Ivermectin
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
Structure for Ivermectin (DB00602)
- Weight
- Average: 1736.1589
Monoisotopic: 1735.000064088 - Chemical Formula
- C95H146O28
- Synonyms
- Ivermectin
- Ivermectina
- Ivermectine
- Ivermectinum
- External IDs
- MK 933
Pharmacology
Accelerate your drug discovery research with the industry’s only fully connected ADMET dataset, ideal for:Accelerate your drug discovery research with our fully connected ADMET dataset- 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
Contraindications & Blackbox WarningsWith our commercial data, access important information on dangerous risks, contraindications, and adverse effects.Our Blackbox Warnings cover Risks, Contraindications, and Adverse Effects- 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.
Target Actions Organism AGlycine receptor subunit alpha-3 agonistHumans UGamma-aminobutyric acid receptor subunit beta-3 agonistHumans - 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
Reduce medical errorsand improve treatment outcomes with our comprehensive & structured data on drug adverse effects.Reduce medical errors & improve treatment outcomes with our adverse effects data- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Ivermectin can be increased when it is combined with Abametapir. Abemaciclib Abemaciclib may decrease the excretion rate of Ivermectin which could result in a higher serum level. Acenocoumarol Ivermectin may increase the anticoagulant activities of Acenocoumarol. Acipimox The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ivermectin is combined with Acipimox. Afatinib Afatinib may decrease the excretion rate of Ivermectin which could result in a higher serum level. Alectinib Alectinib may decrease the excretion rate of Ivermectin which could result in a higher serum level. Alendronic acid The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ivermectin is combined with Alendronic acid. Ambrisentan The excretion of Ambrisentan can be decreased when combined with Ivermectin. Amiodarone The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ivermectin is combined with Amiodarone. Amphotericin B The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ivermectin is combined with Amphotericin B. 
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- Take on an empty stomach.
Products
Comprehensive & structured drug product infoFrom application numbers to product codes, connect different identifiers through our commercial datasets.Easily connect various identifiers back to our datasets- 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
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Rosiver Cream Topical Galderma 2015-05-25 Not applicable Canada 
Sklice Lotion 5 mg/1g Topical Arbor Pharmaceuticals 2016-06-30 Not applicable US 
Sklice Lotion 0.585 g/117g Topical Sanofi Pasteur, Inc 2012-07-09 2017-07-31 US Soolantra Cream 10 mg/1g Topical Galderma Laboratories, L.P. 2015-01-01 Not applicable US Stromectol Tablet 6 mg/1 Oral Merck & Co., Inc. 2006-04-13 2006-04-13 US Stromectol Tablet 3 mg Oral Merck Ltd. 2018-11-06 Not applicable Canada Stromectol Tablet 3 mg/1 Oral Merck Sharp & Dohme Corp. 1996-11-22 Not applicable US 
Stromectol Tablet 3 mg/1 Oral Department Of State Health Services, Pharmacy Branch 1996-11-22 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ivermectin Tablet 3 mg/1 Oral Central Texas Community Health Centers 2014-11-15 Not applicable US Ivermectin Cream 10 mg/1g Topical Prasco Laboratories 2019-10-15 Not applicable US Ivermectin Tablet 3 mg/1 Oral Nucare Pharmaceuticals,inc. 2014-11-15 Not applicable US Ivermectin Tablet 3 mg/1 Oral Edenbridge Pharmaceuticals Llc 2014-11-15 Not applicable US 
Ivermectin Cream 10 mg/1g Topical Actavis Pharma, Inc. 2019-10-14 Not applicable US Ivermectin Tablet 3 mg/1 Oral bryant ranch prepack 2014-11-15 Not applicable US Ivermectin Lotion 5 mg/1g Topical Taro Pharmaceuticals U.S.A., Inc. 2020-05-06 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image 171083 Ivermectin 1% / Metronidazole 1% / Niacinamide 4% Ivermectin (1 g/100g) + Metronidazole (1 g/100g) + Nicotinamide (4 g/100g) Gel Topical Sincerus Florida, LLC 2020-07-02 Not applicable US 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) Gel Topical Sincerus Florida, LLC 2019-05-16 Not applicable US Ivermectin 1% / Metronidazole 1% Ivermectin (1 g/100g) + Metronidazole (1 g/100g) Gel Topical Sincerus Florida, LLC 2019-05-01 Not applicable US Ivermectin 1% / Metronidazole 1% / Niacinamide 4% Ivermectin (1 g/100g) + Metronidazole (1 g/100g) + Nicotinamide (4 g/100g) Gel Topical Sincerus Florida, LLC 2019-05-01 Not applicable US
Categories
- ATC Codes
- P02CF01 — Ivermectin
- P02CF — Avermectines
- P02C — ANTINEMATODAL AGENTS
- P02 — ANTHELMINTICS
- P — ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS
- Drug Categories
- Agents Causing Muscle Toxicity
- Agrochemicals
- Anthelmintics
- Anti-Infective Agents
- Antinematodal Agents
- Antiparasitic Agents
- Antiparasitic Products, Insecticides and Repellents
- Avermectines
- BCRP/ABCG2 Substrates
- Compounds used in a research, industrial, or household setting
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Dermatologicals
- Insecticides
- Lactones
- OATP1B1/SLCO1B1 Inhibitors
- OATP1B3 inhibitors
- P-glycoprotein inducers
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- Pediculicides
- Pesticides
- Polyketides
- Scabicides and Pediculicides
- Toxic Actions
- 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
- CO[C@H]1C[C@@H](O[C@@H](C)[C@@H]1O)O[C@H]1[C@H](C)O[C@H](C[C@@H]1OC)O[C@H]1[C@@H](C)\C=C\C=C2/CO[C@@H]3[C@H](O)C(C)=C[C@@H](C(=O)O[C@H]4C[C@@H](C\C=C1/C)O[C@@]1(CC[C@H](C)[C@@H](C(C)C)O1)C4)[C@]23O.CC[C@@H](C)[C@H]1O[C@@]2(CC[C@@H]1C)O[C@@H]1C\C=C(C)\[C@@H](O[C@@H]3O[C@@H](C)[C@H](O[C@@H]4O[C@@H](C)[C@H](O)[C@@H](OC)C4)[C@@H](OC)C3)[C@@H](C)\C=C\C=C3/CO[C@@H]4[C@H](O)C(C)=C[C@@H](C(=O)O[C@@H](C1)C2)[C@]34O
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
- External Links
- Human Metabolome Database
- HMDB0014740
- KEGG Drug
- D00804
- KEGG Compound
- C07970
- PubChem Compound
- 46936176
- PubChem Substance
- 46506810
- ChemSpider
- 30776735
- 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
Phase Status Purpose Conditions Count 4 Completed Basic Science Loiasis 1 4 Completed Treatment Acne Rosacea 2 4 Completed Treatment Coronavirus Disease 2019 (COVID‑19) 2 4 Completed Treatment Epilepsies 1 4 Completed Treatment Epilepsies / Ivermectin / Onchocerciasis 1 4 Completed Treatment Helminth Infection / Lymphatic Filariasis 1 4 Completed Treatment Impetigo / Scabies / Yaws 1 4 Completed Treatment Lymphatic Filariasis 1 4 Not Yet Recruiting Treatment Lymphatic Filariases / Trachoma 1 4 Recruiting Health Services Research Healthy Volunteers 1
Pharmacoeconomics
- Manufacturers
- Merck and co inc
- Packagers
- Gallipot
- Merck & Co.
- Dosage Forms
Form Route Strength Injection Subcutaneous Solution Subcutaneous Granule Oral Paste Oral Tablet, chewable Oral Tablet, chewable Oral Liquid Topical Injection Parenteral Suspension Oral Injection, solution Subcutaneous Solution Oral Cream Topical 10 mg/1g Powder Not applicable 1 kg/1kg Gel Topical Powder Oral Capsule, liquid filled Oral Tablet Oral Lotion Topical 0.585 g/117g Lotion Topical 5 mg/1g Cream Topical Tablet Oral 3 mg Tablet Oral 3 mg/1 Tablet Oral 6 mg/1 Solution Topical Tablet Oral 6 mg Tablet, film coated - Prices
Unit description Cost Unit Stromectol 20 3 mg tablet Box 116.13USD box Ivermectin powder 14.0USD g Stromectol 3 mg tablet 5.58USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8927595 No 2015-01-06 2027-10-12 US US8791153 No 2014-07-29 2027-10-12 US US6103248 No 2000-08-15 2018-05-22 US US9089587 No 2015-07-28 2034-03-13 US US8470788 No 2013-06-25 2024-04-22 US US9233118 No 2016-01-12 2034-03-13 US US9233117 No 2016-01-12 2034-03-13 US US7550440 No 2009-06-23 2024-04-22 US US8815816 No 2014-08-26 2024-04-22 US US8093219 No 2012-01-10 2024-04-22 US US8080530 No 2011-12-20 2024-04-22 US US6133310 No 2000-10-17 2019-04-26 US US5952372 No 1999-09-14 2018-09-18 US US8415311 No 2013-04-09 2024-04-22 US US9782425 No 2017-10-10 2034-03-13 US US10206939 No 2019-02-19 2034-03-13 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 155 °C Not Available water solubility Insoluble Not Available - Predicted Properties
Property Value Source logP 5.83 ChemAxon pKa (Strongest Acidic) 12.47 ChemAxon pKa (Strongest Basic) -3.4 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 13 ChemAxon Hydrogen Donor Count 3 ChemAxon Polar Surface Area 170.06 Å2 ChemAxon Rotatable Bond Count 15 ChemAxon Refractivity 230.33 m3·mol-1 ChemAxon Polarizability 96.87 Å3 ChemAxon Number of Rings 14 ChemAxon Bioavailability 0 ChemAxon Rule of Five No ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule Yes ChemAxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.8146 Blood Brain Barrier - 0.549 Caco-2 permeable - 0.8192 P-glycoprotein substrate Substrate 0.8771 P-glycoprotein inhibitor I Inhibitor 0.805 P-glycoprotein inhibitor II Inhibitor 0.8192 Renal organic cation transporter Non-inhibitor 0.7384 CYP450 2C9 substrate Non-substrate 0.8877 CYP450 2D6 substrate Non-substrate 0.886 CYP450 3A4 substrate Substrate 0.7714 CYP450 1A2 substrate Non-inhibitor 0.9129 CYP450 2C9 inhibitor Non-inhibitor 0.8366 CYP450 2D6 inhibitor Non-inhibitor 0.928 CYP450 2C19 inhibitor Non-inhibitor 0.8793 CYP450 3A4 inhibitor Non-inhibitor 0.7957 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8073 Ames test Non AMES toxic 0.8295 Carcinogenicity Non-carcinogens 0.9622 Biodegradation Not ready biodegradable 0.9759 Rat acute toxicity 3.5285 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9471 hERG inhibition (predictor II) Non-inhibitor 0.5536
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Targets
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- 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
- 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]
- 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]
- 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]
- 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
- 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]
- 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]
- 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
- 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
- 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]
- 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]
- 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]
- 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
- SubstrateInhibitorInducer
- 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
- 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]
- 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]
- 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]
- 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]
- 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]
- 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
- 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
- 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
- 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
- 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
- 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 13:24 / Updated on April 13, 2021 00:29