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Aromatase inhibitors (AIs) are a class of drugs used in the treatment of breast cancer in postmenopausal women and in men, [1] [2] and gynecomastia in men. They may also be used off-label to reduce estrogen conversion when supplementing testosterone exogenously. They may also be used for chemoprevention in women at high risk for breast cancer.
Chemical structure of the endogenous androstenedione. In the human body, the enzyme aromatase converts androstenedione to estrogen. Aromatase is an enzyme that belongs to the cytochrome P450 family located on chromosome 15. In the human body, the aromatase consists of 10 β-strands (1 major sheet and 3 minor sheets) and 12 α-helixes.
Two distinct drug classes in which cardiotoxicity can occur are in anti-cancer and antiarrhythmic drugs. Anti-cancer drug classes that cause cardiotoxicity include anthracyclines, monoclonal antibodies, and antimetabolites. This form generally manifests as a progressive form of heart failure, but can also manifest as an harmful arrhythmia. [2]
The medication has been found to achieve 96.7% to 97.3% inhibition of aromatase at a dosage of 1 mg/day and 98.1% inhibition of aromatase at a dosage of 10 mg/day in humans. [3] [2] As such, 1 mg/day is considered to be the minimal dosage required to achieve maximal suppression of aromatase with anastrozole. [3]
Cardiotoxicity is the occurrence of heart dysfunction as electric or muscle damage, resulting in heart toxicity. [1] This can cause heart failure, arrhythmia, myocarditis, and cardiomyopathy in patients. [2] Some effects are reversible, while in others, permanent damage requiring further treatment may arise.
Steroidal aromatase inhibitors are a class of drugs that are mostly used for treating breast cancer in postmenopausal women. High levels of estrogen in breast tissue increases the risk of developing breast cancer and the enzyme aromatase is considered to be a good therapeutic target when treating breast cancer due to it being involved in the final step of estrogen biosynthetic pathway and also ...
A new meta-analysis confirms that semaglutide drugs like Ozempic are not only effective for weight loss, but can also protect the heart. However, certain doses and delivery systems can lead to ...
[13] [6] The medication was one of the first adrenal steroidogenesis inhibitors as well as the first aromatase inhibitor to be discovered and used clinically, and led to the development of other aromatase inhibitors. [18] [4] [30] [9] Along with testolactone, it is described as a "first-generation" aromatase inhibitor. [7]