Nonsteroidal antiandrogen
Overview
Nonsteroidal antiandrogens (NSAAs) are a class of pharmacological agents that act as antagonists of the androgen receptor (AR). They are primarily used in the treatment of prostate cancer, but are also used in the treatment of other androgen-dependent conditions.
Mechanism of Action
NSAAs work by binding to the androgen receptor, preventing androgens such as testosterone and dihydrotestosterone (DHT) from binding and activating the receptor. This inhibits the effects of these hormones in the body, which can slow the growth of androgen-dependent cancers.
Types of Nonsteroidal Antiandrogens
There are several types of NSAAs, including flutamide, bicalutamide, and enzalutamide. These drugs differ in their chemical structures, but all act as antagonists of the androgen receptor.
Flutamide
Flutamide is a first-generation NSAA that was introduced in the 1980s. It is primarily used in the treatment of prostate cancer, and works by binding to the androgen receptor and preventing the action of androgens.
Bicalutamide
Bicalutamide is a second-generation NSAA that is more potent and selective than flutamide. It is used in the treatment of prostate cancer, and has also been used off-label in the treatment of hirsutism and transgender hormone therapy.
Enzalutamide
Enzalutamide is a third-generation NSAA that is even more potent and selective than bicalutamide. It is used in the treatment of prostate cancer, and has also been used in the treatment of breast cancer.
Clinical Uses
NSAAs are primarily used in the treatment of prostate cancer. They are often used in combination with other treatments, such as surgery, radiation therapy, and chemotherapy. NSAAs can also be used in the treatment of other androgen-dependent conditions, such as hirsutism and transgender hormone therapy.
Side Effects and Risks
Like all medications, NSAAs can have side effects. These can include nausea, vomiting, diarrhea, and fatigue. More serious side effects can include liver damage and an increased risk of cardiovascular disease. It is important for patients to discuss these risks with their healthcare provider before starting treatment with NSAAs.
Future Directions
Research is ongoing into the development of new NSAAs and the potential for these drugs to be used in the treatment of other conditions. This includes research into the use of NSAAs in the treatment of breast cancer, as well as research into the development of new NSAAs that are more potent and selective.