Entrectinib Brand Name– ROZLYTREK
What is Entrectinib
Entrectinib is an oral kinase inhibitor approved for the treatment of adults with ROS1-positive non-small cell lung cancer (NSCLC).
It is also approved for adults and pediatric patients 12 years and older whose solid tumors have a neurotrophic tyrosine receptor kinase (NTRK) gene fusion without a known acquired resistance mutation, are metastatic or where surgical resection is likely to result in severe morbidity, and who have progressed following treatment or have no satisfactory alternative therapy; entrectinib is tissue agnostic for treatment of solid tumors with this genetic mutation.
Entrectinib was associated with a wide range of CNS-related adverse reactions across clinical trials and should be used with caution in patients with baseline cognitive impairment, mood disorders, dizziness, and sleep disturbances.
It has also been associated with QT prolongation and should be avoided with other medications that can cause QT prolongation and used with caution in patients otherwise at increased risk.
Indications
- neurotrophic receptor tyrosine kinase-positive solid tumors
- non-small cell lung cancer (NSCLC)
For the treatment of non-small cell lung cancer (NSCLC)
for the treatment of metastatic ROS1-positive non-small cell lung cancer (NSCLC)
NOTE: The FDA has designated entrectinib as an orphan drug for the treatment of ROS1-positive non-small cell lung cancer (NSCLC)
NOTE: Select patients for treatment based on the presence of ROS1 rearrangement(s) in tumor specimens. An FDA-approved test for detection of ROS1 rearrangement(s) in NSCLC is not available.
Side Effects
- abdominal pain
- agitation
- amnesia
- anemia
- anorexia
- anxiety
- aphasia
- arthralgia
- asthenia
- ataxia
- back pain
- blurred vision
- bone fractures
- cataracts
- confusion
- constipation
- corneal erosion
- cough
- dehydration
- depression
- diarrhea
- diplopia
- dizziness
- drowsiness
- dysesthesia
- dysgeusia
- dysphagia
- dyspnea
- edema
- elevated hepatic enzymes
- emotional lability
- euphoria
- fatigue
- fever
- fluid retention
- GI perforation
- hallucinations
- headache
- heart failure
- hepatotoxicity
- hyperamylasemia
- hyperesthesia
- hyperglycemia
- hyperkalemia
- hypernatremia
- hyperuricemia
- hypoalbuminemia
- hypocalcemia
- hypoesthesia
- hypophosphatemia
- hypotension
- hypoxia
- infection
- insomnia
- irritability
- lymphopenia
- maculopapular rash
- memory impairment
- musculoskeletal pain
- myalgia
- myasthenia
- myocarditis
- nausea
- neuropathic pain
- neutropenia
- orthostatic hypotension
- palmar-plantar erythrodysesthesia (hand and foot syndrome)
- paresthesias
- peripheral edema
- peripheral neuropathy
- photophobia
- photopsia
- pleural effusion
- pruritus
- pulmonary embolism
- QT prolongation
- rash
- renal failure (unspecified)
- retinal hemorrhage
- syncope
- thrombocytopenia
- tumor lysis syndrome (TLS)
- vertigo
- visual impairment
- vomiting
- weight gain
Monitoring Parameters
- echocardiogram
- LFTs
- pregnancy testing
- serum uric acid
Contraindications
- angina
- anxiety
- apheresis
- AV block
- behavioral changes
- bone fractures
- bradycardia
- breast-feeding
- cardiac disease
- cardiomyopathy
- celiac disease
- children
- contraception requirements
- coronary artery bypass graft surgery (CABG)
- depression
- driving or operating machinery
- electrolyte imbalance
- females
- fever
- geriatric
- heart failure
- hepatic disease
- hepatotoxicity
- human immunodeficiency virus (HIV) infection
- hyperparathyroidism
- hyperuricemia
- hypocalcemia
- hypokalemia
- hypomagnesemia
- hypothermia
- hypothyroidism
- infants
- long QT syndrome
- male-mediated teratogenicity
- myocardial infarction
- myocarditis
- pheochromocytoma
- pregnancy
- pregnancy testing
- QT prolongation
- reproductive risk
- rheumatoid arthritis
- sickle cell disease
- sleep deprivation
- stroke
- systemic lupus erythematosus (SLE)
- tumor lysis syndrome (TLS)
- ventricular dysfunction
- visual impairment
Interactions
- Acetaminophen; Butalbital
- Acetaminophen; Butalbital; Caffeine
- Acetaminophen; Butalbital; Caffeine; Codeine
- Aclidinium; Formoterol
- Albuterol
- Albuterol; Ipratropium
- Alfuzosin
- Amiodarone
- Amitriptyline
- Amitriptyline; Chlordiazepoxide
- Amobarbital
- Amoxicillin; Clarithromycin; Lansoprazole
- Amoxicillin; Clarithromycin; Omeprazole
- Anagrelide
- Apalutamide
- Apomorphine
- Aprepitant, Fosaprepitant
- Arformoterol
- Aripiprazole
- Arsenic Trioxide
- Artemether; Lumefantrine
- Asenapine
- Aspirin, ASA; Butalbital; Caffeine
