Synthetic Procedure and Cancer Treatment Using Cisplatin Derivatives


Invention Summary

A series of cisplatin derivatives were synthesized and characterized, superseding cisplatin, carboplatin, and oxaliplatin—compounds used for the clinical treatment of various cancers. The synthetic process for the manufacture of these compounds and their analogues are provided. The antitumor activities of these compounds were examined in lung cancer cell lines using MTS cell proliferation assay (a colorimetric method that identifies cytotoxicity) and the results were compared to that of cisplatin. Several compounds were found to be more effective than cisplatin after a one-hour treatment.


Market Opportunity

Cisplatin, approved for clinical treatment by the Food and Drug Administration (FDA) in 1978, belongs to a family of platinum-containing compounds used in the treatment of various types of cancers such as bladder, ovarian, and testicular cancers. While effective as an antitumor agent, its application is limited due to toxic side effects especially nephrotoxicity. Numerous analogues have been developed and studied with the goal of finding compounds that could be more effective and have less toxicity. In 1989, Carboplatin was the first cisplatin analogue approved by the FDA for the treatment of lung and ovarian cancer. Oxaliplatin became the third platinum-containing compound approved by the FDA for the treatment of colorectal cancer. Although carboplatin and oxaliplatin are less toxic than cisplatin, they are either only as effective as, or in many cases, less effective than cisplatin. Additionally, these analogues have dose limiting side effects such as myelosuppression. The cisplatin derivatives can be manufactured to be effective chemotherapeutic drugs.


Features & Benefits


 The anti-proliferative activities of these compounds against a panel of human cancer cell lines are more effective than cisplatin—a gold standard for cancer therapy. Cisplatin had no effect on the lung cancer cell lines up to 1 mM concentration. Cisplatin was also tested on prostate, breast, and melanoma cancer cell lines. Cisplatin had little or no effect on the cell lines tested even up to 1 mM concentration.


 This method does not require the use of strong bases and gives high yields, resulting in cost-effective preparation of prospective antitumor drugs.


Intellectual Property Patent No. 8,703,756

Patent Information:
For Information, Contact:
John Minnick
Business Development Officer
University of Nevada, Las Vegas
Pradip Bhowmik
Haesook Han
Bryan Spangelo
Pear (ontida) Tanthmanatham
Van Vo
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