Entrectinib (ROZYLTREK)

Solid tumors with NTRK fusion-positive status, advanced or metastatic

Non-small cell lung cancer (ROS1-positive), advanced or metastatic

Solid tumors with NTRK fusion-positive status, advanced or metastatic

• Dose – Oral: 600 mg once daily continuously until disease progression or unacceptable toxicity

Non-small cell lung cancer (ROS1-positive), advanced or metastatic

• Dose – Oral: 600 mg once daily continuously until disease progression or unacceptable toxicity

Available as 100 mg and 200 mg hard-shell capsules. Capsules contain lactose. Capsules should NOT be opened. Store at room temperature.

Multi-targeted TKI (tyrosine kinase inhibitor) which includes action as a Tropomyosin Receptor Kinase (TRK) inhibitor and a ROS1 inhibitor

Take with or without food

If a dose is missed, patients should be instructed to take it as soon as they can if it is within 12 hours of the missed dose. If it is over 12 hours since the missed dose, patients should skip the missed dose and resume with the next scheduled dose.

Common: Anemia, Neutropenia, Visual disorders, Diarrhea, Edema, Fatigue, ALT increase, AST increase, Hyperuricemia, Myalgia, Cognitive disorders, Dizziness, Dysesthesia/paresthesia, Dyspnea.

Less Common: Congestive heart failure, Large intestine perforation, Pneumonia, Sepsis, Bone fractures, QT interval prolongation, Tumor lysis syndrome, Respiratory failure, Pulmonary embolism, Fracture risk.

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, total bilirubin, ALT, alkaline phosphatase, LDH, calcium, albumin, sodium, potassium, phosphorus, magnesium, uric acid, ECG, MUGA scan or echocardiogram to assess LVEF.

During treatment: CBC & differential, platelets, alkaline phosphatase, ALT, total bilirubin and LDH should be checked two weeks after starting entrectinib and at each subsequent visit thereafter.

If clinically indicated: calcium, albumin, sodium, potassium, phosphorus, magnesium, ECG, MUGA scan or echocardiogram to assess LVEF, uric acid, creatinine, GGT, C-reactive protein, alkaline phosphatase, chest X-ray.

• 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 in pregnancy and lactation.
• CNS effects, such as cognitive impairment, mood disorders, dizziness, and sleep disturbances have been reported with entrectinib.

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

Lexicomp. Entrectinib Monograph. In: Lexi-Drugs. Hudson, Ohio: Lexi-Comp, Inc. Available at:  https://online.lexi.com/lco/action/doc/retrieve/docid/patch_f/6852673?cesid=075lfoO38hj&searchUrl=%2Flco%2Faction%2Fsearch%3Fq%3Dentrectinib%26t%3Dname%26acs%3Dtrue%26acq%3Dentrectinib. Updated January 26, 2024. Accessed January 30, 2024.

Cancer Care Ontario. Entrectinib Monograph. Drug Formulary. Toronto, Ontario: Cancer Care Ontario. Available at: https://www.cancercareontario.ca/en/drugformulary/drugs/monograph/71886. Updated June 2023. Accessed January 22, 2024.

Hoffman La-Roche Limited. ROZLYTREK® Product Monograph. Mississauga, Ontario. Updated November 9, 2023.