Ivermectin

Identification

Summary

Ivermectin is an anti parasite medication used to treat head lice, onchocerciasis, strongyloidiasis, ascariasis, trichuriasis, and enterobiasis.

Brand Names
Sklice, Soolantra, Stromectol
Generic Name
Ivermectin
DrugBank Accession Number
DB00602
Background

Ivermectin is a semi-synthetic antiparasitic medication derived from avermectins, a class of highly-active broad-spectrum antiparasitic agents isolated from the fermentation products of Streptomyces avermitilis.8 Ivermectin itself is a mixture of two avermectins, comprising roughly 90% 5-O-demethyl-22,23-dihydroavermectin A1a (22,23-dihydroavermectin B1a) and 10% 5-O-demethyl-25-de(1-methylpropyl)-22,23-dihydro­-25-(1-methylethyl)avermectin A1a (22,23-dihydroavermectin B1b).8

Ivermectin is mainly used in humans in the treatment of onchocerciasis, but may also be effective against other worm infestations (such as strongyloidiasis, ascariasis, trichuriasis and enterobiasis). Applied topically, it may be used in the treatment of head lice infestation.

With the advent of 2020 and the COVID-19 pandemic, ivermectin began garnering notoriety due to its off-label use for the prophylaxis and treatment of COVID-19. While studies are still ongoing, much of the evidence for ivermectin in COVID-19 relies on pre-print in vitro data, and the clinical utility of this data remains unclear. Due to a number of factors - for example, the relatively low number of patients per trial and the speed at which these trials were conducted - studies on the use of ivermectin in COVID-19 have been fraught with statistical errors and accusations of plagiarism.9,5 In addition, the use of aggregate patient data in large-scale meta-analyses (as opposed to individual patient data (IPD)) has been shown to disguise otherwise blatant data errors, such as extreme terminal digit bias and the duplication of blocks of patient records.5

Until high-quality, peer-reviewed data regarding both the safety and efficacy of ivermectin for COVID-19 in humans becomes available, the use of ivermectin for these purposes should be avoided in favour of thoroughly-vetted therapies (e.g. COVID-19 vaccines like Comirnaty).

Type
Small Molecule
Groups
Approved, Investigational, Vet approved
Structure
Thumb
Weight
Average: 1736.185
Monoisotopic: 1735.000064061
Chemical Formula
C95H146O28
Synonyms
  • Ivermectin
  • Ivermectina
  • Ivermectine
  • Ivermectinum
External IDs
  • L 640471
  • L-640471
  • MK 933
  • MK-0933
  • MK-933

Pharmacology

Indication

Administered topically, ivermectin cream is indicated for the treatment of inflammatory lesions associated with rosacea.7 An over-the-counter ivermection lotion is commercially available and indicated for the topical treatment of head lice infestations in patients ≥6 months of age.6

Orally administered ivermectin is indicated as a broad-spectrum anti-parasitic for the treatment of intestinal strongyloidiasis caused by Strongyloides stercoralis and onchocerciasis caused by Onchocerca volvulus.8 Systemic ivermectin therapy is used internationally for the treatment of various tropical diseases, including filariasis, cutaneous larva migrans, and Loa loa infection, amongst others.2

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Ivermectin is a semisynthetic, anthelminitic agent. It is an avermectin, a group of pentacyclic sixteen-membered lactones (i.e. a macrocyclic lactone disaccharide) derived from the soil bacterium Streptomyces avermitilis. Avermectins are potent and broad-spectrum anti-parasitic agents.

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.

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.

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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

Following oral administration, the half-life of ivermectin is approximately 18 hours.8

Clearance

Not Available

Adverse Effects
Adverseeffects
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Toxicity

Used appropriately, topically applied ivermectin lotions and creams are unlikely to cause significant toxicity. With accidental or intentional significant exposure to unknown quantities of veterinary formulations of ivermectin (by ingestion, inhalation, injection, or significant body surface area exposure) patients have reported rash, edema, headache, dizziness, asthenia, nausea, vomiting, and diarrhea. Other less common effects include seizure, ataxia, dyspnea, abdominal pain, paresthesia, urticaria, and contact dermatitis.8 Overdosage with orally administered ivermectin was lethal in mice and rats (at doses several-fold higher than the recommended dose), with death preceded by significant ataxia, bradypnea, tremors, ptosis, decreased activity, emesis, and mydriasis.8

If overdosage of ivermectin is suspected, initiate supportive therapy as clinically indicated, including the use of parenteral fluids and electrolytes, respiratory support, and pressor agents to manage hypotension. Induction of emesis and/or gastric lavage may be considered alongside other purgatives and routine anti-poison measures if clinically indicated.8

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 Ivermectin can be decreased when combined with Abiraterone.
AcenocoumarolIvermectin may increase 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.
AlectinibAlectinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Alendronic acidThe risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ivermectin is combined with Alendronic acid.
AmbrisentanThe excretion of Ambrisentan can be decreased when combined with Ivermectin.
AmiodaroneThe metabolism of Ivermectin can be decreased when combined with Amiodarone.
Interactions
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Food Interactions
  • Take on an empty stomach. Oral ivermectin should be taken on an empty stomach with a glass of water.

