Drug (ID: DG00173) and It's Reported Resistant Information
Name
Plazomicin
Synonyms
ACHN-490; UNII-LYO9XZ250J; 1154757-24-0; LYO9XZ250J; Plazomicin [USAN:INN]; Plazomicin (USAN); ZINC68150640; DB12615; D10151; D-Streptamine,
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Indication
In total 4 Indication(s)
Bronchitis [ICD-11: CA20]
Approved
[1], [2]
Prostate disease [ICD-11: GA91]
Approved
[1], [2]
Urinary tract infection [ICD-11: GC08]
Approved
[1], [2]
Pancreatic cancer [ICD-11: 2C10]
Phase 3
[1], [2]
Structure
Drug Resistance Disease(s)
Disease(s) with Clinically Reported Resistance for This Drug (2 diseases)
Bacterial infection [ICD-11: 1A00-1C4Z]
[1], [2]
Bacterial meningitis [ICD-11: 1D02]
[3]
Target Mitochondrial rRNA methyltransferase 2 (MRM2) MRM2_HUMAN [1]
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Formula
C25H48N6O10
IsoSMILES
C[C@@]1(CO[C@@H]([C@@H]([C@H]1NC)O)O[C@H]2[C@@H](C[C@@H]([C@H]([C@@H]2O)O[C@@H]3[C@@H](CC=C(O3)CNCCO)N)N)NC(=O)[C@H](CCN)O)O
InChI
1S/C25H48N6O10/c1-25(37)11-38-24(18(35)21(25)29-2)41-20-15(31-22(36)16(33)5-6-26)9-14(28)19(17(20)34)40-23-13(27)4-3-12(39-23)10-30-7-8-32/h3,13-21,23-24,29-30,32-35,37H,4-11,26-28H2,1-2H3,(H,31,36)/t13-,14+,15-,16+,17+,18-,19-,20+,21-,23-,24-,25+/m1/s1
InChIKey
IYDYFVUFSPQPPV-PEXOCOHZSA-N
PubChem CID
42613186
TTD Drug ID
D0E6BB
INTEDE ID
DR2136
DrugBank ID
DB12615
Type(s) of Resistant Mechanism of This Drug
  DISM: Drug Inactivation by Structure Modification
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-01: Infectious/parasitic diseases
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Bacterial infection [ICD-11: 1A00-1C4Z]
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Drug Resistance Data Categorized by Their Corresponding Mechanisms
       Drug Inactivation by Structure Modification (DISM) Click to Show/Hide
Key Molecule: Bifunctional AAC/APH (AAC/APH) [1], [2]
Molecule Alteration Expression
Up-regulation
Resistant Disease Bacterial infection [ICD-11: 1A00-1C4Z]
Experimental Note Identified from the Human Clinical Data
In Vitro Model Staphylococcus aureus ATCC 29213 1280
Staphylococcus aureus isolates 1280
Experiment for
Molecule Alteration
Whole genome sequence assay
Mechanism Description AAC(6')-APH(2") is an enzyme with 6'-N-acetyltransferase and 2"-O-phosphotransferase activities.The bifunctional AAC(6')-APH(2") has the capacity to inactivate virtually all clinically important aminoglycosides through N- and O-acetylation and phosphorylation of hydroxyl groups.
Bacterial meningitis [ICD-11: 1D02]
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Drug Resistance Data Categorized by Their Corresponding Mechanisms
       Drug Inactivation by Structure Modification (DISM) Click to Show/Hide
Key Molecule: Aminoglycoside phosphotransferase (APH) [3]
Molecule Alteration Expression
Inherence
Resistant Disease Enterococcus faecium meningitis [ICD-11: 1D01.2]
Experimental Note Identified from the Human Clinical Data
In Vitro Model Enterococcus faecium SF11770 1352
Escherichia coli kHE5-2a 562
Escherichia coli strain DH10b(pMW119) 316385
Experiment for
Molecule Alteration
PCR
Mechanism Description High-level gentamicin resistance (MIC >= 500 ug/ml) in enterococci is predominantly mediated by aac(6')-Ie-aph(2")-Ia, which encodes the bifunctional aminoglycoside-modifying enzyme AAC(6')-APH(2"). Found less commonly is aph(2")-Id, another gene recently reported to be associated with high-level gentamicin resistance in enterococci.
References
Ref 1 Prodigious substrate specificity of AAC(6')-APH(2"), an aminoglycoside antibiotic resistance determinant in enterococci and staphylococci. Chem Biol. 1999 Feb;6(2):99-110. doi: 10.1016/S1074-5521(99)80006-4.
Ref 2 The aacA-aphD gentamicin and kanamycin resistance determinant of Tn4001 from Staphylococcus aureus: expression and nucleotide sequence analysis. J Gen Microbiol. 1987 Nov;133(11):3039-52. doi: 10.1099/00221287-133-11-3039.
Ref 3 Detection of the high-level aminoglycoside resistance gene aph(2")-Ib in Enterococcus faecium. Antimicrob Agents Chemother. 2000 Oct;44(10):2876-9. doi: 10.1128/AAC.44.10.2876-2879.2000.

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