Identification

Name
Ivermectin
Accession Number
DB00602
Description

Ivermectin is a broad-spectrum anti-parasite medication. It was first marketed under the name Stromectol® and used against worms (except tapeworms), but, in 2012, it was approved for the topical treatment of head lice infestations in patients 6 months of age and older, and marketed under the name Sklice™ as well. Ivermectin is mainly used in humans in the treatment of onchocerciasis, but is also effective against other worm infestations (such as strongyloidiasis, ascariasis, trichuriasis and enterobiasis).

Type
Small Molecule
Groups
Approved, Investigational, Vet approved
Structure
Thumb
Weight
Average: 1736.1589
Monoisotopic: 1735.000064088
Chemical Formula
C95H146O28
Synonyms
  • Ivermectin
  • Ivermectina
  • Ivermectine
  • Ivermectinum
External IDs
  • MK 933

Pharmacology

Indication

For the treatment of intestinal (i.e., nondisseminated) strongyloidiasis due to the nematode parasite Strongyloides stercoralis. Also for the treatment of onchocerciasis (river blindness) due to the nematode parasite Onchocerca volvulus. Can be used to treat scabies caused by Sarcoptes scabiei.

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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Pharmacodynamics

Ivermectin is a semisynthetic, anthelminitic agent. It is an avermectin which a group of pentacyclic sixteen-membered lactone (i.e. a macrocyclic lactone disaccharide) derived from the soil bacterium Streptomyces avermitilis. Avermectins are potent anti-parasitic agents. Ivermectin is the most common avermectin. It is a broad spectrum antiparasitic drug for oral administration. It is sometimes used to treat human onchocerciasis (river blindness). It is the mixture of 22,23-dihydro-avermectin B1a (at least 90%) and 22,23-dihydro-avermectin B1b (less than 10%).

Mechanism of action

Ivermectin binds selectively and with high affinity to glutamate-gated chloride ion channels in invertebrate muscle and nerve cells of the microfilaria. This binding causes an increase in the permeability of the cell membrane to chloride ions and results in hyperpolarization of the cell, leading to paralysis and death of the parasite. Ivermectin also is believed to act as an agonist of the neurotransmitter gamma-aminobutyric acid (GABA), thereby disrupting GABA-mediated central nervous system (CNS) neurosynaptic transmission. Ivermectin may also impair normal intrauterine development of O. volvulus microfilariae and may inhibit their release from the uteri of gravid female worms.

TargetActionsOrganism
AGlycine receptor subunit alpha-3
agonist
Humans
UGamma-aminobutyric acid receptor subunit beta-3
agonist
Humans
Absorption

Moderately well absorbed. Improved absorption with high fat meal.

Volume of distribution

The volume of distribution is 3 to 3.5 L/kg and it does not cross the blood-brain barrier.

Protein binding

93%

Metabolism

Primarily hepatic. Ivermectin and/or its metabolites are excreted almost exclusively in the feces over an estimated 12 days, with less than 1 % of the administered dose excreted in the urine.

Route of elimination

Ivermectin is metabolized in the liver, and ivermectin and/or its metabolites are excreted almost exclusively in the feces over an estimated 12 days, with less than 1% of the administered dose excreted in the urine.

Half-life

16 hours (also reported at 22-28 hours)

Clearance
Not Available
Adverse Effects
Learn about our commercial Adverse Effects data.
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Toxicity

LD50 = 29.5 mg/kg (Mouse, oral). LD50 = 10 mg/kg (Rat, oral). Adverse effects include muscle or joint pain, dizziness, fever, headache, skin rash, fast heartbeat.