Products

Products2
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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
RosiverCream1 % w/wTopicalGalderma2015-05-25Not 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
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
IvermectinTablet3 mg/1OralEdenbridge Pharmaceuticals Llc2014-11-15Not applicableUS flag42799 0806 01 nlmimage10 04460200
IvermectinTablet3 mg/1OralNucare Pharmaceuticals,inc.2014-11-15Not applicableUS flag
IvermectinCream10 mg/1gTopicalActavis Pharma, Inc.2019-10-14Not applicableUS flag
IvermectinTablet3 mg/1OralA-S Medication Solutions2014-11-15Not applicableUS flag
IvermectinTablet3 mg/1Oralbryant ranch prepack2014-11-15Not applicableUS flag
IvermectinLotion5 mg/1gTopicalTaro Pharmaceuticals U.S.A., Inc.2020-05-06Not applicableUS flag
IvermectinTablet3 mg/1OralCentral Texas Community Health Centers2014-11-15Not applicableUS flag
IvermectinCream10 mg/1gTopicalPaddock Laboratories, LLC.2021-06-07Not applicableUS flag
IvermectinCream10 mg/1gTopicalPrasco Laboratories2019-10-15Not applicableUS flag
IvermectinCream10 mg/1gTopicalbryant ranch prepack2019-10-14Not applicableUS flag
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
IvermectinLotion5 mg/1gTopicalTaro Pharmaceuticals U.S.A., Inc.2020-05-06Not applicableUS flag
SkliceLotion5 mg/1gTopicalArbor Pharmaceuticals2021-08-01Not applicableUS flag
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
Classification
Not classified
Affected organisms
  • Parasitic nematodes and other roundworms
  • Head lice

Chemical Identifiers

UNII
8883YP2R6D
CAS number
70288-86-7
InChI Key
SPBDXSGPUHCETR-JFUDTMANSA-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+/m00/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[15.6.1.1^{4,8}.0^{20,24}]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-[(2S)-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[15.6.1.1^{4,8}.0^{20,24}]pentacosane]-10',14',16',22'-tetraen-2'-one
SMILES
[H][C@@]12OC\C3=C/C=C/[C@H](C)[C@H](O[C@H]4C[C@H](OC)[C@@H](O[C@H]5C[C@H](OC)[C@@H](O)[C@H](C)O5)[C@H](C)O4)\C(C)=C\C[C@]4([H])C[C@@]([H])(C[C@]5(CC[C@H](C)[C@]([H])(O5)C(C)C)O4)OC(=O)[C@]([H])(C=C(C)[C@H]1O)[C@@]23O.[H][C@@]12OC\C3=C/C=C/[C@H](C)[C@H](O[C@H]4C[C@H](OC)[C@@H](O[C@H]5C[C@H](OC)[C@@H](O)[C@H](C)O5)[C@H](C)O4)\C(C)=C\C[C@]4([H])C[C@@]([H])(C[C@]5(CC[C@H](C)[C@]([H])(O5)[C@@H](C)CC)O4)OC(=O)[C@]([H])(C=C(C)[C@H]1O)[C@@]23O

