U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
This repository is under review for potential modification in compliance with Administration directives.

Details

Stereochemistry ABSOLUTE
Molecular Formula C12H20N4O6S.H2O
Molecular Weight 366.391
Optical Activity UNSPECIFIED
Defined Stereocenters 3 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of RELEBACTAM

SMILES

O.OS(=O)(=O)ON1[C@H]2C[N@]([C@@H](CC2)C(=O)NC3CCNCC3)C1=O

InChI

InChIKey=TWFRCSHLWKJBQH-UXQCFNEQSA-N
InChI=1S/C12H20N4O6S.H2O/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);1H2/t9-,10+;/m1./s1

HIDE SMILES / InChI

Molecular Formula C12H20N4O6S
Molecular Weight 348.375
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Molecular Formula H2O
Molecular Weight 18.0153
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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
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
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
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
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
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
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
1.2 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
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
Sources:
healthy, 24 to 42 years
Health Status: healthy
Age Group: 24 to 42 years
Sex: M+F
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
Sources:
unhealthy, mean age 49.7 years
Health Status: unhealthy
Age Group: mean age 49.7 years
Sex: M+F
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
Sources:
unhealthy, mean age 56.4 years and 49.1 years
Health Status: unhealthy
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
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
Sources:
healthy, median age 27 years
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
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
Sources:
healthy, median age 53.3
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 60 years
Health Status: unhealthy
Age Group: median age 60 years
Sex: M+F
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
Sources:
healthy, 24 to 42 years
Health Status: healthy
Age Group: 24 to 42 years
Sex: M+F
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
Sources:
healthy, 24 to 42 years
Health Status: healthy
Age Group: 24 to 42 years
Sex: M+F
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
Sources:
healthy, 24 to 42 years
Health Status: healthy
Age Group: 24 to 42 years
Sex: M+F
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
Sources:
healthy, 24 to 42 years
Health Status: healthy
Age Group: 24 to 42 years
Sex: M+F
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
Sources:
healthy, 24 to 42 years
Health Status: healthy
Age Group: 24 to 42 years
Sex: M+F
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
Sources:
unhealthy, mean age 49.7 years
Health Status: unhealthy
Age Group: mean age 49.7 years
Sex: M+F
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
Sources:
unhealthy, mean age 49.7 years
Health Status: unhealthy
Age Group: mean age 49.7 years
Sex: M+F
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
Sources:
unhealthy, mean age 49.7 years
Health Status: unhealthy
Age Group: mean age 49.7 years
Sex: M+F
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
Sources:
unhealthy, mean age 49.7 years
Health Status: unhealthy
Age Group: mean age 49.7 years
Sex: M+F
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
Sources:
unhealthy, mean age 56.4 years and 49.1 years
Health Status: unhealthy
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
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
Sources:
unhealthy, mean age 56.4 years and 49.1 years
Health Status: unhealthy
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
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
Sources:
unhealthy, mean age 56.4 years and 49.1 years
Health Status: unhealthy
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
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
Sources:
unhealthy, mean age 56.4 years and 49.1 years
Health Status: unhealthy
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
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
Sources:
unhealthy, mean age 56.4 years and 49.1 years
Health Status: unhealthy
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
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
Sources:
unhealthy, mean age 56.4 years and 49.1 years
Health Status: unhealthy
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
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
Sources:
unhealthy, mean age 56.4 years and 49.1 years
Health Status: unhealthy
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
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
Sources:
unhealthy, mean age 56.4 years and 49.1 years
Health Status: unhealthy
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
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
Sources:
unhealthy, mean age 56.4 years and 49.1 years
Health Status: unhealthy
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
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
Sources:
unhealthy, mean age 56.4 years and 49.1 years
Health Status: unhealthy
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
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
Sources:
unhealthy, mean age 56.4 years and 49.1 years
Health Status: unhealthy
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
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
Sources:
