NAPLEX Oncology 2: Common cancer
types and treatment
✅✅
How long should a patient be on hormone therapy for ER/PR positive breast cancer?
What class of medications are used? - -5-10 years
1. premenopausal: SERMS aka tamoxifen
2. postmenopausal: AI and SERMs
Why are aromatase inhibitors ineffective in premenopausal women? - ✅✅-AIs do
not stop the production of ovarian estradiol productions
✅✅
What is the pro and con to using raloxifene for breast cancer prevention? -
-Helps improve bone mineral density and is indicated for osteoporosis however
has a high risk of causing hot flashes and blood clots
What situations would you use AIs in premenopausal women? - ✅✅
-If
premenopausal women have had menopause induced via ovarian suppression (such
as taking a GnRH agonist gosrelin or leuprolide) or ablation
GnRH agonists decreases LH and FSH production via negative feedback
What is the MOA of aromatase inhibitors? - ✅✅ -Blocks the aromatase enzyme,
which catalyzes the conversion of androgens to estrogen in the peripheral tissues
which is the primary source of estrogen in post-menopause
✅✅
How does HER2 promote cancer growth and what are the agents used against
HER2+ BCA? - -1. HER2 receptors regulate and promote cell growth. In BCA,
overexpression there is unregulated cell growth leading to breast cancer as the
HER2 dimerize and send signals to amplify cell growth
2. Agents like trastuzumab (Herceptin) stop the dimerization of HER receptors to
stop cell growth
✅✅
What are the class side effects for SERMs? How do you manage hot flashes and
why that drug? - -Side Effects:
-Hot flashes/night sweats
-vaginal bleeding/spotting
-vaginal discharge/dryness/pruritus
-decrease libido
Hot flashes should be managed with Venlafaxine as all the other agents including
agents for depression are potent CYP2D6
What SERMs are used for BCA and what are the brand names? - ✅✅-Drugs:
✅✅
What is the unique pharmacokinetic profile of tamoxifen and what are the boxed
warnings and side effects? - -1. Tamoxifen is a prodrug converted by CYP2D6
to endoxifen
2. Boxed Warnings
-increased risk of uterine or endometrial cancer
-thromboembolic risk
3. Side Effects:
-decreased BMD: supplement with Ca/Vit D
-Teratogenic
What is the boxed warning for raloxifene? - ✅✅-Increased risk of venous
thromboembolism and death from stroke
✅✅
Which drug is considered a selective estrogen receptor degrader and how does it
work> - -1. Fulvestrant (Faslodex) an IM injection
2. estrogen receptor antagonist that causes receptor degradation and
downregulation
What are expected side effects of fulvestrant? - ✅✅-Side Effects:
-increased LFTs
-injection site pain
-hot flashes
Which aromatase inhibitors are most commonly used in BCA? - ✅✅-1. Anastrozole
(Arimidex)
2. Letrozole (Femara)
3. Exemestane (Aromasin)
What are the risks of AIs and most common side effects? - ✅✅-1. Risks:
-Risk of osteoporosis
-Risk of CVD
2. Side effects:
-hot flashes/night sweats
-arthralgia/myalgia
What CDK4/6 inhibitors are approved for BCA? - ✅✅-1. Palbociclib (Ibrance)
2. Abemaciclib (Verzenio)
3. Ribociclib (Kisqali)
Which drugs are contraindicated with BCA? - ✅✅-Estrogen-containing medications
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