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Med Chem 3 - Final Exam > Misc Anticancer Agents > Flashcards

Misc Anticancer Agents Flashcards

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1
Q

Which of the following statements is incorrect?

A. Demethylation always restores normal gene function
B. DNA methylation is often used for gene silencing and regulation
C. Azacitidine is teratogenic
D. Endocrine (hormone) therapy seldom causes major organ toxicity
E. Prostate cancer can be detected early using PSA

A

(A) Demethylation can SOMETIMES restore normal gene function while selectively killing cells that have stopped responding to the body’s cellular proliferation control process

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2
Q

True or False - If hormones are withdrawn or antagonized, tumors that are derived from tissues that are dependent on endogenous hormones for growth and function will be expected to regress?

A

True

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3
Q

Which of the following statements regarding hormone anticancer therapy is incorrect?

A. Useful in the Tx of certain leukemias and lymphomas
B. Alternative therapy for tumors that derive from tissues dependent on endogenous hormones for growth and function
C. Most common hormone dependent cancers are prostate cancer and breast cancer
D. PSA test cannot differentiate between cancer and other prostate problems
E. All of the above are true

A

(D) PSA test CAN differentiate between cancer and other prostate problems and is essential for screening for prostate cancer

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4
Q

Which of the following statements regarding hormone agonists is incorrect?

A. They suppress production of testosterone in the testis and/or block its effect at tissue receptors
B. Hormone agonists resemble LHRH (luteinizing hormone-releasing hormone)
C. Slow onset of therapeutic effects
D. Common SE are hot flashes, loss of libido, impotence
E. All of the above are true

A

(E) all of the above are true

*A - Even though they are hormone AGONISTS, they block the effects of testosterone at the receptor. This occurs b/c of a negative feedback mechanism which results in a decreased number of receptors

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5
Q

All of the following are Hormone agonists, except?

A. Leuprolide
B. Goserelin
C. Buserelin
D. Toremifene
E. All of the above are hormone agonists
A

(D) Toremifene is NOT a hormone agonist, it is a SERM used in breast cancer Tx

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6
Q

True or False - 5a-reductase inhibitors, 17a-hydroxylase inhibitors (ketaconazol), and aromatase inhibitors can all be used in combination with traditional anticancer meds to Tx cancer?

A

True

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7
Q

Which androgen antagonist is orally available, has long plasma half-life (1 week), and is used in the Tx of non-metastatic prostate cancer?

A

Bicalutamide (Casodex ®)

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8
Q

Which SERM with poor oral availability that is administered IM should you NOT give to pregnant women, patients on anticoagulants, or patients with thrombocytopenia?

A

Fulvestrant (Faslodex ®)

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9
Q

Which androgen antagonist used in the Tx of prostate cancer has an active metabolite that can also bind to and block the androgen receptor?

A

Flutamide (Eulexin ®)

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10
Q

Which SERM, that can be used successfully for years without resistance issues, is less potent than Tamoxifen b/c it’s halogenated?

A

Toremifene (Fareston ®)

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11
Q

Which anticancer agent administered SQ is used in the Tx of myelodysplastic syndrome?

A

Azacitidine (Vidaza ®)

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12
Q

Which androgen antagonist, used in Tx of metastatic prostate cancer, has an intermediate plasma half-life in-between Bicalutamide and Flutamide?

A

Nilutamide

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13
Q

Which SERM is used in the Tx of estrogen-dependent breast cancer AFTER primary Tx with chemo or surgery

A

Tamoxifen

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14
Q

Which SERM, used in Tx of breast and uterine cancer where Tamoxifen failed, undergoes hydrolysis generating Acolbifene which is 200x more potent than Tamoxifen?

A

EM-800

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15
Q

Which of the following statements regarding enzyme therapy is incorrect?

A. Normal cells are able to synthesize their own asparagine
B. Effective as a monotherapy
C. Adding asparaginase enzyme therapy keeps proliferation of leukemia under control by increasing asparagine concentration
D. malignant lymphocytic leukemia cells can’t synthesize their own asparagine
E. Both B & C

A

(E) both B and C are false - Aspariginase is NOT effective as a monotherapy and is used in combination with other drugs. Also aspariginase will DEPLETE serum asparaginase and the leukemia cells will no longer be able to survive

*D - malignant lymphocytic leukemia cells need exogenous asparagine to survive b/c they can’t produce it themselves

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16
Q

Which enzyme therapy drug used in the Tx of acute lymphoblastic leukemia can result in severe allergic reactions and should only be administered in a hospital?

