Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C12H20N4O6S |
Molecular Weight | 348.375 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 3 / 3 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
OS(=O)(=O)ON1[C@H]2C[N@]([C@@H](CC2)C(=O)NC3CCNCC3)C1=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
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 |
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
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: 1.6834582E7 Gene Symbol: blaKPC-2 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26498989 |
210.0 nM [IC50] | ||
Target ID: 878149.0 Gene Symbol: ampC Sources: https://www.ncbi.nlm.nih.gov/pubmed/26498989 |
410.0 nM [IC50] |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29914955/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29914955/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29914955/ |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29914955/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29914955/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29914955/ |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Dose | Population | Adverse 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) Sources: cilastatin(500 mg; IV; 4 per day) |
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%) Other AEs:Nausea (grade 2, 5.9%) Vomiting (grade 2, 5.9%) Fatigue (grade 1, 5.9%) Sources: Blood creatinine increased (grade 1, 5.9%) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: Nausea (>5) Vomiting (>5) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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%) Sources: 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%) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 27 years n = 6 Health Status: healthy Age Group: median age 27 years Sex: M Population Size: 6 Sources: |
Other AEs: Upper abdominal pain, Diarrhea... Other AEs: Upper abdominal pain (grade 1-2, 16.7%) Sources: 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%) |
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 Health Status: healthy Age Group: median age 28.5 years Sex: M Population Size: 6 Sources: |
Other AEs: Feeling of body temperature change... Other AEs: Feeling of body temperature change (grade 1-2, 16.7%) Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 53.3 n = 24 Health Status: healthy Age Group: median age 53.3 Sex: M Population Size: 24 Sources: |
Other AEs: Diarrhea, ALT increased... Other AEs: Diarrhea (grade 1-2, 8.3%) Sources: 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%) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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%) Sources: 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%) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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%) Other AEs:Rash (1%) Thrombocytosis (2%) Sources: 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%) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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
AE | Significance | Dose | Population |
---|---|---|---|
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 27 years n = 6 Health Status: healthy Age Group: median age 27 years Sex: M Population Size: 6 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 27 years n = 6 Health Status: healthy Age Group: median age 27 years Sex: M Population Size: 6 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 27 years n = 6 Health Status: healthy Age Group: median age 27 years Sex: M Population Size: 6 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 27 years n = 6 Health Status: healthy Age Group: median age 27 years Sex: M Population Size: 6 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 27 years n = 6 Health Status: healthy Age Group: median age 27 years Sex: M Population Size: 6 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 27 years n = 6 Health Status: healthy Age Group: median age 27 years Sex: M Population Size: 6 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 27 years n = 6 Health Status: healthy Age Group: median age 27 years Sex: M Population Size: 6 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 27 years n = 6 Health Status: healthy Age Group: median age 27 years Sex: M Population Size: 6 Sources: |
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 Health Status: healthy Age Group: median age 28.5 years Sex: M Population Size: 6 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 53.3 n = 24 Health Status: healthy Age Group: median age 53.3 Sex: M Population Size: 24 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 53.3 n = 24 Health Status: healthy Age Group: median age 53.3 Sex: M Population Size: 24 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 53.3 n = 24 Health Status: healthy Age Group: median age 53.3 Sex: M Population Size: 24 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 53.3 n = 24 Health Status: healthy Age Group: median age 53.3 Sex: M Population Size: 24 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 53.3 n = 24 Health Status: healthy Age Group: median age 53.3 Sex: M Population Size: 24 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 53.3 n = 24 Health Status: healthy Age Group: median age 53.3 Sex: M Population Size: 24 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 53.3 n = 24 Health Status: healthy Age Group: median age 53.3 Sex: M Population Size: 24 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 53.3 n = 24 Health Status: healthy Age Group: median age 53.3 Sex: M Population Size: 24 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 53.3 n = 24 Health Status: healthy Age Group: median age 53.3 Sex: M Population Size: 24 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 53.3 n = 24 Health Status: healthy Age Group: median age 53.3 Sex: M Population Size: 24 