VEGF Inhibitors

Question 1

What drugs are in the VEGF Inhibitors class?

Answer 1

Drugs in this class are:
- Axitinib
- Cabozantinib
- Lenvatinib
- Vandetanib
- Pazopanib
- Regorafenib
- Sorafenib
- Sunitinib

Question 2

What is the brand name of Axitinib?

Answer 2

The brand name of this generic drug is:
- Inlyta

Question 3

What is the brand name of Cabozantinib?

Answer 3

The brand name of this generic drug is:
- Cabometyx
- Cometriq

Question 4

What is the brand name of Lenvatinib?

Answer 4

The brand name of this generic drug is:
- Lenvima

Question 5

What is the brand name of Vandetanib?

Answer 5

The brand name of this generic drug is:
- Caprelsa

Question 6

What is the brand name of Pazopanib?

Answer 6

The brand name of this generic drug is:
- Votrient

Question 7

What is the brand name of Regorafenib?

Answer 7

The brand name of this generic drug is:
- Stivarga

Question 8

What is the brand name of Sorafenib?

Answer 8

The brand name of this generic drug is:
- NexAVAR

Question 9

What is the brand name of Sunitinib?

Answer 9

The brand name of this generic drug is:
- Sutent

Question 10

What is the generic of name of Inlyta?

Answer 10

The generic name of this brand name drug is:
- Axitinib

Question 11

What is the generic of name of Cabometyx?

Answer 11

The generic name of this brand name drug is:
- Cabozantinib

Question 12

What is the generic of name of Cometriq?

Answer 12

The generic name of this brand name drug is:
- Cabozantinib

Question 13

What is the generic of name of Lenvima?

Answer 13

The generic name of this brand name drug is:
- Lenvatinib

Question 14

What is the generic of name of Caprelsa?

Answer 14

The generic name of this brand name drug is:
- Vandetanib

Question 15

What is the generic of name of Votrient?

Answer 15

The generic name of this brand name drug is:
- Pazopanib

Question 16

What is the generic of name of Stivarga?

Answer 16

The generic name of this brand name drug is:
- Regorafenib

Question 17

What is the generic of name of NexAVAR?

Answer 17

The generic name of this brand name drug is:
- Sorafenib

Question 18

What is the generic of name of Sutent?

Answer 18

The generic name of this brand name drug is:
- Sunitinib

Question 19

What are the main/common indications of the VEGF Inhibitors class?

Answer 19

The main/common indications of this drug class are:
- Endometrial cancer
- Hepatocellular carcinoma
- Renal cell carcinoma
- Thyroid cancer

Question 20

What is the class and MOA of Axitinib?

Answer 20

This drug in the following class:
- VEGF Inhibitors

This drug’s MOA is as follows:
- Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels

Question 21

What is the class and MOA of Cabozantinib?

Answer 21

This drug in the following class:
- VEGF Inhibitors

This drug’s MOA is as follows:
- Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels

Question 22

What is the class and MOA of Lenvatinib?

Answer 22

This drug in the following class:
- VEGF Inhibitors

This drug’s MOA is as follows:
- Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels

Question 23

What is the class and MOA of Vandetanib?

Answer 23

This drug in the following class:
- VEGF Inhibitors

This drug’s MOA is as follows:
- Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels

Question 24

What is the class and MOA of Pazopanib?

Answer 24

This drug in the following class:
- VEGF Inhibitors

This drug’s MOA is as follows:
- Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels

Question 25

What is the class and MOA of Regorafenib?

Answer 25

This drug in the following class: - VEGF Inhibitors This drug's MOA is as follows: - Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels

Question 26

What is the class and MOA of Sorafenib?

Answer 26

This drug in the following class: - VEGF Inhibitors This drug's MOA is as follows: - Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels

Question 27

What is the class and MOA of Sunitinib?

Answer 27

This drug in the following class: - VEGF Inhibitors This drug's MOA is as follows: - Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels

Question 28

What are the notable/common monitoring parameters for the VEGF Inhibitors class?

Answer 28

The notable/common monitoring parameters for this drug class are: - Blood pressure after 1 week, then every 2 weeks for 2 months, and at least monthly thereafter - Check urine for proteinuria at baseline and periodically during treatment (frequency depends on institutional standards, likely every 1-2 cycles) - TSH at baseline, then monthly for 4 months, then every 2 to 3 months - Baseline echocardiogram (sunitinib, pazopanib)

Question 29

Describe the emetic potential of the VEGF Inhibitors class.

Answer 29

The emetic potential of this drug class is: - Minimal-Low for all except cabozantinib and high dose Lenvatinib (>12 mg/day - Moderate-High)

Question 30

What is the emetic potential of Axitinib?

Answer 30

The emetic potential of this drug is: - Minimal-Low

Question 31

What is the emetic potential of Cabozantinib?

Answer 31

The emetic potential of this drug is: - Moderate-High

Question 32

What is the emetic potential of Lenvatinib?

Answer 32

The emetic potential of this drug is: - Minimal-Low if low dose <12 mg/day - Moderate-High if high dose >12 mg/day

Question 33

What is the emetic potential of Vandetanib?

Answer 33

The emetic potential of this drug is: - Minimal-Low

Question 34

What is the emetic potential of Pazopanib?

