Drug (ID: DG00573) and It's Reported Resistant Information
Name
Ivermectin
Synonyms
IVERMECTIN; Ivermectin B1a; 70288-86-7; Dihydroavermectin B1a; 22,23-Dihydroavermectin B1a; avermectin H2B1a; 71827-03-7; UNII-91Y2202OUW; 70161-11-4; Ivermectin Component B1a; CHEBI:63941; 91Y2202OUW; (2ae,4e,5's,6s,6'r,7s,8e,11r,13r,15s,17ar,20r,20ar,20bs)-6'-[(2s)-Butan-2-Yl]-20,20b-Dihydroxy-5',6,8,19-Tetramethyl-17-Oxo-3',4',5',6,6',10,11,14,15,17,17a,20,20a,20b-Tetradecahydro-2h,7h-Spiro[11,15-Methanofuro[4,3,2-Pq][2,6]benzodioxacyclooctadecine-13,2'-Pyran]-7-Yl 2,6-Dideoxy-4-O-(2,6-Dideoxy-3-O-Methyl-Alpha-L-Arabino-Hexopyranosyl)-3-O-Methyl-Alpha-L-Arabino-Hexopyranoside; 5-O-demethyl-22,23-dihydroavermectin A1a; MK-933; (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; C48H74O14 (B1a form); Ivermectin B1a-d2; C48H74O14; 22,23-Dihydroavermectin B(1)a; NCGC00163233-01; Ivermectin (IVM); IVM; EINECS 276-046-2; dihydro avermectin Bla; BRN 4643153; 22,23-Dihydro-5-O-demethylavermectin A1a; H2B1a; Prestwick3_000156; DSSTox_CID_3181; Ivermectin (MK-0933); DSSTox_RID_76909; DSSTox_GSID_23181; BSPBio_000292; SCHEMBL312795; BPBio1_000322; CHEMBL263291; DTXSID8023181; CHEBI:94551; HMS2089M09; HMS2095O14; HMS3712O14; WCA82703; Tox21_112034; BDBM50409816; MFCD00869511; s1351; AKOS027470116; ZINC238808778; ZINC252286706; AC-6014; CCG-220156; NCGC00186639-01; NCGC00186639-03; AS-14167; BI166167; CAS-71827-03-7; HY-126937; AB00513813; CS-0108408; J10179; 22,23-DIHYDROAVERMECTIN B1A; IVERMECTIN; AB00513813-02; AB00513813-03; AB00513813_04; Avermectin A1a, 22,23-dihydro-5-O-demethyl-; 288I867; Ivermectin, Antibiotic for Culture Media Use Only; Q-201262; BRD-K24652731-001-02-7; BRD-K85554912-001-08-9; Q27132923; Ivermectin, British Pharmacopoeia (BP) Reference Standard; Ivermectin, European Pharmacopoeia (EP) Reference Standard; UNII-8883YP2R6D component AZSNMRSAGSSBNP-XPNPUAGNSA-N; Ivermectin, United States Pharmacopeia (USP) Reference Standard; Ivermectin, Pharmaceutical Secondary Standard; Certified Reference Material; (2aE,4E,5'S,6S,6'R,7S,8E,11R,13R,15S,17aR,20R,20aR,20bS)-6'-[(2S)-butan-2-yl]-20,20b-dihydroxy-5',6,8,19-tetramethyl-17; 22,23-Dihydroavermectin B1; ; ; Heartgard 30; ; ; Ivomec; ; ; Ivosint; ; ; Mectizan; ; ; Stromectol; ; ; Uvemec; ; ; Vermic; ; ; Zimecterin; clooctadecine-13,2'-pyran]-7-yl 2,6-dideoxy-4-O-(2,6-dideoxy-3-O-methyl-alpha-L-arabino-hexopyranosyl)-3-O-methyl-alpha-L-arabino-hexopyranoside
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Indication
In total 1 Indication(s)
Intestinal strongyloidiasis due to nematode parasite [ICD-11: 1F6B]
Approved
[1]
Structure
Drug Resistance Disease(s)
Disease(s) with Clinically Reported Resistance for This Drug (3 diseases)
Onchocerciasis [ICD-11: 1F6A]
[2]
Pediculosis [ICD-11: 1G00]
[1]
Scabies [ICD-11: 1G04]
[3]
Target Onchocerca Glutamate-gated chloride channel (Onchoc GluCl) Q25634_ONCVO [3]
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Formula
C48H74O14
IsoSMILES
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
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
InChIKey
AZSNMRSAGSSBNP-XPNPUAGNSA-N
PubChem CID
6321424
ChEBI ID
CHEBI:63941
TTD Drug ID
D09YHJ
VARIDT ID
DR00147
INTEDE ID
DR0899
DrugBank ID
DB00602
Type(s) of Resistant Mechanism of This Drug
