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Details

Stereochemistry ABSOLUTE
Molecular Formula C12H20N4O6S
Molecular Weight 348.377
Optical Activity UNSPECIFIED
Defined Stereocenters 3 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of RELEBACTAM ANHYDROUS

SMILES

C1C[C@@]([H])(C(=NC2CCNCC2)O)N3C[C@]1([H])N(C3=O)OS(=O)(=O)O

InChI

InChIKey=SMOBCLHAZXOKDQ-ZJUUUORDSA-N
InChI=1S/C12H20N4O6S/c17-11(14-8-3-5-13-6-4-8)10-2-1-9-7-15(10)12(18)16(9)22-23(19,20)21/h8-10,13H,1-7H2,(H,14,17)(H,19,20,21)/t9-,10+/m1/s1

HIDE SMILES / InChI

Molecular Formula C12H20N4O6S
Molecular Weight 348.377
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Relebactum sodium (MK-7655) is a piperidine analog 3 that inhibits class A and C β-lactamases (in vitro). It is being investigated for use in treatment of infectious diseases, such as treatment of gram-negative bacterial infections. Its potential as an alternative to existing medicines in the treatment of drug-resistant bacterial infections is being studied. Clinical trials have been conducted and are still ongoing to evaluate the efficacy and safety of relebactum sodium in treatment of intra-abdominal infections, urinary tract infections (such as pyelonephritis), hospital-acquired and ventilator-associated bacterial pneumonias, and gram-negative bacterial infections.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: 1.6834582E7
Gene Symbol: blaKPC-2
210.0 nM [IC50]
Target ID: 878149.0
Gene Symbol: ampC
410.0 nM [IC50]
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
64 μM
250 mg 4 times / day multiple, intravenous
dose: 250 mg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered: IMIPENEM
RELEBACTAM ANHYDROUS plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
427.3 μM × h
250 mg 4 times / day multiple, intravenous
dose: 250 mg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered: IMIPENEM
RELEBACTAM ANHYDROUS plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
396 μM × h
1150 mg single, intravenous
dose: 1150 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
RELEBACTAM ANHYDROUS plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
7.97 μM × h
25 mg single, intravenous
dose: 25 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
RELEBACTAM ANHYDROUS plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
81.8 μM × h
250 mg single, intravenous
dose: 250 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
RELEBACTAM ANHYDROUS plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
1.2 h
250 mg 4 times / day multiple, intravenous
dose: 250 mg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered: IMIPENEM
RELEBACTAM ANHYDROUS plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
1.78 h
1150 mg single, intravenous
dose: 1150 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
RELEBACTAM ANHYDROUS plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1.39 h
25 mg single, intravenous
dose: 25 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
RELEBACTAM ANHYDROUS plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1.63 h
250 mg single, intravenous
dose: 250 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
RELEBACTAM ANHYDROUS plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
78%
250 mg 4 times / day multiple, intravenous
dose: 250 mg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered: IMIPENEM
RELEBACTAM ANHYDROUS plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
250 mg 4 times / day multiple, intravenous
Recommended
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, 24 to 42 years
n = 17
Health Status: healthy
Age Group: 24 to 42 years
Sex: M+F
Population Size: 17
Sources:
Disc. AE: Diarrhea, Nausea...
Other AEs: Fatigue, Blood creatinine increased...
AEs leading to
discontinuation/dose reduction:
Diarrhea (grade 1, 5.9%)
Nausea (grade 2, 5.9%)
Vomiting (grade 2, 5.9%)
Other AEs:
Fatigue (grade 1, 5.9%)
Blood creatinine increased (grade 1, 5.9%)
Sources:
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, mean age 49.7 years
n = 87
Health Status: unhealthy
Condition: Complicated Intra-Abdominal Infection
Age Group: mean age 49.7 years
Sex: M+F
Population Size: 87
Sources:
Disc. AE: Decreased creatinine clearance...
Other AEs: Diarrhea, Nausea...
