Lecture 8: Pharmacogenetics

Question 1

First antisense drug to be approved by the FDA

Answer 1

Vitravene

Question 2

An antibody → binds to HER2 receptor

Answer 2

Herceptin (trastuzumab)

Question 3

Is used in metastatic breast cancer treatment

Answer 3

Herceptin (trastuzumab)

Question 4

Only effective in about 20% of patients overexpressing the target HER2R

Answer 4

Herceptin (trastuzumab)

Question 5

Targeting responders only avoids cardiotoxicity and other ADRs (adverse drug reactions).

Answer 5

Herceptin (trastuzumab)

Question 6

Mechanism of action of Herceptin (trastuzumab)

Answer 6

Mechanism of action:

• Herceptin attaches to a HER2 cancer cell and may tell the body’s defense system to target the HER2 cancer
• May also stop the HER2 cancer cell from telling itself to grow and divide into more cancer cells (targets signalling and prevents growth)
• It prevents the receptor from receiving any growth factor signalling as these receptors become nonfunctional (prevent the cell from growing & dividing)

Question 7

Without this drug, the HER2 cancer cell keeps telling itself to grow and divide into more cancer cells.

Answer 7

Herceptin (trastuzumab)

Question 8

Is an antihypertensive drug

Answer 8

Debrisoquine

Question 9

Affected by the polymorphisms in cytochrome P450 2D6 (CYP2D6) = leads to excessive hypotension

Answer 9

Debrisoquine

Question 10

Anti-depressant

Answer 10

Paroxetine

Question 11

Response of this drug is affected by SNPs (single nucleotide polymorphisms) in the serotonin 2A receptor (5HT2A)

Answer 11

Paroxetine

Question 12

Depressed patients with C/C genotype at codon 102 that were treated with this drug, were significantly more likely to discontinue drug use due to adverse effects (46.3%) than those with the T/C and T/T genotypes (16%).

Answer 12

Paroxetine