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Scemblix
asciminib
Adult Dosing .
Dosage forms: TAB: 20 mg, 40 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
Ph-positive CML, chronic phase
- [T315I-negative disease]
- Dose: 80 mg PO daily; Alt: 40 mg PO bid; Info: avoid food for at least 2h before and 1h after administration; do not cut/crush/chew tab
- [T315I-positive disease]
- Dose: 200 mg PO bid; Info: avoid food for at least 2h before and 1h after administration; do not cut/crush/chew tab
renal dosing
- [see below]
- eGFR >15: no adjustment; eGFR <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
- avoid: breastfeeding during tx and x1wk after D/C
- caution: patients of childbearing potential
- caution: electrolyte abnormalities
- caution: long QT syndrome, congenital
- caution: QT prolongation
- caution: QT prolongation family history
- caution: torsades de pointes history
- caution: ventricular arrhythmia
- caution: bradycardia
- caution: MI, recent
- caution: CHF
Drug Interactions .
Overview
asciminib
kinase inhibitor
- CYP3A4 substrate
- CYP2C8 inhibitor, weak
- CYP2C9 inhibitor, moderate
- CYP3A4 inhibitor, weak
- BCRP inhibitor
- P-gp inhibitor, weak
- cardiotoxic effects
- hypertensive effects
- immunomodulatory effects
- myelosuppressive oncologic agent
- prolongs QT interval (conditional)
- thrombogenic effects
Contraindicated
- adenovirus vaccine, live
- chikungunya vaccine, live
- cholera vaccine, live
- cisapride
- colchicine
- dengue vaccine, live
- deuruxolitinib
- eliglustat
- influenza nasal vaccine, live
- measles/mumps/rubella vaccine, live
- pimozide
- rotavirus vaccine, live
- smallpox vaccine, live
- thioridazine
- typhoid vaccine, live
- varicella vaccine, live
- yellow fever vaccine, live
Avoid/Use Alternative
- abrocitinib
- alpelisib
- alprazolam
- apixaban
- arsenic trioxide
- bedaquiline
- bosentan
- chloramphenicol
- cladribine oral
- codeine
- dabigatran
- deferiprone
- domperidone
- dronedarone
- ensartinib
- ephedra
- epinephrine inhaled
- epirubicin
- erdafitinib
- etrasimod
- fexinidazole
- fosfomycin injection
- furosemide
- ganciclovir
- hydrocodone
- hydroxychloroquine
- idarubicin
- itraconazole
- lefamulin
- lonafarnib
- macitentan
- meloxicam
- meperidine
- methadone
- midodrine
- mobocertinib
- neratinib
- oxycodone
- pacritinib
- palifermin
- pazopanib
- penicillamine
- pentamidine
- pirfenidone
- pralsetinib
- primaquine
- propafenone
- quizartinib
- rabies vaccine
- radium Ra 223 dichloride
- relugolix
- repotrectinib
- rivaroxaban
- ropeginterferon alfa-2b
- simvastatin
- sirolimus albumin-bound
- sotalol
- topotecan
- toremifene
- tranexamic acid
- vaccinia immune globulin
- valganciclovir
- vandetanib
- venetoclax
- ziprasidone
Monitor/Modify Tx
- abemaciclib
- abiraterone acetate
- acalabrutinib
- acebutolol
- adagrasib
- adalimumab
- ado-trastuzumab emtansine
- afatinib
- aflibercept
- albendazole
- albuterol
- albuterol inhaled
- aldesleukin
- alemtuzumab
- alfentanil
- aliskiren
- allopurinol
- almotriptan
- alogliptin
- amiloride
- aminocaproic acid
- amiodarone
- amlodipine
- amphetamine
- anagrelide
- angiotensin II
- anthrax immune globulin
- anthrax vaccine
- anti-inhibitor coagulant complex
- anti-thymocyte globulin
- antihemophilic factor (factor VIII)/von Willebrand factor complex
- apalutamide
- apomorphine
- aprocitentan
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- armodafinil
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- asenapine
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- atenolol
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- atropine ophthalmic
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- avapritinib
- avatrombopag
- avelumab
