Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C17H18N4O3 |
| Molecular Weight | 326.3498 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)CCN1C(=O)C2=CC(NC(N)=O)=CC3=CC=CC(C1=O)=C23
InChI
InChIKey=WCKZRLOUKYFJDY-UHFFFAOYSA-N
InChI=1S/C17H18N4O3/c1-20(2)6-7-21-15(22)12-5-3-4-10-8-11(19-17(18)24)9-13(14(10)12)16(21)23/h3-5,8-9H,6-7H2,1-2H3,(H3,18,19,24)
| Molecular Formula | C17H18N4O3 |
| Molecular Weight | 326.3498 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
UNBS5162 is a naphthalimide that binds to DNA by intercalation and suppresses CXCL chemokine elaboration. In vivo and in vitro studies demonstrated potent antineoplastic properties of the compound. The phase 1 dose-escalation trial demonstrated that despite pre-clinical data suggesting low risk of QTc prolongation with UNBS5162 administration, there was a statistically significant relationship noted in
study patients. The magnitude of QTc prolongation at the highest doses warranted the study drug to be terminated.
Originator
Approval Year
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
5913.7 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23053399 |
234 mg/m² 1 times / week multiple, intravenous dose: 234 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
UNBS-5162 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
12786 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23053399 |
234 mg/m² 1 times / week multiple, intravenous dose: 234 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
UNBS-5162 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
7.94 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23053399 |
234 mg/m² 1 times / week multiple, intravenous dose: 234 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
UNBS-5162 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
234 mg/m2 1 times / week multiple, intravenous Highest studied dose Dose: 234 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 234 mg/m2, 1 times / week Sources: Page: p.5 |
unhealthy, ADULT n = 3 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 3 Sources: Page: p.5 |
Sample Use Guides
Phase I study of UNBS5162 was conducted to establish pharmacokinetics (PK), maximum tolerated dose (MTD), dose-limiting toxicity, safety and anti-tumor activity in patients with advanced solid tumors or lymphoma. UNBS5162 was administered in a 3 + 3 dose escalation scheme by intravenous infusion over 1 h weekly for 3 weeks of a 4-week cycle. Twenty-four patients with metastatic carcinoma and 1 patient with lymphoma were treated at eight dose levels (18-234 mg/m(2)). The MTD or dose-limiting toxicity for UNBS5162 was not reached due to the magnitude of QTc prolongation at the highest dose of 234 mg/m(2)/week that led to study termination.
Route of Administration:
Intravenous
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 10:53:12 GMT 2023
by
admin
on
Sat Dec 16 10:53:12 GMT 2023
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| Record UNII |
JY9JF7D78N
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| Record Status |
Validated (UNII)
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| Record Version |
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956590-23-1
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C102850
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16048966
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