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Endocrine Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Exemestane was approved by the FDA in 2005 for the adjuvant treatment of postmenopausal women with ER+ve early breast cancer who had received 2–3 years treatment with tamoxifen. Patients were then switched to exemestane to complete a total of five consecutive years of adjuvant hormonal therapy. The approval was based on a number of clinical trials including one Phase III trial involving 4,560 postmenopausal women. After 35 months of exemestane treatment at a dose of 25 mg/day, a 65% reduction in the risk of incidence of invasive breast cancer compared with placebo was observed. Another large open-label trial (the TEAM trial) showed that 25 mg/day of oral exemestane for 2–3 years of adjuvant therapy was generally more effective than five years of continuous adjuvant tamoxifen in the treatment of postmenopausal women with early-stage ER+ve breast cancer (or those of unknown status). In the UK, exemestane is now recommended by NICE for the adjuvant treatment of ER+ve early breast cancer in postmenopausal women following 2–3 years of tamoxifen therapy, and for advanced breast cancer in postmenopausal women in whom antiestrogen therapy has failed. It is now approved for similar indications in most countries of the world.
Hormone Receptors and Endocrine Therapy in Breast Cancer
Published in Sherry X. Yang, Janet E. Dancey, Handbook of Therapeutic Biomarkers in Cancer, 2021
Sherry X. Yang, Nancy E. Davidson
The Intergroup Exemestane Study (IES) evaluated the effect of exemestane after 2 to 3 years of tamoxifen for a total of 5 years versus tamoxifen for 5 years in 4,724 postmenopausal women with ER-positive or ER unknown breast cancer. After a median follow-up of 30.6 months, a significant improvement in DFS favoring the exemestane arm was reported [60]. In a subsequent analysis after a median follow-up of 55.7 months, DFS benefit was confirmed although OS benefit was not statistically significant [61]. Patients on exemestane had more arthralgia, diarrhea, hypertension, fractures, arthritis, musculoskeletal pain, carpal tunnel syndrome, insomnia, and osteoporosis. Those on tamoxifen had more gynecologic symptoms, thromboembolic disease, endometrial hyperplasia and uterine polyps.
Hormonal therapy of breast cancer
Published in A. R. Genazzani, Hormone Replacement Therapy and Cancer, 2020
Exemestane has also been compared with megestrol acetate. Given orally at a dose of 25 mg in a study of 769 patients, exemestane demonstrated a longer time to progression (20 weeks vs. 17 weeks, p = 0.037), time to treatment failure and overall survival at a median follow-up of 11 months (not reached vs. 28 months, p = 0.039). Response rates favored exemestane (15% vs. 12%) in both visceral and non-visceral disease, although the difference did not reach statistical signifi cance37. A separate, phase II study of 242 patients also addressed the activity of exemestane following the failure of a non-steroidal aromatase inhibitor (44% had received aminoglutethimide). The response rate was 7%, and an additional 17% of patients had stable disease for at least 6 months. The median duration of response was 14 months, and the median time to progression was 15 weeks42.
A drift on liposomes to proliposomes: recent advances and promising approaches
Published in Journal of Liposome Research, 2022
Neha Dhiman, Jayrajsinh Sarvaiya, Poorti Mohindroo
Jukati et al. prepared Exemestane containing proliposome gel using PC and cholesterol and evaluated them for physicochemical and permeability characteristics. Exemestane is reported as a third-generation steroidal aromatase inhibitor, used to treat progressive breast cancer in post-menopausal women (Deeks and Scott 2009, Goss et al.2011). Low solubility and comprehensive first-pass metabolism, reflect low bioavailability (42%) of the drug. The size of the PLs was reported as 440–700 nm, and a drug release study was done by the research group. Pharmacokinetic studies revealed that the slow elimination of Exemestane from systemic circulation reflects the sustained release of drugs from PLs. Thus, proliposomal gels prove to be efficient carriers for improved and sustained transdermal delivery of Exemestane (Valle et al.2005, Jukanti et al.2011).
From clinical trials to clinical practice: the use of everolimus and exemestane in the treatment of hormone receptor-positive metastatic breast cancer: real-world data
Published in Journal of Chemotherapy, 2022
Hikmat Abdel-Razeq, Baha' Sharaf, Hazem Abdulelah, Nayef Abdel-Razeq, Mourad Salam, Bayan Inserat, Rayan Bater
Patients were treated using everolimus in combination with exemestane. Everolimus was started at a standard dose of 10 mg orally once daily, while exemestane was given at a dose of 25 mg orally once daily. Before starting treatment, the following tests were performed: complete blood count (CBC) with differential, creatinine, blood urea nitrogen (BUN), random glucose, total bilirubin, alanine transaminase (ALT); aspartate transaminase (AST); alkaline phosphatase (ALP); lactate dehydrogenase (LDH), Chest X-ray, oxygen (O2) saturation, hepatitis B surface antigen (HBsAg) and hepatitis B core antibodies (HBcAb). CBC, liver, and kidney function tests were obtained before subsequent cycles. Four weeks of treatment comprised one cycle, and treatment was continued until disease progression or unacceptable toxicity was encountered.
Redox-sensitive TRP channels: a promising pharmacological target in chemotherapy-induced peripheral neuropathy
Published in Expert Opinion on Therapeutic Targets, 2021
Ramandeep Singh, Pratik Adhya, Shyam Sunder Sharma
Aromatase inhibitors (AIs), like exemestane, letrozole, and anastrozole, are endocrine therapies that are often employed as adjuvant therapies in postmenopausal women with hormone-dependent breast cancer [66]. These agents are effective in preventing the recurrence of breast cancer through estrogen deprivation. Adverse effects have been reported that impair the quality of life of the patient and compliance to treatment [67]. Adverse effects of AIs include musculoskeletal symptoms, for example, joint pain, joint stiffness, tendinitis, carpal tunnel syndrome and bone pain. Moreover, AIs lead to the development of neuropathic pain in almost 50% of patients [68,69]. In clinical studies, patients develop pain after approximately 2 months of treatment initiation and after 6 months, the pain intensity peaks [70]. The cumulative dose of these agents that causes neuropathy is unknown in clinical scenario however, preclinical studies have demonstrated that a 0.5 mg/kg intragastric administration in mice have led to letrozole-induced mechanical allodynia [69]. Mechanical allodynia was also observed in ovariectomized rats treated with a single intraperitoneal dose of 1 mg/kg or 5 mg/kg letrozole [71]. Exemestane induces neuropathic pain in mice on a single intragastric administration of 10 mg/kg [69].