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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.
Non-Steroidal Aromatase Inhibitors (NSAIs) are one of two categories of aromatase inhibitors (AIs). AIs are divided into two categories, steroidal aromatase inhibitors (SAIs, type 1 inhibitors) and non-steroidal aromatase inhibitors (type 2 inhibitors) that is based on their mechanism of action and structure.
Pages in category "Aromatase inhibitors" The following 76 pages are in this category, out of 76 total. This list may not reflect recent changes. ...
This is a list of 5α-reductase inhibitors (5α-RIs), drugs which inhibit one or more isoforms of the enzyme 5α-reductase.This enzyme is responsible for the conversion of the androgen hormone testosterone into the more potent dihydrotestosterone (DHT) and is essential for the production of neurosteroids like allopregnanolone, tetrahydrodeoxycorticosterone (THDOC), and 3α-androstanediol from ...
Letrozole is an orally active, nonsteroidal, selective aromatase inhibitor and hence an antiestrogen. It prevents aromatase from producing estrogens by competitive, reversible binding to the heme of its cytochrome P450 unit. The action is specific, and letrozole does not reduce production of corticosteroids. [citation needed
Like the aromatase inhibitors formestane and atamestane, exemestane is a steroid that is structurally similar to 4-androstenedione, the natural substrate of aromatase. It is distinguished from the natural substance only by the methylidene group in position 6 and an additional double bond in position 1. [15]
SERMs that have not been approved for medical use include arzoxifene, brilanestrant, clomifenoxide (clomiphene N-oxide; metabolite of clomifene), [3] droloxifene (3-hydroxytamoxifen), etacstil, fispemifene, GW-7604 (4-hydroxyetacstil; metabolite of etacstil), idoxifene (pyrrolidino-4-iodotamoxifen), levormeloxifene ((L)-ormeloxifene), miproxifene, nafoxidine, nitromifene (CI-628), NNC 45-0095 ...
Tyrosine kinase inhibitor (TKI) with selective activity against RET, VEGFR-2 and EGFR: Medullary thyroid cancer. Diarrhoea, hypertension, QT interval prolongation, depression, electrolyte anomalies, hypothyroidism and GI perforation (uncommon). 2.3 mTOR inhibitors: Everolimus: PO: mTOR inhibitor.
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