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- azilsartan medoxomil
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- baricitinib
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- benznidazole
- benzphetamine
- betamethasone
- betaxolol
- betibeglogene autotemcel
- bevacizumab
- bezlotoxumab
- binimetinib
- bismuth subsalicylate
- bisoprolol
- bortezomib
- bosutinib
- botulism immune globulin
- brigatinib
- brolucizumab
- budesonide
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- bupropion
- C1 esterase inhibitor
- cabozantinib
- caffeine
- caffeine citrate
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- candesartan cilexetil
- cannabis
- capecitabine
- capivasertib
- captopril
- carbamazepine
- carfilzomib
- carvedilol
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- certolizumab pegol
- chikungunya vaccine
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- chorionic gonadotropin
- cidofovir
- cilostazol
- citalopram
- clarithromycin
- clevidipine
- clofazimine
- clonidine
- clozapine
- coagulation factor IX
- coagulation factor VIIa
- coagulation factor XIII A-subunit
- cobicistat
- cobimetinib
- cocaine
- concizumab
- copanlisib
- corticotropin
- cortisone
- COVID-19 vaccine
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- cyclophosphamide
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- cytomegalovirus immune globulin
- dabrafenib
- danazol
- dapsone
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- daunorubicin
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- degarelix
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- dextroamphetamine
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- digoxin
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- disopyramide
- dobutamine
- docetaxel
- dofetilide
- donepezil
- dopamine
- dordaviprone
- doxapram
- doxazosin
- doxorubicin
- dronabinol
- droperidol
- drospirenone (contraceptive)
- drospirenone (hormone replacement)
- droxidopa
- ebola vaccine, live
- edoxaban
- efbemalenograstim alfa
- eflapegrastim (G-CSF)
- eletriptan
- elivaldogene autotemcel
- eltrombopag
- enalapril
- enalaprilat
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- enfortumab vedotin
- entrectinib
- enzalutamide
- ephedrine injection
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- epinephrine
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- erenumab
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- estrogens, conjugated (hormone replacement)
- estrogens, esterified (hormone replacement)
- etanercept
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- ethinyl estradiol (hormone replacement)
- ethynodiol (contraceptive)
- etodolac
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- everolimus
- exagamglogene autotemcel
- factor XIII concentrate
- fam-trastuzumab deruxtecan
- faricimab
- fedratinib
- felodipine
- fenfluramine
- fenofibrate
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- fenoldopam
- fenoprofen
- fentanyl
- filgrastim (G-CSF)
- finerenone
- fingolimod
- fitusiran
- flecainide
- flibanserin
- flucytosine
- fludrocortisone
- fluorouracil
- fluphenazine
- flurbiprofen
- fluvastatin
- follitropin
- formoterol inhaled
- foscarnet
- fosinopril
- fosphenytoin
- fostamatinib
- fremanezumab
- frovatriptan
- fruquintinib
- galcanezumab
- gepirone
- gilteritinib
- givinostat
- glasdegib
- glimepiride
- glipizide
- glyburide
- golimumab
- goserelin
- guanfacine
- Haemophilus b vaccine
- haloperidol
- hepatitis A vaccine
- hepatitis B immune globulin
- hepatitis B vaccine
- histrelin
- hoodia
- human papillomavirus vaccine
- hydralazine
- hydrochlorothiazide
- hydrocortisone
- hydroxocobalamin IV
- hydroxyurea
- hydroxyzine
- ibrutinib
- ibuprofen
- ibutilide
- idelalisib
