ROZLYTREK (Entrectinib)

ROZLYTREK (Entrectinib)

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What is this medication?

Entrectinib, Rozlytrek
Antineoplastic Agent, Tropomyosin Receptor Kinase (TRK) Inhibitor, Tyrosine Kinase Inhibitor

Entrectinib, Rozlytrek is indicated for treatment of non-small cell lung cancer, solid tumors. 

How does this medication work?

Entrectinib, Rozlytrek inhibits tropomyosin receptor tyrosine kinases (TRK) TRKA, TRKB, and TRKC. TRKA, TRKB, and TRKC are encoded by neurotrophic receptor tyrosine kinase (NTRK) genes NTRK1, NTRK2, and NTRK3, respectively. Entrectinib, Rozlytrek also inhibits proto-oncogenic tyrosine-protein kinase ROS1 and anaplastic lymphoma kinase (ALK). M5 (the major active entrectinib metabolite) demonstrated similar activity (in vitro) against TRK, ROS1, and ALK. Fusion proteins that include TRK, ROS1, or ALK kinase domains act as oncogenic drivers to promote hyperactivation of downstream signaling pathways, resulting in unchecked cell proliferation.

How should I take this medication?

Oral: 600mg once daily.

Take with or without food.  Swallow the capsule whole; do not open, crush, chew or dissolve the contents of the capsule.

What should I watch for while using this medication?

Before starting Entrectinib, Rozlytrek make sure your physician is aware of any allergies or medications you currently take.  Entrectinib, Rozlytrek has been shown to cause heart failure and as a result monitoring for clinical signs/symptoms of heart failure, including shortness of breath and edema along with measuring ejection fraction is important prior and during the course of therapy.  Entrectinib, Rozlytrek can cause central nervous system effects, increase risk of bone fracture, hepatotoxicity and ocular toxicity.

What if I miss a dose?

If you miss a dose of medication, try to take it as soon as possible.  However, if it is almost time for your next dose, take only that scheduled dose.  Do not take double or extra doses.

How should I store this medication?

Keep out of the reach of children at all times.  Store at room temperature, 59 to 86° F (15 to 30° C).  Protect from light.  Keep the container tightly closed.  Properly dispose of any unused medication after the expiration date.

What are the possible side effects of using this medication?

Edema, hypotension, fatigue, dizziness, dyesthesia, cognitive dysfunction, headache, peripheral sensory neuropathy, sleep disorder, myasthenia, skin rash, electrolyte disturbances (i.e. hyperuricemia, hypernatremia, hypocalcemia, hypophosphatemia, hyperkalemia), constipation, diarrhea, nausea, abdominal pain, dysgeusia, urinary tract infection, hematologic disturbances (i.e. anemia, lymphocytopenia, neutropenia), elevated liver enzymes, myalgia, bone fracture, joint pain, back pain, limb pain, visual disturbance, dyspepsia, cough and fever.

Note this is not a complete list of side effects, only common ones.