Topotecan
Topotecan is a DNA topoisomerase I inhibitor of the camptothecin derivative class. The water solubility of camptothecin and hydroxycamptothecin is very poor, but the increase of base side chains has greatly increased the water solubility of topotecan, resulting in stronger antitumor activity and less toxic side effects than other camptothecin drugs.
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Topotecan is a DNA topoisomerase I inhibitor of the camptothecin derivative class. The water solubility of camptothecin and hydroxycamptothecin is very poor, but the increase of base side chains has greatly increased the water solubility of topotecan, resulting in stronger antitumor activity and less toxic side effects than other camptothecin drugs. The active lactone on the E ring of topotecan is easily hydrolyzed under neutral and alkaline conditions and becomes an inactive carboxylic acid structure. Therefore, Topotecan is easily inactivated in the intestinal tract when administered orally, and its stability is poor, which seriously affects oral absorption and in vivo efficacy. Selecting a suitable carrier to increase the stability of topotecan in the intestinal tract can reduce the dose and stabilize the blood concentration, which is beneficial to antitumor chemotherapy. The reversed lipid-based nanoparti-cles (RLBN) technology wraps water-soluble drugs with amphiphilic phospholipid molecules to form oil-soluble nanoparticles with hydrophilic groups inward and hydrophobic groups outward in the oil phase.
Cas:123948-87-8
Molecular formula:C23H23N3O5-xHCl-yH20
Molecular weight:421.45(nhydrous free base basis)
MDL No.: MFCD0870670
Storage conditions: room temperature, dry, sealed
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