U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula 2C25H48N6O10.5H2O4S
Molecular Weight 1675.758
Optical Activity UNSPECIFIED
Defined Stereocenters 24 / 24
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PLAZOMICIN SULFATE

SMILES

OS(O)(=O)=O.OS(O)(=O)=O.OS(O)(=O)=O.OS(O)(=O)=O.OS(O)(=O)=O.CN[C@@H]1[C@@H](O)[C@@H](O[C@H]2[C@@H](C[C@H](N)[C@@H](O[C@H]3OC(CNCCO)=CC[C@H]3N)[C@@H]2O)NC(=O)[C@@H](O)CCN)OC[C@]1(C)O.CN[C@@H]4[C@@H](O)[C@@H](O[C@H]5[C@@H](C[C@H](N)[C@@H](O[C@H]6OC(CNCCO)=CC[C@H]6N)[C@@H]5O)NC(=O)[C@@H](O)CCN)OC[C@]4(C)O

InChI

InChIKey=GUXPJAIJDJSSGJ-CYJQXXSXSA-N
InChI=1S/2C25H48N6O10.5H2O4S/c2*1-25(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;5*1-5(2,3)4/h2*3,13-21,23-24,29-30,32-35,37H,4-11,26-28H2,1-2H3,(H,31,36);5*(H2,1,2,3,4)/t2*13-,14+,15-,16+,17+,18-,19-,20+,21-,23-,24-,25+;;;;;/m11...../s1

HIDE SMILES / InChI

Description

Plazomicin is a novel aminoglycoside antibiotic that binds to the bacterial 30S ribosomal subunit, thus inhibiting protein synthesis in a concentration-dependent manner. Plazomicin displays a broad spectrum of activity against aerobic gram-negative bacteria including extended-spectrum β-lactamase-producing Enterobacteriaceae, carbapenem-resistant Enterobacteriaceae, and organisms with aminoglycoside-modifying enzymes. Plazomicin resistance in Enterobacteriaceae is via modification of the ribosomal binding site due to expression of 16S rRNA methyltransferases. ZEMDRI (plazomicin) injection for intravenous use is indicated for the treatment of patients 18 years of age or older with Complicated Urinary Tract Infections (cUTI) including Pyelonephritis.

Originator

Approval Year

2018
436
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
Approved
8429
ZEMDRI

Approved Use

ZEMDRI is an aminoglycoside antibacterial indicated for the treatment of patients 18 years of age or older with Complicated Urinary Tract Infections (cUTI) including Pyelonephritis.

