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Pharm II Test 4 > Chemo V Target Therapy > Flashcards

Chemo V Target Therapy Flashcards

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1
Q

Imatinib mesylate, Dasatinib, Nilotinib- Mech of Action

A

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

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2
Q

Imatinib mesylate, Dasatinib, Nilotinib- Cell Cycle Specificity

A

No

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3
Q

Imatinib mesylate, Dasatinib, Nilotinib- Kinetics

A

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

PO

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4
Q

Imatinib mesylate, Dasatinib, Nilotinib- Clinical Use

A

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

GI STROMAL TUMORS

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5
Q

Imatinib mesylate, Dasatinib, Nilotinib- Toxicities

A 
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

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6
Q

Cetuximab, Panitumumab- Mech of Action

A

MONOCLONAL ANTIBODY INHIBITOR OF EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR)

target= EGFR

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7
Q

Cetuximab, Panitumumab- Cell Cycle Specificity

A

No

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8
Q

Cetuximab, Panitumumab- Clinical Use

A

METASTATIC COLORECTAL CANCER
lung cancer
head & neck cancers

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

Panitumumab= fully humanized monoclonal antibody

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9
Q

Cetuximab- Toxicities

A

RASH
hypersensitivity
diarrhea
hypomagnesemia

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10
Q

Erlotinib- Mech of Action

A

SMALL MOLECULE INHIBITOR OF EGFR ASSOCIATED TYROSINE KINASE

target= EGFR associated tryosine kinase

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11
Q

Erlotinib- Cell Cycle Specificity

A

No

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12
Q

Erlotinib- Kinetics

A

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

PO

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13
Q

Erlotinib- Clinical Use

A

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

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14
Q

Erlotinib- Toxicities

A

rash
nausea
anorexia
fatigue

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15
Q

Bevacizumab- Mech of Action

A

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

target= VEGF

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16
Q

Bevacizumab- Clinical Use

A

lung cancer

metastatic colorectal cancer

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17
Q

Bevacizumab- Toxicities

A 
perforation of colon
infusion reactions
hypertension
arterial clots
bleeding
reversible posterior leukoencephalopathy syndrome (headache, mental status change, visual changes)
18
Q

Sorafenib, Pazopanib, Sunitinib- Mech of Action

A

SMALL MOLECULE INHIBITORS OF THE VEGF RECEPTOR TYROSINE KINASE

19
Q

Sorafenib, Pazopanib, Sunitinib- Kinetics

A

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

PO

20
Q

Sorafenib, Pazopanib, Sunitinib- Clinical Use

A

RENAL CANCER

Sorafinib for hepatocelllular cancer

sunitinib for pancreatic neuroendocrine cancer and GI stromal tumors

21
Q

Sorafenib, Pazopanib, Sunitinib- Toxicities

A 
rash
hand-foot syndrome
hypertension
reversible posterior leukoencephalopathy syndrome
perforation of GI tract
rare congestive heart failure
22
Q

Bevacizumab, Sorafenib, Pazopanib, Sunitinib- Cell Cycle Specificity

A

No

23
Q

Trastuzumab- Mech of Action

A

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

target= Her2-Neu

24
Q

Trastuzumab, Lapatinib, Pertuzumab- Clinical Use

A

HER-2/NEU POSITIVE BREAST CANCER

Her-2/Neu positive stomach and gastroesophogeal junction cancer

25
Q

Trastuzumab- Toxicities

A

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
26
Q

Lapatinib- Mech of Action

A

SMALL MOLECULE HER-2 TYROSINE KINASE INHIBITOR

27
Q

Pertuzumab- Mech of Action

A

MONOCLONAL ANTIBODY TO HER-2

28
Q

Trastuzumab, Lapatinib, Pertuzumab- Cell Cycle Specificity

A

No

29
Q

Crizotinib- Clinical Use

A

LUNG CANCER WITH ALK REARRANGEMENT

30
Q

Vemurafenib- Mech of Action

A

BRAF INHIBITOR

31
Q

Vemurafenib- Clinical Use

A

MELANOMAS WITH BRAF MUTATION

32
Q

Asparaginase- Mech of Action

A

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

33
Q

Asparaginase- Clinical Use

A

ACUTE LYMPHOCYTIC LEUKEMIA

34
Q

Asparaginase- Toxicities

A 
Allergic rxn
clotting and bleeding
pancreatitis
hyperglycemia
mental status changes
35
Q

Hydroxyurea- Mech of Action

A

ANALOG OF UREA THAT INHIBITS RIBONUCLEOTIDE REDUCTASE THEREBY INHIBITING DNA SYNTHESIS

36
Q

Hydroxyurea- Clinical Use

A

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

37
Q

Hydroxyurea- Toxicities

A

nausea
vomiting
low blood counts
rash

38
Q

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

A

INDUCES TERMINAL DIFFERENTIATION IN LEUKEMIC CELLS

39
Q

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

A

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

40
Q

All-trans-retinoic acid (tretinoin)- Toxicities

A

Dry skin and mucous membranes

Retinoic Syndrome: fever, weight gain, pulmonary infiltrateds, and pleural or pericardial effusions

41
Q

Arsenic Trioxide- Clinical Use

A

ACUTE PROMYELOCYTIC LEUKEMIA (APL, M3)

42
Q

All-trans-retinoic acid (tretinoin)- Toxicities

A

fatigue
QT prolongation
and a syndrome similar to retinoic acid syndrome

Pharm II Test 4 (5 decks)

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