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PHRM 864: Therapeutics IV > Anti-cancer Endocrine Therapies > Flashcards

Anti-cancer Endocrine Therapies Flashcards

1
Q

In what way are corticosteroids used in cancer treatment?

A
  • Used as pallative care to reduce inflammation and manage pain during the chemo
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2
Q

What are the three hormonal therapies that are disease specific?

A
  • Breast, Prostate, Endometrail Cancers
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3
Q

What is the molecular action for the steroid hormones?

A
  • Hormone passes into the cytoplasm where it binds to the receptor then it moves into nucleus
  • DNA will then transcript and tranlate
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4
Q

What are the two major classes of inhibiting steroid signaling?

A
  • STOP steroid receptor function
  • DECREASE production of steroids
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5
Q

Briefly explain the Hypothalamus-Pituitary-Reproductive Axis?

A
  • Hypothalamus makes GnRH that goes to the Pituitary
  • Pituitary makes LH/FSH that goes to the Reproductive Tract
  • Reproductive Tract makes estrogen/tesosterone
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6
Q

What receptors can be measured in tumors?

A
  • Estrogen and Progesterone
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7
Q

What hormone is produced in the pituitary gland?

A
  • LH/FSH
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8
Q

Where does the estrogen receptor primarily bind estrogen in the cell?

A
  • In the cytoplasm
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9
Q

What enzyme converts andostenedione to estrone making estrodial?

A
  • CYP19 or aromatase
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10
Q

What SERM is used within the treatment of Breast Cancer?

A
  • Tamoxifen & Raloxifene
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11
Q

What is Tamoxifen?

A
  • Its a prodrug that get metabolized by CYP2D6
  • FIRST drug approved for prevention of breast cancer
  • PRE and POSTmenopausal women
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12
Q

What is the mechanism of action for Tamoxifen?

A
  • MOA: both AGONIST & ANTAGONIST so it can block or active estrogen receptors
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13
Q

How does Tamoxifen act as an antagonist?

A
  • Inhibits both translocaiton and DNA binding
  • Stops breast cancer cell proliferation
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14
Q

How does Tamoxifen act as an agonist?

A
  • Increases the endometrail cancer risk by 3x
  • Increase bone density in postmenopausal women
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15
Q

In what population is Tamoxifen effective in?

A
  • BOTH pre and postmenopausal women
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16
Q

When should Tamoxifen be used?

A
  • Resected ER+/PR+ breast cancer [3-5 years] OR…
  • Metastatic ER+/PR+ breast cancer
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17
Q

What does Raloxifene [SERM] do differently than Tamoxifen?

A
  • NO endometrial hyperplasia
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18
Q

In what way does a SERD affect cancer?

A
  • Binds to the estrogen receptor then causes it to degraded
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19
Q

What SERD is used in breast cancer?

A
  • Fulvestrant
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20
Q

What is important to know about Fulvestrant?

A
  • “pure” Er antagonist = binds to ER and inhibits DNA binding causing the rapid degradation
  • Treatment for ER+ metastatic breast cancer in POSTmenopausal women
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21
Q

What is the function of Aromatase [CYP19]?

A
  • Helps convert androstenedione to estrone = estrogen
22
Q

What is the mechanism of action for the Aromatase inhibitors?

A
  • Block the synthesis of estrogens but NOT androgens or progesterone
23
Q

What is one way that POSTmenopasual women make estrogen?

A
  • Adiposytes are a source of estrogen
  • CANNOT target oravies as they make too much
24
Q

Are the the two classes of Aromatases?

A
  • Imidazole-Based non-steroidal & Steriodal inhibitors
25
Q

What are the non-steroidal aromatase inhibitors?

A
  • Anastrozole & Letrozole
26
Q

What is the mechanism of action for Anastrozole & Letrozole?

A
  • Competitve inhibitors for aromatase inhibition
27
Q

What is important to know about Anastrozole & Letrozole?

A
  • ER+ treatment of breast cancer in POSTmenopausal women
  • 1st line OR 3-5y after tamoxifen
28
Q

What is the steroidal aromastase inhibitor?

A
  • Exemestane
29
Q

What is the mechanism of action for Exemestane?

A
  • “suicide inhibitor”: binds to the active site of aromatase and reacts; covalently modifying it to inactive it; only way to make it work would be to destory it
30
Q

What is important to know about Exemestane?

A
  • ER+ breast cancer in POSTmenopausal women
31
Q

What are some of the toxicities for Exemestane?

A
  • Hot flashes, weight gain, increase cholesterol
32
Q

Which compound directly inhibits the activity of ER throughout the body?

A
  • Fulvestrant [pure antagoinst]
33
Q

What compound is known as a SERM?

A
  • Tamoxifen
34
Q

Breifly explain the Hypothalamic-Pituitary-Reproductive axis?

A
  • Hypothalamus makes GnRH that goes to pituitary
  • Pituitary makes LH/FSH that goes to reporducitve
  • Reproductive makes Estrogen or Testosterone
35
Q

Explain a way that FSH and LH are controlled?

A
  • Feedback inhibition: when there are too high of estrogen or testosterone levels in the body; it will stop the production of GnRH from being produced
36
Q

What is the mechanism of action for the Gonadotropin Releasing Hormone analogs?

A
  • Induces a surge of LH & FSH that will make A LOT of estrogen or testosterone then shutdown the hypothalamus from making GnRH
  • SAME in men
37
Q

What are the two GnRH analogs?

A
  • Leuprolide & Goserelin
38
Q

What is important to know about Lueprolide & Goserelin in women?

A
  • Have that surge
  • Indicated for PREmenopasual breast cancer = shuting down estrogen IN the ovaries
39
Q

What breast cancer drugs are good for POSTmenopausal women?

A
  • Tamoxifen [1st]
  • Anastrozole & Letrozole
  • Exemestane
  • Fulvestrant
40
Q

What breast cancer drugs are good for PREmenopausal women?

A
  • Goserelin & Leuprolide
  • Surgery
  • Tamoxifen [1st]
41
Q

What is prostate cancer?

A
  • A slowly progressing disease that is commonly diagnosed in men that is caused by rapidly and irreversibly converted by Type II 5-a reductase to dihydrotestosterone in protstate cells
42
Q

What is the normal range for Prostate Specific Antigen [PSA]?

A
  • > 6.5 ng/ml = possible cancer
43
Q

What are the GnRH Analogs that are used in men?

A
  • Same as women; Leuprolide & Goselerin
44
Q

What is important to know about Leuprolide & Goselerin in men?

A
  • Can cause Gynecomastoa [breast enlargement] and sexual dysfunction
45
Q

What is another drug that we can use to prevent DHT [dihydrotestosterone] production ?

A
  • Abiraterone
46
Q

What is the mechanism of action for Abiraterone?

A
  • Inhibits the function of 17 a-hydrolase and C17,20 lyase
  • Causes increased cholesterol
47
Q

What are the androgen receptor antagonists?

A
  • Enzalutamide, Apalutamide, Darolutamide
48
Q

What is the mechanism of action for the Androgen receptor antagonist?

A
  • Inhibits AR from binding to DNA; preventing translocation to the nucleus
49
Q

What is important to know about the AR Antagonists?

A
  • Approved for BOTH metastatic and non-metastatic prostate cancer
50
Q

What is unique about the action of tamoxifen as compared to fluvesterant?

A
  • It can activate ER in the bone

PHRM 864: Therapeutics IV (28 decks)

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