Launch Date

2018
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
73.7 μg/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303orig1s000lbl.pdf
15 mg/kg single, intravenous
dose: 15 mg/kg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
PLAZOMICIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
257 μg × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303orig1s000lbl.pdf
15 mg/kg single, intravenous
dose: 15 mg/kg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
PLAZOMICIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
3.5 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303orig1s000lbl.pdf
15 mg/kg single, intravenous
dose: 15 mg/kg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
PLAZOMICIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
80%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303orig1s000lbl.pdf
15 mg/kg single, intravenous
dose: 15 mg/kg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
PLAZOMICIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
15 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 15 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000ClinPharmR.pdf
https://pubmed.ncbi.nlm.nih.gov/32319833/
https://pubmed.ncbi.nlm.nih.gov/26419762/
healthy, 18 to 65 years
n = 15
Health Status: healthy
Age Group: 18 to 65 years
Population Size: 15
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000ClinPharmR.pdf
https://pubmed.ncbi.nlm.nih.gov/32319833/
https://pubmed.ncbi.nlm.nih.gov/26419762/
Other AEs: Hypotension...
Other AEs:
Hypotension (grade 1-2)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000ClinPharmR.pdf
https://pubmed.ncbi.nlm.nih.gov/32319833/
https://pubmed.ncbi.nlm.nih.gov/26419762/
20 mg/kg 1 times / day single, intravenous
Highest studied dose
Dose: 20 mg/kg, 1 times / day
Route: intravenous
Route: single
Dose: 20 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/30650259/
healthy, adult
n = 57
Health Status: healthy
Age Group: adult
Population Size: 57
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/30650259/
Other AEs: Abdominal pain, Nausea...
Other AEs:
Abdominal pain (1.7%)
Nausea (10.5%)
Dizziness (8.8%)
Headache (7%)
Hypoesthesia (17.5%)
Flushing (1.7%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/30650259/
15 mg/kg 1 times / day multiple, intravenous
Recommended
Dose: 15 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29378708/
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
unhealthy, mean age 39.5 years
n = 74
Health Status: unhealthy
Condition: Complicated Urinary Tract Infections
Age Group: mean age 39.5 years
Sex: M+F
Population Size: 74
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29378708/
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
Disc. AE: Vertigo, Dizziness...
AEs leading to
discontinuation/dose reduction:
Vertigo (1.3%)
Dizziness (2.7%)
Azotaemia (1.4%)
Hypotension (1.4%)
Type 2 diabetes mellitus (1.4%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29378708/
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
15 mg/kg 1 times / day multiple, intravenous
Recommended
Dose: 15 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29378708/
unhealthy, mean age 39.5 years
n = 74
Health Status: unhealthy
Condition: Complicated Urinary Tract Infections
Age Group: mean age 39.5 years
Sex: M+F
Population Size: 74
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29378708/
Other AEs: Ototoxicity, Tinnitus...
Other AEs:
Ototoxicity (2.2%)
Tinnitus (1.3%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29378708/
15 mg/kg 1 times / day multiple, intravenous
Recommended
Dose: 15 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30786187/
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
unhealthy, mean age 59.4 years
n = 303
Health Status: unhealthy
Condition: Complicated Urinary Tract Infections
Age Group: mean age 59.4 years
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30786187/
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
Disc. AE: Blood creatinine increased...
AEs leading to
discontinuation/dose reduction:
Blood creatinine increased (0.3%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30786187/
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
15 mg/kg 1 times / day multiple, intravenous
Recommended
Dose: 15 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
unhealthy, mean age 59.4 years
n = 303
Health Status: unhealthy
Condition: Complicated Urinary Tract Infections
Age Group: mean age 59.4 years
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
Disc. AE: Acute kidney injury, Chronic kidney disease...
AEs leading to
discontinuation/dose reduction:
Acute kidney injury (0.7%)
Chronic kidney disease (0.3%)
Metastatic neoplasm (0.3%)
Metastatic uterine cancer (0.3%)
Renal failure (0.3%)
Renal impairment (0.3%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
AEs

