General
Preferred name
PLAZOMICIN
Synonyms
Zemdri ()
ACHN-490 ()
Plazomicine ()
Plazomicina ()
Plazomicin hemipentasulfate ()
PLAZOMICIN SULFATE ()
P&D ID
PD058519
CAS
1154757-24-0
Tags
drug
Approved by
FDA
First approval
2018
Drug indication
Bronchitis
Prostate disease
Pancreatic cancer
Urinary tract infection
Drug Status
approved
investigational
Max Phase
4.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
MOA
Plazomicin exerts a bactericidal action against susceptible bacteria by binding to bacterial 30S ribosomal subunit [A33942]. Aminoglycosides typically bind to the ribosomal aminoacyl-tRNA site (A-site) and induce a conformational change to further facilitate the binding between the rRNA and the antibiotic [A15783]. This leads to codon misreading and mistranslation of mRNA during bacterial protein synthesis [A15783]. ; ; Plazomicin demonstrates potency against _Enterobacteriaceae_, including species with multidrug-resistant phenotypes such as carbapenemase-producing bacteria and isolates with resistance to all other aminoglycosides [A33942, A33943, A33944]. Its antibacterial activity is not inhibited by aminoglycoside modifying enzymes (AMEs) produced by bacteria, such as acetyltransferases (AACs), phosphotransferases (APHs), and nucleotidyltransferases (ANTs) [A33945, FDA Label]. Plazomicin was shown to be effective against _Enterobacteriaceae_ in presence of some beta-lactamases [FDA Label]. In clinical settings and _in vivo_, bacteria shown to be susceptible toward plazomicin include _Escherichia_ _coli_, _Klebsiella pneumoniae_, _Proteus mirabilis_, and _Enterobacter cloacae_ [FDA Label]. Other aerobic bacteria that may be affected by plazomicin are _Citrobacter freundii_, _Citrobacter koseri_, _Enterobacter aerogenes_, _Klebsiella oxytoca_, _Morganella morganii_, _Proteus vulgaris_, _Providencia stuartii_, and _Serratia marcescens_ [FDA Label].
DESCRIPTION
Plazomicin is a semisynthetic derivative of and belongs to the aminoglycoside class of antibacterial compounds .
(GtoPdb)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
11
ChEMBL Approved Drugs
ChEMBL Drugs
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
Guide to Pharmacology
Natural product-based probes and drugs
NCATS Inxight Approved Drugs
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
28
Molecular Weight
592.34
Hydrogen Bond Acceptors
15
Hydrogen Bond Donors
11
Rotatable Bonds
13
Ring Count
3
Aromatic Ring Count
0
cLogP
-5.36
TPSA
269.29
Fraction CSP3
0.88
Chiral centers
12.0
Largest ring
6.0
QED
0.09
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Biosynthetic Origin
Carbohydrate (Aminoglycoside)
Therapeutic Indication
Antibacterial
Therapeutic Class
Antimicrobial
Source data