AEs leading to
discontinuation/dose reduction:
Decreased creatinine clearance (1.1%)
Other AEs:
Diarrhea (>5)
Nausea (>5)
Vomiting (>5)
Sources:
250 mg 4 times / day multiple, intravenous
Recommended
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, mean age 56.4 years and 49.1 years
n = 216
Health Status: unhealthy
Condition: Complicated Urinary Tract Infection or Complicated Intra-Abdominal Infection
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
Population Size: 216
Sources:
Other AEs: Anemia, Diarrhea...
Other AEs:
Anemia (1%)
Diarrhea (6%)
Nausea (6%)
Vomiting (3%)
Infusion site phlebitis (2%)
Pyrexia (2%)
Alanine aminotransferase increased (3%)
Aspartate aminotransferase increased (3%)
Lipase increased (1%)
Blood creatinine increased (<1%)
Headache (4%)
Central nervous system disorder NOS (1%)
Hypertension (2%)
Sources:
625 mg 4 times / day multiple, intravenous
MTD
Dose: 625 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 625 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 27 years
n = 6
Other AEs: Upper abdominal pain, Diarrhea...
Other AEs:
Upper abdominal pain (grade 1-2, 16.7%)
Diarrhea (grade 1-2, 16.7%)
Infusion site erythema (grade 1-2, 50%)
Infusion site pain (grade 1-2, 50%)
Infusion site pruritus (grade 1-2, 16.7%)
Infusion site swelling (grade 1-2, 16.7%)
Dizziness (grade 1-2, 16.7%)
Headache (grade 1-2, 16.7%)
Sources:
1150 mg 1 times / day single, intravenous
MTD|Highest studied dose
Dose: 1150 mg, 1 times / day
Route: intravenous
Route: single
Dose: 1150 mg, 1 times / day
Sources:
healthy, median age 28.5 years
n = 6
Other AEs: Feeling of body temperature change...
500 mg 4 times / day multiple, intravenous
MTD
Dose: 500 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 500 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 53.3
n = 24
Other AEs: Diarrhea, ALT increased...
Other AEs:
Diarrhea (grade 1-2, 8.3%)
ALT increased (grade 1-2, 4.2%)
Discoloration tongue (grade 1-2, 33.3%)
Discoloration tooth (grade 1-2, 4.2%)
Asthenia (grade 1-2, 4.2%)
Feeling hot (grade 1-2, 4.2%)
Feeling of body temperature change (grade 1-2, 4.2%)
Infusion site erythema (grade 1-2, 37.5%)
Infusion site pain (grade 1-2, 25%)
Infusion site swelling (grade 1-2, 20.8%)
AST increased (grade 1-2, 4.2%)
Decreased appetite (grade 1-2, 4.2%)
Arthralgia (grade 1-2, 4.2%)
Muscle twitching (grade 1-2, 4.2%)
Myalgia (grade 1-2, 4.2%)
Headache (grade 1-2, 12.5%)
Rash (grade 1-2, 4.2%)
Sources:
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Other AEs: Thrombocytosis, Abdominal pain...
Other AEs:
Thrombocytosis (1%)
Abdominal pain (2%)
Diarrhoea (2%)
Nausea (6.1%)
Bacteriuria (2%)
ALT increased (1%)
AST increased (2%)
Bacterial test positive (1%)
Blood creatinine increased (1%)
White blood cells urine positive (1%)
Dysgeusia (2%)
Headache (3%)
Hypertension (2%)
Transaminases increased (1%)
Sources:
250 mg 4 times / day multiple, intravenous
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Disc. AE: Diarrhoea, Rash...
Other AEs: Thrombocytosis, Diarrhoea...
AEs leading to
discontinuation/dose reduction:
Diarrhoea (1%)
Rash (1%)
Other AEs:
Thrombocytosis (2%)
Diarrhoea (5.1%)
Nausea (4%)
Pyrexia (2%)
Bacteriuria (1%)
Influenza (2%)
ALT increased (2%)
AST increased (1%)
Bacterial test positive (1%)
Protein urine present (1%)
Red blood cells urine positive (1%)
White blood cells urine positive (1%)
Headache (7.1%)
Hypertension (3%)
Transaminases increased (1%)
Sources:
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 60 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 60 years
Sex: M+F
Population Size: 99
Sources:
Disc. AE: Nausea...