- ifosfamide
- imatinib
- immune globulin
- indapamide
- indomethacin
- infliximab
- influenza H5N1 vaccine
- influenza vaccine
- inotuzumab ozogamicin
- interferon beta 1a
- interferon beta 1b
- interferon gamma 1b
- iohexol
- iomeprol
- iopamidol
- irbesartan
- irinotecan
- isoflurane
- isradipine
- ivabradine
- ivosidenib
- ixabepilone
- Japanese encephalitis vaccine
- ketamine
- ketoconazole
- ketoprofen
- ketorolac
- labetalol
- lanreotide
- lapatinib
- lazertinib
- leflunomide
- lemborexant
- lenalidomide
- lenvatinib
- leuprolide
- levalbuterol inhaled
- levofloxacin
- levoketoconazole
- levomilnacipran
- levonorgestrel (contraceptive)
- levonorgestrel (hormone replacement)
- licorice
- linagliptin
- linezolid
- lisdexamfetamine
- lisinopril
- lofexidine
- lomitapide
- lopinavir/ritonavir
- lorlatinib
- losartan
- lovastatin
- lovotibeglogene autotemcel
- lumacaftor/ivacaftor
- lumateperone
- lurasidone
- lurbinectedin
- luspatercept
- lusutrombopag
- lymphocyte immune globulin, anti-thymocyte globulin
- macimorelin
- magnesium salicylate
- margetuximab
- mavacamten
- mavorixafor
- meclofenamate
- medroxyprogesterone (contraceptive)
- medroxyprogesterone (hormone replacement)
- mefenamic acid
- megestrol
- meningococcal vaccine
- menotropins
- mercaptopurine
- mesalamine
- mesalamine rectal
- methamphetamine
- methotrexate
- methoxy polyethylene glycol-epoetin beta
- methyldopa
- methylergonovine
- methylphenidate
- methylprednisolone
- methyltestosterone
- metoclopramide
- metolazone
- metoprolol
- midazolam
- mifepristone
- milnacipran
- minoxidil
- mirabegron
- mirdametinib
- mitoxantrone
- modafinil
- moexipril
- momelotinib
- morphine
- moxifloxacin
- mycophenolate mofetil
- mycophenolic acid
- nabumetone
- nadolol
- naproxen
- naratriptan
- nateglinide
- naxitamab
- nebivolol
- necitumumab
- nefazodone
- nelfinavir
- nicardipine
- nifedipine
- nilotinib
- nimodipine
- nintedanib
- niraparib
- nisoldipine
- norelgestromin (contraceptive)
- norepinephrine
- norethindrone (contraceptive)
- norethindrone (hormone replacement)
- norgestimate (contraceptive)
- norgestrel (contraceptive)
- obinutuzumab
- olaparib
- oliceridine
- olmesartan medoxomil
- olodaterol inhaled
- olsalazine
- ondansetron
- osilodrostat
- osimertinib
- ospemifene
- oxaprozin
- oxymetazoline nasal
- oxytocin
- ozanimod
- paclitaxel
- paliperidone
- palonosetron
- pasireotide
- pegaspargase
- pegfilgrastim (G-CSF)
- peginterferon alfa 2a
- peginterferon beta 1a
- pemigatinib
- perindopril
- pertuzumab
- pexidartinib
- phendimetrazine
- phenobarbital
- phenoxybenzamine
- phentermine
- phentolamine
- phenylephrine
- phenylephrine injection
- phenylephrine nasal
- phenylephrine ophthalmic
- phenylephrine rectal
- phenytoin
- pindolol
- pioglitazone
- piroxicam
- pitavastatin
- pneumococcal vaccine
- poliovirus vaccine
- pomalidomide
- ponatinib
- ponesimod
- porfimer
- posaconazole
- pravastatin
- prazosin
- prednisolone
- prednisone
- procainamide
- progesterone (hormone replacement)
- progesterone vaginal (hormone replacement)
- proguanil
- propranolol
- prothrombin complex concentrate (human)
- pseudoephedrine
- pyrimethamine
- quetiapine
- quinapril
- quinidine (antiarrhythmic)
- quinidine (CYP2D6 inhibitor)
- quinine
- raloxifene
- ramipril
- ramucirumab
- ranibizumab
- ranolazine
- red yeast rice
- regorafenib
- repaglinide
- respiratory syncytial virus vaccine
- revumenib
- Rho(D) immune globulin
- ribavirin
- ribociclib
- rifabutin
- rimegepant
- riociguat
- ripretinib
- ritlecitinib
- ritonavir
- rituximab
- rizatriptan
- romidepsin
- romiplostim
- ropinirole
- rosiglitazone
- rosuvastatin
- rotigotine transdermal
- rucaparib
- ruxolitinib
- ruxolitinib topical
- salmeterol inhaled
- salsalate
