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Spring 2018 Pharm Exam 2 > Lecture 5: Drugs for Breast CA > Flashcards

Lecture 5: Drugs for Breast CA Flashcards

(49 cards)

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1
Q

How are the subtypes of BCA determined?

A

immunochemistry

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2
Q

What are the 3 main subtypes of BCA

which is MC?
which has best prognosis?

A
  1. ER + BCA (MC & best prognosis)
  2. HER 2+ BCA
  3. Triple Negative BCA
    (ER-, PR-, HER2 not amplified)
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3
Q

Other than surgery and/or radiation what is the main Tx for ER+ BCA?

A 
hormone therapy (tamoxifen)
(+/- cytotoxic chemo)
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4
Q

Which pts respond best to tamoxifen for BCA?

A

ER+, PR+ & HER2- pts respond best

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5
Q

Other than surgery and/or radiation what is the main Tx for HER2+ BCA?

A

Target therapy w/biologics

Trastuzumab

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6
Q

Other than surgery and/or radiation what is the main Tx for Triple Negative BCA?

why does this CA have the worst prognosis

A

cytotoxic chemo

pts not candidates for ER+ (tamoxifen) or HER2+ (biologic) Tx –> CA wont respond to drugs b/c not rec +

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7
Q 
What class of drugs Tx PREmenopausal women?
POSTmenopausal women?

What drug class can tx both pre and post?

A 
PRE = GnRH agonists 
POST = Aromatase Inhibitors 
Both = SERMs (tamoxifen)
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8
Q

What does hormonal therapy target for BCA?

What 3 classes of drugs Tx ER + BCA?

A

Targets the HPG axis

  1. SERMs
  2. GnRH agonists
  3. Aromatase inhibitors
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9
Q

What are the two drugs in the SERM class that Tx ER+ BCA?

A
  1. Tamoxifen

2. Toremifene

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10
Q

What is major difference about Toremifene in regards to Tx population (vs. Tamoxifen)?

What can NOT approved to Tx?
What is its ONLY Tx indication?

A

ONLY Txs POST menopausal women

Not approved for DCIS (early stage dz) or risk reduction

Only approved to Tx metastatic ER+ BCA

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11
Q

What are the two active metabolites of Tamoxifen?

A
  1. 4-hdroxyTAM

2. Endoxifen

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12
Q

Where are 4-hdroxyTAM and Endoxifen antagonists? partial agonists?

A

antagonists in breast tissue (alpha/beta rec)

partial agonists in bone and endometrial tissue

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13
Q

What is the MOA of 4-hdroxyTAM and Endoxifen?

What does chronic inhibition cause? why?

A

block estrogen binding–> prevents transcription pro-proliferative/survival genes

chronic inhibition–> apoptosis
- higher activity of co-repressors

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14
Q

What is the RLS for endoxifen?

A

activity of liver enzyme CYP2D6

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15
Q

What are the 3 polymorphisms of CYP2D6?

which has worst survival?

A
  1. normally active/wild type allele (*1) - EM
  2. supraactive (*2xN) - UM
  3. Totally inactive allele (*4) - PM = worst survival
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16
Q

What is the MC AE a/w tamoxifen? What population is it worse in?

What does this S/E indicate?

A

Menopausal Sxs (hot flashes)

  • more severe in POSTmenopausal women
  • indicates drug is working
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17
Q

What are the 2 BBW a/w tamoxifen?

A
  1. incr risk of DVT, PE
    (agonist activity–> stim clotting factors)
  2. incr risk of endometrial CA if on drug more than 5 yrs
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18
Q

Why are pts not on tamoxifen more than 5 yrs?

A

incr risk of endometrial CA

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19
Q

6 uses/Tx for tamoxifen

A
  1. Metastatic BCA in women and men
  2. Adjuvant for metastatic BCA
  3. Adjuvant for DCIS
  4. BCA prevention in high risk pts
  5. DoC for EM & UM pts
  6. Txs early stage & metastatic ER+ BCA
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20
Q

What is the drug in the GnRH class that Txs ER+ BCA?

21
Q

MOA for Leuprolide?

Overall result?

Study These Flashcards
A

GnRH agonist in pituitary:
- constitently stim GnRH rec–> downreg/desensitization of GnRH rec

Result: decr levels of FSH and LH–> decr progesterone and estrogen

22
Q

What occurs w/Leuprolide admin in the first few wks/months?

Study These Flashcards
A

before down regulation –> initial incr in FSH and LH rel–> incr testosterone and estrogen levels –> transient worsening of CA Sxs

23
Q

3 major AEs a/w Leuprolide?

CI of Leuprolide?