AEs leading to
discontinuation/dose reduction:
Nausea (1%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Blood creatinine increased grade 1, 5.9%
250 mg 4 times / day multiple, intravenous
Recommended
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, 24 to 42 years
n = 17
Health Status: healthy
Age Group: 24 to 42 years
Sex: M+F
Population Size: 17
Sources:
Fatigue grade 1, 5.9%
250 mg 4 times / day multiple, intravenous
Recommended
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, 24 to 42 years
n = 17
Health Status: healthy
Age Group: 24 to 42 years
Sex: M+F
Population Size: 17
Sources:
Diarrhea grade 1, 5.9%
Disc. AE
250 mg 4 times / day multiple, intravenous
Recommended
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, 24 to 42 years
n = 17
Health Status: healthy
Age Group: 24 to 42 years
Sex: M+F
Population Size: 17
Sources:
Nausea grade 2, 5.9%
Disc. AE
250 mg 4 times / day multiple, intravenous
Recommended
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, 24 to 42 years
n = 17
Health Status: healthy
Age Group: 24 to 42 years
Sex: M+F
Population Size: 17
Sources:
Vomiting grade 2, 5.9%
Disc. AE
250 mg 4 times / day multiple, intravenous
Recommended
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, 24 to 42 years
n = 17
Health Status: healthy
Age Group: 24 to 42 years
Sex: M+F
Population Size: 17
Sources:
Decreased creatinine clearance 1.1%
Disc. AE
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, mean age 49.7 years
n = 87
Health Status: unhealthy
Condition: Complicated Intra-Abdominal Infection
Age Group: mean age 49.7 years
Sex: M+F
Population Size: 87
Sources:
Diarrhea >5
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, mean age 49.7 years
n = 87
Health Status: unhealthy
Condition: Complicated Intra-Abdominal Infection
Age Group: mean age 49.7 years
Sex: M+F
Population Size: 87
Sources:
Nausea >5
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, mean age 49.7 years
n = 87
Health Status: unhealthy
Condition: Complicated Intra-Abdominal Infection
Age Group: mean age 49.7 years
Sex: M+F
Population Size: 87
Sources:
Vomiting >5
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, mean age 49.7 years
n = 87
Health Status: unhealthy
Condition: Complicated Intra-Abdominal Infection
Age Group: mean age 49.7 years
Sex: M+F
Population Size: 87
Sources:
Anemia 1%
250 mg 4 times / day multiple, intravenous
Recommended
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, mean age 56.4 years and 49.1 years
n = 216
Health Status: unhealthy
Condition: Complicated Urinary Tract Infection or Complicated Intra-Abdominal Infection
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
Population Size: 216
Sources:
Central nervous system disorder NOS 1%
250 mg 4 times / day multiple, intravenous
Recommended
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, mean age 56.4 years and 49.1 years
n = 216
Health Status: unhealthy
Condition: Complicated Urinary Tract Infection or Complicated Intra-Abdominal Infection
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
Population Size: 216
Sources:
Lipase increased 1%
250 mg 4 times / day multiple, intravenous
Recommended
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, mean age 56.4 years and 49.1 years
n = 216
Health Status: unhealthy
Condition: Complicated Urinary Tract Infection or Complicated Intra-Abdominal Infection
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
Population Size: 216
Sources:
Hypertension 2%
250 mg 4 times / day multiple, intravenous
Recommended
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, mean age 56.4 years and 49.1 years
n = 216
Health Status: unhealthy
Condition: Complicated Urinary Tract Infection or Complicated Intra-Abdominal Infection
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
Population Size: 216
Sources:
Infusion site phlebitis 2%
250 mg 4 times / day multiple, intravenous
Recommended
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, mean age 56.4 years and 49.1 years
n = 216
Health Status: unhealthy
Condition: Complicated Urinary Tract Infection or Complicated Intra-Abdominal Infection
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
Population Size: 216
Sources:
Pyrexia 2%
250 mg 4 times / day multiple, intravenous
Recommended
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, mean age 56.4 years and 49.1 years
n = 216
Health Status: unhealthy
Condition: Complicated Urinary Tract Infection or Complicated Intra-Abdominal Infection
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
Population Size: 216
Sources:
Alanine aminotransferase increased 3%
250 mg 4 times / day multiple, intravenous
Recommended
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, mean age 56.4 years and 49.1 years
n = 216
Health Status: unhealthy
