Chemo V Target Therapy

Question 1

Imatinib mesylate, Dasatinib, Nilotinib- Mech of Action

Answer 1

BIND ATP BINDING SITE OF BCR-ABL FUSION PROTEIN OR C-KIT= INHIBIT CRITICAL SIGNALING PATHWAYS IN CANCER CELLS THAT ARE CONSTITUTIVELY ACTIVE

target= Bcr-Abl, c-kit tyrosine kinases

Question 2

Imatinib mesylate, Dasatinib, Nilotinib- Cell Cycle Specificity

Answer 2

No

Question 3

Imatinib mesylate, Dasatinib, Nilotinib- Kinetics

Answer 3

METABOLIZED BY CYP3A4- AVOID ADMINISTRATION WITH INDUCERS (ST. JOHN’S WORT) OR INHIBITORS (GRAPEFRUIT JUICE)

PO

Question 4

Imatinib mesylate, Dasatinib, Nilotinib- Clinical Use

Answer 4

CHRONIC MYELOGENOUS LEUKEMIA (PHILADELPHIA CHROMOSOME 9:21- BCR-ABL)

GI STROMAL TUMORS

Question 5

Imatinib mesylate, Dasatinib, Nilotinib- Toxicities

Answer 5

superficial edema
nausea
muscle cramps
abdominal pain
musculoskeletal pain
rash
diarrhea
anemia
neutropenia
thrombocytopenia
rarely congestive heart failure

Imatinib mesylate- may increase clearance of thyroid hormone; monitor thyroid function in patients taking thyroid replacement therapy

Dasatinib, Nilotinib- useful if imatinib resistant

Question 6

Cetuximab, Panitumumab- Mech of Action

Answer 6

MONOCLONAL ANTIBODY INHIBITOR OF EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR)

target= EGFR

Question 7

Cetuximab, Panitumumab- Cell Cycle Specificity

Answer 7

No

Question 8

Cetuximab, Panitumumab- Clinical Use

Answer 8

METASTATIC COLORECTAL CANCER
lung cancer
head & neck cancers

Cetuximab- K-RAS MUTATION MALIGNANCIES WILL BE UNRESPONSIVE TO THE DRUG

Panitumumab= fully humanized monoclonal antibody

Question 9

Cetuximab- Toxicities

Answer 9

RASH
hypersensitivity
diarrhea
hypomagnesemia

Question 10

Erlotinib- Mech of Action

Answer 10

SMALL MOLECULE INHIBITOR OF EGFR ASSOCIATED TYROSINE KINASE

target= EGFR associated tryosine kinase

Question 11

Erlotinib- Cell Cycle Specificity

Answer 11

No

Question 12

Erlotinib- Kinetics

Answer 12

METABOLIZED BY CYP3A4- AVOID ADMINISTRATION WITH INDUCERS (ST. JOHN’S WORT) OR INHIBITORS (GRAPEFRUIT JUICE)

PO

Question 13

Erlotinib- Clinical Use

Answer 13

NON-SMALL CELL LUNG CANCER- ESPECIALLY IF THERE IS AN ACTIVATING MUTATION OF EGFR PRESENT

HEAD AND NECK CANCER

pancreas cancer in combination with gemcitabine

Question 14

Erlotinib- Toxicities

Answer 14

rash
nausea
anorexia
fatigue

Question 15

Bevacizumab- Mech of Action

Answer 15

MONOCLONAL ANTIBODY THAT BINDS TO VASCULAR ENDOTHELIAL GROWTH FACTOR (VEGF) LIGAND AND IMPAIRS TUMOR GROWTH

target= VEGF

Question 16

Bevacizumab- Clinical Use

Answer 16

lung cancer

metastatic colorectal cancer

Question 17

Bevacizumab- Toxicities

Answer 17

perforation of colon
infusion reactions
hypertension
arterial clots
bleeding
reversible posterior leukoencephalopathy syndrome (headache, mental status change, visual changes)

Question 18

Sorafenib, Pazopanib, Sunitinib- Mech of Action

Answer 18

SMALL MOLECULE INHIBITORS OF THE VEGF RECEPTOR TYROSINE KINASE

Question 19

Sorafenib, Pazopanib, Sunitinib- Kinetics

Answer 19

METABOLIZED BY CYP3A4- AVOID ADMINISTRATION WITH INDUCERS (ST. JOHN’S WORT) OR INHIBITORS (GRAPEFRUIT JUICE)

