Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C23H22N4O5 |
| Molecular Weight | 434.4446 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC[C@@]1(O)C(=O)OCC2=C1C=C3N(CC4=C(\C=N\OCCN)C5=C(C=CC=C5)N=C34)C2=O
InChI
InChIKey=IBTISPLPBBHVSU-UVOOVGFISA-N
InChI=1S/C23H22N4O5/c1-2-23(30)17-9-19-20-15(11-27(19)21(28)16(17)12-31-22(23)29)14(10-25-32-8-7-24)13-5-3-4-6-18(13)26-20/h3-6,9-10,30H,2,7-8,11-12,24H2,1H3/b25-10+/t23-/m0/s1
Namitecan (ST1968) is a camptothecin analogue being developed by sigma-tau (a subsidiary of Alfasigma) in Switzerland for the treatment of cancer. Namitecan, a novel hydrophilic camptothecin analog of the 7-oxyiminomethyl series, was selected for clinical development on the basis of its promising preclinical efficacy. Namitecan is a topoisomerase I inhibitor. Namitecan exhibited an acceptable toxicity profile, with neutropenia being the dose-limiting toxic effect, and clinical benefit was appreciable in patients with different tumor types, particularly bladder and endometrium carcinomas.
Originator
Approval Year
Sample Use Guides
Advanced solid tumours: With a target for haematological dose-limiting toxicity of <20%, the recommended dose was defined as 12.5 mg for the D1,8 regimen, 23 mg for the once every 3 week regimen and 7 mg for the D1-3 regimen.
Route of Administration:
Intravenous
In Vitro Use Guide
Curator's Comment: Namitecan induces a comparable level of apoptosis in A431 and A431/TPT cells with IC50 of 0.21 and 0.29 uM. https://www.ncbi.nlm.nih.gov/pubmed/19765546
The cellular response to Namitecan was heterogeneous with IC(50) (2 h) ranging between 0.14 and 13.26 uM, whereas SN38 (the active metabolite of Irinotecan) appeared more effective (IC(50): 0.03-11.7 uM). Interestingly, prolonged drug incubation times up to 72 h enhanced Namitecan cytotoxicity, with similar colony inhibition curves between the two analogues (IC(50), nM-SN38: 0.9 ± 0.2; Namitecan: 0.7 ± 0.4).
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C2843
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ACTIVE MOIETY
