Chemistry:Diflomotecan

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Short description: Chemical compound


Diflomotecan
Diflomotecan.png
Clinical data
Trade namesDiflomotecan
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEBI
ChEMBL
Chemical and physical data
FormulaC21H16F2N2O4
Molar mass398.366 g·mol−1
3D model (JSmol)

Diflomotecan (also known as BN80905) is a chemotherapeutic agent that is a topoisomerase inhibitor (Top1). It varies from other camptothecin based Top1 inhibitors like topotecan in having a 7-membered E-ring. The oxepan-2-one ring in the homocamptothecin analogues is more stable in plasma compared to the 6-membered lactone in camptothecin.[1] Diflomotecan was the first homocamptothecin to enter clinical trials[2] and is currently in phase I for treating patients with sensitive small cell lung cancer (SCLC).[3]

References

  1. "Homocamptothecins: potent topoisomerase I inhibitors and promising anticancer drugs". Critical Reviews in Oncology/Hematology 45 (1): 91–108. 2003. doi:10.1016/s1040-8428(02)00090-2. PMID 12482574. 
  2. "Diflomotecan, a promising homocamptothecin for cancer therapy.". Expert Opin Investig Drugs 18 (1): 69–75. 2009. doi:10.1517/13543780802571674. PMID 19053883. 
  3. "Diflomotecan (BN80915) Administered Once Every 3 Weeks in Treating Patients With Sensitive Small Cell Lung Cancer (SCLC) - Full Text View - ClinicalTrials.gov". https://clinicaltrials.gov/ct2/show/NCT00080015.