Exemestane is a potent oral steroidal aromatase inhibitor primarily used in the treatment of estrogen-receptor positive breast cancer in postmenopausal women. By irreversibly binding to the aromatase enzyme, exemestane effectively reduces estrogen levels in the body, thereby inhibiting the growth of estrogen-dependent cancer cells.

This mechanism of action makes it a critical component in hormone therapy, particularly for patients who have shown resistance to other treatments such as tamoxifen. Exemestane is often utilized in sequential therapy, following initial treatment with non-steroidal aromatase inhibitors, to enhance therapeutic outcomes.

Its pharmacokinetic profile is characterized by rapid absorption and extensive distribution, with a half-life that supports once-daily dosing. Exemestane is metabolized primarily in the liver, and its metabolites are excreted via urine and feces, necessitating careful consideration in patients with hepatic or renal impairment.

Common side effects include hot flashes, fatigue, and joint pain, which are generally manageable but require monitoring. Due to its impact on bone density, concurrent use of bone-modifying agents may be recommended to mitigate the risk of osteoporosis.

Exemestane's efficacy and safety profile make it a valuable option in the management of hormone-sensitive breast cancer, offering a targeted approach that aligns with personalized treatment strategies. Its role in reducing recurrence risk and improving survival rates underscores its importance in oncological care.