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D-19466, a new cyclobutane-platinum complex with antitumor activity
R Voegeli1, W Schumacher, J Engel
1ASTA Pharma AG, Frankfurt, Federal Republic of Germany.
Journal of Cancer Research and Clinical Oncology
|January 1, 1990
Summary
A novel platinum complex, D-19466, demonstrates potent anticancer activity against various tumors, including cisplatin-resistant types, without causing kidney damage. Its promising profile has led to clinical trials.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Oncology
Background:
- Platinum-based chemotherapy is a cornerstone in cancer treatment.
- Development of new platinum complexes aims to overcome resistance and reduce side effects.
- Nephrotoxicity is a significant dose-limiting toxicity of cisplatin.
Purpose of the Study:
- To characterize a novel platinum complex, D-19466.
- To evaluate the in vitro and in vivo anticancer efficacy of D-19466.
- To assess the nephrotoxic potential of D-19466.
Main Methods:
- Characterization of D-19466.
- In vitro cytotoxicity assays against tumor cell lines.
- In vivo efficacy studies in murine tumor models.
- Assessment of nephrotoxicity via blood urea measurement.
Main Results:
- D-19466 exhibited no significant nephrotoxic side-effects.
- In vitro studies showed D-19466 was cytotoxic to tumor cells at concentrations comparable to or lower than cisplatin.
- D-19466 demonstrated excellent in vivo anticancer activity, including against a cisplatin-resistant P388 cell line.
Conclusions:
- D-19466 is a promising novel platinum complex with potent anticancer activity and a favorable safety profile.
- The compound's efficacy against cisplatin-resistant tumors warrants further investigation.
- Clinical evaluation of D-19466 has been initiated based on preclinical findings.