Select a medication above to begin.
Augtyro
repotrectinib
Adult Dosing .
Dosage forms: CAP: 40 mg, 160 mg
Special Note
- [uses, dosing may vary]
- Info: refer to institution protocols and pkg insert prior to prescribing for uses and dosing incl. toxicity-related dose adjustments
ROS1-positive non-small cell lung CA, locally advanced or metastatic
- [160 mg PO bid]
- Start: 160 mg PO qd x14 days; Info: do not open/crush/chew/dissolve cap
NTRK fusion-positive solid tumors, locally advanced or metastatic
- [160 mg PO bid]
- Start: 160 mg PO qd x14 days; Info: for pts w/ progressive dz; do not open/crush/chew/dissolve cap
renal dosing
- [see below]
- eGFR >30: no adjustment; eGFR <30: not defined
- HD/PD: not defined
hepatic dosing
- [see below]
- bilirubin 1.1-1.5x ULN or AST >ULN: no adjustment; bilirubin >1.5x ULN: not defined
Peds Dosing .
- Dosage forms: CAP: 40 mg, 160 mg
Special Note
- [uses, dosing may vary]
- Info: refer to institution protocols and pkg insert prior to prescribing for uses and dosing incl. toxicity-related dose adjustments
NTRK fusion-positive solid tumors, locally advanced or metastatic
- [12 yo and older]
- Dose: 160 mg PO bid; Start: 160 mg PO qd x14 days; Info: for pts w/ progressive dz; do not open/crush/chew/dissolve cap
renal dosing
- [see below]
- eGFR >30: no adjustment; eGFR <30: not defined
- HD/PD: not defined
hepatic dosing
- [see below]
- bilirubin 1.1-1.5x ULN or AST >ULN: no adjustment; bilirubin >1.5x ULN: not defined
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- avoid: breastfeeding during tx and x10 days after D/C
- caution: pts of childbearing potential
- caution: male pts of reproductive potential
Drug Interactions .
Overview
repotrectinib
kinase inhibitor
- CYP3A4 substrate
- P-gp substrate
- CYP3A4 inducer, moderate
- CNS depression
- hyperuricemic effects
Contraindicated
- lonafarnib
- mavacamten
- ranolazine
Avoid/Use Alternative
- abemaciclib
- abrocitinib
- adagrasib
- alfentanil
- alpelisib
- amiodarone
- apalutamide
- aprepitant
- artemether/lumefantrine
- asciminib
- atazanavir
- atogepant
- atrasentan
- avacopan
- avapritinib
- axitinib
- azithromycin
- bedaquiline
- belumosudil
- berotralstat
- bictegravir
- bisoprolol
- bosentan
- bosutinib
- brigatinib
- buprenorphine
- buspirone
- butalbital
- cabozantinib
- canagliflozin
- cannabidiol
- capivasertib
- capmatinib
- captopril
- carbamazepine
- cariprazine
- carvedilol
- cenobamate
- ceritinib
- chloramphenicol
- cimetidine
- ciprofloxacin
- clarithromycin
- clofazimine
- clonidine
- cobicistat
- cobimetinib
- codeine
- conivaptan
- crizotinib
- cyclosporine
- dabrafenib
- danazol
- danicopan
- daridorexant
- darolutamide
- darunavir
- defactinib
- deflazacort
- desogestrel (contraceptive)
- diazoxide
- dienogest (contraceptive)
- dihydrocodeine
- diltiazem
- diosmin
- dolutegravir
- doravirine
- doxorubicin
- doxylamine
- dronedarone
- drospirenone (contraceptive)
- duvelisib
- efavirenz
- elacestrant
- elagolix
- elbasvir
- elexacaftor/tezacaftor/ivacaftor
- eliglustat
- elvitegravir
- enasidenib
- encorafenib
- ensartinib
- entrectinib
- enzalutamide
- erdafitinib
- erlotinib
- erythromycin
- estradiol (contraceptive)
- ethanol
- ethinyl estradiol (contraceptive)
- ethynodiol (contraceptive)
- etonogestrel (contraceptive)
- etravirine
- everolimus
- fedratinib
- felodipine
- fentanyl
- fexinidazole
- finerenone
- flibanserin
- fluconazole
- fluvoxamine
- fosamprenavir
- fosaprepitant
- fosphenytoin
- fostamatinib
- fruquintinib
- futibatinib
- ganaxolone
- gilteritinib
