Anti Cancer Drugs Lecture PDF

Question 1

Administration of cytotoxic drugs

Answer 1

Prolonged infusion or in multiple doses over an extended period of time, require special handling as can be very toxic to handle with direct contact

Question 2

Alkylating agents mech of action

Answer 2

Transfer alkyl group to DNA molecule, tie up DNA molecule eliminating ability of DNA to untwist and allow replication of genetic code or vital protein production, can occur during any stage of the cell cycle (cell cycle nonspecific)

Question 3

Cyclophosphamide (cytoxan, neosar) drug class and function

Answer 3

Nitrogen mustard alkylating agent most commonly used for different types of leukemia

Question 4

Chlorambucil (leukaran) drug class and function

Answer 4

Nitrogen mustard alkylating agent that is the safest to use for cancer treatment

Question 5

Major dose limiting toxicity in the nitrosureas chemo agent drug class

Answer 5

Delayed bone marrow suppression

Question 6

Carmustine (BCNU, glaidel) drug classand function

Answer 6

Nitrosureas alkylating agent, used to easily penetrate BBB and act on metastatic tumors of brain, can be administered by biodegradable wafer implanted into cavity when tumor is removed

Question 7

Cisplatin (platinol) drug class and function and ADR’s (3)

Answer 7

Platinum compound (forms cross links with DNA similar to alkylating agents),used to treat metastatic testicular and ovarian cancers or advanced bladder cancer but has many adverse effects including nephrotoxicity, neurotoxicity, and GI distress

Question 8

Antimetabolites mech of action

Answer 8

Structurally similar to endogenous metabolites to compete with compounds during DNA/RNA biosynthesis forming nonfunctional gene product making it particularly toxic to cells with large growth fraction and acts during the S phase

Question 9

3 classes of antimetabolites and example of each

Answer 9

Folic acid analogues - methotrexate
Pyrimidine analogues - cytarabine, 5-FU
Purine analogues - mercaptopurine

Question 10

2 ways to get methotrexate to be taken up by the cancer cells

Answer 10

• massive dosing forces drug into cell

- leucovorin

Question 11

Methotrexate indications (3)

Answer 11

• choriocarcinoma
• ALL
• skin disorders

Question 12

Cytarabine indications (1)

Answer 12

-AML in 7+3 regimen

Question 13

5-FU indications (2) and ADR’s (2)

Answer 13

• solid tumors
• topical premalignant keratosis

-Bone marrow suppression, hyperpigmentation

Question 14

Hypomethylating agents mech of action

Answer 14

Induce apoptosis and restore normal frunction to genes involved with cell differentiation and proliferation

Question 15

Antineoplastic antibiotics function and 2 subcategories

Answer 15

Classified as antibiotics but reserved for neoplastic disease because of high toxicity
-anthracyclines and nonanthracyclines

Question 16

Doxorubicin drug class, primary indication (1), ADR (1)

Answer 16

Anthracycline antineoplastic antibiotics

• lymphomas
• cardiotoxicity related to total cumulative dose

Question 17

Liposomal (doxil)/daunorubicin

Answer 17

Reformulations similar to doxorubicin with different function, daunorubicin used only for AIDS related kaposi’s sarcoma

Question 18

Bleomycin (blenoxane) drug class, ADR (1)

Answer 18

Nonanthracycline antineoplastic antibiotic

-pulmonary toxicity dose limiting toxicity

Question 19

Vinca alkaloids mech of action

Answer 19

Work during M phase to bind to microtubules and initiate destruction and dissolution of the microtubules

Question 20

Mitotic inhibitors sub divisions

Answer 20

vinca alkaloids and taxanes

Question 21

Vincristine vs vinblastine drug class and differences

Answer 21

Both vinca alkaloid mitotic inhibitors vincristine is toxic to peripheral nerves but does little damage to bone marrow, vise versa for vinblastine

