. Epub 2010 Jun 23. [Article]

Drug created at October 23, 2015 16:47 / Updated at August 13, 2021 04:44