Chemotherapy and Its Side Effects: Chapter 2 - Alkylating Agents (Cont'd)

A.4. Cisplatin and other platinum drugs

Cisplatin, cis-dichlorodiammine platinum(II) (Fig. 1.4), is the grandparent of all platinum drugs. It is a widely prescribed anticancer drug with therapeutic activity against various solid tumors, but also with substantial side effects. The anticancer activity of cisplatin was discovered by Dr. Barnett Rosenberg of Michigan State University in 1965 [2]. In 1978, the first formulated pharmaceutical product of cisplatin, Platinol, was approved by the FDA and sold by Byistol-Myer Squibb.

As an alkylating agent, the platinum ion of cisplatin forms coordination bonds mostly with guanine on DNA. This crosslinking causes the interference of DNA replication, thus, inhibits the replication of cancer cells.

Fig. 1.4   Cisplatin, carboplatin, and oxaliplatin

Since the discovery of cisplatin’s anticancer activity, thousands of cisplatin analogues have been made and/or studied. Two of the notable platinum drugs successfully developed by Bristol-Myers Squibb are carboplatin and oxaliplatin (Fig. 1.4); both were approved by the FDA for treating a variety of cancers.

In the last thirty years or so, the impact of platinum drugs on cancer treatment has been tremendous and has benefited many cancer patients. However, because platinum drugs are often associated with significant side effects, scientists are still working on finding better platinum compounds with fewer/less side effects. Currently, there are a number of new platinum drugs under investigation or development, including some of the platinum compounds synthesized by one of the co-authors, Dr. Jiajiu Shaw. A couple of these new platinum compounds are shown in Fig. 1.5. The dinuclear platinum compound is the first to show a coordination bond between the amide oxygen and platinum(II).

Fig. 1.5  Examples of a 3-Nitrogen Pt compound (left) and a dinuclear Pt compound (right)

© Jiajiu Shaw, 2018

Disclaimer: This blog is written solely for informational purposes. It does not constitute the practice of any medical, nursing or other medical professional health care advice, diagnosis, or treatment. All contents posted are extracted from the book, "SIDE EFFECTS OF CHEMOTHERAPY AND RADIOTHERAPY", prepared by Dr. Jiajiu Shaw, Dr. Frederick Valeriote, and Dr. Ben Chen.