Question 22

Paclitaxel (abraxane) drug class and ADR (1)

Answer 22

Taxane mitotic inhibitor

-severe hypersensitivity

Question 23

Topoisomerase inhibitors mech of action

Answer 23

Block enzymes that cut apart DNA strand

Question 24

Topotecan (hycamtin) drug class function

Answer 24

Topoisomerase inhibitor

Question 25

Asparaginase (elspar) mech of action

Answer 25

Some tumor cells especially leukemic require extracellular supply of aspargine and these break it down in the blood stream depriving tumors

Question 26

Presence of TILs

Answer 26

Tumor infiltrating lymphocytes that indicate the immune system is responding to a tumor and is associated with better outcome

Question 27

Immune checkpoint proteins

Answer 27

Surface proteins on the surface of T cells that recognize specific partner proteins on other cells sending an off signal not to attack those cells, expressed in high levels of some tumor cells to avoid immune destruction

Question 28

Check point inhibitor drug mech of action

Answer 28

Blocks interaction between T cell and cancer cell at the check point to allow the T cell to target and kill the cancer cell - a potentiator of the T cell response

Question 29

Pembolizumab (keytruda) and nivolumab (opdivo) drug class

Answer 29

Check point inhibitor drugs

Question 30

CAR-T cell therapy and one big ADR

Answer 30

Genetically modifying patient’s T cell in lab to express protein known as chimeric antigen receptor to attach to receptor on surface of cancer cells improving ability to attack (requires chemo and whole body radiation to remove current immune cells that can impede activty of the incoming modified T cells)
-cytokine release syndrome

Question 31

Tumor infiltrating lymphocyte therapy and one big ADR

Answer 31

Growth in lab T cells naturally found against tumor before reinfusion to kill tumor before it becomes immunoresistant
-capillary leak syndrome

Question 32

Antibody drug conjugates and example

Answer 32

Linking of an antibody to a toxic substance for use in treatment of cancer, adotrastuzumab emantasine

Question 33

Sipuleucel T (provenge)

Answer 33

cancer treatment vaccine designed to stimulate the immune attack against prostate cancer cells in asymptomatic or minimally symptomatic metastatic castration resistant prostate cancer

Question 34

Thalidomide drug class and function

Answer 34

Immunomodulatory drug that helps inhibit angiogenesis

Question 35

Common side effects of biological cancer therapies (3)

Answer 35

• soreness or itching
• flu like symptoms
• long term autoimmune disorders

Question 36

Hormonal agents taken for years to reduce recurrence of breast cancer or in high risk patients as a prevantitve measure or to treat estrogen receptor tumors (2)

Answer 36

Antiestrogens such as tamoxifen, aromatase inhibitors such as anastrazole

Question 37

Raloxifene (evista) key differences from tamoxifen

Answer 37

Does NOT increase risk of endometrial cancer

Question 38

Most widely used therapy for prostate cancer treatment

Answer 38

Androgen deprivation therapy

Question 39

Why is drug therapy better than castration at reducing androgen levels?

Answer 39

It acts at both the testes and the adrenals (produce up to 10% of the androgens)

Question 40

Leuprolide (eligard) drug class and function, ADR’s (3)

Answer 40

Synthetic analogue agonist of GnRH indicated in advanced carcinoma of the prostate to offer palliative care and as an alternative to orchiectomy or estrogen therapy by suppressing testosterone production long term thru desensitizing the GnRH receptors which then cause a drop in LH release and testosterone production
-hot flashes, impotence and loss of libido, and elevation of testosterone early in treatment

Question 41

Degarelix (firmagon) drug class and function

Answer 41

GnRH antagonist, often used for palliative therapy of advanced prostate cancer as alternative agonists

Question 42

Flutamide (eulexin) drug class, function

Answer 42

Androgen receptor blocker, used alongside a GnRH agonist indicated only for metastatic prostate cancer to prevent tumor flaring caused by the GnRH agonist