AEs

AESignificanceDosePopulation
Hypotension grade 1-2
15 mg/kg 1 times / day multiple, intravenous
MTD
Dose: 15 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000ClinPharmR.pdf
https://pubmed.ncbi.nlm.nih.gov/32319833/
https://pubmed.ncbi.nlm.nih.gov/26419762/
healthy, 18 to 65 years
n = 15
Health Status: healthy
Age Group: 18 to 65 years
Population Size: 15
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000ClinPharmR.pdf
https://pubmed.ncbi.nlm.nih.gov/32319833/
https://pubmed.ncbi.nlm.nih.gov/26419762/
Abdominal pain 1.7%
20 mg/kg 1 times / day single, intravenous
Highest studied dose
Dose: 20 mg/kg, 1 times / day
Route: intravenous
Route: single
Dose: 20 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/30650259/
healthy, adult
n = 57
Health Status: healthy
Age Group: adult
Population Size: 57
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/30650259/
Flushing 1.7%
20 mg/kg 1 times / day single, intravenous
Highest studied dose
Dose: 20 mg/kg, 1 times / day
Route: intravenous
Route: single
Dose: 20 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/30650259/
healthy, adult
n = 57
Health Status: healthy
Age Group: adult
Population Size: 57
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/30650259/
Nausea 10.5%
20 mg/kg 1 times / day single, intravenous
Highest studied dose
Dose: 20 mg/kg, 1 times / day
Route: intravenous
Route: single
Dose: 20 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/30650259/
healthy, adult
n = 57
Health Status: healthy
Age Group: adult
Population Size: 57
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/30650259/
Hypoesthesia 17.5%
20 mg/kg 1 times / day single, intravenous
Highest studied dose
Dose: 20 mg/kg, 1 times / day
Route: intravenous
Route: single
Dose: 20 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/30650259/
healthy, adult
n = 57
Health Status: healthy
Age Group: adult
Population Size: 57
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/30650259/
Headache 7%
20 mg/kg 1 times / day single, intravenous
Highest studied dose
Dose: 20 mg/kg, 1 times / day
Route: intravenous
Route: single
Dose: 20 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/30650259/
healthy, adult
n = 57
Health Status: healthy
Age Group: adult
Population Size: 57
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/30650259/
Dizziness 8.8%
20 mg/kg 1 times / day single, intravenous
Highest studied dose
Dose: 20 mg/kg, 1 times / day
Route: intravenous
Route: single
Dose: 20 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/30650259/
healthy, adult
n = 57
Health Status: healthy
Age Group: adult
Population Size: 57
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/30650259/
Vertigo 1.3%
Disc. AE
15 mg/kg 1 times / day multiple, intravenous
Recommended
Dose: 15 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29378708/
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
unhealthy, mean age 39.5 years
n = 74
Health Status: unhealthy
Condition: Complicated Urinary Tract Infections
Age Group: mean age 39.5 years
Sex: M+F
Population Size: 74
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29378708/
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
Azotaemia 1.4%
Disc. AE
15 mg/kg 1 times / day multiple, intravenous
Recommended
Dose: 15 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29378708/
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
unhealthy, mean age 39.5 years
n = 74
Health Status: unhealthy
Condition: Complicated Urinary Tract Infections
Age Group: mean age 39.5 years
Sex: M+F
Population Size: 74
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29378708/
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
Hypotension 1.4%
Disc. AE
15 mg/kg 1 times / day multiple, intravenous
Recommended
Dose: 15 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29378708/
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
unhealthy, mean age 39.5 years
n = 74
Health Status: unhealthy
Condition: Complicated Urinary Tract Infections
Age Group: mean age 39.5 years
Sex: M+F
Population Size: 74
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29378708/
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
Type 2 diabetes mellitus 1.4%
Disc. AE
15 mg/kg 1 times / day multiple, intravenous
Recommended
Dose: 15 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29378708/
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
unhealthy, mean age 39.5 years
n = 74
Health Status: unhealthy
Condition: Complicated Urinary Tract Infections
Age Group: mean age 39.5 years
Sex: M+F
Population Size: 74
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29378708/
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
Dizziness 2.7%
Disc. AE
15 mg/kg 1 times / day multiple, intravenous
Recommended
Dose: 15 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29378708/
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
unhealthy, mean age 39.5 years
n = 74
Health Status: unhealthy
Condition: Complicated Urinary Tract Infections
Age Group: mean age 39.5 years
Sex: M+F
Population Size: 74
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29378708/
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
Tinnitus 1.3%
15 mg/kg 1 times / day multiple, intravenous
Recommended
Dose: 15 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29378708/
unhealthy, mean age 39.5 years
n = 74
Health Status: unhealthy
Condition: Complicated Urinary Tract Infections
Age Group: mean age 39.5 years
Sex: M+F
Population Size: 74
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29378708/
Ototoxicity 2.2%
15 mg/kg 1 times / day multiple, intravenous
Recommended
Dose: 15 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29378708/
unhealthy, mean age 39.5 years
n = 74
Health Status: unhealthy
Condition: Complicated Urinary Tract Infections
Age Group: mean age 39.5 years
Sex: M+F
Population Size: 74
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/29378708/
Blood creatinine increased 0.3%
Disc. AE
15 mg/kg 1 times / day multiple, intravenous
Recommended
Dose: 15 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30786187/
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
unhealthy, mean age 59.4 years
n = 303
Health Status: unhealthy
Condition: Complicated Urinary Tract Infections
Age Group: mean age 59.4 years
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210303Orig1s000lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/30786187/
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
Chronic kidney disease 0.3%
Disc. AE
15 mg/kg 1 times / day multiple, intravenous
Recommended
Dose: 15 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
unhealthy, mean age 59.4 years
n = 303
Health Status: unhealthy
Condition: Complicated Urinary Tract Infections
Age Group: mean age 59.4 years
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
Metastatic neoplasm 0.3%
Disc. AE
15 mg/kg 1 times / day multiple, intravenous
Recommended
Dose: 15 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
unhealthy, mean age 59.4 years
n = 303
Health Status: unhealthy
Condition: Complicated Urinary Tract Infections
Age Group: mean age 59.4 years
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
Metastatic uterine cancer 0.3%
Disc. AE
15 mg/kg 1 times / day multiple, intravenous
Recommended
Dose: 15 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
unhealthy, mean age 59.4 years
n = 303
Health Status: unhealthy
Condition: Complicated Urinary Tract Infections
Age Group: mean age 59.4 years
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
Renal failure 0.3%
Disc. AE
15 mg/kg 1 times / day multiple, intravenous
Recommended
Dose: 15 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
unhealthy, mean age 59.4 years
n = 303
Health Status: unhealthy
Condition: Complicated Urinary Tract Infections
Age Group: mean age 59.4 years
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
Renal impairment 0.3%
Disc. AE
15 mg/kg 1 times / day multiple, intravenous
Recommended
Dose: 15 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
unhealthy, mean age 59.4 years
n = 303
Health Status: unhealthy
Condition: Complicated Urinary Tract Infections
Age Group: mean age 59.4 years
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
Acute kidney injury 0.7%
Disc. AE
15 mg/kg 1 times / day multiple, intravenous
Recommended
Dose: 15 mg/kg, 1 times / day
Route: intravenous
Route: multiple
Dose: 15 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
unhealthy, mean age 59.4 years
n = 303
Health Status: unhealthy
Condition: Complicated Urinary Tract Infections
Age Group: mean age 59.4 years
Sex: M+F
Population Size: 303
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inducer
781
inhibitor
1767

