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Influence of exposure and infusion times on the cytotoxicity and pharmacokinetics of cis-malonato[(4R, 5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane]platinum(II)
DC Field | Value | Language |
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dc.contributor.author | Kim, Hun-Taek | - |
dc.contributor.author | Kim, D.-K. | - |
dc.contributor.author | Cho, Yong-Baik | - |
dc.contributor.author | Kim, Taek-Soo | - |
dc.contributor.author | Jung, I | - |
dc.contributor.author | Kim, Key H. | - |
dc.contributor.author | Heo, Dae Seog | - |
dc.contributor.author | Bang, Yung-Jue | - |
dc.contributor.author | Shin, Sang-Goo | - |
dc.contributor.author | Kim, Noe Kyeong | - |
dc.date.accessioned | 2021-01-31T11:06:08Z | - |
dc.date.available | 2021-01-31T11:06:08Z | - |
dc.date.created | 2020-12-16 | - |
dc.date.issued | 1998-01 | - |
dc.identifier.citation | Cancer Chemotherapy and Pharmacology, Vol.41 No.2, pp.109-116 | - |
dc.identifier.issn | 0344-5704 | - |
dc.identifier.other | 119218 | - |
dc.identifier.uri | https://hdl.handle.net/10371/173024 | - |
dc.description.abstract | The effect of exposure time on the in vitro cytotoxicity of a new platinum complex, cis-malonato-[(4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane]platinum(II) (SKI 2053R) and cisplatin (CDDP) toward two human lung-adenocarcinoma cell lines (PC-9, PC-14) and two human stomach-adenocarcinoma cell lines (KATO III, MKN-45) was investigated by variation of the exposure time (1, 4, 12, and 24 h) and drug concentration to yield a constant product of drug concentration times exposure time (C x T). Exposure of cancer cells to low concentrations of SKI 2053R for 12 or 24 h resulted in a greater killing effect than did 1- or 4-h exposure to 24- or 6-fold higher concentrations; the inhibitory effects of SKI 2053R on the colony formation of all tumor cell lines except for KATO III were significantly increased with increasing exposure time (P < 0.05), However, the inhibitory effects of CDDP against all tumor cell lines tested except for PC-14 were inversely correlated with increasing exposure time (P < 0.05). The intracellular accumulation of SKI 2053R and CDDP was measured under the same conditions used in the cell-survival assay using MKN-45 cells. The amount of platinum accumulated from SKI 2053R into MKN-45 cells was greater for the treatment involving low concentrations and long-term exposures (12 and 24 h) than for that using high concentrations and short-term exposures (1 and 4 h) at the constant C x T values, however, the increased accumulation of CDDP was more prominent as the concentration was increased, even if the exposure rime became shorter. The pharmacokinetics studies of SKI 2053R following 1-, 4-, 12-, and 24-h infusions were performed in beagle dogs. A single dose of SKI 2053R (5.0 mg/kg) was successively given over various infusion periods to three beagle dogs at 3-week intervals. The peak levels of ultrafiltrable platinum observed for SKI 2053R at the 1-, 4-, 12-, and 24-h infusions were 3.10 +/- 0.49 (mean +/- SD), 1.24 +/- 0.06, 0.43 +/- 0.07, and 0.25 +/- 0.04 mu g/ml, respectively. The mean binding ratios of platinum from SKI 2053R to plasma protein at the end of 1-, 4-, 12-, and 24-h infusions were approximately 91%, 73%, 53%, and 51%, respectively. The steady-state level of free platinum was maintained during long-term infusions (12 and 24 h) after short periods (1-3 h) from the start of the infusion. This study strongly suggests that the therapeutic efficacy of SKI 2053R given by continuous long-term infusion should be investigated in future clinical studies. | - |
dc.language | 영어 | - |
dc.publisher | Springer Verlag | - |
dc.title | Influence of exposure and infusion times on the cytotoxicity and pharmacokinetics of cis-malonato[(4R, 5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane]platinum(II) | - |
dc.type | Article | - |
dc.contributor.AlternativeAuthor | 방영주 | - |
dc.identifier.doi | 10.1007/s002800050716 | - |
dc.citation.journaltitle | Cancer Chemotherapy and Pharmacology | - |
dc.identifier.wosid | A1998YK93900004 | - |
dc.identifier.scopusid | 2-s2.0-0031882342 | - |
dc.citation.endpage | 116 | - |
dc.citation.number | 2 | - |
dc.citation.startpage | 109 | - |
dc.citation.volume | 41 | - |
dc.identifier.sci | A1998YK93900004 | - |
dc.description.isOpenAccess | N | - |
dc.contributor.affiliatedAuthor | Heo, Dae Seog | - |
dc.contributor.affiliatedAuthor | Bang, Yung-Jue | - |
dc.contributor.affiliatedAuthor | Shin, Sang-Goo | - |
dc.contributor.affiliatedAuthor | Kim, Noe Kyeong | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.subject.keywordPlus | CIS-DIAMMINEDICHLOROPLATINUM II | - |
dc.subject.keywordPlus | SCHEDULE DEPENDENCY | - |
dc.subject.keywordPlus | ANTITUMOR-ACTIVITY | - |
dc.subject.keywordPlus | ANTICANCER DRUGS | - |
dc.subject.keywordPlus | CLONOGENIC-ASSAY | - |
dc.subject.keywordPlus | CYTO-TOXICITY | - |
dc.subject.keywordPlus | PHASE-I | - |
dc.subject.keywordPlus | PLATINUM | - |
dc.subject.keywordPlus | CELLS | - |
dc.subject.keywordPlus | CARBOPLATIN | - |
dc.subject.keywordAuthor | SKI 2053R | - |
dc.subject.keywordAuthor | in vitro cytotoxicity | - |
dc.subject.keywordAuthor | pharmacokinetics | - |
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