Olanzapine (Molecule of the Month for January 2007)
Zyprexa®, Zyprexa Zydis®, Symbyax®
Olanzapine is one of the most commonly used drugs for atypical antipsychotics. Olanzapine has been approved by the FDA for the treatment of schizophrenia, acute mania in bipolar disorder, agitation associated with schizophrenia and bipolar disorder, and as maintenance treatment in bipolar disorder and psychotic depression. Zyprexa is Lilly’s top-selling drug, with sales of $4.2 billion last year.
Olanzapine has a high affinity for dopamine and serotonin receptors. Olanzapine's antipsychotic activity is mediated primarily by antagonism (blocking or inhibition) at dopamine receptors.
Recently the FDA required the manufacturers of all atypical antipsychotics to include a warning about the risk of hyperglycemia and diabetes with atypical antipsychotics. The results of a large, random-design study funded by NIH's National Institute of Mental Health (NIMH) were published in September 2005. The 18-month study, which involved 1,400 participants at 57 sites around the country, found that "patients on olanzapine also experienced substantially more weight gain and metabolic changes associated with an increased risk of diabetes than those participants taking the other drugs." According to a New York Times article published on December 17, 2006, Eli Lilly has engaged in a decade-long effort to play down the health risks of Zyprexa, its best-selling medication for schizophrenia, according to hundreds of internal Lilly documents and e-mail messages among top company managers. These documents and e-mail messages were soon made publicly available and then made available on the public Internet. Eli Lilly got a temporary restraining order from a US District Court signed on January 4th, 2007 to stop the dissemination or downloading of Eli Lilly documents about Zyprexa, and this allowed them to get a few US-based websites to remove them. The documents, given to New York Times by a lawyer representing mentally ill patients, show that Lilly executives kept important information from doctors about Zyprexa’s links to obesity and its tendency to raise blood sugar — both known risk factors for diabetes.
Formal Chemical Name (IUPAC)
Update by Karl Harrison
(Molecule of the Month for January 2007 )