nk-121 and Lung-Neoplasms

New cisplatinum derivatives of 254-S, DWA2114R and NK121 developed in Japan were reviewed. These three compounds have less nephrotoxicity and nausea/vomiting than cisplatinum, but have more myelotoxicity. 254-S showed activities against carcinomas of the head and neck, lung, esophagus, urinary tract, prostate, testis, ovary and cervix. DWA2114R showed activities against carcinoma of the ovary, prostate, testis and breast. NK121 is under phase II study. A randomized controlled study of 254-S for non-small-cell lung cancer and DWA2114R for ovarian cancer was performed compared to cisplatinum. The antitumor activity of these compounds was not different from cisplatinum, however the hydration was much less than cisplatinum. These cisplatinum derivatives of 254-S and DWA2114R were thought to be useful for QOL of the patients treated with cisplatinum compound.

Topics: Adult; Aged; Antineoplastic Agents; Carboplatin; Carcinoma, Non-Small-Cell Lung; Cisplatin; Female; Humans; Lung Neoplasms; Male; Middle Aged; Organoplatinum Compounds; Ovarian Neoplasms; Prostatic Neoplasms; Testicular Neoplasms

A number of platinum compounds have been synthesized and screened on the basis of structure-activity strategy. In Japan, clinical trials of three analogues (NK-121, DWA-2114R and 254-S) have been undertaken. NK-121, which have the same leaving group as carboplatin, the dose limiting factor (DLF) was leukopenia, while renal toxicity was extremely mild. DWA-2114R, also with the same leaving group, was less nephrotoxic than CDDP or less marrow toxic than CBDCA. DLF was also leukopenia. Phase II study revealed 29% and 12% response rates for small cell carcinoma (SCLC) and non-small cell carcinoma (NSCLC), respectively. In 254-S which has the same carrier ligand (NH2) as CDDP and CBDCA. DLF was thrombocytopenia with mild nephrotoxicity. Response rates of 41% and 21% were obtained for SCLC and NSCLC, respectively. In a randomized study comparing 254-S plus VDS with CDDP plus VDS, equivalent response rate and milder toxicity were observed for the 254-S group. Since highly active agents other than platinum compounds have been currently evaluated for the cases of lung cancer, preclinical screening for substantially active compounds is essential in developing new platinum analogues.

Topics: Antineoplastic Agents; Carboplatin; Carcinoma, Non-Small-Cell Lung; Carcinoma, Small Cell; Female; Humans; Lung Neoplasms; Male; Organoplatinum Compounds

New cisplatinum derivatives of 254-S, DWA2114R and NK121 developed in Japan were reviewed. These three compounds have less nephrotoxicity and nausea/vomiting than cisplatinum, but have more myelotoxicity. 254-S showed activities against carcinomas of the head and neck, lung, esophagus, urinary tract, prostate, testis, ovary and cervix. DWA2114R showed activities against carcinoma of the ovary, prostate, testis and breast. NK121 is under phase II study. A randomized controlled study of 254-S for non-small-cell lung cancer and DWA2114R for ovarian cancer was performed compared to cisplatinum. The antitumor activity of these compounds was not different from cisplatinum, however the hydration was much less than cisplatinum. These cisplatinum derivatives of 254-S and DWA2114R were thought to be useful for QOL of the patients treated with cisplatinum compound.

Topics: Adult; Aged; Antineoplastic Agents; Carboplatin; Carcinoma, Non-Small-Cell Lung; Cisplatin; Female; Humans; Lung Neoplasms; Male; Middle Aged; Organoplatinum Compounds; Ovarian Neoplasms; Prostatic Neoplasms; Testicular Neoplasms

A number of platinum compounds have been synthesized and screened on the basis of structure-activity strategy. In Japan, clinical trials of three analogues (NK-121, DWA-2114R and 254-S) have been undertaken. NK-121, which have the same leaving group as carboplatin, the dose limiting factor (DLF) was leukopenia, while renal toxicity was extremely mild. DWA-2114R, also with the same leaving group, was less nephrotoxic than CDDP or less marrow toxic than CBDCA. DLF was also leukopenia. Phase II study revealed 29% and 12% response rates for small cell carcinoma (SCLC) and non-small cell carcinoma (NSCLC), respectively. In 254-S which has the same carrier ligand (NH2) as CDDP and CBDCA. DLF was thrombocytopenia with mild nephrotoxicity. Response rates of 41% and 21% were obtained for SCLC and NSCLC, respectively. In a randomized study comparing 254-S plus VDS with CDDP plus VDS, equivalent response rate and milder toxicity were observed for the 254-S group. Since highly active agents other than platinum compounds have been currently evaluated for the cases of lung cancer, preclinical screening for substantially active compounds is essential in developing new platinum analogues.

Topics: Antineoplastic Agents; Carboplatin; Carcinoma, Non-Small-Cell Lung; Carcinoma, Small Cell; Female; Humans; Lung Neoplasms; Male; Organoplatinum Compounds

Topics: Antineoplastic Agents; Carboplatin; Carcinoma, Small Cell; Carcinoma, Squamous Cell; Cell Line; Cisplatin; Humans; In Vitro Techniques; Lung Neoplasms; Organoplatinum Compounds; Tumor Cells, Cultured; Tumor Stem Cell Assay