Affected organisms
  • Parasitic nematodes and other roundworms
  • Head lice
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
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
AbametapirThe serum concentration of Ivermectin can be increased when it is combined with Abametapir.
AbemaciclibAbemaciclib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
AbirateroneThe metabolism of Abiraterone can be increased when combined with Ivermectin.
AcalabrutinibThe metabolism of Acalabrutinib can be increased when combined with Ivermectin.
AcenocoumarolIvermectin may decrease the anticoagulant activities of Acenocoumarol.
AcipimoxThe risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ivermectin is combined with Acipimox.
AfatinibAfatinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
AlbendazoleThe metabolism of Albendazole can be increased when combined with Ivermectin.
AlectinibThe metabolism of Ivermectin can be increased when combined with Alectinib.
Alendronic acidThe risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ivermectin is combined with Alendronic acid.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Take on an empty stomach.

Products

Product Images
International/Other Brands
Ascapil (Abbott) / Detebencil (Roux-Ocefa) / Ermetin (Unipharm) / Gotax (Metlen) / Imectin (Pulse) / Ivectin (Aristopharma) / Ivera (Beximco) / Ivergot (Licol) / Ivermec (UCI) / Ivexterm (Valeant) / Ivori (Invision) / Kaonol (Mediderm) / Kilox (Bussié) / Maikeding (Hisun) / Quanox (Dermacare) / Revectina (Solvay) / Scabo (Delta) / Scavista (Zuventus) / Securo (Valeant) / Vermectin (Atlantic Lab)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
RosiverCreamTopicalGalderma2015-05-25Not applicableCanada flag
SkliceLotion5 mg/1gTopicalArbor Pharmaceuticals2016-06-30Not applicableUS flag
SkliceLotion0.585 g/117gTopicalSanofi Pasteur, Inc2012-07-092017-07-31US flag
SoolantraCream10 mg/1gTopicalGalderma Laboratories, L.P.2015-01-01Not applicableUS flag
StromectolTablet3 mg/1OralMerck Sharp & Dohme Corp.1996-11-22Not applicableUS flag00006 0032 20 nlmimage10 df16efc7
StromectolTablet3 mg/1OralDepartment Of State Health Services, Pharmacy Branch1996-11-22Not applicableUS flag
StromectolTablet6 mg/1OralMerck & Co., Inc.2006-04-132006-04-13US flag
StromectolTablet3 mgOralMerck Ltd.2018-11-06Not applicableCanada flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
IvermectinTablet3 mg/1OralEdenbridge Pharmaceuticals Llc2014-11-15Not applicableUS flag42799 0806 01 nlmimage10 04460200
IvermectinCream10 mg/1gTopicalPrasco Laboratories2019-10-15Not applicableUS flag
IvermectinCream10 mg/1gTopicalActavis Pharma, Inc.2019-10-14Not applicableUS flag
IvermectinTablet3 mg/1OralNucare Pharmaceuticals,inc.2014-11-15Not applicableUS flag
IvermectinTablet3 mg/1Oralbryant ranch prepack2014-11-15Not applicableUS flag
IvermectinTablet3 mg/1OralCentral Texas Community Health Centers2014-11-15Not applicableUS flag
IvermectinLotion5 mg/1gTopicalTaro Pharmaceuticals U.S.A., Inc.2020-05-06Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
171083 Ivermectin 1% / Metronidazole 1% / Niacinamide 4%Ivermectin (1 g/100g) + Metronidazole (1 g/100g) + Nicotinamide (4 g/100g)GelTopicalSincerus Florida, LLC2020-07-02Not applicableUS flag
Brimonidine Tartrate 0.25% / Ivermectin 1% / Metronidazole 1% / Niacinamide 4%Ivermectin (1 g/100g) + Brimonidine tartrate (0.25 g/100g) + Metronidazole (1 g/100g) + Nicotinamide (4 g/100g)GelTopicalSincerus Florida, LLC2019-05-16Not applicableUS flag
Ivermectin 1% / Metronidazole 1%Ivermectin (1 g/100g) + Metronidazole (1 g/100g)GelTopicalSincerus Florida, LLC2019-05-01Not applicableUS flag
Ivermectin 1% / Metronidazole 1% / Niacinamide 4%Ivermectin (1 g/100g) + Metronidazole (1 g/100g) + Nicotinamide (4 g/100g)GelTopicalSincerus Florida, LLC2019-05-01Not applicableUS flag

