Diflomotecan
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Trade names | Diflomotecan |
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Formula | C21H16F2N2O4 |
Molar mass | 398.366 g·mol−1 |
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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
[edit]- ^ Bailly C (2003). "Homocamptothecins: potent topoisomerase I inhibitors and promising anticancer drugs". Critical Reviews in Oncology/Hematology. 45 (1): 91–108. doi:10.1016/s1040-8428(02)00090-2. PMID 12482574.
- ^ Kroep JR, Gelderblom H (2009). "Diflomotecan, a promising homocamptothecin for cancer therapy". Expert Opin Investig Drugs. 18 (1): 69–75. doi:10.1517/13543780802571674. PMID 19053883. S2CID 73027318.
- ^ "Diflomotecan (BN80915) Administered Once Every 3 Weeks in Treating Patients With Sensitive Small Cell Lung Cancer (SCLC) - Full Text View - ClinicalTrials.gov". clinicaltrials.gov.