What Is Belzutifan and How Is It Used in Kidney Cancer?

Belzutifan (brand name Welireg) is a new targeted therapy approved for certain patients with kidney cancer, especially those with genetic conditions like von Hippel-Lindau (VHL) disease. It represents a new class of drugs called HIF-2α inhibitors, which work differently from older therapies by targeting a specific protein that fuels tumor growth in the kidneys and other organs.

How Does Belzutifan Work?

Belzutifan targets a protein called hypoxia-inducible factor 2-alpha (HIF-2α). In people with kidney cancer—especially those with VHL syndrome—this protein is often overactive, even when oxygen levels are normal. Overactivity of HIF-2α promotes:

  • Tumor cell survival
  • New blood vessel growth
  • Abnormal cell proliferation

By blocking HIF-2α, belzutifan disrupts the cancer’s energy supply, slowing or halting tumor growth.

Who Can Benefit?

Belzutifan is currently:

  • Approved for patients with von Hippel-Lindau disease-associated RCC
  • Being studied in clinical trials for broader use in sporadic advanced RCC, including patients who have progressed on immunotherapy or tyrosine kinase inhibitors

If trials confirm its effectiveness, belzutifan could become part of the mainstream treatment landscape for many forms of kidney cancer.

How Is It Taken?

  • Taken orally once daily, usually 120 mg
  • No food restrictions
  • Treatment continues until disease progression or unacceptable side effects

What Are the Side Effects?

Belzutifan is generally well tolerated, but may cause:

  • Low red blood cell count (anemia)
  • Fatigue
  • Headache
  • Dizziness
  • Shortness of breath
  • Low oxygen levels (hypoxia) — requires careful monitoring

Because of its unique mechanism, doctors may order regular oxygen level checks and blood tests during treatment.

Is It Effective?

In early trials, belzutifan has shown promising response rates, particularly in VHL-related tumors. Tumors have been observed to shrink or stop growing for extended periods, with relatively few severe side effects. Its role is expanding, and ongoing trials may soon make it available to more kidney cancer patients.

Looking for more questions?

Visit our Kidney Cancer Questions page for all other topics explained in plain language.

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