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PHRM 864 > Endocrine therapies > Flashcards

Endocrine therapies Flashcards

1
Q

Breast cancer

A

estradiol

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2
Q

Endometrial cancer

A

estradiol

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3
Q

Prostate cancer

A

DHT

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4
Q

Adipocytes

A

source of estrogen in postmenopausal women

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5
Q

Normal action of steroids

A
  1. Lipophilic steroids are transported by protein carrier and release from carrier into blood diffusing into the cell
  2. Steroid hormones bind to estrogen/androgen receptors in cytoplasm
  3. Translocated from the cytoplasm to nucleus binding to DNA activating/repressing one or more genes
  4. Activated genes create new mRNA that moves back to cytoplasm to produce new proteins
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6
Q

How do we inhibit steroid signaling?

A
  1. Stop steroid receptor function
  2. Stop production of steroids
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7
Q

HPA Axis

A

GnRH in hypothalamus activates the release of LH and FSH in the anterior pituitary gland

LH and FSH stimulate the production of estrogens and androgens

LH: actives cholesterol side chain cleavage
FSH: activates aromatase

NEGATIVE FEEDBACK LOOP

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8
Q

Well-differentiated

A

More likely to be ER+

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9
Q

Poorly differentiated

A

More likely to be ER-

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10
Q

Luminal A/B

A

Receptor expression: ER+/PR+
Histologic grade: low grade (well-differentiated)
Tx: endocrine therapy

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11
Q

HER2

A

Receptor expression: HER2 (oncogene)
Histologic grade: high grade (low differentiated)
Tx: anti-HER2 therapy

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12
Q

Basal-like (BRCA1)

A

Receptor expression: ER-, PR-, HER2-
Histologic grade: high grade (low differentiated)
Tx: chemotherapy

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13
Q

Claudin-low

A

Receptor expression: ER-, PR-, HER2-
Histologic grade: high grade (low differentiated)
Tx: chemotherapy

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14
Q

Prostate cancer and hormones

A
  1. DHT binds to AR receptor in the prostate cells
  2. DHT-AR complex is activated and translocated to nucleus.
  3. DNA binding stimulates transcription of AR responsive genes
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15
Q

Biomarker for Prostate cancer

A

Prostate Specific Antigen
Low PSA level: normal
High PSA level: Prostate cancer OR
UTI, vigorous exercise, ejaculation, anal sex, certain medications

> 6.5 ng/mL=prostate cancer

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16
Q

Glucocorticoids

A

Methylprednisolone, prednisolone, dexamethasone

Anti-cancer effects:
Pediatric acute lymphoblastic leukemia (ALL)
Multiple myeloma
Lymphomas

Palliative to reduce inflammation, edema, and pain during chemo
Reduce hypersensitivity reactions, N/V, and immune-related effects

17
Q

Tamoxifen

A

PRODRUG

Metabolized by CYP2D6 into 4OH-TAM

If poor metabolizer, do not use tamoxifen

MOA:
Antagonist (CoR): Blocks estrogen-dependent breast cancer cell proliferation, Hot flashes/thermoregulation

Agonist (CoA): preservation of bone density in pre/post menopausal women, VTE and clot risk, endometrial hyperplasia

18
Q

Fulvestrant, Elecestrant

A

SERD

MOA: Full ER antagonist with no agonist effects @ high doses that binds to ER and inhibits DNA binding causing rapid receptor degradation

Indication: Treatment of metastatic ER+ breast cancer in POSTMENOPAUSAL women who have progressed on antiestrogens

Administration:
Fulvestrant:IM
Eleacetrant: oral

19
Q

Anastrozole, Letrozole

A

Non-steroidal aromatase inhibitors

MOA: potent and selective competitive inhibitors of aromatase

Indication: treatment of breast cancer in POSTMENOPAUSAL women

Administration: oral
Side effects: osteoporosis (low bone density)

20
Q

Exemestane

A

Steroidal aromatase inhibitor

MOA: structurally similar to androstenedione acting as a false substrate that aromatase converts to a reactive intermediate
Intermediate binds irreversibly at the active site

Indication: breast cancer in postmenopausal women who have progressed on antiestrogen therapy

SE: hot flashes, peripheral edema and weight gain, increased cholesterol levels

21
Q

Leuprolide, Goserelin, Triptorelin

A

GnRH agonists

Chronic administration downregulates pituitary GnRH receptors and leads to pituitary desensitization–> decreases LH and FSH production lead to decreased aromatase leading to decreased estrogen and androgen

Severe loss of estrogen/androgen within 3-4 weeks

SAR: Modified 6th and 10th amino acids to increase potency and t1/2 life

Treatment of breast cancer in PREMENOPAUSAL women

Palliative treatment of advance prostate cancer
SubQ depot
Flare up
SE: hot flashes, gynecomastia, sexual dysfunction

22
Q

Degarelix, Relugolix

A

GnRH antagonists

Treatment of advanced prostate cancer with need for androgen deprivation therapy

NO FLARE

SE: gynecomastia, sexual dysfunction

23
Q

Enzalutamide

A

MOA: binds to the AR and prevents translocation to the nucleus and DNA binding

Treatment of non-metastatic and metastatic prostate cancer

24
Q

Abiraterone (Zytiga)

A

inhibits 17-alpha hydroxylase and 17,20 lyase

SE: increased cholesterol levels

25
Q

Castration resistant prostate cancer

A

mutations in AR resulting in androgen independent activation

PHRM 864 (9 decks)

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