Targeting Renal Cell Carcinoma with a HIF-2 antagonist

What is it about?

We used a mouse tumorgraft model to investigate the effectiveness of a new class of kidney cancer drug, the HIF-2 inhibitors. In the tumorgraft model, tumor samples from patients with a type of kidney cancer called renal cell carcinoma (RCC) are implanted into mice where they grow and look like the human tumor. HIF-2 is a key driver of RCC, and blocking its activity should inhibit tumor growth. We found that 50% of our mouse tumorgraft lines were inhibited by the HIF-2 inhibitor, PT2399.

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Why is it important?

Novel treatments for RCC have been lacking, and the HIF-2 inhibitor represents a new class of treatment. We show that the HIF-2 inhibitor, PT2399, is more efficacious and better tolerated than sunitinib. We also identify a potential biomarker of drug responsiveness, and identify mutations responsible for acquired resistance to the drug.