B / 33 : Drugs Used In Cancer Treatment IV (small Molecule Signal Transduction Inhibitors)

Question 1

How do low molecular weight inhibitors work?

Answer 1

Targets the activated proto-oncogenes and the kinases that are constantly activated due to inactivation of tumor suppressor genes

Question 2

What are the types of small molecule inhibitors?

Answer 2

• TK inhibitors
• Serine / threonine kinase signaling inhibitors
• Proteasome inhibitors
• Vitamin analog : retinoid

Question 3

What is an example of a BCR-ABL TK inhibitor?

Answer 3

Imatinib

Question 4

Imatinib
- MOA
- Effect
- Indication
- SE

Answer 4

• Tyrosine kinase inhibitor
• Inhibits kinase activity of the protein product of the BCR-ABL gene
• for CML, GIST (gastrointestinal stromal tumors)
• Diarrhea, edema, cardiotoxicity

(I’m a tiny B - TK : sword (to kill in cs:go)

Question 5

What are the EGFR TK inhibitors?

Answer 5

• Gefitinib
• Erlotinib
• Lapatinib

Question 6

Gefitinib, Erotinib
- MOA
- Effect
- Indication
- SE

Answer 6

• EGFR inhibitor
• Inhibition of tumorigenesis
• Non-small cell lung carcinoma, pancreatic cancer
• Rashes, diarrhea

(Get fit : muscles - ero : ear lobe - tiny b)

Question 7

Lapatinib
- MOA
- Effect
- Indication
- SE

Answer 7

• EGFR inhibitor
• Inhibition of tumorigenesis
• Breast cancer
• Diarrhea, cardiotoxicity

Question 8

What is an example of a multiTIK signaling drug?

Answer 8

Sunitinib

Question 9

Sunitinib
- MOA
- Effect
- Indication
- SE

Answer 9

• TK receptor inhibitor (PDGF, VEGF)
• Inhibition of tumorigenesis
• Kidney cancer, GIST
• Diarrhea, vomiting, hypertension

Question 10

Ibrutinib
- MOA
- Indication
- SE

Answer 10

• TK inhibitor
• CLL, lymphocytic lymphoma
• URT infections

Question 11

Crizotinib
- MOA
- Effect
- Indication
- SE

Answer 11

• ALK kinase inhibitor
• ROS1 oncogene inhibitor
• For non small cell lung carcinoma
• Diarrhea, vomiting

Question 12

What are the serine / threonine kinase signaling inhibitors?

Answer 12

• Everolimus
• Dabrafenib + trametinib

Question 13

Everolimus
- MOA
- Indication
- SE

Answer 13

• mTOR inhibitor
• Breast and kidney cancer
• Anemia, stomatitis

Question 14

Dabrafenib + trametinib
- MOA
- Indiation
- SE

Answer 14

• Dabrafenib : BRAF inhibitor / Trametinib : MEK inhibitor
• For melanoma
• Hyperkeratosis, hand-foot syndrome

Question 15

What is an example of a proteasome inhibitor?

Answer 15

Bortezomib

Question 16

Bortezomib
- MOA
- Effect
- Indication
- SE

Answer 16

• Proteasome inhibitor
• Prevent degradation of pro-apoptotic factors
• For multiple myeloma
• Peripheral neuropathy, thrombocytopenia

Question 17

Tretinoin
- MOA
- Effect
- Indication
- SE

Answer 17

• Synthetic form of vitamin A
• Promotes differenciation of promyelocytes
• For AML
• Teratogenic, edema, fever