Fitzpatrick - Targeted Therapy and Biologicals Flashcards Preview

Hematology and Oncology > Fitzpatrick - Targeted Therapy and Biologicals > Flashcards

Flashcards in Fitzpatrick - Targeted Therapy and Biologicals Deck (23):
1

Bcr-abl inhibitor name and MOA

- Imatibib or Dasintinib (CML tx).
- MOA - Occupies ATP cofactor binding stie on Bcl-abl, inhibiting transfer of phosphate to TK.

2

Tx for Imatinib resistant CML

Dasatinib

3

Selectivity of imatinib v. Dasatinib.

- Imatinib - Bcr-abl c-kit, PDGFR = CML, GIST
- Dasatinib - Bcr-abl, src = CML(imatinib resistant forms), (Ph+)ALL

4

Tx for Imatinib resistant GIST

Sunitinib

5

HER2+ is expressed in 1/4 of ___ cancer
overexpression v expression means what for survival?

breast cancer
Overexpression=3yr survival v. expression=6-7yr survival

6

Drugs that inhibit TK ERB Family signaling/target: HER2 receptor
Drugs that inhibit TK ERB Family signaling/target: EGFR receptor

HER2 = Lapatanib
EGFR2 = Erolotinib, Gefitinib, Lapatinib

7

Drugs that inhibit TK signaling/target: PDGFR receptor, VEGFR receptor

Sunitinib and Sorafenib

8

antibodies to drugs that inhibit EGFR receptors
antibodies to drugs that inhibit HER2 receptors
antibodies to drugs that inhibit VEGF LIGAND

EGFR receptor - PaCe = Panitumumab/Cetiximab
HER2 receptor - LapaTra = Trastuzumab
VEGF-ligand = bevacizumab

9

Vemurafinib inhibits mutant ___

Mutant BRAF V600E = Metastatic Malignant Melanoma

10

Drugs that inhibit TK signaling/target: BCR-Abl

Dasatinib, Imatinib

11

EGFR-receptor target/Cetuximab ab = ___ clinical use

colorectal; H/N (**no KRAS mutation)

12

EGFR-receptor target/panitumumab ab = ___ clinical use

Colorectal cancer (**no KRAS mutation)

13

HER2+ receptor target/trastuzumab ab = ___ clinical use

Breast cancer

14

VEGF ligand target/bevacizumab ab = ___ clinical use

Renal cell carcinoma

15

Why is KRAS a determinant of response to antibodies that inhibit EGFR activation?

Mutant KRAS is permanently activated; bypasses EGFR TK signaling.

16

Name the angiogenesis inhibitors (1 ab and 2 RTK inhibitors)

Ab - bevacizumab (targets a GF LIGAND --> used esp for RCC)
RTK inhibitors - Sunitinib, sorafenib

17

Why does RCC respond well to angiogenesis inhibitors?

Bc arises from mutation in VHL. VHL degrades HIF. Impaired VHL=more HIF=highly vascularized tumor.

18

Rituxomab treats what?

CD20+ B Cell Lymphoma

19

Breast cancer drugs: three

1. Lapatinib/Trastuzumab
2. Anastrazole (aromatase inhibitor = reversible)
3. Exemestane (aromatase inactivator = irreversible)

20

NSCLC drugs

(EGFR) Erlotinib, Gefitinib

21

Breast Cancer

Lapatinib - EGFR and HER2

22

GIST and RCC

Sunatinib (c-kit, PDGFR, VEGFR)

23

RCC and HCC

SoRAFenib (PDGFR, VEGFR)