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Krazati
adagrasib
Adult Dosing .
Dosage forms: TAB: 200 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
KRAS G12C-mutated non-small cell lung CA, locally advanced or metastatic
- [600 mg PO bid]
- Info: for pts who have received at least 1 prior tx; do not cut/crush/chew tab
KRAS G12C-mutated colorectal CA, locally advanced or metastatic
- [600 mg PO bid]
- Info: for pts who have received prior fluoropyrimidine-, oxaliplatin-, and irinotecan-based tx; use w/ cetuximab; may cont. as monotherapy if cetuximab permanently D/C'd; do not cut/crush/chew tab
renal dosing
- [see below]
- CrCl >15: no adjustment; CrCl <15: not defined
- HD/PD: not defined
hepatic dosing
- [no adjustment]
Peds Dosing .
Peds dosing is currently unavailable or not applicable for this drug.
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- long QT syndrome, congenital
- QT prolongation
- avoid: breastfeeding during tx and x1wk after D/C
- caution: electrolyte abnormalities
- caution: QT prolongation family hx
- caution: torsades de pointes hx
- caution: ventricular arrhythmia
- caution: bradycardia
- caution: recent MI
- caution: CHF
Drug Interactions .
Overview
adagrasib
KRAS inhibitor
- CYP3A4 substrate
- CYP2C9 inhibitor, moderate
- CYP2D6 inhibitor, moderate
- CYP3A4 inhibitor, strong
- P-gp inhibitor, moderate
- prolongs QT interval (known)
Contraindicated
- alfuzosin
- alprazolam
- cisapride
- colchicine
- conivaptan
- deuruxolitinib
- dihydroergotamine
- domperidone
- dronedarone
- eliglustat
- eplerenone
- ergotamine
- finerenone
- flibanserin
- gepirone
- isavuconazonium
- ivabradine
- levoketoconazole
- lomitapide
- lonafarnib
- lovastatin
- lurasidone
- naloxegol
- pacritinib
- pimozide
- posaconazole
- ranolazine
- silodosin
- simvastatin
- suzetrigine
- thioridazine
- tolvaptan
- triazolam
- ubrogepant
- venetoclax
- voclosporin
Avoid/Use Alternative
- abrocitinib
- acalabrutinib
- ado-trastuzumab emtansine
- alfentanil
- almotriptan
- amiodarone
- anagrelide
- apalutamide
- apixaban
- apomorphine
- aprepitant
- aripiprazole bimonthly injection
- aripiprazole lauroxil
- aripiprazole monthly injection
- arsenic trioxide
- artemether/lumefantrine
- asenapine
- atazanavir
- atogepant
- avanafil
- avapritinib
- axitinib
- azithromycin
- bedaquiline
- bosentan
- bosutinib
- brigatinib
- bromocriptine
- budesonide
- budesonide rectal
- buprenorphine
- buspirone
- butalbital
- cabazitaxel
- cabozantinib
- capivasertib
- carbamazepine
- ceritinib
- chloramphenicol
- chloroquine
- citalopram
- clarithromycin
- clofazimine
- cobicistat
- cobimetinib
- codeine
- copanlisib
- crizotinib
- dabigatran
- dabrafenib
- daridorexant
- dasatinib
- defactinib
- degarelix
- desflurane
- desipramine
- dexamethasone
- dexmedetomidine
- dexmedetomidine injection
- dihydrocodeine
- disopyramide
- docetaxel
- dofetilide
- donepezil
- doxorubicin
- droperidol
- duvelisib
- efavirenz
- elacestrant
- elagolix
- elbasvir
- eletriptan
- encorafenib
- ensartinib
- entrectinib
- enzalutamide
- ephedra
- epirubicin
- erdafitinib
- eribulin
- erlotinib
- erythromycin
- estazolam
- etrasimod
- everolimus
- fedratinib
- fentanyl
- fesoterodine
- fexinidazole
- flecainide
- fluconazole
- fluorouracil
- fluoxetine
- fluticasone propionate
- fosaprepitant
- foscarnet
- fosphenytoin
- futibatinib
- gepotidacin
- gilteritinib
- givinostat
- glasdegib
- goserelin
- grapefruit
- grazoprevir
- haloperidol
- histrelin
- hydrocodone
- hydroxychloroquine
- hydroxyzine
- ibrutinib