- ginkgo
- glasdegib
- glecaprevir
- grapefruit
- grazoprevir
- hydrocodone
- ibrexafungerp
- ibrutinib
- idelalisib
- imatinib
- indomethacin
- irinotecan
- isavuconazonium
- isocarboxazid
- isradipine
- istradefylline
- itraconazole
- ivacaftor
- ivosidenib
- kava
- ketoconazole
- kratom
- lapatinib
- larotrectinib
- lasmiditan
- lazertinib
- ledipasvir
- lefamulin
- lemborexant
- lenacapavir
- leniolisib
- letermovir
- levacetylleucine
- levoketoconazole
- levonorgestrel (contraceptive)
- levonorgestrel (post-coital contraceptive)
- lomitapide
- lopinavir/ritonavir
- lorlatinib
- lumacaftor/ivacaftor
- lumateperone
- macitentan
- maraviroc
- maribavir
- mavorixafor
- medroxyprogesterone (contraceptive)
- meperidine
- metaxalone
- methadone
- metoclopramide
- midazolam
- midostaurin
- mifepristone
- milk thistle
- mirabegron
- mitapivat
- mitotane
- mobocertinib
- modafinil
- nafcillin
- naldemedine
- naloxegol
- naproxen
- nefazodone
- nelfinavir
- neratinib
- netupitant
- nevirapine
- nicardipine
- nifedipine
- nilotinib
- nirmatrelvir
- nirogacestat
- nisoldipine
- norelgestromin (contraceptive)
- norethindrone (contraceptive)
- norgestimate (contraceptive)
- norgestrel (contraceptive)
- olaparib
- oliceridine
- olutasidenib
- omaveloxolone
- osimertinib
- oxybate
- oxycodone
- pacritinib
- palbociclib
- palovarotene
- paroxetine
- pemigatinib
- pentobarbital
- pexidartinib
- phenelzine
- phenobarbital
- phenytoin
- pibrentasvir
- pimavanserin
- pirtobrutinib
- ponatinib
- posaconazole
- pralsetinib
- praziquantel
- pretomanid
- primidone
- promethazine
- propafenone
- quercetin
- quinidine (antiarrhythmic)
- quinidine (CYP2D6 inhibitor)
- quinine
- quizartinib
- revumenib
- ribociclib
- rifabutin
- rifampin
- rifapentine
- rilpivirine
- rimegepant
- ripretinib
- ritonavir
- rivaroxaban
- roflumilast
- rolapitant
- ropeginterferon alfa-2b
- rucaparib
- samidorphan
- sarecycline
- sebetralstat
- segesterone (contraceptive)
- selpercatinib
- selumetinib
- simvastatin
- siponimod
- sonidegib
- sorafenib
- sotagliflozin
- sotorasib
- sparsentan
- St. John's wort
- stiripentol
- sufentanil
- sunvozertinib
- suvorexant
- suzetrigine
- tacrolimus
- tadalafil
- tamoxifen
- tasimelteon
- tazemetostat
- telmisartan
- temsirolimus
- tepotinib
- tezacaftor/ivacaftor
- thalidomide
- thiotepa
- ticagrelor
- tipranavir
- tofacitinib
- tolvaptan
- toremifene
- tramadol
- tranylcypromine
- trazodone
- trimethobenzamide
- trimethoprim
- tucatinib
- turmeric
- ulipristal (post-coital contraceptive)
- uridine triacetate
- valbenazine
- vandetanib
- vanzacaftor/tezacaftor/deutivacaftor
- velpatasvir
- vemurafenib
- venetoclax
- verapamil
- vilazodone
- vimseltinib
- voclosporin
- vonoprazan
- voriconazole
- voxelotor
- voxilaprevir
- xanomeline
- zanubrutinib
- zonisamide
- zuranolone
Monitor/Modify Tx
- abiraterone acetate
- acalabrutinib
- aldesleukin
- allopurinol
- alprazolam
- aminophylline
- amlodipine
- avatrombopag
- baclofen intrathecal
- betamethasone
- brexpiprazole
- butorphanol
- calcitriol
- chlordiazepoxide
- chlorpromazine
- cholecalciferol (vitamin D3)
- clobazam
- clonazepam
- clorazepate
- clozapine
- crinecerfont
- cyclophosphamide
- desflurane
- dexmedetomidine
- dexmedetomidine injection
- diazepam
- disopyramide
- doxercalciferol
- droperidol
- esketamine
- estazolam
- eszopiclone
- ethanol (in some formulations)
- ethosuximide
- etomidate
- febuxostat
- fludrocortisone
- fluphenazine
- flurazepam
- gabapentin
- gabapentin enacarbil
- guanfacine
- haloperidol
- hydrocortisone
