Chem167_L17_May30

Cytochrome p450s undesirable side eects

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Unformatted text preview: ause of death among women In US annually: > 200k women diagnosed, 40k will die > 2k men, ~400 will die Hormone- driven breast cancer •  80% of breast cancer cases •  Treatments: –  MedicaKons that block hormones from a6aching to cancer cells (selecKve estrogen receptor modulators, SERMs) –  MedicaKons that stop the body from making estrogen (aromatase inhibitors) –  Drugs that target estrogen receptors for destrucKon (Faslodex, fulvestrant) –  Surgery or other meds to stop ovarian hormone producKon (ovary removal) An5cancer drugs: hormone- based therapies Aromatase: catalyzes biosynthesis of estrogens from androgens InhibiKng this enzyme is a frontline chemotherapy for estrogen- dependent breast cancer à༎ an example of a non- metabolizing P450 enzyme à༎ uniquely highly substrate specific Catalyzes aroma5c ring forma5on: Converts testosterone to estradiol Converts androstenedione to estrone An5cancer drugs: hormone- based therapies Reversible compeKKve inhibitors of aromatase Binds to other cytochrome P450s à༎  undesirable side effects aminoglutethimide (Cytadren) Other compounds developed from aminoglutethimide as lead compound O]en prescribed to women who have completed tamoxifen therapy The retail price of Femara in the United States is approximately $1,015 per month Letrozole (Femara) Hercep5n (Trastuzumab) Monoclonal anKbody that binds to HER2 (Human Epidermal growth factor Receptor 2) protein Approximately 20- 30% of breast cancers have an amplificaKon of the HER2/neu gene or overexpression of its protein product Cost of course of treatment: $70- 100k per pa5ent per year Genentech + UC Los Angeles Hercep5n (Trastuzumab) “A subgroup analysis suggested that coamplificaKon of topoisom...
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This note was uploaded on 01/15/2014 for the course CHEM 167 taught by Professor Amaro during the Winter '13 term at UCSD.

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