Condition: Complicated Urinary Tract Infection or Complicated Intra-Abdominal Infection
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
Population Size: 216
Sources:
Aspartate aminotransferase increased 3%
250 mg 4 times / day multiple, intravenous
Recommended
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, mean age 56.4 years and 49.1 years
n = 216
Health Status: unhealthy
Condition: Complicated Urinary Tract Infection or Complicated Intra-Abdominal Infection
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
Population Size: 216
Sources:
Vomiting 3%
250 mg 4 times / day multiple, intravenous
Recommended
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, mean age 56.4 years and 49.1 years
n = 216
Health Status: unhealthy
Condition: Complicated Urinary Tract Infection or Complicated Intra-Abdominal Infection
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
Population Size: 216
Sources:
Headache 4%
250 mg 4 times / day multiple, intravenous
Recommended
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, mean age 56.4 years and 49.1 years
n = 216
Health Status: unhealthy
Condition: Complicated Urinary Tract Infection or Complicated Intra-Abdominal Infection
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
Population Size: 216
Sources:
Diarrhea 6%
250 mg 4 times / day multiple, intravenous
Recommended
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, mean age 56.4 years and 49.1 years
n = 216
Health Status: unhealthy
Condition: Complicated Urinary Tract Infection or Complicated Intra-Abdominal Infection
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
Population Size: 216
Sources:
Nausea 6%
250 mg 4 times / day multiple, intravenous
Recommended
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, mean age 56.4 years and 49.1 years
n = 216
Health Status: unhealthy
Condition: Complicated Urinary Tract Infection or Complicated Intra-Abdominal Infection
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
Population Size: 216
Sources:
Blood creatinine increased <1%
250 mg 4 times / day multiple, intravenous
Recommended
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, mean age 56.4 years and 49.1 years
n = 216
Health Status: unhealthy
Condition: Complicated Urinary Tract Infection or Complicated Intra-Abdominal Infection
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
Population Size: 216
Sources:
Diarrhea grade 1-2, 16.7%
625 mg 4 times / day multiple, intravenous
MTD
Dose: 625 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 625 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 27 years
n = 6
Dizziness grade 1-2, 16.7%
625 mg 4 times / day multiple, intravenous
MTD
Dose: 625 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 625 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 27 years
n = 6
Headache grade 1-2, 16.7%
625 mg 4 times / day multiple, intravenous
MTD
Dose: 625 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 625 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 27 years
n = 6
Infusion site pruritus grade 1-2, 16.7%
625 mg 4 times / day multiple, intravenous
MTD
Dose: 625 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 625 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 27 years
n = 6
Infusion site swelling grade 1-2, 16.7%
625 mg 4 times / day multiple, intravenous
MTD
Dose: 625 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 625 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 27 years
n = 6
Upper abdominal pain grade 1-2, 16.7%
625 mg 4 times / day multiple, intravenous
MTD
Dose: 625 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 625 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 27 years
n = 6
Infusion site erythema grade 1-2, 50%
625 mg 4 times / day multiple, intravenous
MTD
Dose: 625 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 625 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 27 years
n = 6
Infusion site pain grade 1-2, 50%
625 mg 4 times / day multiple, intravenous
MTD
Dose: 625 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 625 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 27 years
n = 6
Feeling of body temperature change grade 1-2, 16.7%
1150 mg 1 times / day single, intravenous
MTD|Highest studied dose
Dose: 1150 mg, 1 times / day
Route: intravenous
Route: single
Dose: 1150 mg, 1 times / day
Sources:
healthy, median age 28.5 years
n = 6
Headache grade 1-2, 12.5%
500 mg 4 times / day multiple, intravenous
MTD
Dose: 500 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 500 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 53.3
n = 24
Infusion site swelling grade 1-2, 20.8%
500 mg 4 times / day multiple, intravenous
MTD
Dose: 500 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 500 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 53.3
