Exam 1 Ch 54 Cancer: Biological and Emerging Therapies Flashcards
What kind of hormonal anticancer agent is Tamoxifen and What does Tamoxifen do ?
From Cancer Biology Lecture
- Gonadal Hormone Antagonists
- Selective Estrogen Receptor Modulator
- Prototypic “molecularly targeted” agent
- Blocks binding of estrogen to receptors of estrogen-sensitive cancer cells in breast tissue
- Partial estrogen receptor antagonist
- 10-fold greater antitumor activity in breast cancer patients whose tumors express estrogen receptors than those who have low or no levels of expression
What is the specific use of Tamoxifen and what are the adverse effects of Tamoxifen?
From Cancer Biology Lecture
Use:
-Receptor-positive breast carcinoma, which is a necessary demonstration of target hormone receptor
-Preventive effect in women at high risk for breast cancer
Adverse Effects:
-Due to its agonist activity in the endometrium, tamoxifen increases risk of endometrial hyperplasia and neoplasia
-Nausea and vomiting
-Hot flushes
-Vaginal bleeding
-Venous thrombosis
What kind of hormonal anticancer agent are 5 alpha-Reductase Inhibitors (Finasteride) and what are its uses and why?
From Cancer Biology Lecture
-Gonadal Hormone Antagonist
Uses:
-Benign prostatic hyperplasia
-At lower dose: to prevent hair loss in men
Why?:
-Testosterone is converted to dihydrotestosterone (DHT) by 5alpha-reductase
-Some tissues (prostate cells & hair follicles) depend on DHT rather than testosterone for androgenic stimulation
-Therefore, 5alpha-reductase inhibited by finasteride
-Does NOT interfere with testosterone action so less likely than other antiandrogens to cause impotence, infertility, and loss of libido
Flutamide is a Gonadal Hormone Antagonist that does what to receptors and what adverse effects does this drug have?
From Cancer Biology Lecture
-Nonsteroidal competitive antagonist of androgen receptors Adverse Effects: -Gynecomastia -Hot Flushes -Hepatic Dysfunction
Name 4 Epidermal Growth Factor (EGF) Receptors and what do they do?
From Cancer Biology Lecture
1) ErbB1 (EGFR)
2) ErbB2 (Her/Neu)
3) ErbB3 (HER3)
4) ErbB4 (HER4)
EGFR regulates signaling pathways involved in cellular proliferation, invasion and metastasis, and angiogenesis. They are implicated in inhibiting cytotoxic activity fo some anticancer drugs and radiation therapy
What is Trastuzumab and what does Trastuzumab do?
It is a growth factor receptor inhibitor anticancer agent.
It was first humanized monoclonal antibody approved for treatment.
It targets extracellular domain of Her2 Receptor & inhibit its signaling in breast cancer cells that overexpress HER2/neureceptor.
It is administered by IV route and does not penetrate the BBB
What is a major adverse effect from using Trastuzumab for treating cancer?
Cardiac dysfunction including heart failure
Worsened if given in combo with anthracycline
Extreme caution when given to a patient with preexisting cardiac dysfunction
Describe Cetuximab. What does it do? What is it for? What are the adverse effects?
- Growth Factor Receptor Inhibitor Anticancer agent
- Chimeric monoclonal antibody
- Directed to extracellular domain of epidermal growth factor receptor (EGFR)
- Clinical Use: (1) Metastatic colon cancer in combo w/ irinotecan & oxaliplatin (2) Head & neck cancer in bombo wi/ radiation
- Adverse Effects: Skin rash and hypersensitivity infusion reaction
What kind of drug is Imatinib and what does it do?
- Tyrosine Kinase Inhibitor Anticancer Agent
- Selective anticancer drug
- Inhibits tyrosine kinase activity of protein product of bcr-abl oncogene
- Commonly expressed in Chronic Myelogenous Leukenia (CML) associated with Philadelphia Chromosome Translocation
- Also blocks tyrosine kinase activity of c-KIT (stem-cell factor receptor) and platelet-derived growth factor receptor (PDGFR)
Which growth factor receptor Inhibitor anticancer agent binds to vascular endothelial growth factor (VEGF) & prevents it from interacting with VEGF receptors?
Bevacizumab