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 53.3 n = 24 Health Status: healthy Age Group: median age 53.3 Sex: M Population Size: 24 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 53.3 n = 24 Health Status: healthy Age Group: median age 53.3 Sex: M Population Size: 24 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 53.3 n = 24 Health Status: healthy Age Group: median age 53.3 Sex: M Population Size: 24 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 53.3 n = 24 Health Status: healthy Age Group: median age 53.3 Sex: M Population Size: 24 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 53.3 n = 24 Health Status: healthy Age Group: median age 53.3 Sex: M Population Size: 24 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 53.3 n = 24 Health Status: healthy Age Group: median age 53.3 Sex: M Population Size: 24 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
healthy, median age 53.3 n = 24 Health Status: healthy Age Group: median age 53.3 Sex: M Population Size: 24 Sources: |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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) Sources: cilastatin(500 mg; IV; 4 per day) |
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
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical 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
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
yes | ||||
yes | ||||
yes | ||||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 19:09:03 GMT 2023
by
admin
on
Sat Dec 16 19:09:03 GMT 2023
|
Record UNII |
1OQF7TT3PF
|
Record Status |
Validated (UNII)
|
Record Version |
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-
Download
Name | Type | Language | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Code | English | ||
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Common Name | English | ||
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Systematic Name | English | ||
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Common Name | English |
Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C258
Created by
admin on Sat Dec 16 19:09:04 GMT 2023 , Edited by admin on Sat Dec 16 19:09:04 GMT 2023
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Code System | Code | Type | Description | ||
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m12234
Created by
admin on Sat Dec 16 19:09:04 GMT 2023 , Edited by admin on Sat Dec 16 19:09:04 GMT 2023
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PRIMARY | |||
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DTXSID601027689
Created by
admin on Sat Dec 16 19:09:04 GMT 2023 , Edited by admin on Sat Dec 16 19:09:04 GMT 2023
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PRIMARY | |||
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Relebactam
Created by
admin on Sat Dec 16 19:09:04 GMT 2023 , Edited by admin on Sat Dec 16 19:09:04 GMT 2023
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PRIMARY | |||
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10027
Created by
admin on Sat Dec 16 19:09:04 GMT 2023 , Edited by admin on Sat Dec 16 19:09:04 GMT 2023
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PRIMARY | |||
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1OQF7TT3PF
Created by
admin on Sat Dec 16 19:09:04 GMT 2023 , Edited by admin on Sat Dec 16 19:09:04 GMT 2023
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PRIMARY | |||
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1OQF7TT3PF
Created by
admin on Sat Dec 16 19:09:04 GMT 2023 , Edited by admin on Sat Dec 16 19:09:04 GMT 2023
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PRIMARY | |||
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SUB184909
Created by
admin on Sat Dec 16 19:09:04 GMT 2023 , Edited by admin on Sat Dec 16 19:09:04 GMT 2023
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PRIMARY | |||
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C152175
Created by
admin on Sat Dec 16 19:09:04 GMT 2023 , Edited by admin on Sat Dec 16 19:09:04 GMT 2023
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PRIMARY | |||
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44129647
Created by
admin on Sat Dec 16 19:09:04 GMT 2023 , Edited by admin on Sat Dec 16 19:09:04 GMT 2023
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PRIMARY | |||
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100000170770
Created by
admin on Sat Dec 16 19:09:04 GMT 2023 , Edited by admin on Sat Dec 16 19:09:04 GMT 2023
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PRIMARY | |||
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1174018-99-5
Created by
admin on Sat Dec 16 19:09:04 GMT 2023 , Edited by admin on Sat Dec 16 19:09:04 GMT 2023
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PRIMARY | |||
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2268500
Created by
admin on Sat Dec 16 19:09:04 GMT 2023 , Edited by admin on Sat Dec 16 19:09:04 GMT 2023
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PRIMARY |
Related Record | Type | Details | ||
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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 μM.
BINDING
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SOLVATE->ANHYDROUS |
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TRANSPORTER -> SUBSTRATE |
in vitro
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TRANSPORTER -> SUBSTRATE |
in vitro
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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
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SALT/SOLVATE -> PARENT |
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TARGET -> INHIBITOR |
koff
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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Volume of Distribution | PHARMACOKINETIC |
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