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Tivozanib

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Tivozanib

Tivozanib, sold under the brand name Fotivda, is a medication used for the treatment of advanced renal cell carcinoma (kidney cancer). It is an oral VEGF receptor tyrosine kinase inhibitor.

The most common side effects include fatigue (tiredness), hypertension (high blood pressure), diarrhea, decreased appetite, nausea, dysphonia (voice changes), hypothyroidism, cough, and stomatitis.

Tivozanib was approved for medical use in the European Union in August 2017, and in the United States in March 2021.

In the United States, tivozanib is indicated for the treatment of adults with relapsed or refractory advanced renal cell carcinoma following two or more prior systemic therapies.

In the European Union, it is indicated for the treatment of adults with advanced renal cell carcinoma; and for the first line treatment of adults with advanced renal cell carcinoma and for adults who are VEGFR and mTOR pathway inhibitor-naïve following disease progression after one prior treatment with cytokine therapy for advanced renal cell carcinoma.

Tivozanib must not be combined with St. John's Wort, an inducer of the liver enzyme CYP3A4. It should not be taken during pregnancy as it is teratogenic, embryotoxic and fetotoxic in rats.

The most common side effects in studies were hypertension (high blood pressure, in 48% of patients), dysphonia (hoarse voice, 27%), fatigue and diarrhea (both 26%). A hypertensive crisis occurred in 1% of patients.

Administration of a single dose of tivozanib with rifampicin, a strong inducer of the enzyme CYP3A4, cuts the biological half-life and total exposure (area under the curve) of tivozanib in half, but has no relevant influence on highest concentrations in the blood. Combination with ketoconazole, a strong CYP3A4 inhibitor, has no relevant effects. The clinical significance of these findings is not known.

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