Antineoplastic agents irinotecan’s research progress
March 27, 2012Irinotecan is one of the new cytostatic drugs listed in the new family of camptothecin derivatives. In 1966, the substance was extracted from camptotheca acuminata Chinese plants with antitumor activity of camptothecin. But because of its solubility in water is low and it is difficult to predict severe toxicity, its use further study was discontinued. Until 1985, due to the development of molecular biology to explain mechanism of action of camptothecin and topoisomerase special topology of the target DNA, I These findings and clinical pharmacology studies in depth, inspired design efficient, water-soluble camptothecin analogues top good, irinotecan is one of the results of these studies.
Irinotecan Japanese developed in order to clear the value of treating solid tumors of many studies worldwide. Extensive clinical studies have shown that it is an effective treatment for metastatic colorectal cancer, plant extracts fluorouracil-resistant cases is still valid. Currently the drug is approved together with the United States and the European Union, which are listed on more than 100 countries around the world. In March 2001, the drug market in China.
In vitro studies have shown that irinotecan irinotecan and its metabolites with a broad spectrum of antitumor activity of various tumor cell lines. In vivo studies, intravenous, intraperitoneal and oral antitumor activity observed with CPT-11 syngeneic mice transplanted tumor, the same broad spectrum of antitumor activity.
In recent years, according to the results of animal experiments and in vitro experiments, people started with irinotecan for the treatment of other cancers. The study found that compared with the standards of the program may be the use of irinotecan, topotecan in combination with cisplatin to treat non-small cell lung cancer, significantly prolonged survival. Similarly, in a comparative study of standard treatment program for lung cancer cells to small, also got the same conclusion. Together they present the number of irinotecan with various resveratrol drugs to treat non-small cell lung cancer clinical studies are ongoing, the results of these studies help to clarify the role of irinotecan in the treatment of lung cancer. Moreover, except for the treatment of non-small cell lung, small cell lung cancer, cervical cancer and ovarian cancer, irinotecan irinotecan other tumors such as breast cancer, malignant glioma and gastric cancer have some effect.
A 5-FU, over the years has been the drug of choice for treatment of advanced colorectal cancer, the efficiency of about 11%. The extension of the 5-FU infusion or in combination with biochemical modulator can improve the effectiveness of treatment failure is still a lack of effective drugs for further processing. Irinotecan for semi-synthetic derivative of camptothecin derivatives, has a unique molecular structure and mechanism of action, clinical determination of unique advantages, does not affect the quality of life and prolongs survival.
Now, although the research was conducted on irinotecan but does not address the effectiveness and effects on the metabolism of drugs, there are many problems including significant others irinotecan pharmacokinetic differences L Kang major metabolites production and disposal of the track late in the pathogenesis of diarrhea, the correlation between pharmacokinetic and pharmacodynamic parameters of assessment and how to deal with side effects, to avoid increasing the dose, which needs further study. Briefly, disable the above mechanism, optimization of dosing regimens, improve tumor response to the direction of future research efforts. Source:http://www.cospcn.com
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