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Oncology > Cancer Hormone Agents > Flashcards

Cancer Hormone Agents Flashcards

1
Q

Hormones are known as

A

1st messengers: natural substances

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2
Q

Glucocorticoids use

A

have anti proliferative and lympholytic properties

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3
Q

For breast and prostate cancer which classes of hormones are effective?

A

estrogen and androgen antagonists, steroid synthesis inhibitors, gonadotropin-releasing hormone (GnRH) analogues and antagonists

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4
Q

Hormone therapy interrupts

A

stimulatory axis created by androgens and estrogens

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5
Q

Are all cancers fueled by hormones?

A

NO

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6
Q

Breast cancer

A

estrogen and progesterone

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7
Q

Ovarian cancer

A

estrogen

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8
Q

Uterine/endometrial cancer

A

estrogen and progesterone

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9
Q

prostate cancer

A

testosterone

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10
Q

Is glucocorticoid receptos considered an oncogene?

A

NO

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11
Q

Glucocorticoids MOA

A

arrest growth and induce apoptosis in lymphoid tissue

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12
Q

Glucocorticoids for which cancer?

A

Lymphatic cancers

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13
Q

Glucocorticoids Usage?

A

cytotoxic agents for Acute leukemia in children and malignant lymphoma
suppresses mitosis in lymphocytes

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14
Q

What drugs are glucocorticoids?

A

Prednisone and Dexamethasone

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15
Q

What are the preferred agents for remission induction in multiple myeloma?

A

Glucocorticoids in combo with anthracyclines

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16
Q

Estrogen receptor?

A

drives cell growth, proliferation and metastasis in breast cancer

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17
Q

Androgen receptor?

A

drives cell growth, proliferation and metastasis in prostate cancer

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18
Q

Goal for breast cancer?

A

Reducing estrogen production and interrupting estrogen induced signaling

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19
Q

patients with ER+ and PR+

A

are more likely to respond to hormonal therapy

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20
Q

ER- and PR- ?

A

Do Not respond to hormonal therapy

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21
Q

If patient is ER+ and PR+ and HER2+

A

will have lower response to hormonal therapy

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22
Q

Drugs that are selective estrogen receptor modulators

A

Tamoxifen and Toremifene

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23
Q

Drugs that are selective estrogen receptor downregulator?

A

Fulvestrant

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24
Q

Drugs that decrease Estrogen levels?

A

Aromatase Inhibitors and GnRH agonists

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25
Q

Drugs of Aromatase Inhibitors?

A

Anastrazole, Letrozole, and Exemestane

26
Q

Drugs that are GnRH Agonists?

A

Triptorelin, Goserelin, Leuprolide

27
Q

Drugs that target Progesterone Receptors?

A

Medroxyprogesterone Acetate

28
Q

Tamoxifen drug?

A

Antiestrogenic drug for breast cancer and estrogenic agonist effects for non-beast tissues –>this gives the therapeutic effect

29
Q

Tamoxifen MOA?

A

Competitive Inhibitor of estrogen, binds to ER and antagonizes estrogen induced proliferation of human breast cancer

30
Q

Tamoxifen AE?

A

Vasomotor symptoms (hot flashes)

31
Q

The partial agonist activity of Tamoxifen?

A

increases the incidence of endometrial cancer by 2 to 3 folds especially in post-menopausal women

32
Q

Tamoxifen endocrine resistance

A

loss of ER expression
changes in coregulator expression
ER with mutations
Cross talk between the ER and the HER2 pathway

33
Q

Tamoxifen usage?

A

ER+ Metastatic breast cancer or given after removal of an ER+ tumor

34
Q

In postmenopausal women tamoxifen may be used but ________ are preferred.

A

Aromatase Inhibitors

35
Q

For preventive measures, Tamoxifen only works on?

A

ER+ tumors

36
Q

Palbociclib is a ?

A

CDK 4/6 Inhibitor

37
Q

Treament for postmenopausal women with HR+ metastatic breast cancer that has progressed on antiestrogen therapy?

A

Fulvestrant (alone) or with Palbociclib

38
Q

Fulvestrant MOA?

A

steroidal antiestrogen
-proteasomal degradation
Less than 1% excreted in urine

39
Q

Fulvestrant AE?

A

Hot Flashes

40
Q

Aromatase Inhibitors MOA?

A

Aromatase converts androgens to estrogens
-Blocks aromatase activity by reducing estrogen production

41
Q

Aromatase Inhibitors lowers only?

A

Extra-ovarian estrogen production

42
Q

Aromatase Inhibitors in premenopausal women ?

A

increase gonadotropin production and increases ovarian stimulation

43
Q

In postmenopausal women where is estrogen primarily produced?

A

Nonovarian tissues so an aromatase inhibitor would be preferred

44
Q

In premenopausal women estrogen is primarily produced where?

A

the ovaries, so AIs are not effective ALONE, must be combined with ovarian suppression such as GnRH analogues

45
Q

Standard care for adjuvant treatment of postmenopausal women with ER+ breast cancer?

A

Aromatase Inhibitors

46
Q

AIs: Type 1 inhibitors

A

are steroidal analogues of androstenedione–>binds covalently and irreversibly to the same site on AI causing aromatase inactivators

47
Q

AIs: Type 2 Inhibitors

A

Are non-steroidal—>binds reversibly to the heme group producing reversible inhibition

48
Q

What drug is a type 1 steroidal agent?

A

Exemestane-irreversibly inactivates aromatase

49
Q

What drug is a type 2 nonsteroidal imidazole?

A

Anastrazole and Letrozole both approved for postmenopausal women

50
Q

Anastrozole AE?

A

loss of bone mineral density so give Bisphosphonates

51
Q

Anastrazole use?

A

premenopausal women combined with ovarian suppression or following treatment prior to Tamoxifen in postmenopausal women

52
Q

Letrozole + CDK 4/6 inhibitor is for?

A

improved progression of HR+ Advanced Stage breast cancer

53
Q

For advanced stage breast cancer that has progressed on nonsteroidal type 2 AIs

A

mTOR inhibitor everolimus + Exemestane

54
Q

GnRH agonists MOA?

A

LH and FSH (gonadotropins) secreted and stimulate the testes and ovaries

55
Q

FSH stimulates

A

ovarian follicles

56
Q

LH stimulates

A

sex steroids from both sexes

57
Q

GnRH agonists MOA?

A

downregulate GnRH receptors in the pituitary gland this suppresses the release of gonadotropins and prevents follicular maturation—–>estrogen is reduced to those with postmenopausal women or whose had an oophorectomy

58
Q

GnRH agonists injection affect?

A

initial rise in luteinizing hormone and FSH but after 14-21 days a sustained decrease in LH and estrogen is observed

59
Q

GnRH agonists use?

A

Adjuvant therapy with AIs or Tamoxifen in very young women or high risk premenopausal women
use in metastatic breast cancer in premenopausal women

60
Q

If AI use plus GnRH analogue this increases _______

A

menopausal symptoms and sexual dysfunction

61
Q

Progesterone receptor durgs MOA?

A

binds to PR (breast and endometrium) —->activates PR causing antiproliferative in the endometrium

Oncology (10 decks)

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