Drug Class and MOA

Question 1

5-azaC

Answer 1

1. Cytidine analog
2. Thought to inhibit methyltransferase leading to cytotoxicity and Also cause disassembly of ribosomes when used in RNA.

Question 2

SAHA (Vorinostat)

Answer 2

1. HDAC inhibitor

2. Accumulation of acetylated residues, inhibiting expression of genes and disrupting protein activity. (Cell death)

Question 3

Herceptin (Trastuzumab)

Answer 3

1. mAb against HER2 (EGFR) in breast tissue.
2. Binds EGFR and prevents signal transduction (MAPK/KRAS) and activation of signal cascade and causes receptor internalization.

Question 4

Erbitux (Cetuximab)

Answer 4

1. mAb against EGFR.
2. Binds EGFR and prevents signal transduction (MAPK/KRAS) and activation of signal cascade and causes receptor internalization.

Question 5

Tarceva (Erlotinib)

Answer 5

1. Reversible EGFR tyrosine kinase inhibitor.

2. Binds EGFR Tyrosine kinase activation (ATP binding site)

Question 6

Gleevec (imatinib)

Answer 6

1. BCR-ABL Tyrosine Kinase Inhibitor.

2. Inhibits substrate site on BCR-ABL fusion protein, preventing signaling for cell proliferation.

Question 7

Avastin (bevacizumab)

Answer 7

1. mAb angiogenesis inhibitor.

2. Inhibits VEGF-A, preventing it from binding the receptor which would initiate angiogenesis.

Question 8

Thalidomide

Answer 8

1. Anti-angiogenic.

2. Mainly teratogenic, inhibits angiogenesis.

Question 9

Vincristine

Answer 9

1. Organic drug - mitotic inhibitor. plant alkaloid.

2. Inhibits tuulin and disrupts mitotic spindle, then cell undergoes apoptosis.

Question 10

5-FU

Answer 10

1. Antimetabolite- inhibit DNA synthesis.
2. Inhibits Thymidylate synthase, therefore inhibiding PYRIMIDINE synthesis. Competes w/ endogenous dUMP which is normally used to make dTMP.

Question 11

Methotrexate

Answer 11

1. Antimetabolite - inhibit DNA synthesis.

2. Inhibits dihydrofolate reductase. therefore inhibits DNA base synthesis (pyrimidine and purine)

Question 12

Gardasil

Answer 12

1. HPV vaccine

2. Immunizes host against human papillomavirus.

Question 13

Cisplatin

Answer 13

1. Platinum alkylating agent - mainly Guanine.

2. Covalently cross-link DNA. May lead to apoptosis. Work in all phases of Cell cycle.

Question 14

Rituxan (rituximab)

Answer 14

1. mAb against CD20 on B cells.

2. Targets B cells - normal and malignant.

Question 15

Zytiga (abiraterone acetate)

Answer 15

1. Steroidal Anti-Androgen.
2. Inhibits CYP17A1 - decreasing circulating levels of androgens and DHEA. decreasing these slows the growth rate or prostate tumors.

Question 16

Opdivo (Nivolumab)

Answer 16

1. mAb against PD-1.
2. Binds PD-1 on activated T cells. Tumor cells expressing PD-1 ligand (PD-L1) can induce cell death in activated T cells when bound to PD-1 receptor.