Drug Information

Drug (ID: DG00442) and It's Reported Resistant Information

• Name: Tilmicosin
• Synonyms: Tilmicosin; 108050-54-0; Micotil 300; UNII-XL4103X2E3; EL-870; EL870; XL4103X2E3; Ly177370; LY-177370; Tilmicosina; Tilmicosine; Tilmicosinum; Tilmicosine [INN-French]; Tilmicosinum [INN-Latin]; Tilmicosina [INN-Spanish]; C46H80N2O13; HSDB 7446; NSC-759584; Tilmicosin [USAN:USP:INN:BAN]; NCGC00096003-01; (4R,5S,6S,7R,9R,11E,13E,15R,16R)-6-[(2R,3R,4S,5S,6R)-4-(dimethylamino)-3,5-dihydroxy-6-methyloxan-2-yl]oxy-7-[2-[(3S,5R)-3,5-dimethylpiperidin-1-yl]ethyl]-16-ethyl-4-hydroxy-15-[[(2R,3R,4R,5R,6R)-5-hy; droxy-3,4-dimethoxy-6-methyloxan-2-yl]oxymethyl]-5,9,13-trimethyl-1-oxacyclohexadeca-11,13-diene-2,10-dione; LY-177370;EL-870; Micotil (TN); Tilmicosin (USP/INN); DSSTox_CID_26011; DSSTox_RID_81287; DSSTox_GSID_46011; 4(sup A)-O-de(2,6-Dideoxy-3-C-methyl-alpha-L-ribo-hexopyranosyl)-20-deoxo-20-(cis-3,5-dimethylpiperidino)tylosin; SCHEMBL149192; CHEMBL1908333; DTXSID5046011; ACT06683; HY-B0905; Tox21_111546; s4122; ZINC238809114; ZINC245204941; CCG-270545; DB11471; NSC 759584; NCGC00348375-01; NCGC00348375-02; Tilmicosin 100 microg/mL in Acetonitrile; Tylosin, 4(sup A)-O-de(2,6-dideoxy-3-C-methyl-alpha-L-ribo-hexopyranosyl)-20-deoxo-20-(3,5-dimethyl-1-piperidinyl)-, 20(cis)-; Tylosin, 4A-O-de(2,6-dideoxy-3-C-methyl-alpha-L-ribo-hexopyranosyl)-20-deoxo-20-(3,5-dimethyl-1-piperidinyl)-; CAS-108050-54-0; D02492; AB01566912_01; 050T540; Q722387; Tilmicosine, Antibiotic for Culture Media Use Only; Q-100992; 20-Deoxo-20-(3,5-dimethyl-1-piperidinyl)desmycosin; Tylosin, 4A-O-de(2,6-dideoxy-3-C-methyl-alpha-L-ribo-hexopyranosyl)-20-deoxo-20-((3R,5S)-3,5-dimethyl-1-piperidinyl)-
• Drug Resistance Disease(s):
  Disease(s) with Resistance Information Validated by in-vivo Model for This Drug (1 diseases)
  Pasteurellosis [ICD-11: 1B99]; [1]
• Formula: C46H80N2O13
• IsoSMILES: CC[C@@H]1[C@H](/C=C(/C=C/C(=O)[C@@H](C[C@@H]([C@@H]([C@H]([C@@H](CC(=O)O1)O)C)O[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)C)O)N(C)C)O)CCN3C[C@@H](C[C@@H](C3)C)C)C)\\C)CO[C@H]4[C@@H]([C@@H]([C@@H]([C@H](O4)C)O)OC)OC
• InChI: 1S/C46H80N2O13/c1-13-36-33(24-57-46-44(56-12)43(55-11)40(53)31(8)59-46)19-25(2)14-15-34(49)28(5)20-32(16-17-48-22-26(3)18-27(4)23-48)42(29(6)35(50)21-37(51)60-36)61-45-41(54)38(47(9)10)39(52)30(7)58-45/h14-15,19,26-33,35-36,38-46,50,52-54H,13,16-18,20-24H2,1-12H3/b15-14+,25-19+/t26-,27+,28-,29+,30-,31-,32+,33-,35-,36-,38+,39-,40-,41-,42-,43-,44-,45+,46-/m1/s1
• InChIKey: JTSDBFGMPLKDCD-XVFHVFLVSA-N
• PubChem CID: 5282521
• DrugBank ID: DB11471

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

Pasteurellosis [ICD-11: 1B99]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Drug Inactivation by Structure Modification (DISM)

Key Molecule: Erm methyltransferase (ERM42) [1]

• Molecule Alteration: Expression; Inherence
• Resistant Disease: Pasteurella multocida infection [ICD-11: 1B99.0]
• Experimental Note: Discovered Using In-vivo Testing Model
• In Vitro Model: Escherichia coli ATCC 25922; 1322345
• In Vitro Model: Staphylococcus aureus ATCC 29213; 1280
• In Vitro Model: Pasteurella multocida 36950; 1075089
• Experiment for Molecule Alteration: Whole genome sequence assay; Allelic frequency measurement assay
• Experiment for Drug Resistance: Broth microdilution method assay
• Mechanism Description: The analysis of one representative P. multocida isolate identified an 82 kb integrative and conjugative element (ICE) integrated into the chromosomal DNA. This ICE, designated ICEPmu1, harboured 11 resistance genes, which confer resistance to streptomycin/spectinomycin (aadA25), streptomycin (strA and strB), gentamicin (aadB), kanamycin/neomycin (aphA1), tetracycline [tetR-tet(H)], chloramphenicol/florfenicol (floR), sulphonamides (sul2), tilmicosin/clindamycin [erm(42)] or tilmicosin/tulathromycin [msr(E)-mph(E)].

Irregularity in Drug Uptake and Drug Efflux (IDUE)

Key Molecule: ABC transporter (ABCT) [1]

• Molecule Alteration: Expression; Inherence
• Resistant Disease: Pasteurella multocida infection [ICD-11: 1B99.0]
• Experimental Note: Discovered Using In-vivo Testing Model
• In Vitro Model: Escherichia coli ATCC 25922; 1322345
• In Vitro Model: Staphylococcus aureus ATCC 29213; 1280
• In Vitro Model: Pasteurella multocida 36950; 1075089
• Experiment for Molecule Alteration: Whole genome sequence assay; Allelic frequency measurement assay
• Experiment for Drug Resistance: Broth microdilution method assay
• Mechanism Description: The analysis of one representative P. multocida isolate identified an 82 kb integrative and conjugative element (ICE) integrated into the chromosomal DNA. This ICE, designated ICEPmu1, harboured 11 resistance genes, which confer resistance to streptomycin/spectinomycin (aadA25), streptomycin (strA and strB), gentamicin (aadB), kanamycin/neomycin (aphA1), tetracycline [tetR-tet(H)], chloramphenicol/florfenicol (floR), sulphonamides (sul2), tilmicosin/clindamycin [erm(42)] or tilmicosin/tulathromycin [msr(E)-mph(E)].

References

• Ref 1: ICEPmu1, an integrative conjugative element (ICE) of Pasteurella multocida: analysis of the regions that comprise 12 antimicrobial resistance genes. J Antimicrob Chemother. 2012 Jan;67(1):84-90. doi: 10.1093/jac/dkr406. Epub 2011 Oct 14.