Targeted Therapies - Fitz Flashcards Preview

Heme/Lymph 2 > Targeted Therapies - Fitz > Flashcards

Flashcards in Targeted Therapies - Fitz Deck (26):
1

How do tyrosine kinase inhibitors work?

Bind to ATP-binding site on TK and prevent enzyme from using ATP to phosphorylate target proteins

2

Imatinib

Bcr-Abl tyrosine kinase inhibitor

3

Dasatinib

Bcr-Abl tyrosine kinase inhibitor (Imatinib-resistance)

4

How does CML become resistant to Imatinib?

Slight mutation of Bcr-Abl TK ATP binding site

5

Imatinib uses

CML, GIST

6

Dasatinib

CML (Imatinib-resistant), [Ph]+ ALL

7

GIST has what TK mutations?

C-Kit, PDGFR

8

EGFR inhibitors

Lapatinib, Gefitinib, Erlotinib

9

HER2 receptor inhibitor

Lapatinib

10

PDGFR/VEGFR inhibitors

Sunitinib, Sorafenib

11

Inhibiting RTKs causes inhibition of what?

Downstream RAS/PI3K, AKT oncogenic signaling

12

EGFR...what cancer?

What drugs?

NSCLC

Erlotinib, Gefitinib

13

EGFR + HER2...what cancer?

What drug?

Breast

Lapatinib

14

C-KIT...what cancer?

What drugs?

GIST

Sunitinib, Imatinib

15

PDGFR, VEGFR...what cancer?

What drugs?

RCC

Sunitinib, Sorafenib

16

BRAF kinase...what cancer?

What drug?

Melanoma

Vemurafinib

17

Anti-EGFR antibody drugs

Cetuximab, Panitumumab

18

Anti-HER2 receptor antibody drug

Trastuzumab

19

Anti-VEGF ligand antibody drug

Bevacizumab

20

Bevacizumab (anti-VEGF) is used in what cancer?

Why is it good in this cancer?

RCC

Prevents angiogenesis, since RCC (VHL mutation) causes VEGF overproduction due to HIF accumulation causes highly vascular tumor

21

If a tumor is K-RAS positive, think what?

Cannot use an RTK inhibitor drug, must think otherwise

22

Rituximab

Anti-CD20 antibody, used for B-cell lymphoma (NHL) and leukemia (CLL)

23

3 "degrees" of Rituximab action on B-cells

- Complement-mediated cell lysis
- NK/T-cell cell lysis
- Apoptosis signal

24

When during treatment should antibody drugs be used?

Before chemo (sensitize tumor) or after (BM recovery 1st)

25

Aromatase inhibitor drugs

Anastrazole, Exemestane

26

When are Aromatase inhibitors beneficial?

Age group?

If the breast cancer is producing estrogen

Post-menopause (ovaries can't override the estrogen block)