- sargramostim (GM-CSF)
- sarilumab
- satralizumab
- saxagliptin
- segesterone (contraceptive)
- selpercatinib
- selumetinib
- sevoflurane
- siponimod
- sipuleucel-T
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- smallpox/mpox vaccine, live
- sodium tetradecyl sulfate
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- spironolactone
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- succimer
- sufentanil
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- tacrolimus
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- taletrectinib
- tamoxifen
- telavancin
- telmisartan
- temsirolimus
- tenofovir alafenamide
- tenofovir disoproxil
- teplizumab
- terazosin
- terbutaline
- teriflunomide
- testosterone
- tetrabenazine
- thalidomide
- tick-borne encephalitis vaccine
- timolol
- tipranavir
- tivozanib
- tocilizumab
- tofacitinib
- tolmetin
- tolvaptan
- torsemide
- trabectedin
- tramadol
- trametinib
- trandolapril
- trastuzumab
- tretinoin
- triamcinolone
- triamterene
- triazolam
- triclabendazole
- trifluridine
- trimethoprim
- triptorelin
- tucatinib
- typhoid vaccine
- ubrogepant
- upadacitinib
- vadadustat
- valoctocogene roxaparvovec
- valproic acid
- valsartan
- vamorolone
- vancomycin
- vardenafil
- varicella zoster immune globulin
- vasopressin
- vemurafenib
- venlafaxine
- verapamil
- vilanterol inhaled
- viloxazine
- vinblastine
- vincristine
- vinorelbine
- voclosporin
- von Willebrand factor
- voriconazole
- vorinostat
- warfarin
- yohimbe
- zanidatamab
- zanubrutinib
- zavegepant
- zenocutuzumab
- zidovudine
- ziftomenib
- ziv-aflibercept
- zolmitriptan
- zongertinib
- zopapogene imadenovec
Caution Advised
- butalbital
- cariprazine
- conivaptan
- daridorexant
- darolutamide
- elinzanetant
- glecaprevir
- mitotane
- naldemedine
- palovarotene
- pentobarbital
- pibrentasvir
- primidone
- rifampin
- rilzabrutinib
- roflumilast
- roflumilast topical
- seladelpar
- sirolimus topical
- St. John's wort
Adverse Reactions .
Serious Reactions
- thrombocytopenia
- neutropenia
- anemia
- pancreatitis
- HTN
- hypersensitivity reaction
- cardiotoxicity
- cardiac failure
- arrhythmia
- QT prolongation
Common Reactions
- hypersensitivity reaction
- thrombocytopenia
- musculoskeletal pain
- neutropenia
- fatigue
- rash
- URI
- lipase incr.
- amylase incr.
- headache
- HTN
- diarrhea
- abdominal pain
- anemia
- nausea
- arthralgia
- dyslipidemia
- arrhythmia
- cardiac failure
- vomiting
- pancreatitis
- ALT or AST incr.
- lymphocytes decr.
- phosphate decr.
- CK incr.
- calcium decr.
Safety/Monitoring .
Monitoring Parameters
pregnancy test at baseline; CBC w/ diff at baseline, q2wk x3mo, then qmo or as clinically indicated; lipase, amylase at baseline, then qmo or as clinically indicated, or more frequently if pancreatitis history; BP
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy; no human data available; risk of teratogenicity, embryo-fetal death, and incr. development rate based on animal data at <1x systemic exposure and drug's mechanism of action
Individuals of Reproductive Potential
obtain pregnancy test before tx start; avoid pregnancy by using effective contraception during tx and x1wk after D/C in patients of childbearing potential
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: for asciminib: unknown; CYP450: 3A4 substrate; UGT: 2B7, 2B17 substrate
Excretion: for asciminib: feces 80% (57% unchanged), urine 11% (2.5% unchanged); Half-life: 5.5h (80 mg/day dose), 9h (400 mg/day dose)
Subclass: Kinase Inhibitors, BCR-ABL Inhibitors
Mechanism of Action
for asciminib: binds BCR-ABL myristoyl pocket, inhibiting BCR-ABL tyrosine kinase, incl. both wild-type and T315I mutant
Formulary .
No Formulary Selected
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