- ibutilide
- idelalisib
- iloperidone
- inotuzumab ozogamicin
- irinotecan
- isoflurane
- itraconazole
- ivacaftor
- ivosidenib
- ixabepilone
- ketoconazole
- lapatinib
- larotrectinib
- lefamulin
- lemborexant
- lenacapavir
- leniolisib
- leuprolide
- levofloxacin
- lisdexamfetamine
- lofexidine
- loperamide
- lopinavir/ritonavir
- lorlatinib
- lumacaftor/ivacaftor
- lurbinectedin
- macimorelin
- macitentan
- mefloquine
- meloxicam
- meperidine
- methadone
- methylergonovine
- midazolam
- midostaurin
- mifepristone
- mitapivat
- mitotane
- mobocertinib
- moxifloxacin
- nefazodone
- nelfinavir
- neratinib
- nilotinib
- nimodipine
- nirogacestat
- nisoldipine
- olaparib
- oliceridine
- omaveloxolone
- ondansetron
- osimertinib
- ospemifene
- oxaliplatin
- oxycodone
- ozanimod
- palbociclib
- paliperidone
- palonosetron
- palovarotene
- panobinostat
- pasireotide
- pazopanib
- pemigatinib
- pentamidine
- pentobarbital
- pexidartinib
- phenobarbital
- phenytoin
- pimavanserin
- pirfenidone
- pirtobrutinib
- pitolisant
- ponatinib
- ponesimod
- pralsetinib
- primidone
- procainamide
- propafenone
- quetiapine
- quinidine (antiarrhythmic)
- quinidine (CYP2D6 inhibitor)
- quinine
- quizartinib
- red yeast rice
- regorafenib
- relugolix
- repotrectinib
- retapamulin topical
- revumenib
- ribociclib
- rifabutin
- rifampin
- rilpivirine
- rimegepant
- ritonavir
- rivaroxaban
- romidepsin
- rucaparib
- ruxolitinib
- ruxolitinib topical
- salmeterol inhaled
- selpercatinib
- selumetinib
- sertraline
- sevoflurane
- sildenafil
- siponimod
- sirolimus
- sirolimus albumin-bound
- solifenacin
- sonidegib
- sorafenib
- sotalol
- sparsentan
- St. John's wort
- sufentanil
- sunitinib
- suvorexant
- tadalafil
- tamsulosin
- tazemetostat
- telavancin
- temsirolimus
- tetrabenazine
- thiotepa
- ticagrelor
- tipranavir
- topotecan
- toremifene
- trabectedin
- tramadol
- trazodone
- tretinoin
- triclabendazole
- trifluridine
- triptorelin
- tucatinib
- vandetanib
- vardenafil
- vemurafenib
- vinblastine
- vincristine
- vinorelbine
- vorapaxar
- voriconazole
- ziprasidone
Monitor/Modify Tx
- abemaciclib
- afatinib
- albuterol
- albuterol inhaled
- aminophylline
- amisulpride
- amitriptyline
- amlodipine
- arformoterol inhaled
- aripiprazole oral
- asciminib
- atorvastatin
- avacopan
- avatrombopag
- berotralstat
- bortezomib
- brentuximab vedotin
- brexpiprazole
- butorphanol
- cariprazine
- carvedilol
- celecoxib
- chlordiazepoxide
- chlorpromazine
- cilostazol
- cinacalcet
- ciprofloxacin
- clomipramine
- clonazepam
- clozapine
- cyclosporine
- danazol
- darifenacin
- darunavir
- deflazacort
- deutetrabenazine
- dextroamphetamine
- diazepam
- diazoxide
- diclofenac
- digoxin
- diltiazem
- doxercalciferol
- drospirenone (contraceptive)
- drospirenone (hormone replacement)
- edoxaban
- elexacaftor/tezacaftor/ivacaftor
- enfortumab vedotin
- escitalopram
- esomeprazole
- estradiol (contraceptive)
- eszopiclone
- ethinyl estradiol (contraceptive)
- felodipine
- fingolimod
- fluvastatin
- formoterol inhaled
- fosamprenavir
- fostamatinib
- fostemsavir
- gemtuzumab ozogamicin
- glimepiride
- glipizide
- glyburide
- granisetron
- guanfacine
- hydrocortisone
- ibrexafungerp
- imatinib
- imipramine
- isradipine
- istradefylline
- lacosamide
- lenvatinib
- letermovir
- levalbuterol inhaled
- levomilnacipran
- lidocaine
- lumateperone
- maraviroc
- mavacamten
- mavorixafor
- methylprednisolone
- metoprolol
- metronidazole
- mirtazapine
- morphine
- nateglinide
- nebivolol
- netupitant
- nicardipine
- nifedipine
