anti-cancer: mAb

Question 1

first anti-cancer mAb approved against cancers

Answer 1

rituximab

Question 2

how can rituximab kill cells

Answer 2

• antibody-dependent cell-mediated cytotoxicity
• complement
• apoptosis

Question 3

rarely trastuzumab can cause

Answer 3

cardiac dysfunction: risk increased if given with other cardiotoxic agents e.g. anthracyclines

Question 4

antibody that binds VEGF

Answer 4

bevacizumab

Question 5

how is bevacizumab given? for?

Answer 5

• with 5-fluorouracil
• for metastatic colon cancer, NSCLC & breast cancer

Question 6

inhibits EGFR

Answer 6

• cetuximab (receptor)
• erlotinib (receptor Tyr kinase)

Question 7

how to reverse irinotecan (topoisomerases inhibitor) resistance in colorectal cancers

Answer 7

give cetuximab (if EGFR overexpressed)

Question 8

erlotinib - use, side effects

Answer 8

• advanced NSCLC
• advanced pancreatic cancer

se: skin rashes, diarrhoea

Question 9

how to inhibit Bcr-Abl

Answer 9

imatinib mesylate

Question 10

imatinib use

Answer 10

• CML
• gastrointestinal stromal tumours (because can inhibit c-kit too)

Question 11

new small molecular ligands as new drug targets

Answer 11

• mTOR
• telomerase
• epigenetics, e.g. histone deacetylases

Question 12

how selectively toxic

Answer 12

IMPORTANCE: alkylating and cross linking agents, anti microtubule drugs and antifolates; antibodies and small molecule inhibitors
ACCUMULATION: anthracyclines trapped in reduced pH, and tumour cells more glycolysis > reduced pH
ACTIVATION: e.g. mitomycin C needs to be reduced and tumour cells are more hypoxic