  DISM: Drug Inactivation by Structure Modification
  IDUE: Irregularity in Drug Uptake and Drug Efflux
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-01: Infectious/parasitic diseases
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Pediculosis [ICD-11: 1G00]
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Drug Resistance Data Categorized by Their Corresponding Mechanisms
       Drug Inactivation by Structure Modification (DISM) Click to Show/Hide
Key Molecule: Cytochrome P450 family 1 subfamily A member 1 (CYP1A1) [1]
Molecule Alteration Expression
Up-regulation
Resistant Disease Pediculosis [ICD-11: 1G00.0]
Experimental Note Identified from the Human Clinical Data
In Vitro Model Pediculus humanus 121225
Experiment for
Molecule Alteration
qRT-PCR
Experiment for
Drug Resistance
Disk diffusion assay
Mechanism Description Phylogenetic relatedness of P450 and ABC transporter genes over-transcribed following ivermectin exposure.Knockdown of CYP9AG2 P450 and ABCC4 transporter gene expression by RNA interference and subsequent increase in the sensitivity of lice to ivermectin.
       Irregularity in Drug Uptake and Drug Efflux (IDUE) Click to Show/Hide
Key Molecule: ATP-binding cassette sub-family C4 (ABCC4) [1]
Molecule Alteration Expression
Up-regulation
Resistant Disease Pediculosis [ICD-11: 1G00.0]
Experimental Note Identified from the Human Clinical Data
In Vitro Model Pediculus humanus 121225
Experiment for
Molecule Alteration
qRT-PCR
Experiment for
Drug Resistance
Disk diffusion assay
Mechanism Description Phylogenetic relatedness of P450 and ABC transporter genes over-transcribed following ivermectin exposure.Knockdown of CYP9AG2 P450 and ABCC4 transporter gene expression by RNA interference and subsequent increase in the sensitivity of lice to ivermectin.
Scabies [ICD-11: 1G04]
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Drug Resistance Data Categorized by Their Corresponding Mechanisms
       Drug Inactivation by Structure Modification (DISM) Click to Show/Hide
Key Molecule: Glutathione S-transferase kappa (GST) [3]
Molecule Alteration Expression
Up-regulation
Resistant Disease Scabies [ICD-11: 1G04.0]
Experimental Note Identified from the Human Clinical Data
In Vitro Model Sarcoptes scabiei isolates 52283
Mechanism Description The enzyme GST catalyzes the formation of a thioester bond between reduced glutathione and drugs. This bond tags the drug for elimination from the body. Increased activity or expression of GST has been linked to resistance to both permethrin and ivermectin in different mite species.
References
Ref 1 Ivermectin: From theory to clinical application .Int J Antimicrob Agents. 2019 Aug;54(2):134-142. doi: 10.1016/j.ijantimicag.2019.05.003. Epub 2019 May 7. 10.1016/j.ijantimicag.2019.05.003
Ref 2 Anti-Wolbachia drug discovery and development: safe macrofilaricides for onchocerciasis and lymphatic filariasis .Parasitology. 2014 Jan;141(1):119-27. doi: 10.1017/S0031182013001108. Epub 2013 Jul 18. 10.1017/S0031182013001108
Ref 3 Scabies in the age of increasing drug resistance .PLoS Negl Trop Dis. 2017 Nov 30;11(11):e0005920. doi: 10.1371/journal.pntd.0005920. eCollection 2017 Nov. 10.1371/journal.pntd.0005920

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