Chemotherapy

Question 1

AZA, 6-MP

Answer 1

ANTIMETABOLITES (S phase)

• Purine analogs that dec den novo purine synthesis
• AZA metabolized to 6-MP
• Myelosuppression and metabolized by xanthin oxidase so inc toxicity if on allopurinol

Question 2

Cladribine

Answer 2

ANTIMETABOLITE

• Purine analog - inhibits DNA polymerase and causes DNA strand breaks
• Treats hairy cell leukemia
• Myelosuppression, neurotoxic and nephrotoxic

Question 3

Cytarabine

Answer 3

ANTIMETABOLITES

• Pyrimidine analog that inhibits DNA polymerase
• CYTopenia + anemia

Question 4

5 - FU

Answer 4

ANTIMETABOLITE

• Pyrimidine analog act –> 5-FdUMP which attached to thymidylate synthase –> no dTMP –> dec DNA synthesis
• Myelosupression and hand-foot syndrome

Question 5

Methotrexate

Answer 5

ANTIMETABOLITE

• Folic acid analog that competitively inhibits dihydrofolate reductase –> dec dTMP –> dec DNA synthesis
• PULM FIBROSIS, myelosupression, hepatotoxic, mouth ulcers

Question 6

Which work on M phase?

Answer 6

• microtubule inhibitors (block mitosis)
• Paclitaxel - microtubules hyperstabilized so no breakdown/ no anaphase (stay on axel)
• Vincristine/vinblastine - bind beta-tubulin so no polymerization –> microtubules (no vines)

Question 7

Topoisomerase Inhibitors

Answer 7

Topo I inhibitors - Irinotecan/ topotecan –> DNA cannot unwind and replicate (S phase)

Topo II inhibitors - (“two sides”) Etoposide/teniposide–> DNA degraded (G2 phase)

Question 8

Cell Cycle Independent

Answer 8

Platinum - cisplatin, carboplatin (cross-link DNA); ototoxic

Alkylating agents also crosslink DNA - busulfan (used in CML, causes pulm fibrosis), cyclophosphamide, ifosfamide, nitrosurea (brain tumors but also CNS side effects)

Question 9

Anti-tumor Abx

Answer 9

Bleomycin (G2 phase) - free radical break DNA strandsl causes pulm fibrosis and skin pigmentation

Doxorubicin/daunorubicin - intercalate DNA BUT cardiotoxic (give dexrazoxane)

Question 10

Hydroxyurea

Answer 10

ANTIMETABOLITE (S phase)

• inhibits ribonucleotide reductase –> dec DNA synthesis
• CML, PV, sickle cell, melanoma
• SEVERE MYELOSUPPRESSION

Question 11

Bevacizumab

Answer 11

MAB against VEGF

-Hemorrhage, clots, impaired wound healing

Question 12

Erlotinib

Answer 12

EGFR tyrosine kinase inhibitor for non-small cell lung caner

Rash, diarrhea

Question 13

Cetuximab

Answer 13

MAB against EGFR

Rash, diarrhea, inc LFTs

Question 14

Imatinib

Answer 14

TK inhibitor of BCR-ABL fusion protein (CML) and c-kit (GI stromal tumors)

-Fluid retention

Question 15

Rituximab

Answer 15

MAB against CD20 on B cells

-inc risk leukoencephalopathy

Question 16

Bortezomib/carfilzomib

Answer 16

Proteosome inhibitor (arrest at G2-M)

• In mult myeloma and mantle cell lymphoma
• Herpes zoster reactivation and peripheral neuropathy

Question 17

Tamoxifen / Raloxifene

Answer 17

SERMS - block estrogen from binding receptor

Tamox = endometrial cancer and hot flashes while ralox not (“you can relax”)

Question 18

Trastuzumab

Answer 18

MAB against HER-2

Cardiotoxicity

Question 19

Vemurafenib

Answer 19

Small molecule inhibitor of BRAF for melanoma