- hydromorphone
- hydroxyzine
- ifosfamide
- imipramine
- isoflurane
- ketamine
- levorphanol
- lorazepam
- lurasidone
- macimorelin
- methohexital
- mirtazapine
- morphine
- nalbuphine
- nelarabine
- nimodipine
- nortriptyline
- olanzapine
- opicapone
- opium
- oxazepam
- oxybutynin
- oxymorphone
- pegloticase
- pentazocine
- perampanel
- perphenazine
- pregabalin
- probenecid
- propofol
- quazepam
- quetiapine
- rasburicase
- remifentanil
- remimazolam
- repaglinide
- sevoflurane
- sildenafil
- sirolimus
- tapentadol
- temazepam
- theophylline
- thioridazine
- thiothixene
- tiagabine
- triazolam
- ubrogepant
- vortioxetine
- warfarin
- zaleplon
- ziconotide
- zolpidem
Caution Advised
- 5-HTP
- albendazole
- aliskiren
- almotriptan
- amantadine
- amitriptyline
- amoxapine
- apixaban
- apomorphine
- apraclonidine ophthalmic
- apremilast
- aripiprazole bimonthly injection
- aripiprazole lauroxil
- aripiprazole monthly injection
- aripiprazole oral
- armodafinil
- asenapine
- atorvastatin
- avanafil
- baclofen
- belzutifan
- berberine
- bexarotene
- bicalutamide
- bortezomib
- brimonidine ophthalmic
- brimonidine topical
- brivaracetam
- bromocriptine
- brompheniramine
- budesonide
- cannabis
- carbinoxamine
- carisoprodol
- cetirizine
- chamomile, German
- chlophedianol
- chlorpheniramine
- chlorzoxazone
- cilostazol
- citalopram
- clemastine
- clindamycin
- clomipramine
- clotrimazole oropharyngeal
- colchicine
- copanlisib
- cortisone
- cranberry
- cyclobenzaprine
- cyproheptadine
- danshen
- dantrolene
- dapsone
- darifenacin
- dasatinib
- desipramine
- desvenlafaxine
- deutetrabenazine
- dexamethasone
- dexbrompheniramine
- dexchlorpheniramine
- dichlorphenamide
- dicloxacillin
- difelikefalin
- difenoxin
- dimenhydrinate
- diphenhydramine
- diphenoxylate
- domperidone
- doxepin
- doxepin topical
- dronabinol
- drospirenone (hormone replacement)
- duloxetine
- echinacea
- elafibranor
- eletriptan
- enfortumab vedotin
- entacapone
- escitalopram
- eslicarbazepine acetate
- esomeprazole
- ethinyl estradiol (hormone replacement)
- etoposide
- etrasimod
- exemestane
- felbamate
- fenfluramine
- fesoterodine
- finasteride
- fluoxetine
- foslevodopa
- fostemsavir
- frovatriptan
- garlic
- gefitinib
- gepirone
- gepotidacin
- ginseng, Asian
- givinostat
- givosiran
- glofitamab
- glyburide
- glycerol phenylbutyrate
- glycopyrrolate
- goldenseal
- griseofulvin
- hyoscyamine
- iloperidone
- isoniazid
- isotretinoin
- ivabradine
- ixabepilone
- ixazomib
- lacosamide
- lamotrigine
- levetiracetam
- levocetirizine
- levodopa
- levomilnacipran
- levonorgestrel (hormone replacement)
- levonorgestrel intrauterine device (contraceptive)
- linvoseltamab
- lofexidine
- lovastatin
- loxapine
- meclizine
- mefloquine
- melatonin
- meprobamate
- meropenem
- methocarbamol
- methsuximide
- methyldopa
- methylprednisolone
- metyrapone
- metyrosine
- milnacipran
- molindone
- mosunetuzumab
- mycophenolate mofetil
- naltrexone
- naratriptan
- nintedanib
- norethindrone (hormone replacement)
- odevixibat
- omeprazole
- ondansetron
- orphenadrine
- osilodrostat
- oxcarbazepine
- paclitaxel
- paliperidone
- panobinostat
- passion flower
- pazopanib
- peppermint
- pheniramine
- pimozide
- pioglitazone
- pitolisant
- polatuzumab vedotin
- pramipexole
- prednisolone
- prednisone
- procarbazine
- prochlorperazine
- progesterone (hormone replacement)
- progesterone vaginal (hormone replacement)
- protriptyline
- pyrilamine
- ramelteon
- rasagiline
- regorafenib
- relugolix
- remdesivir
- resveratrol
- risperidone
- ritlecitinib
