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

Details

Stereochemistry ABSOLUTE
Molecular Formula C25H48N6O10
Molecular Weight 592.6828
Optical Activity UNSPECIFIED
Defined Stereocenters 12 / 12
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PLAZOMICIN

SMILES

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

InChI

InChIKey=IYDYFVUFSPQPPV-PEXOCOHZSA-N
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

HIDE SMILES / InChI
Molecular Formula C25H48N6O10
Molecular Weight 592.6828
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 12 / 12
E/Z Centers 0
Optical Activity UNSPECIFIED

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
425
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8504
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
Approved
8583
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
Health Status: healthy
Age Group: 18 to 65 years
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
Health Status: healthy
Age Group: adult
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
Health Status: unhealthy
Age Group: mean age 39.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean age 39.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean age 59.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean age 59.4 years
Sex: M+F
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
Health Status: healthy
Age Group: 18 to 65 years
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
Health Status: healthy
Age Group: adult
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
Health Status: healthy
Age Group: adult
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
Health Status: healthy
Age Group: adult
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
Health Status: healthy
Age Group: adult
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
Health Status: healthy
Age Group: adult
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
Health Status: healthy
Age Group: adult
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
Health Status: unhealthy
Age Group: mean age 39.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean age 39.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean age 39.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean age 39.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean age 39.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean age 39.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean age 39.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean age 59.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean age 59.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean age 59.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean age 59.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean age 59.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean age 59.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean age 59.4 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210303Orig1s000MedR.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inducer
1087
inhibitor
2438

activator
23
inhibitor
2507

activator
25
inhibitor
2217

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
2153

CYP3A4/5
296

CYP2B6
926

CYP2C8
1057

CYP2C19
2057

P-gp
1741

BCRP
910

MRP2
499

OATP1B1
1079

OATP1B3
961

OAT1
725

OAT3
747

OCT1
620

OCT2
779

BSEP
550

MATE1
415

MATE2
267
P-gp
2052

BCRP
697
CYP1A2
832

CYP2B6
669
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
OCT2
782
 no [IC50 6111 uM]
CYP1A2
2333
 no [IC50 8712 uM]
CYP2C8
1117
 no [IC50 8951 uM]
BCRP
985
 no
BSEP
554
 no
CYP1A2
2333
 no
CYP2B6
1160
 no
CYP2B6
1160
 no
CYP2C19
2141
 no
CYP2C9
2497
 no
CYP2D6
2546
 no
CYP3A4
2633
 no
CYP3A4/5
357
 no
MRP2
625
 no
OAT1
730
 no
OAT3
749
 no
OATP1B1
1095
 no
OATP1B3
970
 no
OCT1
656
 no
P-gp
1932
 no
MATE1
416
 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
267
 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
1160
 yes
CYP2C19
2141
 yes
CYP2C9
2497
 yes
CYP2D6
2546
 yes
CYP3A4/5
357
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
BCRP
697
 no
P-gp
2052
 no
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
2263
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
eNovation Chemicals
D666958
https://www.enovationchem.com/ProductDetails.asp?ProductID=D666958
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
PubMed