unhealthy, mean age 56.4 years and 49.1 years
Health Status: unhealthy
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
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
Sources:
unhealthy, mean age 56.4 years and 49.1 years
Health Status: unhealthy
Age Group: mean age 56.4 years and 49.1 years
Sex: M+F
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
Sources:
healthy, median age 27 years
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
Sources:
healthy, median age 27 years
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
Sources:
healthy, median age 27 years
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
Sources:
healthy, median age 27 years
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
Sources:
healthy, median age 27 years
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
Sources:
healthy, median age 27 years
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
Sources:
healthy, median age 27 years
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
Sources:
healthy, median age 27 years
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
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
Sources:
healthy, median age 53.3
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
Sources:
healthy, median age 53.3
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
Sources:
healthy, median age 53.3
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
Sources:
healthy, median age 53.3
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
Sources:
healthy, median age 53.3
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
Sources:
healthy, median age 53.3
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
Sources:
healthy, median age 53.3
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
Sources:
healthy, median age 53.3
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
Sources:
healthy, median age 53.3
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
Sources:
healthy, median age 53.3
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
Sources:
healthy, median age 53.3
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
Sources:
healthy, median age 53.3
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
Sources:
healthy, median age 53.3
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
Sources:
healthy, median age 53.3
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
Sources:
healthy, median age 53.3
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
Sources:
healthy, median age 53.3
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
Sources:
healthy, median age 53.3
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 58 years
Health Status: unhealthy
Age Group: median age 58 years
Sex: M+F
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
Sources:
unhealthy, median age 60 years
Health Status: unhealthy
Age Group: median age 60 years
Sex: M+F
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 Mon Mar 31 23:30:14 GMT 2025
Edited
by admin
on Mon Mar 31 23:30:14 GMT 2025
Record UNII
Y1MYA2UHFL
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
RELEBACTAM
USAN  
USAN  
Official Name English
RELEBACTAM MONOHYDRATE
WHO-DD  
Preferred Name English
RELEBACTAM [ORANGE BOOK]
Common Name English
RECARBRIO COMPONENT RELEBACTAM MONOHYDRATE
Brand Name English
RELEBACTAM [USAN]
Common Name English
RELEBACTAM HYDRATE [JAN]
Common Name English
RECARBRIO COMPONENT RELEBACTAM
Brand Name English
(-)-RELEBACTAM MONOHYDRATE
Common Name English
SULFURIC ACID, MONO((1R,2S,5R)-7-OXO-2-((4-PIPERIDINYLAMINO)CARBONYL)-1,6-DIAZABICYCLO(3.2.1)OCT-6-YL) ESTER, HYDRATE (1:1)
Systematic Name English
Relebactam monohydrate [WHO-DD]
Common Name English
MK-7655A COMPONENT RELEBACTAM
Code English
MK-7655 MONOHYDRATE
Code English
Classification Tree Code System Code
NCI_THESAURUS C258
Created by admin on Mon Mar 31 23:30:14 GMT 2025 , Edited by admin on Mon Mar 31 23:30:14 GMT 2025
Code System Code Type Description
SMS_ID
100000179908
Created by admin on Mon Mar 31 23:30:14 GMT 2025 , Edited by admin on Mon Mar 31 23:30:14 GMT 2025
PRIMARY
EVMPD
SUB194532
Created by admin on Mon Mar 31 23:30:14 GMT 2025 , Edited by admin on Mon Mar 31 23:30:14 GMT 2025
PRIMARY
DRUG CENTRAL
5342
Created by admin on Mon Mar 31 23:30:14 GMT 2025 , Edited by admin on Mon Mar 31 23:30:14 GMT 2025
PRIMARY
RXCUI
2184137
Created by admin on Mon Mar 31 23:30:14 GMT 2025 , Edited by admin on Mon Mar 31 23:30:14 GMT 2025
PRIMARY
CAS
1174020-13-3
Created by admin on Mon Mar 31 23:30:14 GMT 2025 , Edited by admin on Mon Mar 31 23:30:14 GMT 2025
PRIMARY
USAN
BC-74
Created by admin on Mon Mar 31 23:30:14 GMT 2025 , Edited by admin on Mon Mar 31 23:30:14 GMT 2025
PRIMARY
RXCUI
2184136
Created by admin on Mon Mar 31 23:30:14 GMT 2025 , Edited by admin on Mon Mar 31 23:30:14 GMT 2025
ALTERNATIVE
DRUG BANK
DB12377
Created by admin on Mon Mar 31 23:30:14 GMT 2025 , Edited by admin on Mon Mar 31 23:30:14 GMT 2025
PRIMARY
FDA UNII
Y1MYA2UHFL
Created by admin on Mon Mar 31 23:30:14 GMT 2025 , Edited by admin on Mon Mar 31 23:30:14 GMT 2025
PRIMARY
PUBCHEM
76900350
Created by admin on Mon Mar 31 23:30:14 GMT 2025 , Edited by admin on Mon Mar 31 23:30:14 GMT 2025
PRIMARY
NCI_THESAURUS
C152176
Created by admin on Mon Mar 31 23:30:14 GMT 2025 , Edited by admin on Mon Mar 31 23:30:14 GMT 2025
PRIMARY
ChEMBL
CHEMBL3112741
Created by admin on Mon Mar 31 23:30:14 GMT 2025 , Edited by admin on Mon Mar 31 23:30:14 GMT 2025
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
ANHYDROUS->SOLVATE
Related Record Type Details
IMPURITY -> PARENT
Related Record Type Details
ACTIVE MOIETY