Antitumor Activity of Quinocarmycin Citrate (KW-2152) against Human Tumor Xenografts Serially Transplanted into Nude Mice

• Published in: Keio journal of medicine Vol. 37; no. 4; pp. 355 - 364
• Main Authors: Inoue, So, Kubota, Tetsuro, Ohishi, Takashi, Kuzuoka, Masahiko, Oka, Shoichi, Shimoyama, Yutaka, Kikuyama, Shigehiro, Ishibiki, Kyuya, Abe, Osahiko
• Format: Journal Article
• Language: English
• Published: Japan The Keio Journal of Medicine 1988
• Subjects: Animals; Antibiotics, Antineoplastic - therapeutic use; antitumor activity; Drug Screening Assays, Antitumor; human tumor xenografts; Humans; Isoquinolines - therapeutic use; Male; Mice; Mice, Nude; Neoplasm Transplantation; Neoplasms, Experimental - drug therapy; quinocarmycin citrate (KW-2152); Transplantation, Heterologous
• ISSN: 0022-9717; 1880-1293
• DOI: 10.2302/kjm.37.355

The antitumor spectra of quinocarmycin citrate (KW-2152; QCM), a novel antibiotic with a different molecular structure from conventionally available antitumor agents, was examined using a human tumor xenograft-nude mouse system. One breast (MX-1), one colon (Co-4), seven gastric (St-4, St-15, St-40, SC-2-JCK, SC-6-JCK, Exp-4 and H-111) and two lung small cell (Lu-24 and Lu-130) carcinomas were inoculated into BALB/cA male nude mice, and the treatment was initiated when the tumor started exponential growth. When QCM was given ip in schedules of 2.5mg/kg qd×14, 5mg/kg qd×7, 7mg/kg g3.5d×5 and 10mg/kg q7d×3 for MX-1 and SC-2-JCK, the most effective schedule of administration was 5mg/kg qd×7, which was applied for the other strains. QCM showed excellent antitumor activity against MX-1 and Co-4 which are sensitive to most conventionally available antitumor agents. The antitumor spectra of QCM against human lung small cell carcinomas was obvious; all of the Lu-130 tumors disappeared completely and five out of six Lu-24 tumors also disappeared. The efficiency rate of QCM against gastric carcinomas was 71.4% (5/7), which was almost equivalent to those of mitomycin C and cisplatin and superior to those of adriamycin, 5-fluorouracil, nimustine and aclarubicin. Because the antitumor spectrum of this agent against gastric carcinoma xenografts was excellent, it was thought to he useful for clinical application to gastric carcinomas.