title: Antitumor activity of a new platinum compound (glycolate-o,o') diammineplatinum (II) (254-S), against non-small cell lung carcinoma grown in a human tumor clonogenic assay system.
abstract: (Glycolate-o,o') diammineplatinum (II) (254-S) is one of the platinum derivatives showing high activity against rodent solid tumors and lack of renal toxicity. We have used a human tumor clonogenic assay (HTCA) as a disease-oriented drug screening model for new antitumor drugs, in order to test the antitumor activity of 254-S against non-small cell lung carcinoma (NSCLC) and to compare its activity with that of cisplatin (CDDP) and of carboplatin (CBDCA). The overall in vitro response rate (defined as less than 50% survival of tumor colony forming units) for 254-S was observed in 10/29 and 20/30 evaluable specimens isolated freshly from NSCLC patients with continuous exposure at 1 and 10 micrograms/ml, respectively, indicating a positive dose-response relationship. Dose dependent cytotoxicity was also confirmed in 4 human tumor cell lines derived from NSCLC patients. The antitumor activity of 254-S was 3.6-fold that of CBDCA, but two-fifths that of CDDP. A comparison of these in vitro results with the toxic properties of 254-S such as low nephrotoxicity suggests that 254-S is a promising new drug against NSCLC.
authors.affiliation: Pharmacology Division, National Cancer Center Research Institute, Tokyo, Japan.
authors.forename: F
authors.initials: F
authors.lastname: Kanzawa
authors.forename: Y
authors.initials: Y
authors.lastname: Matsushima
authors.forename: H
authors.initials: H
authors.lastname: Nakano
authors.forename: K
authors.initials: K
authors.lastname: Nakagawa
authors.forename: H
authors.initials: H
authors.lastname: Takahashi
authors.forename: Y
authors.initials: Y
authors.lastname: Sasaki
authors.forename: N
authors.initials: N
authors.lastname: Saijo
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D016190:Carboplatin; D002289:Carcinoma, Non-Small-Cell Lung / Q000473:pathology*; D002945:Cisplatin / Q000494:pharmacology; D006801:Humans; D008175:Lung Neoplasms / Q000473:pathology*; D009944:Organoplatinum Compounds / Q000494:pharmacology*; D014407:Tumor Cells, Cultured / Q000187:drug effects; D014410:Tumor Stem Cell Assay
chemical_list: D000970:Antineoplastic Agents; D009944:Organoplatinum Compounds; C053989:nedaplatin; D016190:Carboplatin; D002945:Cisplatin