Categories

ATC Codes
P02CF01 — IvermectinD11AX22 — Ivermectin
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as milbemycins. These are a group of macrolides with a structure containing a 16-membered lactone ring fused to a 1,7-dioxaspiroundecane ring system and to either a benzofuran (or hydrogenated derivative thereof). In some cases (e.g. Milbemycin E), the tetrahydrofuranyl ring is missing. Milbemycins can be o-glycosylated at C13 to form Avermectins. Milbemycins are produced by Streptomyces species.
Kingdom
Organic compounds
Super Class
Phenylpropanoids and polyketides
Class
Macrolides and analogues
Sub Class
Milbemycins
Direct Parent
Milbemycins
Alternative Parents
O-glycosyl compounds / Disaccharides / Ketals / Oxanes / Tetrahydrofurans / Tertiary alcohols / Secondary alcohols / Lactones / Carboxylic acid esters / Oxacyclic compounds
show 5 more
Substituents
Acetal / Alcohol / Aliphatic heteropolycyclic compound / Carbonyl group / Carboxylic acid derivative / Carboxylic acid ester / Dialkyl ether / Disaccharide / Ether / Glycosyl compound
show 15 more
Molecular Framework
Not Available
External Descriptors
Not Available

Chemical Identifiers

UNII
8883YP2R6D
CAS number
70288-86-7
InChI Key
SPBDXSGPUHCETR-CVSKBELMSA-N
InChI
InChI=1S/C48H74O14.C47H72O14/c1-11-25(2)43-28(5)17-18-47(62-43)23-34-20-33(61-47)16-15-27(4)42(26(3)13-12-14-32-24-55-45-40(49)29(6)19-35(46(51)58-34)48(32,45)52)59-39-22-37(54-10)44(31(8)57-39)60-38-21-36(53-9)41(50)30(7)56-38;1-24(2)41-27(5)16-17-46(61-41)22-33-19-32(60-46)15-14-26(4)42(25(3)12-11-13-31-23-54-44-39(48)28(6)18-34(45(50)57-33)47(31,44)51)58-38-21-36(53-10)43(30(8)56-38)59-37-20-35(52-9)40(49)29(7)55-37/h12-15,19,25-26,28,30-31,33-45,49-50,52H,11,16-18,20-24H2,1-10H3;11-14,18,24-25,27,29-30,32-44,48-49,51H,15-17,19-23H2,1-10H3/b13-12+,27-15+,32-14+;12-11+,26-14+,31-13+/t25-,26+,28+,30+,31+,33-,34+,35+,36+,37+,38+,39+,40-,41+,42+,43-,44+,45-,47-,48-;25-,27-,29-,30-,32+,33-,34-,35-,36-,37-,38-,39+,40-,41+,42-,43-,44+,46+,47+/m10/s1
IUPAC Name
(1'R,2R,4'S,5S,6R,8'R,10'E,12'S,13'S,14'E,16'E,20'R,21'R,24'S)-21',24'-dihydroxy-12'-{[(2R,4S,5S,6S)-5-{[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy}-4-methoxy-6-methyloxan-2-yl]oxy}-5,11',13',22'-tetramethyl-6-(propan-2-yl)-3',7',19'-trioxaspiro[oxane-2,6'-tetracyclo[15.6.1.1⁴,⁸.0²⁰,²⁴]pentacosane]-10',14',16',22'-tetraen-2'-one; (1'R,2R,4'S,5S,6R,8'R,10'E,12'S,13'S,14'E,16'E,20'R,21'R,24'S)-6-[(2R)-butan-2-yl]-21',24'-dihydroxy-12'-{[(2R,4S,5S,6S)-5-{[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy}-4-methoxy-6-methyloxan-2-yl]oxy}-5,11',13',22'-tetramethyl-3',7',19'-trioxaspiro[oxane-2,6'-tetracyclo[15.6.1.1⁴,⁸.0²⁰,²⁴]pentacosane]-10',14',16',22'-tetraen-2'-one
SMILES

References

Synthesis Reference

Shuet-Hing L. Chiu, Josephine R. Carlin, Rae Taub, "Ivermectin derivative compounds and process for preparing the same." U.S. Patent US4963667, issued June, 1982.

