Latest research on Exemestane

Exemestane is an oral steroidal aromatase inhibitor used in the adjuvant treatment of hormonally-responsive (also called hormone-receptor-positive, estrogen-responsive) breast cancer in postmenopausal women. It acts as a false substrate for the aromatase enzyme, and is processed to an intermediate that binds irreversibly to the active site of the enzyme causing its inactivation.

Latest findings

Examples of aromatase inhibitors include letrozole (Femara, Novartis, Basel, Switzerland), Anastrozole (Arimidex, AstraZeneca, London, UK), and Exemestane (Aromasin, Pfizer, New York, NY, USA), which are commonly used to treat breast cancer, and also thought to be helpful in the treatment of EC [167168]. [source, 2016]
Recent trials have indicated that adding Afinitor (everolimus) to Exemestane therapy against advanced breast cancer can significantly improve progression-free survival compared with Exemestane therapy alone. [source, 2016]
The objective of this study was to assess the efficacy and safety of abiraterone acetate with or without Exemestane (E) versus E alone to support the hypothesis that combined inhibition of androgen and Estradiol biosynthesis may provide clinical benefit to patients with NSAI-resistant ER+ postmenopausal breast cancer with and without AR+ disease. [source, 2016]
Patients were excluded if they had received prior Exemestane, Ketoconazole (non-topical, ≥7 days), aminoglutethimide or a CYP17 inhibitor. [source, 2016]
Patients were stratified according to the number of prior therapies in the metastatic setting (0 or 1 versus 2) and the setting of prior NSAI treatment (adjuvant versus metastatic), and randomized (1 : 1 : 1) to receive 1000 mg abiraterone acetate plus 5 mg Prednisone (AA), AA with 25 mg Exemestane (AAE), or 25 mg Exemestane alone (E) once daily in continuous 28-day cycles. [source, 2016]
Exemestane (25mg, daily) was given as a maintenance treatment until the disease progressed 15 months later; her CA 15-3 level increased, new liver metastases appeared and an osteo-medullary infiltration was diagnosed.She was treated with Docetaxel (100mg/m2, every three weeks) and showed a good response after four and half months (seven cycles). [source, 2015]
Patients received the following treatments: Letrozole 2.5 mg orally daily as a monotherapy or with Leuprolide Acetate or triptorelin acetate given intramuscularly at 3.75 mg every 28 days, CPA 100 mg twice a day as a monotherapy or combined with buserelin administered subcutaneously at 1500 μg daily in three doses during the first week and then reduced to 600 μg a day or Goserelin administered at 3.6 mg subcutaneously every 28 days, Exemestane 25 mg once daily or Anastrozole 1 mg once a day. [source, 2015]
This subtype of breast cancer initially shows a high overall response rate to hormonal treatments such as selective estrogen receptor (ER) modulators (eg, Tamoxifen), selective ER down-regulators (eg, fulvestrant), and aromatase inhibitors (ie, Anastrozole, Letrozole, and Exemestane). [source, 2015]
However, everolimus in combination with Exemestane has been investigated in patients with metastatic breast cancer resistant to hormone therapies and has demonstrated improved patient outcomes,9 leading to US Food and Drug Administration (FDA) approval for this indication. [source, 2015]
The positive outcomes of therapy with the everolimus plus Exemestane combination9 demonstrated that blocking an escape pathway clinically restores hormone sensitivity in breast cancer. [source, 2015]