activator
22
inhibitor
1852

activator
23
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1524

CYP3A4/5
278

CYP2B6
810

CYP2C8
911

CYP2C19
1478

P-gp
1461

BCRP
699

MRP2
383

OATP1B1
788

OATP1B3
706

OAT1
599

OAT3
642

OCT1
512

OCT2
647

BSEP
402

MATE1
306

MATE2
263
P-gp
1537

BCRP
561
CYP1A2
701

CYP2B6
547
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
OCT2
648
 no [IC50 6111 uM]
CYP1A2
1692
 no [IC50 8712 uM]
CYP2C8
965
 no [IC50 8951 uM]
BCRP
773
 no
BSEP
403
 no
CYP1A2
1692
 no
CYP2B6
1001
 no
CYP2B6
1001
 no
CYP2C19
1553
 no
CYP2C9
1819
 no
CYP2D6
1891
 no
CYP3A4
1925
 no
CYP3A4/5
335
 no
MRP2
475
 no
OAT1
603
 no
OAT3
644
 no
OATP1B1
803
 no
OATP1B3
715
 no
OCT1
543
 no
P-gp
1650
 no
MATE1
308
 yes [IC50 1552 uM]
no (co-administration study)
Comment: IC50 value given as 1300 mcg/mL; mw of drug: 837.89; not an inhibitor in vivo when administered with metformin
Page: 16134.0
MATE2
263
 yes [IC50 403 uM]
no (co-administration study)
Comment: IC50 value given as 338 mcg/mL; mw of drug: 837.89; not an inhibitor in vivo when administered with metformin
Page: 16,96
CYP2B6
1001
 yes
CYP2C19
1553
 yes
CYP2C9
1819
 yes
CYP2D6
1891
 yes
CYP3A4/5
335
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
BCRP
561
 no
P-gp
1537
 no
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
001 Chemical
DY34492
BLD Pharm
BD01102776
http://www.bldpharm.com/products/1154757-24-0.html
Chemieliva Pharmaceutical Co., Ltd
PBCM1081458
Compound Cloud
42613186
Compound Cloud
71515458
Hangzhou Yuhao Chemical Technology
RT4859
Molcore
MC34492
MuseChem
R057829
https://www.musechem.com/product/R057829.html
Smolecule
S539863
http://www.smolecule.com/products/s539863
THE BioTek
bt-278804
https://www.thebiotek.com/product/inhibitors/bt-278804
Toronto Research Chemicals
P579505
Yuhao Chemical
RT4859
http://www.chemyuhao.com/1154757-24-0.html
ZINC
ZINC000068150640
http://zinc15.docking.org/substances/ZINC000068150640
eNovation Chemicals
D666958
https://www.enovationchem.com/ProductDetails.asp?ProductID=D666958
PubMed

PubMed

TitleDatePubMed
Synthesis and spectrum of the neoglycoside ACHN-490.
2010 Nov
Activity of a novel aminoglycoside, ACHN-490, against clinical isolates of Escherichia coli and Klebsiella pneumoniae from New York City.
2010 Oct
Plazomicin: A Novel Aminoglycoside for the Treatment of Resistant Gram-Negative Bacterial Infections.
2019 Feb
Plazomicin: A Next-Generation Aminoglycoside.
2019 Jan
Patents