Study These Flashcards
A
  1. Hot flashes
  2. osteoporosis
  3. Sexual dysfunction

CI = pregnancy

24
Q

What 2 situations is Leuprolide used for as adjuvant therapy?

Study These Flashcards
A
  1. PREmenopausal metastatic ER+ BCA

2. Metastatic prostate CA

25
2 main drugs for aromatase inhibitors? which one is IRREV?
1. Anastrozole | 2. Exemestane = irreversible
26
What is the MOA for Anastrozole & Exemestane?
inhbit aromatase CYP19A1--> prev conversion of testosterone to estrogen
27
Why are aromatase inhibitors not effective in pre-menopausal women?
Still have fxnl ovaries--> decr estrogen levels--> less neg feedback--> more testosterone produced --> overcomes AI's effects
28
How long can Anastrozole and Exemestane be given as adjuvant monotherapy? When using Anastrozole and Exemestane in sequential adjuvant therapy how long is total Tx time? What drug initially given?
5 yrs total Tx time for sequential therapy = 10 yrs - first give tamoxifen for 5 yrs, then give AI for addtl 5 yrs
29
What drug class Txs HER2+ BCA? what are the 2 main drugs in this class?
class = biologics (monoclonal Abs) Drugs 1. Trastuzumab 2. Pertuzumab
30
How many copies of HER2 gene in normal cells? | How many copies of HER2 gene in BCA cells?
normal cells = 2 copies | BCA cells = 6 copies
31
What 2 methods used to determine HER2+ cells? What will be seen w/each method indicating HER2+ cells ?
1. FISH mapping --> pink spots | 2. Immunochemistry--> brown staining of membrane
32
How do normal and BCA cells in EGF and HER2 receptor signaling?
1. Normal cells = ligand dependent dimerization | 2. BCA cells = ligand INdependent dimerization
33
How does ligand INdependent dimerization in BCA cells lead to CA?
persistent activation of RAS-MAPK pathway--> uncontrolled cell proliferation
34
Major difference in MOA b/t Trastuzumab and Pertuzumab?
Trastuzumab - blocks ligand INdependent dimerization | Pertuzumab - blocks ligand dependent dimerization
35
MAIN 2 MOA for Trastuzumab? end result?
1. Monoclonal Ab: binds to HER2 rec--> downregulation | 2. Inhibits ligand dependent dimerization & RAS-MAPK activation--> inhibits prolif and induces apoptosis
36
Other 2 MOAs for Trastuzumab: - sensitizes CA cells to cytotoxic chemo - Kills CA cells by recruiting host immune cells
`
37
Main S/E a/w Trastuzumab?
Infusion rxn
38
Infusion rxn w/Trastuzumab: - caused by? - Sxs? - Tx? note: normally occur w/in 1st minutes, improves after 1st Tx
d/t rel of histamines and cytokines Sxs = fever and chills, N/V, pain, HA, dizziness, rash Tx = acetaminophen, diphenhydramine
39
What are the 2 BBWs for Trastuzumab?
1. Cardiomyopathy (see CHF, decr LV EF) | 2. Fatal infusion rxn (ARDs)
40
What is the major problem w/ Trastuzumab? | solution?
resistance develops in most w/in 1 yr solution = give Laptinib as replacement therapy
41
What is the 1st line Tx for metastatic HER2+ BCA or early primary HER2+ BCA
Trastuzumab+ Laptinib
42
3 indications/uses for Trastuzumab
1. HER2+ localized BCA (adjuvant) 2. Metastatic HER2+ BCA 3. Metastatic HER2+ GASTRIC CAs
43
What is Pertuzumab typically used in combo w/? What 3 drug combo improved progression free survival? Note: txs all stages HER2+ BCA
Trastuzumab and docetaxel Trastuzumab + Pertuzumab + docetaxel
44
What are the names of the 2 genomic approaches to predicting BCA recurrence?
1. MammaPrint | 2. Oncotype DX
45
What is unique about MammaPrint
It is receptor INdependent--> can be used on all subtypes of BCA (ER, PR, HER2)
46
Which genomic approach is indicated for pts < 61 w/early stage tumors < 5 cm and LN (-)
MammaPrint
47
What does lower recurrence score for Oncotype DX indicate?
better prognosis
48
Which type of tumors based on Oncotype DX will benefit from combo Tx of Tamoxifen + chemo (improved 10 yr survival)
``` High RS (recurrence score tumors) - score > 31 ```
49
What Tx should be give to Low-RS tumors (<18) based on Oncotype DX? why?
ONLY give tamoxifen--> little/no benefit to combo and chemo drugs = toxic/fatal

Spring 2018 Pharm Exam 2 (6 decks)

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