n = 24
Infusion site pain grade 1-2, 25%
500 mg 4 times / day multiple, intravenous
MTD
Dose: 500 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 500 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 53.3
n = 24
Discoloration tongue grade 1-2, 33.3%
500 mg 4 times / day multiple, intravenous
MTD
Dose: 500 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 500 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 53.3
n = 24
Infusion site erythema grade 1-2, 37.5%
500 mg 4 times / day multiple, intravenous
MTD
Dose: 500 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 500 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 53.3
n = 24
ALT increased grade 1-2, 4.2%
500 mg 4 times / day multiple, intravenous
MTD
Dose: 500 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 500 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 53.3
n = 24
AST increased grade 1-2, 4.2%
500 mg 4 times / day multiple, intravenous
MTD
Dose: 500 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 500 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 53.3
n = 24
Arthralgia grade 1-2, 4.2%
500 mg 4 times / day multiple, intravenous
MTD
Dose: 500 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 500 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 53.3
n = 24
Asthenia grade 1-2, 4.2%
500 mg 4 times / day multiple, intravenous
MTD
Dose: 500 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 500 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 53.3
n = 24
Decreased appetite grade 1-2, 4.2%
500 mg 4 times / day multiple, intravenous
MTD
Dose: 500 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 500 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 53.3
n = 24
Discoloration tooth grade 1-2, 4.2%
500 mg 4 times / day multiple, intravenous
MTD
Dose: 500 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 500 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 53.3
n = 24
Feeling hot grade 1-2, 4.2%
500 mg 4 times / day multiple, intravenous
MTD
Dose: 500 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 500 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 53.3
n = 24
Feeling of body temperature change grade 1-2, 4.2%
500 mg 4 times / day multiple, intravenous
MTD
Dose: 500 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 500 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 53.3
n = 24
Muscle twitching grade 1-2, 4.2%
500 mg 4 times / day multiple, intravenous
MTD
Dose: 500 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 500 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 53.3
n = 24
Myalgia grade 1-2, 4.2%
500 mg 4 times / day multiple, intravenous
MTD
Dose: 500 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 500 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 53.3
n = 24
Rash grade 1-2, 4.2%
500 mg 4 times / day multiple, intravenous
MTD
Dose: 500 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 500 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 53.3
n = 24
Diarrhea grade 1-2, 8.3%
500 mg 4 times / day multiple, intravenous
MTD
Dose: 500 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 500 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
healthy, median age 53.3
n = 24
ALT increased 1%
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Bacterial test positive 1%
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Blood creatinine increased 1%
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Thrombocytosis 1%
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Transaminases increased 1%
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
White blood cells urine positive 1%
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
AST increased 2%
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Abdominal pain 2%
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Bacteriuria 2%
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Diarrhoea 2%
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Dysgeusia 2%
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Hypertension 2%
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Headache 3%
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Nausea 6.1%
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
AST increased 1%
250 mg 4 times / day multiple, intravenous
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Bacterial test positive 1%
250 mg 4 times / day multiple, intravenous
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Bacteriuria 1%
250 mg 4 times / day multiple, intravenous
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Protein urine present 1%
250 mg 4 times / day multiple, intravenous
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Red blood cells urine positive 1%
250 mg 4 times / day multiple, intravenous
