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
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
| 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
| 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 |
|---|---|---|---|---|
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 |
|
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 |
|
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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 |
|
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 |
|
1.2 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
| 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 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%) 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 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) 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 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%) 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 Sources: |
healthy, median age 27 years Health Status: healthy Age Group: median age 27 years Sex: M 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 Health Status: healthy Age Group: median age 28.5 years Sex: M 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 Sources: |
healthy, median age 53.3 Health Status: healthy Age Group: median age 53.3 Sex: M 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 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%) 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 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%) 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 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
| 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 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 Health Status: healthy Age Group: median age 27 years Sex: M 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 Sources: |
healthy, median age 27 years Health Status: healthy Age Group: median age 27 years Sex: M 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 Sources: |
healthy, median age 27 years Health Status: healthy Age Group: median age 27 years Sex: M 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 Sources: |
healthy, median age 27 years Health Status: healthy Age Group: median age 27 years Sex: M 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 Sources: |
healthy, median age 27 years Health Status: healthy Age Group: median age 27 years Sex: M 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 Sources: |
healthy, median age 27 years Health Status: healthy Age Group: median age 27 years Sex: M 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 Sources: |
healthy, median age 27 years Health Status: healthy Age Group: median age 27 years Sex: M 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 Sources: |
healthy, median age 27 years Health Status: healthy Age Group: median age 27 years Sex: M 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 Health Status: healthy Age Group: median age 28.5 years Sex: M 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 Sources: |
healthy, median age 53.3 Health Status: healthy Age Group: median age 53.3 Sex: M 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 Sources: |
healthy, median age 53.3 Health Status: healthy Age Group: median age 53.3 Sex: M 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 Sources: |
healthy, median age 53.3 Health Status: healthy Age Group: median age 53.3 Sex: M 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 Sources: |
healthy, median age 53.3 Health Status: healthy Age Group: median age 53.3 Sex: M 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 Sources: |
healthy, median age 53.3 Health Status: healthy Age Group: median age 53.3 Sex: M 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 Sources: |
healthy, median age 53.3 Health Status: healthy Age Group: median age 53.3 Sex: M 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 Sources: |
healthy, median age 53.3 Health Status: healthy Age Group: median age 53.3 Sex: M 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 Sources: |
healthy, median age 53.3 Health Status: healthy Age Group: median age 53.3 Sex: M 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 Sources: |
healthy, median age 53.3 Health Status: healthy Age Group: median age 53.3 Sex: M 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 Sources: |
healthy, median age 53.3 Health Status: healthy Age Group: median age 53.3 Sex: M 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 Sources: |
healthy, median age 53.3 Health Status: healthy Age Group: median age 53.3 Sex: M 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 Sources: |
healthy, median age 53.3 Health Status: healthy Age Group: median age 53.3 Sex: M 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 Sources: |
healthy, median age 53.3 Health Status: healthy Age Group: median age 53.3 Sex: M 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 Sources: |
healthy, median age 53.3 Health Status: healthy Age Group: median age 53.3 Sex: M 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 Sources: |
healthy, median age 53.3 Health Status: healthy Age Group: median age 53.3 Sex: M 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 Sources: |
healthy, median age 53.3 Health Status: healthy Age Group: median age 53.3 Sex: M 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 Sources: |
healthy, median age 53.3 Health Status: healthy Age Group: median age 53.3 Sex: M 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 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
| 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
Mon Mar 31 23:30:14 GMT 2025
by
admin
on
Mon Mar 31 23:30:14 GMT 2025
|
| Record UNII |
Y1MYA2UHFL
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Official Name | English | ||
|
Preferred Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
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 | ||
|---|---|---|---|---|---|
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 |
|