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Kinase inhibitors
Lecture 7
11
Pharmacology
Professional
04/14/2013

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Cards

Term
What are ABL inhibitors?
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 +
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
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
Term
What is an ALK inhibitor?
Definition
- Crizotinib - PO, cardiotoxic
**EML4-ALK fusion is constiutively active in 7% of non-small cell lung cancers
Term
What is a B-raf inhibitor?
Definition
- Vemurafenib
Term
What is an mTOR inhibitor?
Definition
- Everolimus
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
- Ras/Raf/MEK
- P13K/AKT
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
What is ERBB signalling?
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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