Answer 34

The emetic potential of this drug is: - Minimal-Low

Question 35

What is the emetic potential of Regorafenib?

Answer 35

The emetic potential of this drug is: - Minimal-Low

Question 36

What is the emetic potential of Sorafenib?

Answer 36

The emetic potential of this drug is: - Minimal-Low

Question 37

What is the emetic potential of Sunitinib?

Answer 37

The emetic potential of this drug is: - Minimal-Low

Question 38

What drugs in the VEGF Inhibitors class have a moderate-high emetic potential?

Answer 38

Drugs in the class with a high emetic potential are: - Cabozantinib - High dose Lenvatinib (>12 mg/day)

Question 39

What drugs in the VEGF Inhibitors class have a minimal-low emetic potential?

Answer 39

Drugs in the class with a moderate emetic potential are: - All except for Cabozantinib and high dose Lenvatinib (>12 mg/day) - Axitinib - Lenvatinib (low dose <12 mg/day) - Vandetanib - Pazopanib - Regorafenib - Sorafenib - Sunitinib

Question 40

Describe the metabolism of the VEGF Inhibitors class.

Answer 40

The metabolism of this drug class is as follows: - Hepatic (primarily metabolized by CYP3A4)

Question 41

What are the notable ADRs of Sunitinib?

Answer 41

The notable ADRs of this drug are: - This drug can cause yellowing of the skin and hair - Think "shine like the sun" to help you remember

Question 42

What are the notable/common ADRs of the VEGF Inhibitors class?

Answer 42

The notable/common ADRs of this drug class are: - Hypertension - Proteinuria - Bleeding/Thrombotic Events - Impaired Wound Healing - Hepatotoxicity

Question 43

Describe the strategy and rationale for management of hypertension caused by VEGF Inhibitors.

Answer 43

The strategy and rationale for management of this condition caused by this drug class are: - VEGF plays a role in nitric oxide production and vasodilation. When the VEGF-signaling pathway is inhibited, hypertension may occur secondary to the decrease in nitric oxide production. - Hypertension associated with drug class should be managed similarly to hypertension in the general population (JNC guidelines). - A common BP goal is <140/90 mmHg. - Patients should have their BP monitored (and well controlled) prior to starting therapy and then checked at least every 2 to 3 weeks for the duration of treatment.

Question 44

Describe the strategy and rationale for management of proteinuria caused by VEGF Inhibitors.

Answer 44

The strategy and rationale for management of this condition caused by this drug class are: - Proteinuria is a common adverse side effect of any anti-angiogenic agent. - VEGF is critical to the maintenance of normal renal function - Under-expression of VEGF can disrupt normal glomerular function leading to proteinuria. - Patients should have their urine checked for protein on a regular basis during VEGF inhibitor therapy. Frequency may vary per institutional protocol but it is often checked every 1-2 cycles of chemotherapy. - The presence of protein typically requires interruption of anti-VEGF therapy. - In the majority of cases, proteinuria resolves or significantly improves with removal of VEGF inhibitors.

Question 45

Describe the strategy and rationale for management of bleeding/thrombotic events caused by VEGF Inhibitors.

Answer 45

The strategy and rationale for management of this condition caused by this drug class are: - These agents are associated with bleeding events sich as: - Epistaxis - Hemoptysis - Hematemesis - Gastrointestinal bleeding (including GI perforation which is infrequent but potentially life-threatening) - These agents are associated with arterial thromboembolic events such as: - Stroke/transient ischemic attack - Myocardial infarction - This predisposition to thrombosis and bleeding after inhibition ofVEGF signaling reflects the multitude of actions VEGF has on vascular walls and the coagulation system.

Question 46

Describe the strategy and rationale for management of impaired wound healing caused by VEGF Inhibitors.

Answer 46

The strategy and rationale for management of this condition caused by this drug class are: - VEGF receptor inhibitors are associated with impaired wound healing due to decreased angiogenesis. - Therapy should typically be held for at least 1 month prior to surgery and only resumed when adequate wound healing has occurred.

Question 47

Describe the strategy and rationale for management of hepatotoxicity caused by VEGF Inhibitors.

Answer 47

The strategy and rationale for management of this condition caused by this drug class are: - The VEGF inhibitors undergo hepatic metabolism and many of them can cause hepatotoxicity. In fact, many of the TKls have a black boxed warning for hepatotoxicity - Depending on the level of AST/ALT elevations, you may need to hold or reduce the dose of the VEGF inhibitor.

Question 48

What are the risk factors for developing hypertension with VEGF Inhibitors?

Answer 48

Risk factors for developing this ADR with this drug/class are: - Pre-existing hypertension - Obesity - Older age

Question 49

What are the risk factors for developing thrombotic events with VEGF Inhibitors?

Answer 49

Risk factors for developing this ADR with this drug/class are: - Age greater than 65 years - Pre-existing history of thromboembolic events

Question 50

What are the clinical pearls of Cabozantinib?

Answer 50

The clinical pearls of this drug are as follows: - Cabozantinib is used to treat multiple disease states. However, the tablets and capsules are NOT interchangeable. - The tablets are used for renal cell carcinoma and the capsules are used for thyroid cancer.