General
Preferred name
PLAZOMICIN
Synonyms
Zemdri ()
PLAZOMICIN SULFATE ()
ACHN-490 ()
Plazomicin hemipentasulfate ()
P&D ID
PD058519
CAS
1154757-24-0
Tags
natural product
drug
available
Approved by
FDA
First approval
2018
Drug Status
investigational
approved
Drug indication
Pancreatic cancer
Prostate disease
Bronchitis
Urinary tract infection
Max Phase
Phase 4
Structure
Probe scores
P&D probe-likeness score
[[ v.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)
Compound Sets
11
ChEMBL Approved 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
External IDs
28
Properties
(calculated by RDKit )
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
Custom attributes
(extracted from source data)
Biosynthetic Origin
Carbohydrate (Aminoglycoside)
Therapeutic Indication
Antibacterial
Therapeutic Class
Antimicrobial
Source data