Chemo drugs reduced 5

Question 1

Imatinib

Answer 1

Tyrosine Kinase inhibitor of BCR-ABL and c-kit

Use: CML, GI stromal tumors

• resistance will develop
• not known to be curative at this time

Metabolized: CYP3A4-avoid induces and inhibitors

Side effects: superficial edema, nausea, muscle cramps, abdominal pain, anemia, neutropenia, and thrombocytopenia

• oral
• monitor TSH levels-increases clearance of thyroid hormone in hypothyroid patients taking thyroid replacement

Question 2

Cetuximab

Answer 2

Monoclonal antibody to EGFR-inhibits autophosphorylation process
-active in metastatic lung and colon, head and neck cancers receiving radiation treatment

Colorectal cancer:
Kras and Nras mutational analysis
wildtype: may respond
mutated: no response

Lung and Head and Neck:
Not selected on basis of EGFR expression and kras mutational status

Side effects: rash, diarrhea, hypomagnesemia, infusion reaction

Question 3

Erlotinib

Answer 3

Small molecule inhibitor of EGFR tyrosine kinase

• oral
• rash, nausea, anorexia, fatigue

Question 4

What type of lung cancer and lung cancer patient would you want to use EGFR tyrosine kinase inhibitors?

Answer 4

Adenocarcinoma, bronchoalveolar
women, asian, never smokers

-perform mutational analysis on non-small cell lung cancers for EGFR activating mutaiton

Question 5

Bevacizumab

Answer 5

Monoclonal antibody against VEGF. inhibits angiogenesis

Treat: metastatic colon cancer and metastatic lung cancer when combined with chemo

Side effects: hypertension, proteinuria, arterial blood clots, reversible posterior leukoencephalopathy syndrome, infusion reactions

Not active as single agent! administered iv with chemo

Question 6

Sunitinib, Pazopanib, Sorafenib

Answer 6

VEGF receptor tyrosine kinase inhibitors

metabolized by CYP3A4

• hand foot syndrome and rashes, congestive heart failure and bevacizumab side effects
• renal cell cancer

Question 7

Sunitinib also used in

Answer 7

pancreatic neuroendocrine cancer, GI stromal tumor

Question 8

Sorafenib also used in

Answer 8

unresectable hepatocellular cancer

Question 9

Trastuzumab

Answer 9

extracellular domain EGFR receptor, Her-2/neu

-IV with chemo

• Cardiotoxicity
• greatest risk in patients receiving concurrent anthracycline
• not dose dependent
• reversible!!
• serial monitoring of cardiac ejection fraction

Question 10

Crizotinib

Answer 10

Treats patients with ALK- rearrangement with adenocarcinoma
-younger little or no exposure to smoke

perform mutational analysis on lung cancer for ALK rearrangement

Question 11

Vemurafenib

Answer 11

melanoma with BRAF mutation
-mutational analysis in melanoma cancers (V600E mutation in BRAF)

oral drug

Question 12

L-asparaginase

Answer 12

depletes asparagine pools rapidly-decreased protein synthesis

-leukemia cells lack asparagine synthase
Use in: Acute Lymphoblastic Leukemia

-allergic reactions, liver enzyme elevations, clotting, pancreatitis and elevated glucose

Question 13

Hydroxyurea

Answer 13

Inhibits DNA synthesis by inhibiting ribonucleotide reductase

• used initially to control high white count in patients with AML
• oral

Question 14

All-trans retinoic acid

Answer 14

Induces terminal differentiation in leukemic cells in APL

-combined with chemo

• mucocutaneous toxicity
• retinoic acid sydnrome: fever, weight gain, lung infiltrates, and pleural or pericardial effusions

Question 15

Arsenic Trioxide

Answer 15

• relapsed APL

- fatigue, weight gain, retinoic acid syndrome, QT prolongation