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Therapeutics IV > Anti-cancer Endocrine Therapies_Edit > Flashcards

Anti-cancer Endocrine Therapies_Edit Flashcards

1
Q

What regulates the proliferation of breast cancer, prostate cancer and endometrial cancer

A

HORMONES

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2
Q

Receptors are ___________ hormone-dependent transcription factors

A

cytosolic

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3
Q

Describe steroid receptor signal transduction

A

When ligand enters cell and binds to receptor, ligand-receptor complex translocated to nucleus, binds to DNA promoters and induces transcription

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4
Q

Two major classes of endocrine therapy

A
  1. Stop steroid receptor function

2. Decrease production of steroids

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5
Q

Well-differentiated tumors are more likely to be ____

A

ER+

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6
Q

Poorly differentiated tumors are generally ____

A

ER-

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7
Q

Which hormone(s) are produced in the pituitary gland?

A

LH and 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 androstenedione to estrone?

A

CYP19

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10
Q

Tamoxifen is a __________

A

pro-drug

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11
Q

What converts tamoxifen to high-affinity hydroxylated and demethylated metabolites?

A

CYP2D6

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12
Q

Tamoxifen Pharmacology

A

SERM

both agonist and antagonistic activities

block estrogen-dependent breast cancer cell proliferation

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13
Q

Which women for Tamoxifen

A

Pre- and postmenopausal women

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14
Q

Tamoxifen primary use for tx

A

tx for resected ER+/PR+ breast cancer (3 - 5 years Rx)

also used for the tx of metastatic ER+/PR+ breast cancer

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15
Q

Beneficial effects of Tamoxifen

A

Breast: anti-proliferative

Blocks bone resorption

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16
Q

AE of Tamoxifen

A

hot flashes; thermoregulation

increased coagulability; clots, VTE risk

Endometrial hyperplasia

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17
Q

Beneficial effects of Raloxifene

A

Preventative to breast cancer

No endometrial hyperplasia (differs from tamoxifen)

Blocks bone resorption; increases bone mass is osteoporosis

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18
Q

Name a SERD

A

Fulvestrant

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19
Q

What effect does fulvestrant have

A

ER antagonist

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20
Q

What types of breast cancer does fulvestrant treat?

A

Approved for tx of ER+ metastatic breast cancer

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21
Q

What type of women for fulvestrant

A

postmenopausal women who have progressed on other antiestrogen therapy

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22
Q

Alternate name for CYP19

A

aromatase

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23
Q

Adipocytes are a source of estrogen in what type of women

A

postmenopausal

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24
Q

What is the primary target of inhibitors

A

peripheral tissue (adipose tissue)

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25
Q

Primary application of aromatase inhibitor estradiol suppression for what women

A

postmenopausal

26
Q

Name two imidazole-based NON-steroidal aromatase inhibitors

A

anastrozole and letrozole

27
Q

anastrozole and letrozole for which women

A

breast cancer in postmenopausal women

first line therapy OR when started after 3 - 5 years

28
Q

Name steroidal aromatase inhibitors

A

exemestane and androstenedione

29
Q

exemestane for which women

A

tx of estrogen-responsive breast cancer in postmenopausal women who have progressed on anti-estrogen therapy

NOT used in premenopausal women

30
Q

Which compound directly inhibits the activity of the ER receptor throughout the entire body

A

Fulvestrant

31
Q

What do aromatases convert

A

androstenedione –> estrone and testosterone –> estradiol

32
Q

Letrozole and anastrozole are what type of inhibitors

A

competitive

33
Q

how does exemestane bind and what does it do

A

binds irreversibly at active site and inactivates enzyme

34
Q

decreased FSH leads to

A

decreased aromatase and decreased estrogen

35
Q

Describe GnRH analogs

A

peptide analogs of the neurohormone GnRH with modified amino acids to increase potency and reduce degradation

36
Q

GnRH inhibits…

A

…estrogen-dependent breast cancers in women

37
Q

name GnRH analogs

A

leuprolide

goserelin

triptorelin

buserelin

38
Q

leuprolide and goserelin used in what type of women

A

premenopausal

39
Q

For post menopausal women, what hormone therapy can be used

A

Tamoxifen

Nonsteroidal aromatase inhibitors (anastrozole, letrozole)

Steroidal aromatase inhibitor (exemestane)

Pure anti-estrogens (fulvestrant)

40
Q

For pre menopausal women, what hormone therapy can be used

A

GnRH agonists (goserelin and leuprolide)

Surgical oophorectomy

Tamoxifen

41
Q

what drives tumor resistance

A

heterogeneity

42
Q

Name 3 CDK4/6 inhibitors

CDK = cyclin dependent kinase

A

palbociclib

ribociclib

abemaciclib

43
Q

How is testosterone converted to dihydrotestosterone

A

Type II 5-alpha reductase

44
Q

AR is what kind of receptor

A

cytoplasmic

45
Q

binding of AR to DHT does what

A

leads to translocation to the nucleus and action of genes that drive cell growth

46
Q

What PSA level is suggestive of prostate cancer

A

> 6.5 ng/ml

47
Q

GnRH analogs in men

A

just as in women, prolonged treatment with GnRH analogs leads to a decrease in LH production

transient increases in testosterone, but overall results in “chemical castration

48
Q

Name GnRH analogs in men

A

leuprolide acetate and goserelin

49
Q

use GnRH in men when

A

primary indication is for the palliative tx of advanced prostate cancer

50
Q

Name GnRH antagonists for men

A

abarelix and degarelix

51
Q

CYP17 is also

A

17alpha-hydrolase/C17,20 lyase

52
Q

What does CYP17 do

A

CYP17 catalyzes the conversion of pregnenolone and progesterone to DHEA and androstenedione

53
Q

What does abiraterone do

A

inhibit the function of CYP17

54
Q

Name 5-alpha-reductase inhibitors

A

finasteride

dutasteride

55
Q

what does finasteride do

A

inhibits type II isoform of 5-alpha-reductase

56
Q

what does dutasteride do

A

inhibits type I and type II isoform of 5-alpha reductase

57
Q

Prolonged use of 5-alpha-reductase inhibitors does what

A

select for more aggressive AR-independent tumors

58
Q

Name androgen receptor (AR) antagonists

A

enzalutamide

darolutamide

apalutamide

59
Q

AR antagonists approved for what

A

metastatic and non-metastatic prostate cancer

60
Q

177Lu-PSMA-617 is

A

a Purdue success story

61
Q

describe 177Lu-PSMA-617

A
  • 177Lutetium (Lu) is a radioisotope.
  • 177Lu is conjugated to a peptide that binds to Prostate Specific Membrane Antigen (PSMA).
  • In this way the radiation is effectively “delivered” to the prostate tumors.
  • 177Lu radiation only works over short distances, limiting damage to surrounding tissues.
62
Q

Mechanisms of resistance to endocrine therapy for prostate cancer

A

Mutations in AR can arise that result in androgen independent activation and prevent binding of AR antagonists.

Overall, this is referred to castration resistant prostate cancer (CRPC).

Development of new treatments for CRPC is an active area of research.

Therapeutics IV (19 decks)

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