• Tuberculosis and Respiratory Diseases
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• 제66권2호
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• pp.93-97
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• 2009

연구배경: Belotecan (Camtobell, CKD-602, Chongkundang Pharm., Korea)은 camptothecin의 치환체로 topoisomerase I 효소를 억제하여 항암효과를 나타내는 것으로 알려져 있다. 이에 2차 항암화학요법에 치료제로써 Belotecan 의 효과, 생존율 및 부작용에 대해 연구하였다. 방 법: 이에 소세포폐암에서 etoposide와 platinum을 사용한 1차 항암화학요법에서 실패한 49명의 환자들을 대상으로 2차 항암화학요법에 Belotecan을 투약하였다. 결 과: 전체 반응률은 25%였으며, 11명의 환자에서 partial response를 보였다. 또한 1차 항암화학요법 이후 90일 이내에 재발한 군과 90일 이상 경과한 군간에 유의한 차이는 보이지 않았다. 전체 환자의 중심생존기간은 10.3개월(290일)이었고, 비반응군에서는 186일(95% CI; 67-305)로 반응군의 471일(95% CI; 234-568)에 비해 생존기간의 감소 유의하게 있음을 확인하였다(p=0.07). 결 론: 2차 항암화학요법의 치료제로써 Belotecan의 효능과 부작용에 대해서는 향후 무작위 비교 연구가 필요할 것으로 사료된다.

• Biomolecules & Therapeutics
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• 제14권2호
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• pp.90-95
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• 2006

CKD-602 exerts its antitumor effect via inhibition of topoisomerase I in cancer cells. Multicellular spheroid (MCS) and Multicellular layers (MCLs) are known as in vitro 3-dimensional models which closely represent tumor conditions in vivo. In order to investigate the potential of CKD-602 against human colorectal tumors, we evaluated the anti-proliferative activity and penetration ability of CKD-602 in MCS and MCL cultures of DLD-l human colorectal cancer cells, respectively. The maximum effects($E_{max}$) induced by CKD-602 were significantly lower in MCS compared to monolayers (48% vs 92%). With prolonged drug exposure, the $IC_{50's}$ of CKD-602 decreased to $23.5{\pm}1.0nM$ in monolayers after 24 h exposure and $42.3{\pm}1.7nM$ in MCS after 6 days, respectively. However, no further increase in effect was observed for exposure time longer than growth doubling time (Td) in both cultures. Activity of CKD-602 was significantly reduced after penetration through MCL and also with cell-free insert membrane. In conclusion, CKD-602 showed significantly decreased anti-proliferative activity in 3D cultures (MCS) of human colorectal cancer cells. Tumor penetration of CKD-602 could not be determined due to loss of activity after penetration through cell free insert membrane, which warrants further evaluation using a modified model.

• Journal of the Korean Association of Oral and Maxillofacial Surgeons
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• 제31권1호
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• pp.7-12
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• 2005

Purpose: CKD-602, a newly developed water-soluble campthotecin analogue, is a anticancer agent which act as a DNA topoisomerase I inhibitor. CKD-602 is known as more potent and tolerable agent. The main purposes of this study were to measure the cytotoxic effect of CKD-602 on the oral cancer cell lines and to evaluate the apoptotic aspect of dead cells. Materials and Methods: To determine the cytotoxic effect of CKD-602 on the oral cancer cell lines in comparison with various cell lines, such as lung cancer and colon cancer cell lines, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) assay was performed. And apoptosis was analyzed using fluorescence-activated cell sorting(FACS) system. Results: CKD-602 decreased the viability of malignant cells in a dose dependent manner and in a time dependent manner. CKD-602 showed excellent cytotoxicity to the oral cancer cell lines. Also, apoptotic portion was increased in a dose dependent manner. Conclusion: These findings indicated that CKD-602 induced apoptotic cell death in the various cell lines including oral cancer cell lines. From the results, it was suggested that CKD-602 would be a potential therapeutic agent for the oral cancer. More successive researches on the anticancer effect of CKD-602 should be performed.