US4963667
General References
Not Available
Human Metabolome Database
HMDB0014740
KEGG Drug
D00804
KEGG Compound
C07970
PubChem Compound
46936176
PubChem Substance
46506810
ChemSpider
30776735
RxNav
6069
ChEMBL
CHEMBL1200633
Therapeutic Targets Database
DAP000261
PharmGKB
PA450133
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Ivermectin
AHFS Codes
  • 08:08.00 — Anthelmintics
  • 84:04.12 — Scabicides and Pediculicides
FDA label
Download (60.2 KB)
MSDS
Download (73.4 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedBasic ScienceLoiasis1
4CompletedTreatmentAcne Rosacea2
4CompletedTreatmentEpilepsies1
4CompletedTreatmentEpilepsies / Ivermectin / Onchocerciasis1
4CompletedTreatmentHelminth Infection / Lymphatic Filariasis1
4CompletedTreatmentImpetigo / Scabies / Yaws1
4CompletedTreatmentLymphatic Filariasis1
4Not Yet RecruitingTreatmentAsymptomatic Infections / Novel Coronavirus Infectious Disease (COVID-19) / SARS-CoV2 Infection1
4Not Yet RecruitingTreatmentLymphatic Filariases / Trachoma1
4RecruitingHealth Services ResearchHealthy Volunteers1

Pharmacoeconomics

Manufacturers
  • Merck and co inc
Packagers
  • Gallipot
  • Merck & Co.
Dosage Forms
FormRouteStrength
Injection
Solution
Cream10 MG/G
Granule
SolutionOral6 mg
Powder
SolutionOral
SuspensionOral6 mg
SolutionOral0.006 g
CreamTopical10 mg/1g
PowderNot applicable1 kg/1kg
GelTopical
Capsule, liquid filledOral3 mg
SolutionOral0.6 g
Suspension
CreamTopical
Tablet3 mg
LotionTopical0.585 g/117g
LotionTopical5 mg/1g
CreamTopical1 g
TabletOral3 mg/1
TabletOral3 mg
TabletOral6 mg/1
Tablet6 mg
SolutionTopical0.1 g
Prices
Unit descriptionCostUnit
Stromectol 20 3 mg tablet Box116.13USD box
Ivermectin powder14.0USD g
Stromectol 3 mg tablet5.58USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US8927595No2015-01-062027-10-12US flag
US8791153No2014-07-292027-10-12US flag
US6103248No2000-08-152018-05-22US flag
US9089587No2015-07-282034-03-13US flag
US8470788No2013-06-252024-04-22US flag
US9233118No2016-01-122034-03-13US flag
US9233117No2016-01-122034-03-13US flag
US7550440No2009-06-232024-04-22US flag
US8815816No2014-08-262024-04-22US flag
US8093219No2012-01-102024-04-22US flag
US8080530No2011-12-202024-04-22US flag
US6133310No2000-10-172019-04-26US flag
US5952372No1999-09-142018-09-18US flag
US8415311No2013-04-092024-04-22US flag
US9782425No2017-10-102034-03-13US flag
US10206939No2019-02-192034-03-13US flag
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)155 °CNot Available
water solubilityInsolubleNot Available
Predicted Properties
PropertyValueSource
logP5.83ChemAxon
pKa (Strongest Acidic)12.47ChemAxon
pKa (Strongest Basic)-3.4ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count13ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area170.06 Å2ChemAxon
Rotatable Bond Count15ChemAxon
Refractivity230.33 m3·mol-1ChemAxon
Polarizability96.87 Å3ChemAxon
Number of Rings14ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.8146
Blood Brain Barrier-0.549
Caco-2 permeable-0.8192
P-glycoprotein substrateSubstrate0.8771
P-glycoprotein inhibitor IInhibitor0.805
P-glycoprotein inhibitor IIInhibitor0.8192
Renal organic cation transporterNon-inhibitor0.7384
CYP450 2C9 substrateNon-substrate0.8877
CYP450 2D6 substrateNon-substrate0.886
CYP450 3A4 substrateSubstrate0.7714
CYP450 1A2 substrateNon-inhibitor0.9129
CYP450 2C9 inhibitorNon-inhibitor0.8366
CYP450 2D6 inhibitorNon-inhibitor0.928
CYP450 2C19 inhibitorNon-inhibitor0.8793
CYP450 3A4 inhibitorNon-inhibitor0.7957
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8073
Ames testNon AMES toxic0.8295
CarcinogenicityNon-carcinogens0.9622
BiodegradationNot ready biodegradable0.9759
Rat acute toxicity3.5285 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9471
hERG inhibition (predictor II)Non-inhibitor0.5536
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 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

