Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C21H25N5O4 |
| Molecular Weight | 411.4543 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CNCCNC1=CC=C2N(CCNCCO)N=C3C2=C1C(=O)C4=C3C(O)=CC=C4O
InChI
InChIKey=XASBSYHEEHVCSJ-UHFFFAOYSA-N
InChI=1S/C21H25N5O4/c1-22-6-7-24-12-2-3-13-17-16(12)21(30)19-15(29)5-4-14(28)18(19)20(17)25-26(13)10-8-23-9-11-27/h2-5,22-24,27-29H,6-11H2,1H3
Teloxantrone (also known as DuP 937) was developed as an anthrapyrazole intercalator that inhibits DNA synthesis. Teloxantrone interacts with topoisomerase II, thereby inhibiting DNA replication and repair, as well as RNA and protein synthesis. The drug participated in phase II clinical trials in colorectal carcinoma, in non-small cell lung cancer, in metastatic malignant melanoma. However, these studied apparently were discontinued.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| In vitro DNA strand scission and inhibition of nucleic acid synthesis in L1210 leukemia cells by a new class of DNA complexers, the anthra[1,9-cd]pyrazol-6(2H)-ones (anthrapyrazoles). | 1985 Oct 1 |
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| Phase II study on DuP 937 (Teloxantrone) in colorectal carcinoma. A Canadian National Cancer Institute Clinical Trial Group study. | 1993 May-Aug |
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| Phase I pharmacokinetic study of DUP-937, a new anthrapyrazole. | 1993 Nov |
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| A phase II trial of DuP 937 (Teloxantrone) in non-small cell lung cancer. A study of the NCIC Clinical Trials Group. | 1993 Sep |
|
| A phase II study of DuP 937 (Teloxantrone) in metastatic malignant melanoma: a study of the National Cancer Institute of Canada Clinical Trials Group (NCICCTG). | 1993 Sep |
Sample Use Guides
A phase I trial was conducted in which DUP-937 (TELOXANTRONE) was given in an intravenous bolus weekly for 3 weeks. Cycles were repeated every 5 weeks. Twenty men and 13 women with median ECOG performance status of 1 completed 74 cycles. The starting dose was 0.55 mg/m2/week and doses were escalated to 16 mg/m2/week
Route of Administration:
Intravenous
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NCI_THESAURUS |
C2107
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DTXSID001317868
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100000082443
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91441-48-4
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CHEMBL24329
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C046658
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6988
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SUB10875MIG
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96521WL61B
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C1520
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5364123
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)
SALT/SOLVATE (PARENT)
