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Antitumor Activity of Quinocarmycin (KW2152) against Various Cultured Leukemia and Lymphoma Cell Lines in Vitro¹

Hematology-Oncology and Clinical Cancer Chemotherapy Division, National Cancer Center Hospital, 1-1 Tsukiji 5-chome, Chuo-ku, Tokyo 104

Growth inhibitory activity of quinocarmycin citrate (KW2152) against 25 human cultured cell lines derived from leukemias and lymphomas was assessed quantitatively by regrowth assay. EC₉₀ values (drug concentration required for 90% growth inhibition of treated cells) measured at 1-h exposure to the drug in vitro were more than 16 µg/ml in five of six T-cell lines derived from T-lymphoma/leukemia, hence they were insensitive to KW2152. On the other hand, four of six B-cell lines derived from B-lymphoma and three of four cell lines derived from non-T, non-B acute lymphoblastic leukemia were sensitive to KW2152 with EC₉₀ values of 0.3 to 2.2 µg/ml at 1-h exposure. Six myelomonocytoid cell lines derived from acute myelogenous leukemia were also sensitive with EC₉₀ values of 1.8 to 3.0 µg/ml on 1-h exposure, but two myeloid cell lines derived from chronic myelogenous leukemia and one cell line derived from erythroleukemia were insensitive with EC₉₀ values of more than 16 µg/ml. The EC₉₀ values of most cell lines decreased as exposure time increased, and those measured at 24-h exposure were similarly low and mostly in the 0.02 to 0.06 µg/ml range. The kinetics analysis of growth inhibitory activity of KW2152 revealed that the drug showed time-dependent action. These in vitro results, as correlated with in vivo results reported elsewhere (K. Fujimoto, T. Oka, and M. Morimoto, Cancer Res., 47: 1516–1522, 1987), suggest that daily consecutive or continuous dose therapy as well as single or intermittent large-dose therapy would be worthy of testing in the clinical trial of KW2152.

¹ This work was partly supported by Grants-in-Aid for Cancer Research (61-2 and 62S-1), and for the Comprehensive 10-Year Strategy for Cancer Control from the Ministry of Health and Welfare, and by a trust fund under government control for research on Quinocarmycin (KW2152) from Kyowa Hakko Kogyo Co., Ltd.

² Present address: Jikeikai Medical University, Aoto Hospital, Japan.

³ To whom requests for reprints should be addressed.

Received 4/13/88. Revised 7/18/88. Accepted 7/27/88.