Molecular biology

Question 1

Herceptin (Trastuzumab)

Answer 1

Humanised monoclonal antibody. Binds and blocks HER2. Originally licensed for final stage HER2+ cancer but now available to early stage pts.

Question 2

Drugs Herceptin is usually given with

Answer 2

Doxorubicin, cyclophosphamide, paclitaxel.

Question 3

Pertuzumab

Answer 3

Inhibits receptor dimerisation.

Question 4

Advexin

Answer 4

Adenoviral transfer of p53 into tumour cells. Head and neck cancers

Question 5

CDB3/PRIMA-1

Answer 5

Stabilises mutant p53 and restores transcriptional function.

Question 6

Pifithrin

Answer 6

Supreses endogenous p53 in normal tissue to reduce susceptibility to chemotherapy/radiation induce apoptosis.

Question 7

Avastin (Bevacizumab)

Answer 7

Humanised monoclonal antibody - anti-VEGFA. Given in cominbtation with 5-FU or Leucovorin or other kinase inhibitors.

Question 8

Dasatinib and nilotinib

Answer 8

2nd generation CML treatment. Bind active conformation of BCR-Abl. Ineffective against T315I mutation.

Question 9

JAK2 inhibitor

Answer 9

3rd generation CML treatment. Withdrawn from trials due to cardiotoxicity

Question 10

MEK inhibitor

Answer 10

C1-1040 (phase 1 trials for colon cancer)

Question 11

Raf inhibitor

Answer 11

Nexavar (sorafenib) approved for renal carcinoma, also binds VEGFR and PDGFR