A

Asparaginase (Elspar ®)

17
Q

True or False - Both T cells and B cells display antibodies?

A

True

Also they are both part of the acquired immune system

18
Q

Which of the following statements about cytokines is correct?

A. Interferons generally potentiate the immune response and anti-proliferative actions
B. Administering cytokines can prepare immune system to get ready to attack tumors
C. Interleukins stimulate the production of various immune cells
D. TNF can stimulate B cell proliferation
E. All of the above

A

(E) all of the above

19
Q

Which of the following is incorrect?

A. Cytokines are produced via recombinant DNA technology
B. MoAb light chain recognizes the substrate (target) while the heavy chain triggers the innate immune system
C. chimerization blends parts of foreign Ab with parts of human Ab to give passive immunization without provoking a immune response against the Ab
D. Naked Ab is typically conjugated with an immunotoxin
E. Trastuzumab (Herceptin ®) is an anti-Her2 MoAb

A

(D) Naked Ab are NOT conjugated with anything…that’s why their called naked

20
Q

All of the following are uses of MoAbs, except?

A. Immunosuppressants in transplants
B. Immunoconjugates
C. Tumor growth inhibitors
D. Diagnostics
E. All of the above
A

(E) All of the above are uses of MoAbs. They are primarily used as immunoconjugates in which a drug, radionuclide, or toxin/protein is attached to the MoAb

*They are also used for site-directed delivery of radionuclides and enzymes to activate prodrugs

21
Q

Which of the following statements is incorrect?

A. Her receptors are membrane receptors transmitting signals from outside of cell to inside of cell
B. Her proteins regulate cell growth, survival, and differentiation
C. Defective dimerized Her2 receptors in breast cancer are stuck “on” telling cell to constantly proliferate
D. Overexpression by 10-100x of Her2 receptor occurs in all primary tumors of breast cancer
E. Herceptin is very useful in tumors that over express Her2 receptors

A

(D) Overexpression by 10-100x of Her2 receptor ONLY OCCURS in 25-30% of primary tumors…not all breast cancers will have over expression of Her2 receptors

22
Q

True or False - Herceptin’s MOA prevents dimerization of Her2 receptors preventing uncontrolled proliferation AND recruits macrophages to recognize and destroy tumor cells

A

True

23
Q

Which of the following regarding MoAbs is incorrect?

A. Trastuzumab (herceptin) extends the lifespan of only breast cancer patients whose tumors over-express Her2 receptors
B. Herceptin + Paclitaxel is 1st line Tx for metastatic breast cancer
C. Her1 receptor is over-expressed in 30% of human carcinomas and 50% of glioblastomas
D. Her1 is also known as EGF receptor
E. Cetuximab binding to Her1 receptor still allows subsequent EGF binding

A

(E) When Cetuximab binds to the Her1 (EGF) receptor, it PREVENTS subsequent EGF binding causing shutdown of signaling and turning off uncontrolled growth in the cancer cell

24
Q

Which MoAb that blocks Her1 receptor is used in the Tx of colorectal, non-small cell lung cancer, pancreatic cancer, and breast cancer?

A

Cetuximab (Erbitux ®)

25
Q

True or False CD20 antigen is displayed on B cells at specific stages of differentiation (not all the time)?

A

True

26
Q

Which of the following statements regarding Rituximab is incorrect?

A. Rituximab can be used in the Tx of leukemias and lymphomas that display CD20
B. Rituximab selectively destroys malignant B cells that express CD20
C. Rituximab alone can stabilize lymphoma but is NOT curative
D. Rituximab is not efficient for multiple myelomas
E. Rituximab can be conjugated with radioisotopes

A

(B) False! Rituximab wipes out tumor B cells AND normal B cells that express CD20. It is NOT selective for only malignant B cells that express CD20

  • C - must be used in conjunction with classical chemotherapeutic combos to cure
  • D - yes b/c multiple myelomas are no longer proliferating and don’t express CD20
27
Q

Which of the following MoAb is matched correctly with its MOA?

A. Bevacizumab - angiogenesis inhibitor (prevents formation of new blood vessels)
B. Tositumomab - radioisotope 
C. Ibritumomab - radioisotope
D. Rituximab - Her1 antagonist
E. Cetuximab - Her 1 antagonist
A

(D) Rituximab is an ANTI-CD20 MoAb targeting CD20 displayed on B cells

28
Q

True or False - there is a vaccine to treat early-stage bladder carcinomas?

A

True - attenuated form of bacteria (BCG) that was present in bacterial skin infections

Med Chem 3 - Final Exam (5 decks)

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