- rizatriptan
- ropinirole
- rotigotine transdermal
- rufinamide
- ruxolitinib
- safinamide
- sarilumab
- scopolamine
- selegiline
- selegiline transdermal
- selinexor
- sertraline
- sirolimus albumin-bound
- solifenacin
- spironolactone
- sumatriptan
- sunitinib
- tecovirimat
- telotristat ethyl
- terbinafine
- tetrabenazine
- tivozanib
- tizanidine
- tocilizumab
- tolcapone
- tolterodine
- topiramate
- tovorafenib
- trabectedin
- treosulfan
- tretinoin
- triamcinolone
- trifluoperazine
- trihexyphenidyl
- trimipramine
- triprolidine
- trofinetide
- trospium
- upadacitinib
- vaborbactam
- valerian
- valproic acid
- vamorolone
- venlafaxine
- vigabatrin
- viloxazine
- vinblastine
- vincristine
- vinorelbine
- vorapaxar
- vorasidenib
- zileuton
- ziprasidone
- zolmitriptan
Adverse Reactions .
Serious Reactions
- CNS toxicity
- ataxia
- cognitive disorder
- depression
- mania
- somnolence
- interstitial lung dz
- pneumonitis
- hepatotoxicity
- myalgia
- hyperuricemia
- fractures
- pneumonia
- dyspnea
- pleural effusion
- hypoxia
- respiratory failure
- cardiac failure
- cardiac arrest
- DIC
Common Reactions
- dizziness
- dysgeusia
- peripheral neuropathy
- constipation
- hepatotoxicity
- dyspnea
- ataxia
- fatigue
- cognitive dysfxn
- muscular weakness
- headache
- nausea
- sleep disorders
- cough
- weight incr.
- diarrhea
- myalgia
- edema
- vision disorders
- vomiting
- fever
- mood disorders
- hyperuricemia
- pneumonitis
- fractures
- GGT incr.
- lymphocytes decr.
- neutrophils decr.
- CPK incr.
- Hgb decr.
- leukocytes decr.
- ALT or AST incr.
- alk phos incr.
- blood glucose changes
- sodium incr.
- aPTT incr.
- INR incr.
Safety/Monitoring .
Monitoring Parameters
pregnancy test at baseline; uric acid at baseline, then periodically; LFTs at baseline, then q2wk x1mo, then qmo and as clinically indicated; CK q2wk x1mo, then as clinically indicated
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy; no human data available, though possible risk of developmental delays, cognitive impairment based on limited human data w/ congenital TRK mutation; risk of teratogenicity based on animal data at 0.3x or greater recommended human dose
Individuals of Reproductive Potential
obtain pregnancy test before tx start; avoid pregnancy by using effective non-hormonal contraception during tx and x2mo after D/C in pts of childbearing potential and during tx and x4mo in male pts
Lactation
Clinical Summary
avoid breastfeeding during tx and x10 days after D/C; no human data available to assess risk of infant harm or effects on milk production
Pharmacology .
Metabolism: liver primarily, glucuronidation; CYP450: 3A4 substrate
Excretion: feces 88.8% (50.6% unchanged), urine 4.8% (0.6% unchanged); Half-life: 50.6h
Subclass: Kinase Inhibitors, ROS1 Inhibitors ; Kinase Inhibitors, TRK Inhibitors
Mechanism of Action
inhibits proto-oncogene ROS1, tropomyosin receptor kinases (TRK), leading to inhibition of tumor cell proliferation and survival
Formulary .
No Formulary Selected
Join Now to View Patient Handouts!
Create a FREE epocrates Online account to access patient medication instructions. Your patients and caregivers will appreciate you printing these friendly handouts, available in English and Spanish. Each handout addresses common concerns such as how to take the medication, and possible side effects.
Current Members: Sign In.
Pill Pictures
Join Now to View Pill Pictures!
Create a FREE epocrates Online account to access full-color images of medications within the drug monograph.
Current Members: Sign In.