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Endocrine Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
As for the other steroidal aromatase inhibitors, testolactone is thought to exert its anticancer effect by inhibiting aromatase-mediated estrone synthesis from adrenal androstenedione, the major source of estrogen in postmenopausal women. Furthermore, based on in vitro studies, the aromatase inhibition is noncompetitive and irreversible which presumably accounts for the persistence of inhibition of estrogen synthesis after withdrawal of treatment.
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.
Introduction to Human Cytochrome P450 Superfamily
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
Inhibition of CYP19A1 has been of interest because of the enzyme role in estrogen regulation for treatment of estrogen-dependent cancers (Gobbi et al. 2014). The third-generation inhibitors that are in current clinical use include anastrozole, exemestane, and letrozole. Aromatase inhibitors are also beginning to be prescribed to men on testosterone replacement therapy as a way to keep estrogen levels from spiking once doses of testosterone are introduced to their systems. Exemestane is the only third-generation steroidal aromatase inhibitor and its efficacy as a first-line treatment in metastatic breast cancer has been demonstrated (Van Asten et al. 2014). Exemestane is mostly used as part of sequential adjuvant treatment after tamoxifen, but in this setting, it is also active in monotherapy.
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
Everolimus is a rapamycin analog that acts as a potent inhibitor of the mTOR signaling pathway. Clinical studies have shown that it has anticancer effects and that mTOR inhibition can enhance endocrine therapy’s efficacy in breast tumors [14]. Everolimus, combined with the steroidal aromatase inhibitor exemestane, represents an important treatment option for patients diagnosed with HR-positive, HER2-negative mBC. This combination was evaluated in the randomized, phase 3 BOLERO-2 trial. In this study, 724 post-menopausal patients with HR-positive advanced breast cancer who had disease recurrence or progression while on non-steroidal aromatase inhibitors, in both adjuvant and metastatic settings, were randomized to receive everolimus and exemestane or exemestane and placebo. After a median follow-up of 18 months, the median progression-free survival (PFS) was significantly longer with the everolimus-plus-exemestane group compared to placebo-plus-exemestane group; 7.8 versus 3.2 months, respectively; hazard ratio = 0.45 (95% confidence interval 0.38–0.54); p < 0.0001 [15].
Medical management of non-obstructive azoospermia: A systematic review
Published in Arab Journal of Urology, 2021
Mohammad H. Alkandari, Armand Zini
Common ways of increasing intra-testicular testosterone levels in men with NOA and hypergonadotrophic hypogonadism are by use of aromatase inhibitors (steroidal and non-steroidal) and anti-oestrogens. Aromatase inhibitors block aromatase enzyme, which converts testosterone to oestrogen in peripheral tissues. A comparative study on 140 infertile men with an abnormal testosterone:oestrogen ratio showed that both groups of aromatase inhibitors significantly improved that ratio but were never successful in producing sperm in the ejaculate [14]. The same study group also reached the conclusion that patients might benefit from this treatment if they are undergoing a sperm retrieval surgery. Another study showed similar results when men with low testosterone and either a low testosterone:oestrogen ratio or failed clomiphene were prescribed daily anastrozole (non-steroidal aromatase inhibitor) [15]. Although, none of these men had sperm in the ejaculate after treatment, 73% underwent successful micro-TESE after anastrozole.