Antineoplastic Hormones - Trachte Flashcards
What is prostate cancer treated with (drug classes)?
GnRH agonists to suppress testosterone production
GnRH antagonists to suppress testosterone production
5alpha reductase inhibitors to suppress dihydrotestosterone production
Testosterone receptor antagonists
What is Breast cancer treated with (drug classes)?
GnRH agonists to suppress estradiol & estrone production
GnRH antagonists to suppress estradiol & estrone production
Estrogen receptor modulators to block trophic actions of estrogens on the breast
Estrogen receptor disrupters to block trophic action of estrogen on the breast
Aromatase inhibitors to prevent estradiol or estrone production
Anthracyclines are considered “standard of care” (Doxorubicin)
What are the two GnRH receptor agonists (used to inhibit FSH and LH secretion) that will only inhibit testosterone production if administered constantly to desensitize system?
Goserelin and Leuprolide
initially stimulate system, so it is given with a testosterone receptor antagonist
What is the GnRH receptor antagonist used to inhibit FSH and LH secretion?
Degarelix
What are the two Androgen Biosynthesis inhibitor (5 alpha reductase inhibitors) that prevents conversion of testosterone to dihydrotestosterone in order to have a trophic effect on prostate tissue?
Finasteride and Dutasteride
not used as much as GnRH agonists
What is the Androgen biosynthesis inhibitors (17 alpha hydroxylase inhibition) that prevents testosterone synthesis?
Abiraterone acetate
third or fourth line Tx
What are the two Testosterone receptor antagonists that work by blocking testosterone receptors (via transcriptional regulation)?
Bicalutamide and Flutamide
What is the dihydrotestosterone agonist?
Oxandralone
What does the actual treatment of Prostate Cancer involve?
Typically involves depot administration of goserelin or leuprolide in combination with an anti-androgen (bicalutamide => testosterone receptor antagonist)
Results in complete androgen deprivation
Usually bicalutamide is only administered for the first few weeks to prevent the effect of the GnRH agonists which initially stimulate the production of testosterone & dihydrotestosterone.
What drug used in the treatment of prostate cancer blocks pregnenolone synthesis?
Aminoglutethimide
What are the two Aromatase inhibitors that prevent the conversion of testosterone to estradiol and androstendione to estrone?
Anastrazole
Exemestane (irreversibly inhibits enzyme)
What are the three selective estrogen receptor modulators (SERM) that are agonists on some estrogen receptors and antagonists at others; therefore, they are termed “modulators” (all antagonize the trophic actions of estrogens on the breast)?
Tamoxifen, Raloxifene, and Tormifene
What is the selective estrogen receptor disrupter (SERD) that inhibits all estrogen receptor actions and suppresses receptor number?
Fulvestrant
weakens bone, so not used often
What are selective estrogen receptor modulators preferred over estrogen receptor disrupters?
Estrogen has proliferative effects on breast and uterus, but anti-resorptive effects on the bone.
Leads to osteoporosis and uterine cancer.
In what forms of breast cancer is Tamoxifen most successful in treating?
Estrogen receptor + and PR+
