Selpercatinib interactions

Food & lifestyle

• grapefruit juice

  Major

  Metabolism

  Grapefruit juice may increase the plasma concentrations of selpercatinib. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. Inhibition of hepatic CYP450 3A4 may also contribute.

  What to do: Patients should limit or avoid consumption of grapefruit and grapefruit juice during treatment with selpercatinib.

  2 sources

  1. Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0
  2. "Product Information. Retevmo (selpercatinib)." Lilly, Eli and Company (2020):

Conditions

Conditions in which Selpercatinib needs care, as documented in this source.

• Arrhythmias, Cardiac

  Moderate

  Selpercatinib can cause concentration-dependent QT interval prolongation. It is recommended to assess QT interval, electrolytes, and TSH at baseline and periodically during treatment and to adjust treatment based upon risk factors. Correct hypokalemia, hypomagnesemia, and hypocalcemia before initiating treatment. Monitor regularly for these laboratory values and correct them as clinically appropriate. Withhold, reduce the dose or permanently discontinue treatment based on the severity.

  1 source

  1. "Product Information. Retevmo (selpercatinib)." Lilly, Eli and Company (2020):

• Hemorrhage

  Moderate

  Serious including fatal hemorrhagic events can occur with the use of selpercatinib. Care should be exercised when using this agent in patients with bleeding disorders. It is recommended to permanently discontinue treatment in patients with severe or life-threatening hemorrhage.

  1 source

  1. "Product Information. Retevmo (selpercatinib)." Lilly, Eli and Company (2020):

• Hypertension

  Moderate

  Selpercatinib may cause hypertension and therapy should not be initiated in patients with uncontrolled hypertension. Care should be exercised when using this agent in hypertensive patients. Optimize blood pressure before starting treatment. It is recommended to monitor blood pressure after 1 week, and regularly as clinically indicated. Initiate or adjust anti-hypertensive therapy as appropriate. Withhold, reduce dose, or permanently discontinue treatment based on the severity.

  1 source

  1. "Product Information. Retevmo (selpercatinib)." Lilly, Eli and Company (2020):

• Kidney Failure, Chronic

  Moderate

  The use of selpercatinib may increase serum creatinine. It is recommended to consider alternative markers of renal function if persistent elevations in serum creatinine are observed. No dosage modification is recommended for patients with mild to moderate renal impairment. Exercise caution when using this agent in patients with severe renal impairment or end-stage renal disease as the recommended dosage has not been established for these patients.

  1 source

  1. "Product Information. Retevmo (selpercatinib)." Lilly, Eli and Company (2020):

• Liver Diseases

  Moderate

  Selpercatinib is metabolized predominantly by CYP450 3A4. The dose of selpercatinib should be reduced in patients with severe hepatic impairment. No dosage modification is recommended for patients with mild or moderate hepatic impairment. Serious hepatic adverse reactions have been reported in patients treated with selpercatinib. Monitor ALT and AST before starting therapy with selpercatinib, every two weeks during the first three months, then monthly thereafter and as clinically indicated. It is recommended to withhold, reduce dose or permanently discontinue treatment based on the severity of selpercatinib-related adverse reactions in patients with hepatic impairment.

  1 source

  1. "Product Information. Retevmo (selpercatinib)." Lilly, Eli and Company (2020):