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Flashcards in Targeted Therapies Deck (13)
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1
Q

Erlotinib

A

Prevents phosphorylation of EGFR tyrosine kinase receptor

EGFR activates P13K, which leads to cell cycle progression via communication with mTOR

2
Q

Crizotinib

A

Helps to treat EML4-ALK mutations in lung cancer

Mutation is present in about 5% of lung cancers

Cancer is usually an adenocarcinoma

3
Q

Cetuximab

A

Prevents ligand binding to the EGFR tyrosine kinase receptor, which is the gateway to a bunch of different signaling pathways that result in increased cell proliferation, decreased apoptosis, increased invasion and metastasis, or increased angiogenesis.

4
Q

Glioma: definition and graded severity

A

These are the most common kind of brain neoplasm

They are derived from glial cells

Grades I-II are benign.

Grades III-IV are malignant

Grade V is glioblastoma

5
Q

Glioblastoma

A

A grade V glioma

6
Q

Bevacizumab

A

Used to treat glioblastomas

Sequesters VEGF-A and prevents VEGRF-2 activation. In short, it prevents ligand-binding to the VEGFR2 tyrosine kinase receptor. This effectively inhibits the Ras and P13K pathways, both of which lead to cell proliferation and mobility via transcription, protein synthesis, division, and migration.

7
Q

Sunitinib

A

Inhibits the VEGF tyrosine kinase receptor

Median duration of response is about 10 months

8
Q

Tamoxifen

A

This blocks the estrogen receptor. Estrogen can initiate nuclear genomic responses, but in cancer cells, signal cross-talk between it and various tyrosine kinase receptors can lead to inappropriate cell proliferation.

This drug has a 50% response rate and >12 month median response duration in women with metastatic breast cancer.

9
Q

Everolimus added to tamoxifen

A

This combination delayed metastatic breast cancer progression by 4 months

10
Q

Trastuzumab (Herceptin)

A

34% improvement in overall survival in adjuvant setting for HER-2-positive breast cancer

11
Q

Enzalutamide

A

This is an androgen receptor blockade

Survival rate improved by five months in castrate resistant cancer, which is a cancer that progresses despite markedly suppressed testosterone levels

12
Q

Vemurafenib

A

A BRAF inhibitor that fights against BRAF mutations

13
Q

Vismodegib

A

This is a hedgehog inhibitor that shows 43% response in locally advanced basal cell skin cancers