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kyleannkelsey
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What drug is lapatinib (Tykerb) used in combo with?
Capecitabine
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What are the Anti-Mitotic Breast Cancer Drugs?
- ixabepilone (Ixempra)
- eribulen mesylate (Halaven)
- ixabepilone (Ixempra)
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What is the MOA for ixabepilone (Ixempra)?
- Binds to beta tubulin subunits of microtubules
- M phase cell-cycle specific
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What is the indication for ixabepilone (Ixempra)?
Monotherapy or combo with capecitabine for metastatic breast cancer resistant to anthracyclines (like doxorubicin) and taxanes (like Paclitaxel or docetaxel)
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What are the side effects for ixabepilone (Ixempra)?
- Myelosuppression (due to inhibition of mitosis)
- GI
- peripheral neuropathy
- rash (hypersensitivity)
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What is the MOA for eribulen mesylate (Halaven)?
- Microtubule inhibitor isolated from marine sponge
- M phase specific
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What are the indications for eribulen mesylate (Halaven)?
Metastatic breast cancer
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What are the SE for eribulen mesylate (Halaven)?
Myelosuppression, GI, peripheral neuropathy
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What types of Prostate Cancer Drugs are availabale?
- Androgen Receptor Antagonists
- Gonadotropin Releasing Hormone agonist or Luteinizing Hormone-Releasing hormone agonists
- Gonadotropin Releasing Hormone antagonist or Luteinizing Hormone-Releasing hormone antagonists
- Non-hormonal drugs
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What are the Androgen receptor antagonists?
- bicalutamide
- flutamide
- nilutamide
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What is the general mechanism of androgen receptor antagonists?
- Stop testosterone from entering cells
- DO NOT EFFECT TESTOSTERONE LEVELS
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Which Androgen receptor antagonist binds the most tightly to angrogen receptors?
Nilutamide
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Which Andorgen receptor has the longest half-life?
bicalutamide (Casodex)
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Does bicalutamide or flutamide bind tighter to angrogen reeceptors?
bicalutamide (Casodex) (though still less tightly than Nilutamide)
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What is the route of administration for bicalutamide (Casodex)?
oral once a day
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bicalutamide (Casodex) is a derivative of what?
Fluamide
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What is the MOA of bicalutamide (Casodex)?
Blocks androgen receptors primarily in prostate tumor cells depriving them of androgenic stimulation.
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What is the indication of bicalutamide (Casodex)?
Metastatic prostate cancer
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What are the SE for bicalutamide (Casodex)?
- Chemical castration:
- Hot flashes, gynecomastia, vomiting, diarrhea, hepatotoxicity
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How is flutamide (Eulexin) taken?
Orally 3 times a day
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What is the MOA of flutamide (Eulexin)?
Blocks androgen receptors in tumor cells depriving them of androgenic stimulation
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What is the MOA of flutamide (Eulexin) ?
Metastatic prostate cancer
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What are the SE for flutamide (Eulexin)?
- Hot flashes,
- gynecomastia
- vomiting
- diarrhea
- hepatotoxicity
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What is the MOA for nilutamide (Nilandron)?
Blocks all androgen receptors, including adrenal androgen receptors
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What is the indication for nilutamide (Nilandron)?
Metastatic prostate cancer for patients with surgical castration
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Why is nilutamide (Nilandron) used in patients after surgical castration?
Adrenal gland still produces testosterone
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What are the SE for nilutamide (Nilandron)?
- GI
- gynecomastia
- hot flashes
- difficulty in adapting to dark
- pneumonia
- NOT WELL TOLERATED
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What are the Gonadotropin Releasing Hormone agonist or Luteinizing Hormone-Releasing hormone AGONISTS?
- leuprolide (Lupron)
- goserelin (Zoladex)
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What are the indications for leuprolide (Lupron) and goserelin (Zoladex)?
