Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C18H18ClF5N6O.C4H4O4 |
| Molecular Weight | 580.892 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)\C=C\C(O)=O.CNCCCOC1=CC(F)=C(C(F)=C1)C2=C(N[C@@H](C)C(F)(F)F)N3N=CN=C3N=C2Cl
InChI
InChIKey=TUXZQBYIZLWUKK-AFIAKLHKSA-N
InChI=1S/C18H18ClF5N6O.C4H4O4/c1-9(18(22,23)24)28-16-14(15(19)29-17-26-8-27-30(16)17)13-11(20)6-10(7-12(13)21)31-5-3-4-25-2;5-3(6)1-2-4(7)8/h6-9,25,28H,3-5H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1+/t9-;/m0./s1
Cevipabulin is a synthetic, water-soluble tubulin-binding agent with potential antineoplastic activity. Cevipabulin appears to bind at the vinca-binding site on tubulin but seems to act more similar to taxane-site binding agents in that it enhances tubulin polymerization and does not induce tubulin depolymerization. The disruption in microtubule dynamics may eventually inhibit cell division and reduce cellular growth.
Approval Year
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
582 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20697774 |
31.5 mg/m² 1 times / week multiple, intravenous dose: 31.5 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
CEVIPABULIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2768 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20697774 |
31.5 mg/m² 1 times / week multiple, intravenous dose: 31.5 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
CEVIPABULIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
27.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20697774 |
31.5 mg/m² 1 times / week multiple, intravenous dose: 31.5 mg/m² route of administration: Intravenous experiment type: MULTIPLE co-administered: |
CEVIPABULIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
31.5 mg/m2 1 times / week multiple, intravenous Highest studied dose Dose: 31.5 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 31.5 mg/m2, 1 times / week Sources: Page: p.268 |
unhealthy, ADULT n = 7 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 7 Sources: Page: p.268 |
DLT: Febrile neutropenia... Disc. AE: Neutropenia... Dose limiting toxicities: Febrile neutropenia (14.3%) AEs leading todiscontinuation/dose reduction: Neutropenia (grade 3-4, 42.9%) Sources: Page: p.268 |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Febrile neutropenia | 14.3% DLT |
31.5 mg/m2 1 times / week multiple, intravenous Highest studied dose Dose: 31.5 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 31.5 mg/m2, 1 times / week Sources: Page: p.268 |
unhealthy, ADULT n = 7 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 7 Sources: Page: p.268 |
| Neutropenia | grade 3-4, 42.9% Disc. AE |
31.5 mg/m2 1 times / week multiple, intravenous Highest studied dose Dose: 31.5 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 31.5 mg/m2, 1 times / week Sources: Page: p.268 |
unhealthy, ADULT n = 7 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 7 Sources: Page: p.268 |
Sample Use Guides
Patients were treated with TTI-237 (Cevipabulin) intravenously on days 1, 8 and 15 of a 28-day cycle at dose of 4.5, 9, 15, 22.5 and 31.5 mg/m2 .
Route of Administration:
Intravenous
HeLa cells were harvested by trypsinization, washed, counted, and distributed to wells of 96-well flat-bottomed microtiter plates at 1,000 cells per well in 200 AL of medium. All plates were incubated at 37C in humidified 5% CO2 in air for ~24 h. On day 2, compounds for test were diluted and added to wells. Compounds were dissolved in DMSO at 10 to 20 mkmol/L. For each compound, nine serial 2-fold dilutions were prepared in DMSO. Ten microliters of each dilution was transferred to 100 mkL of medium and mixed well, and then 5 AL of this dilution were transferred in triplicate or quadruplicate to wells containing cells. The final high concentration of each compound was typically 5 mkmol/L. All cultures, including controls with no compound, contained a final concentration of 0.27% DMSO. After 3 d of culture with test compounds (day 5 overall), the MTS assay (Promega; CellTiter 96 aqueous nonradioactive cell proliferation assay) was done on all wells.
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71587814
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849550-67-0
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9FDJ70N1KZ
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admin on Sat Dec 16 06:54:37 GMT 2023 , Edited by admin on Sat Dec 16 06:54:37 GMT 2023
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ACTIVE MOIETY
SUBSTANCE RECORD
