Exam IV - Breast Cancer Flashcards

1
Q

Tamoxifen

Indications

A

ER+, 1. Adjuvant for metstatic BC post mastectomy, axillary dissection, or radiation, or ↓ Cancer risk in other breast. 2. Adjuvant for DCIS 3. Prevention in high risk pts

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2
Q

Tamoxifen

Mechanism

A

SERM: selectibe estrogen receptor modulator 4-Hydroxy TAM and endoxifen (ERα antagonists in breast tissue, partial agonists in endomet & bone) prevent cell growth and mitosis →2° apoptosis from growth inhibition

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3
Q

Tamoxifen

ADME

A

A: 10 mg PO bid for 5-10 years. M: Liver. Pharmakogenetic Testing for CYP2D6 (enz is rate limiting step)

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4
Q

Tamoxifen

Advantages

A
  1. Pre & Post menopausal 2. More efficacious than raloxifene
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5
Q

Tamoxifen

Toxicities

A
  1. Menopausal sx: hot flashes 2. Vaginal discharge 3. Cataracts 4. Nausea Black Box: Can cause DVTs & PEs and endometrial cancer↑risk if extendedn beyond 5-10 yrs
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6
Q

Tamoxifen

Resistance

A

3-5 years

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7
Q

Raloxifene

Indications

A

Post menopausal, ER+ BC

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8
Q

Raloxifene

Mechanism

A

SERM: selectibe estrogen receptor modulator

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9
Q

Raloxifene

Advantages

A
  1. Doesn’t req CYP 2D6 activation 2. Less risk for endometrial cancer
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10
Q

Leuprolide

Indications

A

Premenopausal, ER+ BC, Prostate Cancer

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11
Q

Leuprolide

Mechanism

A

GnRH agonist in pituitary leads to ↓ LH and FSH which ↓ estrogen & progesterone reease from ovaries (or testosterone in testes to tx prostate cancer)

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12
Q

Leuprolide

Adverse

A
  1. Inidital admin will cause LH and FSH to ↑ 2. Hot flashes 3. Osteoporosis 4. Sexual dysfunction
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13
Q

Leuprolide

Contraindications

A

Pregnancy

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14
Q

Anastrazole

Indications

A

Postmenopausal ER+ BC

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15
Q

Anastrazole

Mechanism

A

Aromatase Inhibitor: prevents conversion of testosterone to estrogen

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16
Q

Anastrazole

ADME

A

Adjuvant monotherapy for 5 years

17
Q

Anastrazole

Advantages

A
  1. Reversible Inhibitor 2. Can use after Tamoxifen time is up
18
Q

Anastrazole

Adverse

A
  1. Hot flashes 2. Osteopenia 3. Osteoporosis
19
Q

Exemestane

Indications

A

ER+ BC

20
Q

Exemestane

Mechanism

A

Aromatase Inhibitor

21
Q

Exemestane

Advantages

A
  1. Can use after Tamoxifen time is up
22
Q

Exemestane

Adverse

A
  1. Hot flashes 2. Osteopenia 3. Osteoporosis
23
Q

Exemestane

Other

A
  1. Irriversible inhibitor (suicide inhibition) 2. Don’t work in premenopause
24
Q

Trastuzamab

Indications

A
  1. HER2+ BC (localized) 2. HER2+ metsstatic BC
25
Q

Trastuzamab

Mechanism

A

Monoclonal AB binds to HER2: ↓HER protein 2. Inhibition of growth signal by blocking HER2 activation of RAS/MAPK pathway 3. sessitizes cancer cells to cytotoxic chemo tx 4. Kills cancer by recruiting host immune cells

26
Q

Trastuzamab

ADME

A

4mg/kg IV over 90 mins, maintenance dose of 2 mg/kg IV over 30 min q week Testing for overexpression of HER2 required for selection of PTs

27
Q

Trastuzamab

Advantages

A

Increase in response rate in combo w/ paclitaxel, slowing of dz progression

28
Q

Trastuzamab

Adverse

A

Infusion reaction in 40% w/in 1st mins of tx: fever, chills, N&V, pain, HA, dizziness, rash (mild~moderate) Tx w/ acetaminophen, diphendydramine, meperidine Black Box: 1. Cardiomyopathy manifests as CHF and ↓LV ejection fraction 2. Fatal infusion rxn causes ARDS

29
Q

Trastuzamab

Other

A
  1. Resistance develops in many w/in 1 year due to cleavage of extracellular protein 2. Combo w/ lapatinib as 1st line for MetBC or early primary BC
30
Q

Pertuzamab

Indications

A

Combo w/ trastuzimab & docetaxel for early stage HER2+ BC and HER2+ MetBC

31
Q

Pertuzamab

Mechanism

A
  1. Humanized monoclonal AB targets HER2 2. Ligand dependent HER2 dimerization inhibitor
32
Q

Pertuzamab

Adverse

A

Cardiotoxixity, severe hypersensitivity, anaphylaxis Black box: embryo-fetal toxicity