VEGF Inhibitors Flashcards

1
Q

What drugs are in the VEGF Inhibitors class?

A

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

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2
Q

What is the brand name of Axitinib?

A

The brand name of this generic drug is:
- Inlyta

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3
Q

What is the brand name of Cabozantinib?

A

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

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4
Q

What is the brand name of Lenvatinib?

A

The brand name of this generic drug is:
- Lenvima

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5
Q

What is the brand name of Vandetanib?

A

The brand name of this generic drug is:
- Caprelsa

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6
Q

What is the brand name of Pazopanib?

A

The brand name of this generic drug is:
- Votrient

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7
Q

What is the brand name of Regorafenib?

A

The brand name of this generic drug is:
- Stivarga

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8
Q

What is the brand name of Sorafenib?

A

The brand name of this generic drug is:
- NexAVAR

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9
Q

What is the brand name of Sunitinib?

A

The brand name of this generic drug is:
- Sutent

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10
Q

What is the generic of name of Inlyta?

A

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

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11
Q

What is the generic of name of Cabometyx?

A

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

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12
Q

What is the generic of name of Cometriq?

A

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

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13
Q

What is the generic of name of Lenvima?

A

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

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14
Q

What is the generic of name of Caprelsa?

A

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

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15
Q

What is the generic of name of Votrient?

A

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

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16
Q

What is the generic of name of Stivarga?

A

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

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17
Q

What is the generic of name of NexAVAR?

A

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

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18
Q

What is the generic of name of Sutent?

A

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

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19
Q

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

A

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

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20
Q

What is the class and MOA of Axitinib?

A

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

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21
Q

What is the class and MOA of Cabozantinib?

A

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

22
Q

What is the class and MOA of Lenvatinib?

A

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

23
Q

What is the class and MOA of Vandetanib?

A

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

24
Q

What is the class and MOA of Pazopanib?

A

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

25
Q

What is the class and MOA of Regorafenib?

A

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

26
Q

What is the class and MOA of Sorafenib?

A

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

27
Q

What is the class and MOA of Sunitinib?

A

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

28
Q

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

A

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)

29
Q

Describe the emetic potential of the VEGF Inhibitors class.

A

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

30
Q

What is the emetic potential of Axitinib?

A

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

31
Q

What is the emetic potential of Cabozantinib?

A

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

32
Q

What is the emetic potential of Lenvatinib?

A

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

33
Q

What is the emetic potential of Vandetanib?

A

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

34
Q

What is the emetic potential of Pazopanib?

A

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

35
Q

What is the emetic potential of Regorafenib?

A

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

36
Q

What is the emetic potential of Sorafenib?

A

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

37
Q

What is the emetic potential of Sunitinib?

A

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

38
Q

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

A

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

39
Q

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

A

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

40
Q

Describe the metabolism of the VEGF Inhibitors class.

A

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

41
Q

What are the notable ADRs of Sunitinib?

A

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

42
Q

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

A

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

43
Q

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

A

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.

44
Q

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

A

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.

45
Q

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

A

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.

46
Q

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

A

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.

47
Q

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

A

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.

48
Q

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

A

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

49
Q

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

A

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

50
Q

What are the clinical pearls of Cabozantinib?

A

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.