Antitumor activity of menogaril alone, and in combination against human mammary cancer models in mice and rats

Menogaril is an antitumour agent different from other anthracyclines in being active after oral administration. To predict its clinical effectiveness by this route against human breast cancer, we compared its antitumour activity against breast cancer in experimental animals with that of injected Adriamycin. Menogaril had half the much antitumour activity of Adriamycin against human mammary cancer cell lines. Menogaril given orally also had a antitumour activity against mammary cancer caused by 7,12-dimethyl-benz[a]anthracene in rats comparable with that of Adriamycin. The high concentration of menogaril in tumor tissue seemed to contribute to its effectiveness. Of several combinations of cyclophosphamide, Adriamycin, menogaril, and 5-fluorouracil, the combination of cyclophosphamide, meogaril, and 5-fluorourcil was most effective against mouse leukemia L1210 and human breast cancer xenografts in mice. This combination might have antitumor activity against breast cancer superior to that of the therapy currently of first choice (cyclophosphamide, Adriamycin, and 5-fluorouracil) in the clinic.