Term
|
Definition
- Imatinib - PO, hepato/cardiotoxic
- Dasatinib - PO, for resistance to imatinib
- Nilotinib - PO, less hemorrhage
- Bosutinib - PO, myelo
- Ponatinib - PO. Hepato/cardio, hemorrhage
**must be philadelphia chromosome + |
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Term
| What are EGFR inhibitors? |
|
Definition
- Gefitinib - inhibits EGFR. Does not work w/ k-ras mutation and EML4-ALK translocation. PO
- Erlotinib - PO
- Lapatinib - Inhibits EGFR and HER2. PO, cardiotoxic due to HER2
**RASH |
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|
Term
| What are VEGF-R inhibitors? |
|
Definition
- Regorafanib - a multi-kinase inhibitor. PO
- Pazopanib - PO
**VEGF responsible for angiogenesis. Block phosphorylation of receptor
**AE: GI perforation, poor wound healing, hemorrhage |
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Term
| What is an ALK inhibitor? |
|
Definition
- Crizotinib - PO, cardiotoxic
**EML4-ALK fusion is constiutively active in 7% of non-small cell lung cancers |
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|
Term
| What is a B-raf inhibitor? |
|
Definition
|
|
Term
| What is an mTOR inhibitor? |
|
Definition
|
|
Term
| What are the 3 categories of kinases? |
|
Definition
- Tyrosine kinase
- Serine/threonine kinase
- S/T/Th kinase
**Constitutively active in cancer |
|
|
Term
| What are the 2 signalling pathways for tyrosine kinase? |
|
Definition
|
|
Term
| What is the philadelphia chromosome? |
|
Definition
| Translocation of chromosome 9:22 -- BCR-ABL is constitutively active. In 95% of CML |
|
|
Term
| How do ABL inhibitors work? |
|
Definition
Compete for ATP binding on BCR-ABL fusion protein, preventing phosphorylation
Imatinib --> Dasa/Nilo --> bosu --> pona in terms of spectrum and mutants |
|
|
Term
|
Definition
- ERBB1 = EGFR/HER1 - overexpressed in solid tumors
- ERBB2 = HER2 - overexpressed in breast cancer
**Turns on the 2 signalling pathways RAS and P13K |
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