Patents

US20170165374A1
2

Sample Use Guides

In Vivo Use Guide
Administer ZEMDRI 15 mg/kg every 24 hours by intravenous (IV) infusion over 30 minutes to patients 18 years of age or older with creatinine clearance greater than or equal to 90 mL/min.
Route of Administration: Intravenous
In Vitro Use Guide
MIC50/MIC90 values for plazomicin were the lowest of all the drugs tested: 0.5/0.5 mg/L for 96 KPC-producing Klebsiella pneumoniae isolates and 0.5/1 mg/L for all 110 carbapenemase-producing isolates. Plazomicin (ACHN-490) inhibited the growth of AG-resistant Enterobacteriaceae (MIC(90), ≤4 μg/ml), with the exception of Proteus mirabilis and indole-positive Proteae (MIC(90), 8 μg/ml and 16 μg/ml, respectively). ACHN-490 was more active alone in vitro against Pseudomonas aeruginosa and Acinetobacter baumannii isolates with AG-modifying enzymes than against those with altered permeability/efflux. The MIC(90) of ACHN-490 against AG-resistant staphylococci was 2 μg/ml.
Name Type Language
PLAZOMICIN SULFATE
USAN   WHO-DD  
USAN  
Official Name English
PLAZOMICIN HEMIPENTASULFATE
Common Name English
(2S)-4-AMINO-N-((1R,2S,3S,4R,5S)-5-AMINO-4-((2-AMINO-2,3,4,6-TETRADEOXY-6-((2-HYDROXYETHYL)AMINO)-.ALPHA.-D-GLYCERO-HEX-4-ENOPYRANOSYL(OXY)-2-((3-DEOXY-4-C-METHYL-3-(METHYLAMINO)-.BETA.-L-ARABINOPYRANOSYL)OXY(-3-HYDROXYCYCLOHEXYL)-2-HYDROXYBUTANAMIDE SUL
Common Name English
ZEMDRI
Brand Name English
PLAZOMICIN SULFATE [USAN]
Common Name English
PLAZOMICIN SULFATE [ORANGE BOOK]
Common Name English
ACHN-490 SULFATE
Code English
D-STREPTAMINE, O-2-AMINO-2,3,4,6-TETRADEOXY-6-((2-HYDROXYETHYL)AMINO)-.ALPHA.-D-GLYCERO-HEX-4-ENOPYRANOSYL-(1->4)-O-(3-DEOXY-4-C-METHYL-3-(METHYLAMINO)-.BETA.-L-ARABINOPYRANOSYL-(1->6))-N1-((2S)-4-AMINO-2-HYDROXY-1-OXOBUTYL)-2-DEOXY-, SULFATE
Common Name English
Plazomicin sulfate [WHO-DD]
Common Name English
PLAZOMICIN SULFATE [MI]
Common Name English
Code System Code Type Description
FDA UNII
A78L6MT746
Created by admin on Sat Dec 16 05:35:02 GMT 2023 , Edited by admin on Sat Dec 16 05:35:02 GMT 2023
PRIMARY
SMS_ID
100000178212
Created by admin on Sat Dec 16 05:35:02 GMT 2023 , Edited by admin on Sat Dec 16 05:35:02 GMT 2023
PRIMARY
MERCK INDEX
m12109
Created by admin on Sat Dec 16 05:35:02 GMT 2023 , Edited by admin on Sat Dec 16 05:35:02 GMT 2023
PRIMARY
NCI_THESAURUS
C174609
Created by admin on Sat Dec 16 05:35:02 GMT 2023 , Edited by admin on Sat Dec 16 05:35:02 GMT 2023
PRIMARY
RXCUI
2052872
Created by admin on Sat Dec 16 05:35:02 GMT 2023 , Edited by admin on Sat Dec 16 05:35:02 GMT 2023
PRIMARY
DRUG BANK
DBSALT002742
Created by admin on Sat Dec 16 05:35:02 GMT 2023 , Edited by admin on Sat Dec 16 05:35:02 GMT 2023
PRIMARY
USAN
AB-51
Created by admin on Sat Dec 16 05:35:02 GMT 2023 , Edited by admin on Sat Dec 16 05:35:02 GMT 2023
PRIMARY
ChEMBL
CHEMBL1650559
Created by admin on Sat Dec 16 05:35:02 GMT 2023 , Edited by admin on Sat Dec 16 05:35:02 GMT 2023
PRIMARY
PUBCHEM
137528219
Created by admin on Sat Dec 16 05:35:02 GMT 2023 , Edited by admin on Sat Dec 16 05:35:02 GMT 2023
PRIMARY
CAS
1380078-95-4
Created by admin on Sat Dec 16 05:35:02 GMT 2023 , Edited by admin on Sat Dec 16 05:35:02 GMT 2023
PRIMARY
EPA CompTox
DTXSID60160452
Created by admin on Sat Dec 16 05:35:02 GMT 2023 , Edited by admin on Sat Dec 16 05:35:02 GMT 2023
PRIMARY
ACTIVE MOIETY
Structure of PLAZOMICIN
SUBSTANCE RECORD
Structure of PLAZOMICIN SULFATE
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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