Palliative care in Metastatic prostate cancer
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What is the MOA for leuprolide (Lupron) and goserelin (Zoladex)?
- Suppresses androgen production in the testes
- GnRH is continuously supplied
- Inhibits the release of gonadotropin from the pituitary = downregulating testosterone synthesis
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Do leuprolide (Lupron) and goserelin (Zoladex) reduce adrenal androgens?
No, only testicular
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Can you use leuprolide (Lupron) and goserelin (Zoladex) instead of surgical castration?
Yes
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Why would you want to use leuprolide (Lupron) and goserelin (Zoladex) with androgen receptor antagonist?
To counteract testosterone flair
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What are the SE for leuprolide (Lupron) and goserelin (Zoladex)?
Hot flashes, loss of libido, fatigue, nausea/vomiting, loss of muscle mass, increased adipose tissue, possible bone loss
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What hormone other than Testosterone do leuprolide (Lupron) and goserelin (Zoladex) inhibit?
Estrogen
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What is the Gonadotropin Releasing Hormone antagonist or Luteinizing Hormone-Releasing hormone ANTAGONIST?
degarelix (Firmagon)
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What is the MOA for degarelix (Firmagon)?
- Decreases production of testosterone
- By blocking GnRH receptors in pituitary
- Decreases release of LH and FSH
- Deprives testes of stimulation needed for testosterone production
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What are the indications for degarelix (Firmagon)?
Ppalliative advance prostate cancer in those patients not eligible for GnRH agonist or don’t want surgical castration
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What are the SE for degarelix (Firmagon)?
No tumor flare, hot flashes, gynecomastia, POTENTIAL LONG QT SYNDROME, libido, impotence
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What are the Non-Hormonal Prostate Cancer Drugs?
- estramustine (Estracyte)
- ketoconazole
- sipuleucel-T (Provenge)
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What is the MOA of estramustine (Estracyte)?
- Conjugate of estradiol phosphate conjugated with a nitrogen mustard
- Cell cycle specific in M phase
- Inhibits microtubule structure, function and assembly
- Active against estrogen receptor (-) tumor cells including prostate cancer cells
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Does estramustine (Estracyte) have alkylating activity?
No
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What are the indications for estramustine (Estracyte)?
Hormone refractory, metastatic prostate cancer
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What is the MOA for sipuleucel-T (Provenge)?
- Biological Response Modifier = Active Cellular Immunotherapy ( enhance immunoresponse)
- Create an antigen presenting cell from patients own cells that present sipuleucel-T and reinfused back into the patient
- Altered T Cells proliferate and attack cancer cells
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What are the SE for estramustine (Estracyte)?
GI, thromboembolism (from the estradiol), gynecomastia
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What is the indication for sipuleucel-T (Provenge)?
Asymptomatic or minimally symptomatic, metastatic, androgen-independent (hormone refractory) prostate cancer
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What are the SE for sipuleucel-T (Provenge)?
Acute infusion reactions (fever, respiratory, fatigue, nausea, vomiting)
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What is the MOA of abiraterone acetate (Zytiga)?
- Anti-androgen
- Inhibits 17 α-hydroxylase (CYP17) more effectively than ketoconazole.
- Enzyme required for androgen biosynthesis.
- Inhibits in all tissues including testicles, adrenal gland and prostate tumors.
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abiraterone acetate (Zytiga) is used in combo with what else and why?
- Prednisone due to increased mineralocorticoid levels from CYP17 inhibition
- Co-administer with corticosteroid to counter increased production of mineralocorticoids
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What is the indication for abiraterone acetate (Zytiga)?
Metastatic castration-resistant prostate cancer (androgen dependent), resistant to docetaxel.
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What is the pregnancy category of abiraterone acetate (Zytiga) ?
Pregnancy category X
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What are the SE for abiraterone acetate (Zytiga)?
Hypertension, hypokalemia, fluid retention, QT elongation, Joint and muscle discomfort
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