- nintedanib
- nortriptyline
- ofloxacin
- olodaterol inhaled
- omeprazole
- osilodrostat
- paclitaxel
- paricalcitol
- perphenazine
- pitavastatin
- polatuzumab vedotin
- primaquine
- promethazine
- propranolol
- repaglinide
- riociguat
- sacituzumab govitecan
- saxagliptin
- tacrolimus
- talazoparib
- tenofovir alafenamide
- tenofovir disoproxil
- terbutaline
- tezacaftor/ivacaftor
- theophylline
- tofacitinib
- tolterodine
- torsemide
- trimipramine
- upadacitinib
- valbenazine
- vamorolone
- vanzacaftor/tezacaftor/deutivacaftor
- venlafaxine
- verapamil
- vilanterol inhaled
- vilazodone
- warfarin
- yohimbe
- zanubrutinib
- zolpidem
- zuranolone
Caution Advised
- aliskiren
- alosetron
- armodafinil
- betamethasone
- bictegravir
- budesonide inhaled
- budesonide nasal
- cannabis
- capmatinib
- cenobamate
- ciclesonide
- clindamycin
- cortisone
- cyclophosphamide
- darolutamide
- doravirine
- doxazosin
- dronabinol
- dutasteride
- elvitegravir
- eravacycline
- estradiol (hormone replacement)
- estrogens, esterified (hormone replacement)
- ethinyl estradiol (hormone replacement)
- etravirine
- fludrocortisone
- fluticasone furoate
- gefitinib
- glecaprevir
- ifosfamide
- mirvetuximab soravtansine
- modafinil
- mometasone implant
- mometasone inhaled
- mometasone nasal
- nafcillin
- naldemedine
- oxybutynin
- pibrentasvir
- pimecrolimus topical
- prednisolone
- prednisone
- ramelteon
- rifapentine
- ripretinib
- risperidone
- roflumilast
- roflumilast topical
- seladelpar
- sirolimus topical
- sotorasib
- tacrolimus topical
- tamoxifen
- tinidazole
- tisotumab vedotin
- topiramate
- triamcinolone
- vortioxetine
- zaleplon
- zileuton
Adverse Reactions .
Serious Reactions
- GI bleeding
- GI obstruction
- colitis
- ileus
- intestinal stenosis
- QT prolongation
- cardiac failure
- hypotension
- stroke
- pulmonary embolism
- pulmonary hemorrhage
- interstitial lung dz
- pneumonitis
- respiratory failure
- pleural effusion
- pneumonia
- sepsis
- anemia
- hepatotoxicity
- renal impairment
- acute kidney injury
- dehydration
- mental status alterations
Common Reactions
- diarrhea
- nausea
- fatigue
- vomiting
- musculoskeletal pain
- hepatotoxicity
- renal impairment
- dyspnea
- edema
- appetite decr.
- cough
- pneumonia
- dizziness
- constipation
- abdominal pain
- QT prolongation
- interstitial lung dz
- pneumonitis
- GI bleeding
- lymphocytes decr.
- ALT or AST incr.
- sodium decr.
- Hgb decr.
- Cr incr.
- albumin decr.
- lipase incr.
- platelets decr.
- magnesium decr.
- potassium decr.
Safety/Monitoring .
Monitoring Parameters
LFTs at baseline, qmo x3mo or as clinically indicated; ECG, electrolytes at baseline, during tx, and as clinically indicated if QT prolongation risk; s/sx interstitial lung dz
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy; no human data available; risk of decr. fetal wt and skeletal variations based on animal data at 0.11x and 2x systemic exposure
Lactation
Clinical Summary
avoid breastfeeding during tx and x1wk after D/C; no human data available to assess risk of infant harm or effects on milk production
Pharmacology .
Metabolism: liver; CYP450: 3A4 (primary), 1A2, 2B6, 2C8, 2C9, 2D6 substrate
Excretion: feces 75% (14% unchanged), urine 4.5% (2% unchanged); Half-life: 23h
Subclass: KRAS Inhibitors
Mechanism of Action
irreversibly binds unique cysteine of KRAS G12C, blocking KRAS signaling, inhibiting cell growth, and promoting apoptosis in KRAS G12C-mutated tumor cells
Formulary .
No Formulary Selected
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