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
  1. El-Saber Batiha G, Alqahtani A, Ilesanmi OB, Saati AA, El-Mleeh A, Hetta HF, Magdy Beshbishy A: Avermectin Derivatives, Pharmacokinetics, Therapeutic and Toxic Dosages, Mechanism of Action, and Their Biological Effects. Pharmaceuticals (Basel). 2020 Aug 17;13(8). pii: ph13080196. doi: 10.3390/ph13080196. [Article]
  2. Mathachan SR, Sardana K, Khurana A: Current Use of Ivermectin in Dermatology, Tropical Medicine, and COVID-19: An Update on Pharmacology, Uses, Proven and Varied Proposed Mechanistic Action. Indian Dermatol Online J. 2021 Jul 14;12(4):500-514. doi: 10.4103/idoj.idoj_298_21. eCollection 2021 Jul-Aug. [Article]
  3. Alam S, Kamal TB, Sarker MMR, Zhou JR, Rahman SMA, Mohamed IN: Therapeutic Effectiveness and Safety of Repurposing Drugs for the Treatment of COVID-19: Position Standing in 2021. Front Pharmacol. 2021 Jun 14;12:659577. doi: 10.3389/fphar.2021.659577. eCollection 2021. [Article]
  4. Bestetti RB, Furlan-Daniel R, Silva VMR: Pharmacological Treatment of Patients with Mild to Moderate COVID-19: A Comprehensive Review. Int J Environ Res Public Health. 2021 Jul 5;18(13). pii: ijerph18137212. doi: 10.3390/ijerph18137212. [Article]
  5. Lawrence JM, Meyerowitz-Katz G, Heathers JAJ, et al.: The lesson of ivermectin: meta-analyses based on summary data alone are inherently unreliable. Nat Med. [Article]
  6. FDA Approved Drug Products: Sklice (ivermectin 0.5%) topical lotion (OTC) [Link]
  7. FDA Approved Drug Products: Soolantra (ivermectin 1%) topical cream [Link]
  8. FDA Approved Drug Products: Stromectol (Ivermectin) Oral Tablet [Link]
  9. Nature News: Flawed ivermectin preprint highlights challenges of COVID drug studies [Link]
  10. CDC Health Alert Network: Rapid Increase in Ivermectin Prescriptions and Reports of Severe Illness Associated with Use of Products Containing Ivermectin to Prevent or Treat COVID-19 [Link]
Human Metabolome Database
HMDB0014740
KEGG Drug
D00804
KEGG Compound
C07970
PubChem Compound
46936176
PubChem Substance
46506810
ChemSpider
7988461
RxNav
6069
ChEMBL
CHEMBL1200633
Therapeutic Targets Database
DAP000261
PharmGKB
PA450133
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Ivermectin
FDA label
Download (60.2 KB)
MSDS
Download (73.4 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedBasic ScienceLoiasis1
4CompletedTreatmentCoronavirus Disease 2019 (COVID‑19)2
4CompletedTreatmentEpilepsies1
4CompletedTreatmentEpilepsies / Ivermectin / Onchocerciasis1
4CompletedTreatmentHelminths Infection / Lymphatic Filariasis1
4CompletedTreatmentImpetigo / Scabies / Yaws1
4CompletedTreatmentLymphatic Filariasis1
4CompletedTreatmentRosacea2
4Not Yet RecruitingTreatmentCoronavirus Disease 2019 (COVID‑19)1
4Not Yet RecruitingTreatmentCoronavirus Disease 2019 (COVID‑19) / Ivermectin1

Pharmacoeconomics

Manufacturers
  • Merck and co inc
Packagers
  • Gallipot
  • Merck & Co.
Dosage Forms
FormRouteStrength
InjectionSubcutaneous
SolutionOral0.6 g
TabletOral3 mg
SolutionSubcutaneous
GranuleOral
CreamTopical10 MG/G
PasteOral
Tablet, chewableOral
Tablet, chewableOral
LiquidTopical
InjectionParenteral
SolutionOral
SuspensionOral6 mg
Injection, solutionSubcutaneous
SolutionOral0.006 g
CreamTopical10 mg/1g
PowderNot applicable1 kg/1kg
GelTopical
SolutionOral6 mg
PowderOral
Capsule, liquid filledOral3 mg
SolutionOral600 mg
SuspensionOral
SolutionTopical0.1 g
CreamTopical1 % w/w
TabletOral
LotionTopical0.585 g/117g
LotionTopical5 mg/1g
CreamTopical
CreamTopical1 g
TabletOral3 mg/1
TabletOral6 mg/1
SolutionTopical
TabletOral6 mg
Tablet, film coated6 mg
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
US11033565No2004-04-222024-04-22US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)155 °CNot Available
water solubilityInsolubleNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.00614 mg/mLALOGPS
logP4.37ALOGPS
logP5.83ChemAxon
logS-5.2ALOGPS
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
Polarizability95.55 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
Not Available

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
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. 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 . [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  5. FDA Approved Drug Products: Stromectol (Ivermectin) Oral Tablet [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Curator comments
Have shown involvement in the in vitro metabolism of ivermectin, but are likely minor contributors (if at all).
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
References
  1. FDA Approved Drug Products: Stromectol (Ivermectin) Oral Tablet [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Curator comments
Have shown involvement in the in vitro metabolism of ivermectin, but are likely minor contributors (if at all).
General Function
Steroid hydroxylase activity
Specific Function
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
Molecular Weight
56848.42 Da
References
  1. FDA Approved Drug Products: Stromectol (Ivermectin) Oral Tablet [Link]

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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]

Drug created on June 13, 2005 13:24 / Updated on October 20, 2021 19:48