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Topoisomerase Inhibitors
create torsional stress, fragments DNA chains and destroys the cell
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Etoposide -- Etopophos and Teniposide -- Vumon
- cell cycle specific
- inhibits DNA topoisomerase II
- prodrug -- 3A4
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Irinotecan -- Camptosar
- inhibits topoisomerase I
- 2000X more active metabolite
- severe N/V
- UGT1A1*28 -- will accumulate
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topotecan -- Hycamtin
- inhibits topoisomerase I
- don't give to pts with <1500 baseline neutrophil counts
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Hormone and Hormone Antagonists -- classes
- androgens -- progestin
- antiandrogens
- GnRH analogs
- Estrogens -- antiestrogens
- Aromatase inhibitors
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Bicalutamide -- Casodex
- antiandrogen
- advanced prostate cancer
- non-steroid competitive inhibitor
- inhibits testosterone in peripheral tissue
- causes gynecomastia
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Nilutamide -- Nilandron
- antiandrogen
- non-steroid that inhibits cellular uptake of T and nuclear binding
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Megesterol -- Megace
- progestin
- anti-leutinizing effect mediated by pituitary (centrally acting)
- appetite stimulant in HIV related cachexia
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Medroxyprogesterone -- Depo-Provera
- progestin
- inhibits secretion of pituitary gonadotropin
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GnRH analogs -- drugs (4)
- Leuprolide -- Lupron
- Goserelin -- Zoladex
- Triptorelin -- Trelstar Depot
- Degarelix -- Firmagon
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Leuprolide -- Lupron
- GnRH analog
- decreased androgen production
- add Casodex for peripheral inhibition
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Goserelin -- Zoladex and Triptorelin -- Trelstar Depot
Advanced prostate cancer
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Degarelix -- Firmagon
- prostate cancer
- GnRH receptor antagonist
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Estermustine -- Emcyt
- prodrug mustard alkylating agent
- estrogen delivers site specific alkylating agent
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Anti-estrogens -- drugs
- Tamoxifen -- Soltamox
- Toremifene -- Fareston
- Fulvestrant -- Faslodex
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Tamoxifen -- Soltamox
- non-steroid anti-estrogen that competes with estradiol for estrogen receptors
- most widely used RX for breast cancer
- metab -- CYP2D6 (SSRIs)
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Toremifene -- Fareston
- breast cancer
- nonsteroid anti-estrogen that competes with estradiol for estrogen receptors
- metab -- 3A4
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Fluvestrant -- Faslodex
- steroidal estrogen antagonist -- down regulatesthe estrogen receptor protein
- metab --3A4
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Aromatase inhibitors -- drugs (3)
- Letrozole -- Femara
- Anastrozole -- Arimidex
- Exemestane -- Aromasin
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Aromatase inhibitors -- info
- inhibitors of the aromatase enzyme
- NO cross resistance -- can use exemestane if resistant to other 2
- exemestane is a suicide substrate
- exemestane is steroidal
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anastrozole -- Arimidex
- gold standard
- not effective for ER negative tumors
- used when tamoxifen fails
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Sodium iodide (131I) -- Hicon
- thyroid cancer and tx of hyperthyroidism
- have to deplete iodine stores
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Sodium iodine (123I)
- thyroid evaluation
- electron capture decay -- diagnostic, short acting
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Strontium-89 Chloride -- Metastron
- use normal toilet, no urinals to decrease transmission of radioactivity
- mimics Ca2+, used for bone type cancers
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Brachytherapy -- radioactive implants
- Pharmaseed
- contain either Iodine-125 or Palladium-103
- prostate cancer -- localized delivery
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