Hypertension associated with VEGF inhibitors must be detected, treated

  • HemOnc Today, April 25, 2012
    Lisa Lohr, PharmD, BCPS, BCOP

Hypertension is a common adverse effect of chemotherapy agents that inhibit the vascular endothelial growth factor signaling pathway.

These agents include bevacizumab (Avastin, Genentech), sorafenib (Nexavar, Bayer HealthCare), sunitinib (Sutent, Pfizer), pazopanib (Votrient, GlaxoSmithKline) and axitinib (Inlyta, Pfizer).

Lisa Lohr

Lisa K. Lohr

It is important to detect and treat hypertension in patients receiving this therapy, as uncontrolled blood pressure could lead to serious cardiovascular complications.

Hypertension classification

Hypertension is one of the most common nononcologic medication conditions seen in patients with cancer. The reported prevalence of hypertension in the general population of adults in the United States ranges from 28% to 48%. The prevalence of pre-existing hypertension in patients with cancer is probably in the same range. The classification of hypertension by the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure (JNC 7) is noted in Table 1.

Table 1

The NCI–Common Terminology Criteria for Adverse Events describes hypertension as an adverse effect of cancer treatment somewhat differently, although these criteria have been revised to correspond more closely to the JNC 7 criteria than before.

Hypertension induced by VEGF pathway inhibitors can be seen in patients without a history of hypertension, as well as worsening BP control in those with pre-existing hypertension. It can be seen soon after starting therapy or may be delayed. The RR for hypertension is higher with certain VEGF agents, and it is at least partly dose-related.

Proposed mechanisms

VEGF signaling has vasodilation and hypotensive effects on the vascular endothelial cells. Likewise, inhibition of the VEGF pathway can lead to hypertension, likely due to an increase in the peripheral vascular resistance. The precise mechanism of this hypertension is not known, but it might be due to neurohormonal factors or a reduction in the number of microvessels (vascular rarefaction).

However, the leading proposed mechanism for VEGF inhibitor hypertension is the reduction of nitric oxide and prostacylin production seen in the vascular endothelium. This can lead to an increased systemic vascular resistance and hypertension. In addition, it has been proposed that the renin-angiotensin system is down-regulated because of the VEGF inhibitor-induced hypertension. Hypertension associated with VEGF inhibitors may be predictive of antineoplastic effect, as a sign of substantial VEGF pathway inhibition.

Patient management

Patients should be monitored carefully for the development or worsening of hypertension when therapy with a VEGF pathway inhibitor is started. Many patients have access to a home BP monitor, whereas those without access can have their BP monitored at a local clinic, pharmacy or other sites.

Patients can be advised to monitor their BP two to three times per week at the beginning of therapy. The BP goal for most patients is less than 140 mm Hg/90 mm Hg.

The JNC 7 recommends a lower goal of less than 130 mm Hg/80 mm Hg for patients with diabetes or chronic kidney disease. Patients with uncontrolled pre-existing hypertension who are not meeting goal BPs should have their antihypertensive medications adjusted before starting VEGF inhibitor therapy.

Table 2

In the absence of literature-based guidelines, hypertension caused by VEGF inhibitor therapy probably should be treated in the same manner as hypertension in patients without cancer. Lifestyle modifications in diet and exercise probably should be encouraged but may not be appropriate for some patients with cancer.

The recommendations in the JNC 7 report suggest starting with a thiazide diuretic for patients with stage I hypertension, although in the context of VEGF inhibitor chemotherapy, it is unlikely to be effective as monotherapy. Patients with stage II hypertension (systolic BP >160 mm Hg or diastolic BP >100 mm Hg) usually should be started on two antihypertensive agents. Loop diuretics usually are not recommended in these situations because the efficacy is lowered by inhibitors of nitric oxide.

Vasodilating agents such as nitrates might be very effective in treating hypertension caused by VEGF inhibitors, but nitrates possibly could reduce the antineoplastic effects. The choice of antihypertensive agents also should be guided by preferred medications for concomitant medical conditions (see Table 4).

Table 4

Calcium channel blockers

Calcium channel blockers with more cardiac tissue activity, such as verapamil and diltiazem, are less likely to be as effective as the dihydropyridine calcium channel blockers, which have more of an effect on the peripheral vessels. In addition, verapamil and diltiazem are CYP3A4 inhibitors and are likely to inhibit the hepatic metabolism of the anti-VEGF tyrosine kinase inhibitors.

Nifedipine would not be a good choice, as it can induce VEGF secretion. The dihydropyridine calcium channel blockers amlodipine and felodipine are the preferred agents and can be effective in controlling hypertension caused by VEGF inhibitors.

New beta-blocker

A new antihypertensive medication, nebivolol (Bystolic, Forest Labs), is a beta-blocker that reduces peripheral resistance by the nitric oxide pathway. This mechanism makes this agent an attractive choice for treating VEGF inhibitor-induced hypertension.

Treatment algorithm

M. Sitki Copur, MD, FACP, and Angela Obermiller, PharmD, both of Saint Francis Cancer Treatment Center in Grand Island, Neb., recently published their experiences with their algorithm for treating hypertension caused by inhibitors of the VEGF pathway. Besides incorporating the JNC 7 guidelines for medication choice based on comorbid conditions, they recommend secondary antihypertensive choices as shown in Table 3.

Table 3

Conclusion

Development or worsening of hypertension is commonly seen in patients treated with chemotherapy agents that inhibit the VEGF signaling pathway. Patients should have careful monitoring throughout therapy because it can develop early on or later.

The hypertension usually can be controlled with standard antihypertensive agents, although dose modification and dual therapy is often needed. The anti-VEGF therapy usually can be continued with careful management.

References:

  • Chobanian AV. Hypertension. 2003;42:1206-1252.
  • Copur MS. Clin Colorectal Cancer. 2011;10:151-156.
  • Izzedine H. Ann Oncol. 2009;20:807-815.

For more information:

  • Lisa K. Lohr, PharmD, BCPS, BCOP, is a clinical pharmacy specialist and oncology medication therapy management provider at Masonic Cancer Center at the University of Minnesota/Fairview in Minneapolis. She also is a HemOnc Today Editorial Board member. Dr. Lohr reports no relevant financial disclosures.

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