Selpercatinib (RETEVMO)

Differentiated thyroid carcinoma (RET-positive), advanced or metastatic

Medullary thyroid cancer (RET-positive), advanced or metastatic

Non-small cell lung cancer (RET-positive), advanced or metastatic

Differentiated thyroid carcinoma (RET-positive), advanced or metastatic

• Dose – Oral (patients ≥50 kg): 160 mg twice daily continuously until disease progression or unacceptable toxicity
• Dose – Oral (patients <50 kg): 120 mg twice daily continuously until disease progression or unacceptable toxicity

Medullary thyroid cancer (RET-positive), advanced or metastatic

• Dose – Oral (patients ≥50 kg): 160 mg twice daily continuously until disease progression or unacceptable toxicity
• Dose – Oral (patients <50 kg): 120 mg twice daily continuously until disease progression or unacceptable toxicity

Non-small cell lung cancer (RET-positive), advanced or metastatic

• Dose – Oral (patients ≥50 kg): 160 mg twice daily continuously until disease progression or unacceptable toxicity
• Dose – Oral (patients <50 kg): 120 mg twice daily continuously until disease progression or unacceptable toxicity

Available as 40 mg and 80 mg capsules. Capsules should NOT be opened. Store at room temperature.

Rearranged during Transfection (RET) kinase inhibitor

Take with or without food

If a dose is missed, patients should be instructed to take it as soon as they can if there are > 6 hours until the next dose. If there are < 6 hours until the next dose, patients should skip the missed dose and resume with the next scheduled dose.

Common: Thrombocytopenia, Diarrhea, Edema, AST increase, ALT increase, Headache, Dyspnea, Hypertension, Rash.

Less Common: Hemorrhage, Hypersensitivity reactions, Interstitial lung disease/pneumonitis, Pleural effusion, Respiratory failure, QT prolongation, Tumor lysis syndrome, Impaired wound healing, Increased serum creatinine, Hypothyroidism.

The adverse effects listed above are not exhaustive. Please refer to the relevant product monograph for full details.

Baseline before treatment: CBC & differential, platelets, creatinine, alkaline phosphatase, ALT, LDH, total bilirubin, sodium, potassium, magnesium, calcium, albumin, thyroglobulin (Tg), thyroglobulin antibody (TgAb), CEA, calcitonin, TSH, blood pressure, ECG.

One week after starting treatment: sodium, potassium, magnesium, calcium, blood pressure, ECG.

Every two weeks for first 3 months: ALT and total bilirubin  During treatment: CBC & differential, platelets, creatinine, ALT, total bilirubin, sodium, potassium, magnesium, calcium, albumin, TSH, thyroglobulin (Tg), thyroglobulin antibody (TgAb), calcitonin, CEA, blood pressure, ECG, LDH.

If clinically indicated: random glucose, uric acid, phosphorus, total cholesterol, ECG, chest x-ray, BUN.

• This drug can impact or be impacted by metabolic enzymes for absorption and excretion. Many drugs can also affect or be affected by these enzymes, so please consult with pharmacy to assess for interactions.
• May increase the risk for QT interval prolongation. Avoid concurrent therapy with drugs associated with QTc prolongation and/or Torsades de pointes, if possible. If unavoidable, monitor for QT prolongation or cardiac arrhythmias.
• Avoid grapefruit, grapefruit juice, Seville oranges, or Seville orange juice.
• Current drug interaction databases should be consulted for more information.
• Avoid concurrent therapy with proton pump inhibitors, H2 receptor antagonists, and short acting antacids. If concurrent use cannot be avoided:
  • Selpercatinib should be taken with food when co-administered with a proton pump inhibitor
  • Selpercatinib should be taken 2 hours before or 10 hours after administration of an H2 receptor antagonist
  • Selpercatinib should be taken 2 hours before or 2 hours after administration of a locally acting antacid

• Avoid in pregnancy and lactation.
• Be careful with electrolyte disturbances and medications that can prolong the QT interval as selpercatinib can cause prolongation of the QT interval.
• Hypertension is a common side effect. Hypertension should be well controlled prior to starting selpercatinib.
• Impaired wound healing is associated with selpercatinib, drug may need to be held and restarted if patient requires surgery, discuss with team.

BC Cancer. BC Cancer Drug Manual. Selpercatinib. Vancouver, British Columbia: BC Cancer Agency. Available at: http://www.bccancer.bc.ca/drug-database-site/Drug%20Index/Selpercatinib_monograph.pdf.  Updated September 1, 2023. Accessed January 22, 2024.

Lexicomp. Selpercatinib Monograph. In: Lexi-Drugs. Hudson, Ohio: Lexi-Comp, Inc. Available at:  https://online.lexi.com/lco/action/doc/retrieve/docid/patch_f/6947790?cesid=21lOvbaeJQm&searchUrl=%2Flco%2Faction%2Fsearch%3Fq%3Dselpercatinib%26t%3Dname%26acs%3Dtrue%26acq%3Dseller. Updated January 24, 2024. Accessed January 30, 2024.

Cancer Care Ontario. Selpercatinib Provider Monograph. Drug Formulary. Toronto, Ontario: Cancer Care Ontario. Available at: https://www.cancercareontario.ca/en/drugformulary/regimens/monograph/74526. Updated August 2023. Accessed January 22, 2024.

Eli Lilly Canada Inc. RETEVMO® Product Monograph. Toronto, Ontario. Updated March 2, 2023.