PO

Question 20

Sorafenib, Pazopanib, Sunitinib- Clinical Use

Answer 20

RENAL CANCER

Sorafinib for hepatocelllular cancer

sunitinib for pancreatic neuroendocrine cancer and GI stromal tumors

Question 21

Sorafenib, Pazopanib, Sunitinib- Toxicities

Answer 21

rash
hand-foot syndrome
hypertension
reversible posterior leukoencephalopathy syndrome
perforation of GI tract
rare congestive heart failure

Question 22

Bevacizumab, Sorafenib, Pazopanib, Sunitinib- Cell Cycle Specificity

Answer 22

No

Question 23

Trastuzumab- Mech of Action

Answer 23

MONOCLONAL ANTIBODY AGAINST THE EXTRACELLULAR DOMAIN OF THE EPIDERMAL GROWTH FACTOR RECEPTOR HER-2/NEU

target= Her2-Neu

Question 24

Trastuzumab, Lapatinib, Pertuzumab- Clinical Use

Answer 24

HER-2/NEU POSITIVE BREAST CANCER

Her-2/Neu positive stomach and gastroesophogeal junction cancer

Question 25

Trastuzumab- Toxicities

Answer 25

Reversible heart failure- constant monitoring of cardiac function ``` Fever nausea vomiting infusion reaction diarrhea cough headache fatigue shortness of breath back pain rash muscle pain ```

Question 26

Lapatinib- Mech of Action

Answer 26

SMALL MOLECULE HER-2 TYROSINE KINASE INHIBITOR

Question 27

Pertuzumab- Mech of Action

Answer 27

MONOCLONAL ANTIBODY TO HER-2

Question 28

Trastuzumab, Lapatinib, Pertuzumab- Cell Cycle Specificity

Answer 28

No

Question 29

Crizotinib- Clinical Use

Answer 29

LUNG CANCER WITH ALK REARRANGEMENT

Question 30

Vemurafenib- Mech of Action

Answer 30

BRAF INHIBITOR

Question 31

Vemurafenib- Clinical Use

Answer 31

MELANOMAS WITH BRAF MUTATION

Question 32

Asparaginase- Mech of Action

Answer 32

BACTERIAL PRODUCT THAT HYDROLYZES L-ASPARAGINE= TUMOR CELLS CANNOT PRODUCE ASPARAGINE AND THUS PROTEIN SYNTHESIS IS HALTED

Question 33

Asparaginase- Clinical Use

Answer 33

ACUTE LYMPHOCYTIC LEUKEMIA

Question 34

Asparaginase- Toxicities

Answer 34

``` Allergic rxn clotting and bleeding pancreatitis hyperglycemia mental status changes ```

Question 35

Hydroxyurea- Mech of Action

Answer 35

ANALOG OF UREA THAT INHIBITS RIBONUCLEOTIDE REDUCTASE THEREBY INHIBITING DNA SYNTHESIS

Question 36

Hydroxyurea- Clinical Use

Answer 36

TREAT HIGH WBC COUNTS IN ACUTE MYELOGENOUS LEUKEMIA AND GRANULOCYTIC LEUKEMIA WITH BLAST CRISIS

Question 37

Hydroxyurea- Toxicities

Answer 37

nausea vomiting low blood counts rash

Question 38

All-trans-retinoic acid (tretinoin)- Mech of Action

Answer 38

INDUCES TERMINAL DIFFERENTIATION IN LEUKEMIC CELLS

Question 39

All-trans-retinoic acid (tretinoin)- Clinical Use

Answer 39

TREATMENT OF CHOICE IN ACUTE PROMYELOCYTIC LEUKEMIA (APL, M3)

Question 40

All-trans-retinoic acid (tretinoin)- Toxicities

Answer 40

Dry skin and mucous membranes Retinoic Syndrome: fever, weight gain, pulmonary infiltrateds, and pleural or pericardial effusions

Question 41

Arsenic Trioxide- Clinical Use

Answer 41

ACUTE PROMYELOCYTIC LEUKEMIA (APL, M3)

Question 42

All-trans-retinoic acid (tretinoin)- Toxicities

Answer 42

fatigue QT prolongation and a syndrome similar to retinoic acid syndrome