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Transmitter-gated ion channel activity
Specific Function
The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing).
Gene Name
GLRA3
Uniprot ID
O75311
Uniprot Name
Glycine receptor subunit alpha-3
Molecular Weight
53799.775 Da
References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  2. Yates DM, Wolstenholme AJ: An ivermectin-sensitive glutamate-gated chloride channel subunit from Dirofilaria immitis. Int J Parasitol. 2004 Aug;34(9):1075-81. [PubMed:15313134]
  3. McCavera S, Rogers AT, Yates DM, Woods DJ, Wolstenholme AJ: An ivermectin-sensitive glutamate-gated chloride channel from the parasitic nematode Haemonchus contortus. Mol Pharmacol. 2009 Jun;75(6):1347-55. doi: 10.1124/mol.108.053363. Epub 2009 Mar 31. [PubMed:19336526]
  4. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Gaba-gated chloride ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name
GABRB3
Uniprot ID
P28472
Uniprot Name
Gamma-aminobutyric acid receptor subunit beta-3
Molecular Weight
54115.04 Da
References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  2. Feng XP, Hayashi J, Beech RN, Prichard RK: Study of the nematode putative GABA type-A receptor subunits: evidence for modulation by ivermectin. J Neurochem. 2002 Nov;83(4):870-8. [PubMed:12421359]
  3. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inducer
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. Zeng Z, Andrew NW, Arison BH, Luffer-Atlas D, Wang RW: Identification of cytochrome P4503A4 as the major enzyme responsible for the metabolism of ivermectin by human liver microsomes. Xenobiotica. 1998 Mar;28(3):313-21. doi: 10.1080/004982598239597 . [PubMed:9574819]
  2. Kudzi W, Dodoo AN, Mills JJ: Genetic polymorphisms in MDR1, CYP3A4 and CYP3A5 genes in a Ghanaian population: a plausible explanation for altered metabolism of ivermectin in humans? BMC Med Genet. 2010 Jul 14;11:111. doi: 10.1186/1471-2350-11-111. [PubMed:20630055]
  3. Juarez M, Schcolnik-Cabrera A, Duenas-Gonzalez A: The multitargeted drug ivermectin: from an antiparasitic agent to a repositioned cancer drug. Am J Cancer Res. 2018 Feb 1;8(2):317-331. eCollection 2018. [PubMed:29511601]
  4. Skalova L, Szotakova B, Machala M, Neca J, Soucek P, Havlasova J, Wsol V, Kridova L, Kvasnickova E, Lamka J: Effect of ivermectin on activities of cytochrome P450 isoenzymes in mouflon (Ovis musimon) and fallow deer (Dama dama). Chem Biol Interact. 2001 Aug 31;137(2):155-67. doi: 10.1016/s0009-2797(01)00227-7. [PubMed:11551531]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Inducer
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. Schwab D, Fischer H, Tabatabaei A, Poli S, Huwyler J: Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25. [PubMed:12699389]
  2. Pouliot JF, L'Heureux F, Liu Z, Prichard RK, Georges E: Reversal of P-glycoprotein-associated multidrug resistance by ivermectin. Biochem Pharmacol. 1997 Jan 10;53(1):17-25. [PubMed:8960059]
  3. Nagy H, Goda K, Fenyvesi F, Bacso Z, Szilasi M, Kappelmayer J, Lustyik G, Cianfriglia M, Szabo G Jr: Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. Biochem Biophys Res Commun. 2004 Mar 19;315(4):942-9. [PubMed:14985103]
