(8) Antineoplastics: Kinase Inhib & MABs (3.1-3.2)

Question 1

Suffix: Small molecule kinase inhibitors

Answer 1

“-nib”

Question 2

Suffix: Tyrosine kinase inhibitors

Answer 2

”-tinib”

Question 3

Name 2 tyrosine kinases inhibited by Imatinib

Answer 3

(1) c-kit
(2) BCR/ABL
* (Also PDGF via inhibiting its receptor)*

Question 4

What translocation is present in the Philadelphia chromosome?

Answer 4

t(9;22)

Question 5

What type of cancers commonly overexpress c-kit?

Answer 5

Gastrointestinal stromal tumors

Question 6

Adverse Effect: Imatinib

Answer 6

Fluid retention

Question 7

MOA: Erlotinib

Answer 7

EGFR tyrosine kinase inhibitor

Question 8

Which biologic is first line for treating non-small cell lung cancer?

Answer 8

Erlotinib

Question 9

Adverse Effect (2) : Erlotinib

Answer 9

(1) Acneiform rash
(2) Diarrhea

Question 10

Name 2 small molecule tyrosine kinase inhibitors of VEGFR

Answer 10

(1) Sunitinib
(2) Sorafenib

Question 11

Adverse Effects (2) : Sunitinib

Answer 11

(1) Hyperkeratosis and skin rashes
(2) Hemorrhages
* (Sorafenib also carries the same risks)*

Question 12

MOA: Vemurafenib

Answer 12

Inhibits B-Raf

Question 13

What is Vemurafenib used to treat?

Answer 13

(+) BRAF Malignant Melanoma

Question 14

Name a tyrosine kinase inhibitor which is effective against renal cell carcinoma

Answer 14

Sunitinib

(Sorafenib would work too. Renal cell carcinoma often secretes EPO, so it makes sense)

Question 15

Name 2 cancers Imatinib is used to treat

Answer 15

(1) Gastrointestinal stromal tumors
(2) CML – due to t(9;22)
* (Also some forms of ALL that are (+) BCR/ABL)*

Question 16

MOA: Rituximab

Answer 16

anti-CD20

(⇒ Complement mediated lysis and antibody-dependent cell cytotoxicity)

Question 17

MOA: Cetuximab

Answer 17

anti-EGFR

Question 18

MOA: Bevacizumab

Answer 18

anti-VEGF

(Same MOA for Ranibizumab)

Question 19

MOA: Alemtuzumab

Answer 19

anti-CD52

Question 20

MOA: Trastuzumab

Answer 20

anti-HER2

Question 21

Suffix: Chimeric monoclonal antibodies

Answer 21

“-uximab”

Question 22

Name 2 monoclonal antibodies which can be used to treat CLL

Answer 22

(1) Rituximab
(2) Alemtuzumab

Question 23

Indications - Non-neoplastic (2) : Rituximab

Answer 23

(1) Rheumatoid arthritis
(2) Vasculitides

Question 24

What type of cancers does Cetuximab treat?

Answer 24

Solid tumors

Question 25

What is a notable side effect associated with the administration of anti-tumor antibodies?

Answer 25

Infusion reaction

(Hypotension, rash, dyspnea, pruritus)

Question 26

What adverse reaction can occur 7-10 days after administering Rituximab?

Answer 26

Serum sickness

(Type III hypersensitivity reaction, can also occur with Cetuximab, but far less often)

Question 27

Adverse Effect: Cetuximab

Answer 27

Acneiform rash

(Same side effect as Erlotinib, another EGFR inhibitor)

Question 28

What monoclonal antibody inhibits vasculature proliferation in tumors?

Answer 28

Bevacizumab

Question 29

Indication - Non-neoplastic: Bevacizumab

Answer 29

Wet macular degeneration

Question 30

Adverse Effects (3) : Bevacizumab

Answer 30

(1) Bleeding
(2) Thrombotic events
(3) GI perforation

Question 31

Name a drug associated with higher risk of progressive multifocal leukoencephalopathy

Answer 31

Rituximab

(Also Natalizumab, an antibody against α4-integrin)

Question 32

Indication: Trastuzumab

Answer 32

HER2 (+) Breast Cancer

Question 33

Adverse Effect: Trastuzumab

Answer 33

Cardiotoxicity

(“Heartceptin” damages the heart)

Question 34

What type of cancers does Bevacizumab treat?

Answer 34

Metastatic tumors