Exam IV - Breast Cancer Flashcards Preview

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Flashcards in Exam IV - Breast Cancer Deck (32):
1

Tamoxifen
Indications

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

2

Tamoxifen
Mechanism

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

3

Tamoxifen
ADME

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

4

Tamoxifen
Advantages

1. Pre & Post menopausal 2. More efficacious than raloxifene

5

Tamoxifen
Toxicities

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

6

Tamoxifen
Resistance

3-5 years

7

Raloxifene
Indications

Post menopausal, ER+ BC

8

Raloxifene
Mechanism

SERM: selectibe estrogen receptor modulator

9

Raloxifene
Advantages

1. Doesn't req CYP 2D6 activation 2. Less risk for endometrial cancer

10

Leuprolide
Indications

Premenopausal, ER+ BC, Prostate Cancer

11

Leuprolide
Mechanism

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

12

Leuprolide
Adverse

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

13

Leuprolide
Contraindications

Pregnancy

14

Anastrazole
Indications

Postmenopausal ER+ BC

15

Anastrazole
Mechanism

Aromatase Inhibitor: prevents conversion of testosterone to estrogen

16

Anastrazole
ADME

Adjuvant monotherapy for 5 years

17

Anastrazole
Advantages

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

18

Anastrazole
Adverse

1. Hot flashes 2. Osteopenia 3. Osteoporosis

19

Exemestane
Indications

ER+ BC

20

Exemestane
Mechanism

Aromatase Inhibitor

21

Exemestane
Advantages

1. Can use after Tamoxifen time is up

22

Exemestane
Adverse

1. Hot flashes 2. Osteopenia 3. Osteoporosis

23

Exemestane
Other

1. Irriversible inhibitor (suicide inhibition) 2. Don't work in premenopause

24

Trastuzamab
Indications

1. HER2+ BC (localized) 2. HER2+ metsstatic BC

25

Trastuzamab
Mechanism

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

Trastuzamab
ADME

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

Trastuzamab
Advantages

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

28

Trastuzamab
Adverse

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

Trastuzamab
Other

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

Pertuzamab
Indications

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

31

Pertuzamab
Mechanism

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

32

Pertuzamab
Adverse

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