  4. Schinkel AH, Wagenaar E, van Deemter L, Mol CA, Borst P: Absence of the mdr1a P-Glycoprotein in mice affects tissue distribution and pharmacokinetics of dexamethasone, digoxin, and cyclosporin A. J Clin Invest. 1995 Oct;96(4):1698-705. [PubMed:7560060]
  5. Jani M, Makai I, Kis E, Szabo P, Nagy T, Krajcsi P, Lespine A: Ivermectin interacts with human ABCG2. J Pharm Sci. 2011 Jan;100(1):94-7. doi: 10.1002/jps.22262. Epub 2010 Jun 22. [PubMed:20574995]
  6. Menez C, Mselli-Lakhal L, Foucaud-Vignault M, Balaguer P, Alvinerie M, Lespine A: Ivermectin induces P-glycoprotein expression and function through mRNA stabilization in murine hepatocyte cell line. Biochem Pharmacol. 2012 Jan 15;83(2):269-78. doi: 10.1016/j.bcp.2011.10.010. Epub 2011 Oct 18. [PubMed:22024132]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Transporter activity
Specific Function
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotre...
Gene Name
ABCC1
Uniprot ID
P33527
Uniprot Name
Multidrug resistance-associated protein 1
Molecular Weight
171589.5 Da
References
  1. Lespine A, Dupuy J, Orlowski S, Nagy T, Glavinas H, Krajcsi P, Alvinerie M: Interaction of ivermectin with multidrug resistance proteins (MRP1, 2 and 3). Chem Biol Interact. 2006 Feb 25;159(3):169-79. Epub 2005 Dec 27. [PubMed:16384552]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Organic anion transmembrane transporter activity
Specific Function
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name
ABCC2
Uniprot ID
Q92887
Uniprot Name
Canalicular multispecific organic anion transporter 1
Molecular Weight
174205.64 Da
References
  1. Lespine A, Dupuy J, Orlowski S, Nagy T, Glavinas H, Krajcsi P, Alvinerie M: Interaction of ivermectin with multidrug resistance proteins (MRP1, 2 and 3). Chem Biol Interact. 2006 Feb 25;159(3):169-79. Epub 2005 Dec 27. [PubMed:16384552]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. Jani M, Makai I, Kis E, Szabo P, Nagy T, Krajcsi P, Lespine A: Ivermectin interacts with human ABCG2. J Pharm Sci. 2011 Jan;100(1):94-7. doi: 10.1002/jps.22262. Epub 2010 Jun 22. [PubMed:20574995]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. Karlgren M, Vildhede A, Norinder U, Wisniewski JR, Kimoto E, Lai Y, Haglund U, Artursson P: Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. J Med Chem. 2012 May 24;55(10):4740-63. doi: 10.1021/jm300212s. Epub 2012 May 15. [PubMed:22541068]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
Gene Name
SLCO1B3
Uniprot ID
Q9NPD5
Uniprot Name
Solute carrier organic anion transporter family member 1B3
Molecular Weight
77402.175 Da
References
  1. Karlgren M, Vildhede A, Norinder U, Wisniewski JR, Kimoto E, Lai Y, Haglund U, Artursson P: Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. J Med Chem. 2012 May 24;55(10):4740-63. doi: 10.1021/jm300212s. Epub 2012 May 15. [PubMed:22541068]

Drug created on June 13, 2005 07:24 / Updated on October 23, 2020 21:53

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