Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C25H28N2O4Si |
| Molecular Weight | 448.5863 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC[C@@]1(O)C(=O)OCC2=C1C=C3N(CC4=C3N=C5C=CC=CC5=C4CC[Si](C)(C)C)C2=O
InChI
InChIKey=POADTFBBIXOWFJ-VWLOTQADSA-N
InChI=1S/C25H28N2O4Si/c1-5-25(30)19-12-21-22-17(13-27(21)23(28)18(19)14-31-24(25)29)15(10-11-32(2,3)4)16-8-6-7-9-20(16)26-22/h6-9,12,30H,5,10-11,13-14H2,1-4H3/t25-/m0/s1
Cositecan (BNP1350) is semi-synthetic silicon-containing camptothecin and an inhibitor of topoisomerase I. It was engineered by BioNumerik Pharmaceuticals for superior oral bioavailability, lactone stability, and insensitivity to Pgp/MRP/LRP drug resistance. The compound shows a broad spectrum of activity in experimental human tumors. Cositecan was investigated in clinical trials in patients with malignant melanoma, relapsed or refractory non-small cell lung cancer, ovarian and peritoneal cancer, malignant glioma. The compound had little activity in recurrent glioma and ovarian cancer.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Characterization of protein kinase chk1 essential for the cell cycle checkpoint after exposure of human head and neck carcinoma A253 cells to a novel topoisomerase I inhibitor BNP1350. | 2000 Mar |
|
| New highly lipophilic camptothecin BNP1350 is an effective drug in experimental human cancer. | 2000 Oct 15 |
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| Plasma and cerebrospinal fluid pharmacokinetic study of BNP1350 in nonhuman primates. | 2004 Jun |
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C406143
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ACTIVE MOIETY
PARENT (METABOLITE INACTIVE)