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Transaminases increased 1%
250 mg 4 times / day multiple, intravenous
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
White blood cells urine positive 1%
250 mg 4 times / day multiple, intravenous
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Diarrhoea 1%
Disc. AE
250 mg 4 times / day multiple, intravenous
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Rash 1%
Disc. AE
250 mg 4 times / day multiple, intravenous
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
ALT increased 2%
250 mg 4 times / day multiple, intravenous
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Influenza 2%
250 mg 4 times / day multiple, intravenous
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Pyrexia 2%
250 mg 4 times / day multiple, intravenous
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Thrombocytosis 2%
250 mg 4 times / day multiple, intravenous
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Hypertension 3%
250 mg 4 times / day multiple, intravenous
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Nausea 4%
250 mg 4 times / day multiple, intravenous
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Diarrhoea 5.1%
250 mg 4 times / day multiple, intravenous
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Headache 7.1%
250 mg 4 times / day multiple, intravenous
Dose: 250 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 250 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 58 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 58 years
Sex: M+F
Population Size: 99
Sources:
Nausea 1%
Disc. AE
125 mg 4 times / day multiple, intravenous
Dose: 125 mg, 4 times / day
Route: intravenous
Route: multiple
Dose: 125 mg, 4 times / day
Co-administed with::
imipenem(500 mg; IV; 4 per day)
cilastatin(500 mg; IV; 4 per day)
Sources:
unhealthy, median age 60 years
n = 99
Health Status: unhealthy
Condition: complicated urinary tract infections
Age Group: median age 60 years
Sex: M+F
Population Size: 99
Sources:
Overview

Overview

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 >300 uM]
no [IC50 >300 uM]
no [IC50 >300 uM]
no [IC50 >300 uM]
no [IC50 >300 uM]
no [IC50 >300 uM]
no [IC50 >300 uM]
no [IC50 >300 uM]
no [IC50 >300 uM]
no [IC50 >300 uM]
no
no
no
no
no
no
no
no
no
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
yes
yes
yes
yes
Tox targets
Substance Class Chemical
Created
by admin
on Sat Jun 26 03:17:23 UTC 2021
Edited
by admin
on Sat Jun 26 03:17:23 UTC 2021
Record UNII
1OQF7TT3PF
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
RELEBACTAM ANHYDROUS
Common Name English
RELEBACTAM [WHO-DD]
Common Name English
RELEBACTAM [INN]
Common Name English
MK-7655
Code English
(-)-RELEBACTAM ANHYDROUS
Common Name English
SULFURIC ACID MONO-((2S,5R)-7-OXO-2-(PIPERIDIN-4-YLCARBAMOYL)-1,6-DIAZA-BICYCLO(3.2.1)OCT-6-YL) ESTER
Systematic Name English
Classification Tree Code System Code
NCI_THESAURUS C258
Created by admin on Sat Jun 26 03:17:23 UTC 2021 , Edited by admin on Sat Jun 26 03:17:23 UTC 2021
Code System Code Type Description
INN
10027
Created by admin on Sat Jun 26 03:17:23 UTC 2021 , Edited by admin on Sat Jun 26 03:17:23 UTC 2021
PRIMARY
FDA UNII
1OQF7TT3PF
Created by admin on Sat Jun 26 03:17:23 UTC 2021 , Edited by admin on Sat Jun 26 03:17:23 UTC 2021
PRIMARY
EVMPD
SUB184909
Created by admin on Sat Jun 26 03:17:23 UTC 2021 , Edited by admin on Sat Jun 26 03:17:23 UTC 2021
PRIMARY
NCI_THESAURUS
C152175
Created by admin on Sat Jun 26 03:17:23 UTC 2021 , Edited by admin on Sat Jun 26 03:17:23 UTC 2021
PRIMARY
PUBCHEM
44129647
Created by admin on Sat Jun 26 03:17:23 UTC 2021 , Edited by admin on Sat Jun 26 03:17:23 UTC 2021
PRIMARY
CAS
1174018-99-5
Created by admin on Sat Jun 26 03:17:23 UTC 2021 , Edited by admin on Sat Jun 26 03:17:23 UTC 2021
PRIMARY
RXCUI
2268500
Created by admin on Sat Jun 26 03:17:23 UTC 2021 , Edited by admin on Sat Jun 26 03:17:23 UTC 2021
PRIMARY
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BINDER->LIGAND
The binding of Relebactam to human plasma proteins is approxi mately22% and is independent ofconcentration at a range of 5 to 50 ?M.
BINDING
TRANSPORTER -> SUBSTRATE
in vitro
TRANSPORTER -> SUBSTRATE
in vitro
EXCRETED UNCHANGED
In Study PN001, REL was 98.4% and 99.6% excreted in the urine as the parent drug in the two dosing groups that received a single dose of 250 mg.Similarly, in the multiple dose arm, the mean percentage of REL dose excreted unchanged in urine was 90.8% at 250 mg, 99.5% at 125 mg and 95.2% at 375 mg.These results indicate that Relebactam is cleared primarily (>90%) via urinary excretion of the parent drug in humans
URINE
SALT/SOLVATE -> PARENT
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ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC