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| Other Sizes |
| Targets |
In invertebrates, the primary targets are glutamate-gated and gamma-aminobutyric acid (GABA)-gated chloride channels, leading to increased chloride ion conductance and subsequent paralysis in parasites. [2]
For its broad-spectrum antiviral activity, key targets include the inhibition of importin α/β-mediated nuclear transport, which affects the nuclear trafficking of viral proteins. Specific viral targets mentioned include the non-structural 3 helicase (NS3 helicase) of flaviviruses, the nuclear import of HIV-1 integrase and dengue virus NS5 polymerase, the nuclear import of UL42 protein of pseudorabies virus, and the nuclear localization signal-mediated import of the capsid protein (Cap) of porcine circovirus 2. [2] |
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| ln Vitro |
Ivermectin is comprised of a mixture of two homologous molecules, ivermectin B1a (not less than 80%) and ivermectin B1b (not more than 20%), and is a member of the macrocyclic lactone class of avermectins. At a dose of 0.3 μg/ml, the primary component of ivermectin, ivermectin B1a, is inert, while at the same quantity, ivermectin B1b, the lesser component, causes 100% snail mortality[1].
At a concentration of 0.3 μg/ml, Ivermectin B1a was found to be inactive against adult Biomphalaria glabrata snails, causing 0% mortality. This contrasts with the minor component Ivermectin B1b, which at the same concentration caused 100% snail mortality. [1] Ivermectin (the drug, of which Ivermectin B1a is a major component) has demonstrated broad-spectrum antiviral activity in vitro against numerous RNA and DNA viruses. [2] For SARS-CoV-2, a study cited within this literature reported that treating infected Vero-hSLAM cells with ivermectin resulted in an approximately 5000-fold reduction in viral RNA after 48 hours. [2] Against Newcastle disease virus, ivermectin showed strong antiviral activity at a concentration of 100 μg/ml but exhibited cytotoxicity in primary chick fibroblast cells. [2] Antiviral effects in vitro have also been reported against viruses such as Zika virus, influenza A virus, West Nile virus, Venezuelan equine encephalitis virus, porcine reproductive and respiratory syndrome virus, chikungunya virus, HIV-1, yellow fever virus, dengue virus, Japanese encephalitis virus, tick-borne encephalitis virus, pseudorabies virus, porcine circovirus 2, parvoviruses, and bovine herpesvirus 1. [2] |
| ln Vivo |
The in vivo antiviral potential of ivermectin has been reported against West Nile virus and Newcastle disease virus. [2]
However, ivermectin was ineffective in preventing lethal Zika virus infection in an Ifnar1-knockout mouse model. [2] In vivo activity has also been reported against pseudorabies virus and parvoviruses. [2] |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Absorbed well. High-fat meals can improve absorption. Ivermectin is metabolized in the liver, and almost all of it and its metabolites are excreted in the feces, expected to be completed within 12 days. Less than 1% of the administered dose is excreted in the urine. The volume of distribution is 3–3.5 L/kg, and it does not cross the blood-brain barrier. Metabolism/Metabolites Primarily metabolized in the liver. Ivermectin and its metabolites are almost entirely excreted in the feces, expected to be completed within 12 days. Less than 1% of the administered dose is excreted in the urine. Biological Half-Life The half-life of ivermectin after oral administration is approximately 18 hours. |
| Toxicity/Toxicokinetics |
Hepatotoxicity
A single dose of ivermectin was associated with a low incidence of elevated serum transaminases. One case of clinically significant liver injury following ivermectin use (Case 1) has been reported. This patient developed liver injury one month after a single dose, characterized by hepatocellular elevations of serum enzymes, but without jaundice. The patient recovered rapidly and completely. Elevated serum transaminases are not uncommon in trials of ivermectin for the prevention of SARS-CoV-2 infection and for improving the course of early and severe COVID-19, but their incidence was not significantly different between patients treated with ivermectin and those treated with placebo or control drugs. Probability Score: D (Possibly a rare cause of mild, clinically significant liver injury). Protein binding 93% In the molluscicidal activity test against Biomphalaria glabrata, ivermectin B1a at a concentration of 0.3 μg/ml showed no toxicity, and the mortality rate during the observation period was 0%. [1] |