- Aspirin, ASA; Butalbital; Caffeine; Codeine
- Atazanavir
- Atazanavir; Cobicistat
- Atomoxetine
- Atropine; Hyoscyamine; Phenobarbital; Scopolamine
- Azithromycin
- Bedaquiline
- Belladonna Alkaloids; Ergotamine; Phenobarbital
- Bexarotene
- Bismuth Subcitrate Potassium; Metronidazole; Tetracycline
- Bismuth Subsalicylate; Metronidazole; Tetracycline
- Bosentan
- Brigatinib
- Budesonide; Formoterol
- Buprenorphine
- Buprenorphine; Naloxone
- Carbamazepine
- Cenobamate
- Ceritinib
- Chloramphenicol
- Chloroquine
- Chlorpromazine
- Ciprofloxacin
- Cisapride
- Citalopram
- Clarithromycin
- Clofazimine
- Clomipramine
- Clozapine
- Cobicistat
- Codeine; Phenylephrine; Promethazine
- Codeine; Promethazine
- Conivaptan
- Crizotinib
- Cyclosporine
- Dabrafenib
- Danazol
- Darunavir
- Darunavir; Cobicistat
- Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
- Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
- Dasatinib
- Degarelix
- Delavirdine
- Desflurane
- Desipramine
- Deutetrabenazine
- Dexamethasone
- Dextromethorphan; Promethazine
- Dextromethorphan; Quinidine
- Diltiazem
- Disopyramide
- Dofetilide
- Dolasetron
- Dolutegravir; Rilpivirine
- Donepezil
- Donepezil; Memantine
- Doxepin
- Dronedarone
- Droperidol
- Duvelisib
- Efavirenz
- Efavirenz; Emtricitabine; Tenofovir
- Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
- Elagolix
- Elagolix; Estradiol; Norethindrone acetate
- Eliglustat
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
- Emtricitabine; Rilpivirine; Tenofovir alafenamide
- Emtricitabine; Rilpivirine; Tenofovir disoproxil fumarate
- Encorafenib
- Enflurane
- Enzalutamide
- Eribulin
- Erythromycin
- Erythromycin; Sulfisoxazole
- Escitalopram
- Eslicarbazepine
- Etravirine
- Ezogabine
- Fedratinib
- Fingolimod
- Flecainide
- Fluconazole
- Fluoxetine
- Fluoxetine; Olanzapine
- Fluphenazine
- Fluticasone; Salmeterol
- Fluticasone; Umeclidinium; Vilanterol
- Fluticasone; Vilanterol
- Fluvoxamine
- Formoterol
- Formoterol; Mometasone
- Fosamprenavir
- Foscarnet
- Fosphenytoin
- Gemifloxacin
- Gemtuzumab Ozogamicin
- Gilteritinib
- Glasdegib
- Glycopyrrolate; Formoterol
- Goserelin
- Granisetron
- grapefruit juice
- Halogenated Anesthetics
- Haloperidol
- Halothane
- Histrelin
- Hydroxychloroquine
- Hydroxyzine
- Ibutilide
- Idelalisib
- Iloperidone
- Imatinib
- Imipramine
- Indacaterol
- Indacaterol; Glycopyrrolate
- Indinavir
- Inotuzumab Ozogamicin
- Isavuconazonium
- Isoflurane
- Isoniazid, INH; Pyrazinamide, PZA; Rifampin
- Isoniazid, INH; Rifampin
- Itraconazole
- Ivosidenib
- Ketoconazole
- Lapatinib
- Lefamulin
- Lenvatinib
- Letermovir
- Leuprolide
- Leuprolide; Norethindrone
- Levalbuterol
- Levofloxacin
- Lithium
- Lofexidine
- Long-acting beta-agonists
- Loperamide
- Loperamide; Simethicone
- Lopinavir; Ritonavir
- Lorlatinib
- Lumacaftor; Ivacaftor
- Lumacaftor; Ivacaftor
- Macimorelin
- Maprotiline
- Mefloquine
- Meperidine; Promethazine
- Metaproterenol
- Methadone
- Methohexital
- Metronidazole
- Midostaurin
- Mifepristone
- Mirtazapine
- Mitotane
- Modafinil
- Moxifloxacin
- Nafcillin
- Nefazodone
- Nelfinavir
- Netupitant, Fosnetupitant; Palonosetron
- Nevirapine
- Nilotinib
- Nortriptyline
- Octreotide
- Ofloxacin
- Olanzapine
- Olodaterol
- Ombitasvir; Paritaprevir; Ritonavir
- Omeprazole; Amoxicillin; Rifabutin
- Ondansetron
- Osilodrostat
- Osimertinib
- Oxaliplatin
- Ozanimod
- Paliperidone
- Panobinostat
- Pasireotide
- Pazopanib
- Pentamidine
- Perphenazine
- Perphenazine; Amitriptyline
- Pexidartinib
- Phenobarbital
- Phenylephrine; Promethazine
- Phenytoin
- Pimavanserin
- Pimozide
- Pirbuterol
- Pitolisant
- Posaconazole
- Primaquine
- Primidone
- Procainamide
- Prochlorperazine
- Promethazine
- Propafenone
- Protriptyline
- Quetiapine
- Quinidine
- Quinine
- Ranolazine
- Ribociclib
- Ribociclib; Letrozole
- Rifabutin
- Rifampin
- Rifapentine
- Rifaximin
- Rilpivirine
- Risperidone
- Ritonavir
- Romidepsin
- Salmeterol
- Saquinavir
- Secobarbital
- Selpercatinib
- Sertraline
- Sevoflurane
- Short-acting beta-agonists
- Siponimod
- Solifenacin
- Sorafenib
- Sotalol
- St. John’s Wort, Hypericum perforatum
- Sunitinib
- Tacrolimus
- Tamoxifen
- Telavancin
- Telithromycin
- Terbutaline
- Tetrabenazine
- Thioridazine
- Tiotropium; Olodaterol
- Tipranavir
- Tolterodine
- Toremifene
- Trandolapril; Verapamil
- Trazodone
- Triclabendazole
- Tricyclic antidepressants
- Trifluoperazine
- Trimipramine
- Triptorelin
- Tucatinib
- Umeclidinium; Vilanterol
- Vandetanib
- Vardenafil
- Vemurafenib
- Venlafaxine
- Verapamil
- Voriconazole
- Vorinostat
- Ziprasidone
