Rosolutamide

Nonsteroidal antiandrogen

Rosolutamide
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number
PubChem
DrugBank
ChemSpider
KEGG

Rosolutamide is a nonsteroidal antiandrogen (NSAA) that was developed for the treatment of prostate cancer. It belongs to a class of drugs that work by blocking the effects of androgens, such as testosterone, in the body. This action is beneficial in conditions like prostate cancer, where androgens can promote the growth of cancer cells.

Mechanism of Action

Rosolutamide functions by competitively inhibiting the androgen receptor (AR), which is a type of nuclear receptor that is activated by binding any of the androgenic hormones, such as testosterone or dihydrotestosterone (DHT). By blocking these hormones from binding to the AR, Rosolutamide prevents the activation of androgen-responsive genes, thereby inhibiting the growth of androgen-dependent cancer cells.

Pharmacokinetics

The pharmacokinetic profile of Rosolutamide includes its absorption, distribution, metabolism, and excretion. As a nonsteroidal compound, it is absorbed orally and undergoes hepatic metabolism. The metabolites are then excreted primarily through the urine. The half-life of Rosolutamide allows for once-daily dosing, which can improve patient compliance.

Clinical Use

Rosolutamide is primarily used in the treatment of prostate cancer, particularly in cases where the cancer is resistant to other forms of hormone therapy. It is often used in combination with other treatments, such as gonadotropin-releasing hormone (GnRH) analogs, to achieve maximal androgen blockade.

Side Effects

Common side effects of Rosolutamide include gynecomastia, hot flashes, and gastrointestinal disturbances. As with other antiandrogens, there is a risk of liver toxicity, and liver function should be monitored during treatment. Patients may also experience fatigue and decreased libido.

Development and History

Rosolutamide was developed as part of a series of nonsteroidal antiandrogens aimed at providing effective treatment options for prostate cancer with fewer side effects compared to steroidal antiandrogens. Its development was part of a broader effort to improve the quality of life for patients undergoing hormone therapy for prostate cancer.

Related Pages

• Prostate cancer
• Androgen receptor
• Nonsteroidal antiandrogen
• Hormone therapy (oncology)