| References | |
| Additional Infomation |
Pharmacodynamics
Ivermectin is a semi-synthetic anthelmintic. It belongs to the avermectin class, a class of pentacyclic sixteen-membered lactones (i.e., macrocyclic lactone disaccharides) derived from the soil bacterium Streptomyces avermitilis. Avermectin drugs are potent and broad-spectrum antiparasitic drugs. Ivermectin B1a is the main component (approximately 80%) of commercially available avermectin, an antiparasitic drug. [1] It is a 22,23-dihydro derivative of avermectin B1a. [1] In this study evaluating the snail-killing activity of avermectin against snails, intermediate hosts of schistosomiasis, avermectin B1a was found to be inactive, while the minor component avermectin B1b was identified as the bioactive component causing snail death. [1] Ivermectin B1a is a component of ivermectin, a member of the avermectin family of compounds produced by Streptomyces avermitilis. Ivermectin is a 22,23-dihydro derivative of avermectin B1. [2] It is a drug approved by the U.S. Food and Drug Administration (FDA) and widely used for anthelmintic and antiparasitic treatment in humans and animals. [2] Its broad-spectrum antiviral activity is primarily attributed to its ability to inhibit nuclear transport mediated by nuclear import proteins α/β, thereby blocking the nuclear import of viral proteins essential for viral replication. [2] It has been proposed for the treatment of COVID-19, possibly in combination with hydroxychloroquine, but its clinical efficacy and safety for this indication need to be validated through randomized controlled trials. [2] Due to challenges in formulation, such as high cytotoxicity and low solubility, research has begun on delivery systems such as liposomes to improve their properties. [2] |
| Molecular Formula |
C48H74O14
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|---|---|
| Molecular Weight |
875.09
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| Exact Mass |
874.508
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| CAS # |
71827-03-7
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| PubChem CID |
6321424
|
| Appearance |
White to light yellow solid powder
|
| LogP |
5.601
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
14
|
| Rotatable Bond Count |
8
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| Heavy Atom Count |
62
|
| Complexity |
1680
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| Defined Atom Stereocenter Count |
20
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| SMILES |
CC[C@H](C)[C@@H]1[C@H](CC[C@@]2(O1)C[C@@H]3C[C@H](O2)C/C=C(/[C@H]([C@H](/C=C/C=C/4\CO[C@H]5[C@@]4([C@@H](C=C([C@H]5O)C)C(=O)O3)O)C)O[C@H]6C[C@@H]([C@H]([C@@H](O6)C)O[C@H]7C[C@@H]([C@H]([C@@H](O7)C)O)OC)OC)\C)C
|
| InChi Key |
AZSNMRSAGSSBNP-XPNPUAGNSA-N
|
| InChi Code |
InChI=1S/C48H74O14/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/h12-15,19,25-26,28,30-31,33-45,49-50,52H,11,16-18,20-24H2,1-10H3/b13-12+,27-15+,32-14+/t25-,26-,28-,30-,31-,33+,34-,35-,36-,37-,38-,39-,40+,41-,42-,43+,44-,45+,47+,48+/m0/s1
|
| Chemical Name |
(1R,4S,5'S,6R,6'R,8R,10E,12S,13S,14E,16E,20R,21R,24S)-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-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 100 mg/mL (114.27 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.86 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1427 mL | 5.7137 mL | 11.4274 mL | |
| 5 mM | 0.2285 mL | 1.1427 mL | 2.2855 mL | |
| 10 mM | 0.1143 mL | 0.5714 mL | 1.1427 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Insecticide Resistance Management in Burkina Faso and Côte D'Ivoire
CTID: NCT03074435
Phase: Phase 3 Status: Completed
Date: 2024-10-01
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
