Comparative investigation on use of (2''R)-4'-O-tetrahydropyranyl-adriamycin and adriamycin as intravesical chemotherapy for superficial bladder tumors.

An intravesical chemotherapeutic agent must be capable of being rapidly absorbed by the tumor cells and expressing its activity while undergoing little systemic absorption. A comparative investigation was conducted on (2''R)-4'-O-tetrahydropyranyl-doxorubicin (Adriamycin) (THP) and Adriamycin (ADM) from the above viewpoint using cultured MBT-2 and T-24 cell lines. From in vitro experimental systems, it is surmized that THP is taken up by bladder tumor cells more rapidly than ADM is, and that THP is thus able to exert its effect on the bladder tumor within a shorter time than that required by ADM. This pharmacokinetic advantage of THP was proved in an in vivo experimental system; that is, bladder tumor tissue which was established by implanting MBT-2 cells into the mouse (C3H/He) bladder was found to contain THP in a concentration approximately 1.9 times higher than the concentration of ADM. The amount of systemic absorption from the bladder was small in the case of both THP and ADM. THP should be useful as a new agent for intravesical chemotherapy.