Overview: The first antipsychotic drugs, discovered serendipitously in clinical testing, provided a major advance in the treatment of mental disease. However, they were not without side effect liabilities, and this presented an opportunity to address an unmet medical need. Although there were many potential avenues to explore, we selected a combination of D2 dopamine and 5-HT2 serotonin receptor blockade, to ensure efficacy and reduce side effects, respectively. Our strategy led us to a series of oxindoles linked to benzisothiazolyl piperazine, from which we selected ziprasidone as a novel atypical antipsychotic agent for clinical trials.
Ziprasidone's favorable ratio of 5-HT2 to D2 receptor affinity affords antipsychotic efficacy with low side-effect propensity, including a weight neutral profile. Ziprasidone (marketed as Geodon&174;in the U.S.) is a successful atypical antipsychotic drug that has benefited over one million patients.
Areas covered in the webinar:
- History of antipsychotic drug discovery
- Strategy for discovery of novel second generation antipsychotic drugs
- Oxindole and benzisothiazole synthetic chemistry
- SAR of ziprasidone and its analogues
- Clinical results with ziprasidone
Who should attend?
- Organic Chemists
- Medicinal Chemists
- Bioorganic Chemists
- Anyone involved in drug discovery in academic or corporate labs
Dr. John A. Lowe III
Co-inventor of Geodon© at Pfizer
Stuart A. Borman
Deputy Assistant Managing Editor