PubMed

TitleDatePubMed
Plazomicin: A Novel Aminoglycoside for the Treatment of Resistant Gram-Negative Bacterial Infections.
2019-02
Plazomicin: A Next-Generation Aminoglycoside.
2019-01
Synthesis and spectrum of the neoglycoside ACHN-490.
2010-11
Activity of a novel aminoglycoside, ACHN-490, against clinical isolates of Escherichia coli and Klebsiella pneumoniae from New York City.
2010-10
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.
Substance Class Chemical
Created
by admin
on Mon Mar 31 20:57:30 GMT 2025
Edited
by admin
on Mon Mar 31 20:57:30 GMT 2025
Record UNII
LYO9XZ250J
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PLAZOMICIN
INN   USAN   WHO-DD  
USAN   INN  
Official Name English
ACHN-490
Preferred Name English
(2S)-4-AMINO-N-((1R,2S,3S,4R,5S)-5-AMINO-4-(((2S,3R)-3-AMINO-6-(((2-HYDROXYETHYL)AMINO)METHYL)-3,4-DIHYDRO-2H-PYRAN-2-YL)OXY)-2-((3-DEOXY-4-C-METHYL-3-(METHYLAMINO)-.BETA.-L-ARABINOPYRANOSYL)OXY)-3-HYDROXYCYCLOHEXYL)-2-HYDROXYBUTANAMIDE
Common Name English
Plazomicin [WHO-DD]
Common Name English
PLAZOMICIN [MI]
Common Name English
plazomicin [INN]
Common Name English
PLAZOMICIN [USAN]
Common Name English
Code System Code Type Description
EPA CompTox
DTXSID001031303
Created by admin on Mon Mar 31 20:57:30 GMT 2025 , Edited by admin on Mon Mar 31 20:57:30 GMT 2025
PRIMARY
FDA UNII
LYO9XZ250J
Created by admin on Mon Mar 31 20:57:30 GMT 2025 , Edited by admin on Mon Mar 31 20:57:30 GMT 2025
PRIMARY
DRUG CENTRAL
5287
Created by admin on Mon Mar 31 20:57:30 GMT 2025 , Edited by admin on Mon Mar 31 20:57:30 GMT 2025
PRIMARY
INN
9522
Created by admin on Mon Mar 31 20:57:30 GMT 2025 , Edited by admin on Mon Mar 31 20:57:30 GMT 2025
PRIMARY
SMS_ID
100000175065
Created by admin on Mon Mar 31 20:57:30 GMT 2025 , Edited by admin on Mon Mar 31 20:57:30 GMT 2025
PRIMARY
WIKIPEDIA
Plazomicin
Created by admin on Mon Mar 31 20:57:30 GMT 2025 , Edited by admin on Mon Mar 31 20:57:30 GMT 2025
PRIMARY
RXCUI
2049549
Created by admin on Mon Mar 31 20:57:30 GMT 2025 , Edited by admin on Mon Mar 31 20:57:30 GMT 2025
PRIMARY
DAILYMED
LYO9XZ250J
Created by admin on Mon Mar 31 20:57:30 GMT 2025 , Edited by admin on Mon Mar 31 20:57:30 GMT 2025
PRIMARY
USAN
YY-39
Created by admin on Mon Mar 31 20:57:30 GMT 2025 , Edited by admin on Mon Mar 31 20:57:30 GMT 2025
PRIMARY
CAS
1154757-24-0
Created by admin on Mon Mar 31 20:57:30 GMT 2025 , Edited by admin on Mon Mar 31 20:57:30 GMT 2025
PRIMARY
MERCK INDEX
m12109
Created by admin on Mon Mar 31 20:57:30 GMT 2025 , Edited by admin on Mon Mar 31 20:57:30 GMT 2025
PRIMARY
NCI_THESAURUS
C174680
Created by admin on Mon Mar 31 20:57:30 GMT 2025 , Edited by admin on Mon Mar 31 20:57:30 GMT 2025
PRIMARY
ChEMBL
CHEMBL1650559
Created by admin on Mon Mar 31 20:57:30 GMT 2025 , Edited by admin on Mon Mar 31 20:57:30 GMT 2025
PRIMARY
LACTMED
Plazomicin
Created by admin on Mon Mar 31 20:57:30 GMT 2025 , Edited by admin on Mon Mar 31 20:57:30 GMT 2025
PRIMARY
PUBCHEM
42613186
Created by admin on Mon Mar 31 20:57:30 GMT 2025 , Edited by admin on Mon Mar 31 20:57:30 GMT 2025
PRIMARY
DRUG BANK
DB12615
Created by admin on Mon Mar 31 20:57:30 GMT 2025 , Edited by admin on Mon Mar 31 20:57:30 GMT 2025
PRIMARY
Related Record Type Details
MATE-2
TRANSPORTER -> INHIBITOR
KLEBSIELLA PNEUMONIAE
TARGET ORGANISM->INHIBITOR
Structure of PLAZOMICIN
EXCRETED UNCHANGED
Following a single IV dose of 15 mg/kg radiolabeled plazomicin, approximately 97.5% of the dose was recovered in the urine as unchanged plazomicin.
URINE
MULTIDRUG AND TOXIN EXTRUSION PROTEIN 1
TRANSPORTER -> INHIBITOR
ESCHERICHIA COLI
TARGET ORGANISM->INHIBITOR
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
Related Record Type Details
Structure of N-nitroso-plazomicin-1
IMPURITY -> PARENT
Structure of N-nitroso-plazomicin-2
IMPURITY -> PARENT
Related Record Type Details
Structure of PLAZOMICIN
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
NIH
NCATS
PRIVACY NOTICE
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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