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Therapeutics IV > Anti-cancer Endocrine Therapies_Edit > Flashcards

Anti-cancer Endocrine Therapies_Edit Flashcards

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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
Primary application of aromatase inhibitor estradiol suppression for what women
postmenopausal
26
Name two imidazole-based NON-steroidal aromatase inhibitors
anastrozole and letrozole
27
anastrozole and letrozole for which women
breast cancer in postmenopausal women first line therapy OR when started after 3 - 5 years
28
Name steroidal aromatase inhibitors
exemestane and androstenedione
29
exemestane for which women
tx of estrogen-responsive breast cancer in postmenopausal women who have progressed on anti-estrogen therapy NOT used in premenopausal women
30
Which compound directly inhibits the activity of the ER receptor throughout the entire body
Fulvestrant
31
What do aromatases convert
androstenedione --> estrone and testosterone --> estradiol
32
Letrozole and anastrozole are what type of inhibitors
competitive
33
how does exemestane bind and what does it do
binds irreversibly at active site and inactivates enzyme
34
decreased FSH leads to
decreased aromatase and decreased estrogen
35
Describe GnRH analogs
peptide analogs of the neurohormone GnRH with modified amino acids to increase potency and reduce degradation
36
GnRH inhibits...
...estrogen-dependent breast cancers in women
37
name GnRH analogs
leuprolide goserelin triptorelin buserelin
38
leuprolide and goserelin used in what type of women
premenopausal
39
For post menopausal women, what hormone therapy can be used
Tamoxifen Nonsteroidal aromatase inhibitors (anastrozole, letrozole) Steroidal aromatase inhibitor (exemestane) Pure anti-estrogens (fulvestrant)
40
For pre menopausal women, what hormone therapy can be used
GnRH agonists (goserelin and leuprolide) Surgical oophorectomy Tamoxifen
41
what drives tumor resistance
heterogeneity
42
Name 3 CDK4/6 inhibitors CDK = cyclin dependent kinase
palbociclib ribociclib abemaciclib
43
How is testosterone converted to dihydrotestosterone
Type II 5-alpha reductase
44
AR is what kind of receptor
cytoplasmic
45
binding of AR to DHT does what
leads to translocation to the nucleus and action of genes that drive cell growth
46
What PSA level is suggestive of prostate cancer
>6.5 ng/ml
47
GnRH analogs in men
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
Name GnRH analogs in men
leuprolide acetate and goserelin
49
use GnRH in men when
primary indication is for the palliative tx of advanced prostate cancer
50
Name GnRH antagonists for men
abarelix and degarelix
51
CYP17 is also
17alpha-hydrolase/C17,20 lyase
52
What does CYP17 do
CYP17 catalyzes the conversion of pregnenolone and progesterone to DHEA and androstenedione
53
What does abiraterone do
inhibit the function of CYP17
54
Name 5-alpha-reductase inhibitors
finasteride dutasteride
55
what does finasteride do
inhibits type II isoform of 5-alpha-reductase
56
what does dutasteride do
inhibits type I and type II isoform of 5-alpha reductase
57
Prolonged use of 5-alpha-reductase inhibitors does what
select for more aggressive AR-independent tumors
58
Name androgen receptor (AR) antagonists
enzalutamide darolutamide apalutamide
59
AR antagonists approved for what
metastatic and non-metastatic prostate cancer
60
177Lu-PSMA-617 is
a Purdue success story
61
describe 177Lu-PSMA-617
- 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
Mechanisms of resistance to endocrine therapy for prostate cancer
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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