Topotecan hydrochloride

Various antineoplastics altretamine amsacrine 1-asparaginase dacarbazine melanoma theraccine porfimer sodium procarbazine hydrochloride topotecan hydrochloride tretinoin (dil-trans retinoic acid), systemic... 

HCPT (0.364 g 0.01 mmol) and 40% aqueous dimethylamine (12 ml) was added in dichloromethane (50 ml) in which anhydrous potassium carbonate (2.17 g, 15 mmol) has been suspended. The reaction mixture was stirred at room temperature for 5 h, then filtered and solid extracted with ethylacetate (20 ml). The solvent is evaporated in vacuo giving a residue. The residue was triturated with 0.5% aq HCI (50 ml) to dissolve the water-soluble adduct. Water-soluble were partitioned with petroleum ether (3 times 50 ml) and followed by ethylacetate (3 times 50 ml). The aqueous layer was lyophilized as an off white hydrochloride salt of 9-[(dimethylamino)methyl]10-hydroxy(20S)-camptothecin (topotecan hydrochloride) yield 0.236 g (65%). 

Imatinib mesylate 94 containing a 3-substituted pyridine ring <2000EP0564409>, and a trisubstituted quinoline derivative, topotecan hydrochloride 95, are antineoplastic agents <2002EP0802915>. 

Topotecan hydrochloride is a DNA topoisomerase inhibitor. Topotecan hydrochloride is an antitumor drug with topoisomerase I-inhibitory activity. It is indicated in metastatic carcinoma of the ovary after failure of initial or subsequent chemotherapy small-cell-lung-cancer-sensitive disease after failure of first-line chemotherapy. 

Mayron D, Gennaro AR (1999) Stability and compatibility of topotecan hydrochloride with selected drugs. Am J Health Syst Pharm 56 875-881... 

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