Antineoplastic Agent, Tropomyosin Receptor Kinase (TRK) Inhibitor, Tyrosine Kinase Inhibitor
CSA NA – FDA Approved – REMS (N) – Can Ship
How Does It 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.
Indications For Use
Non-Small Cell Lung Cancer, Solid Tumors
Precautions
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.
Usual Dosing
Oral: 600mg once daily.
Pharmacist Tips On Using
Oral: Take with or without food. Swallow the capsule whole; do not open, crush, chew or dissolve the contents of the capsule.
Side Effects
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 for Entrectinib, Rozlytrek only common ones.
Frequently Asked Questions
Why would my physician prescribe a medication with such serious side effects?
Your physician takes the most recent clinical guidelines to make evidence-based decisions on what medication is appropriate in which situations. Your current medications, your allergies, age, cost of medication, comorbid conditions and many other factors will further complicate or limit which medications are appropriate. This medication is used for certain forms of cancer and your physician has determined the benefits outweigh the risks. Furthermore, they will be monitoring your bloodwork and symptoms closely to avoid many of the serious side effects and will keep you on the lowest effective dosage for the shortest amount of time possible.