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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 dz]
- Dose: 80 mg PO daily; Alt: 40 mg PO bid; Info: avoid food for at least 2h before and 1h after admin; do not cut/crush/chew tab
- [T315I-positive dz]
- Dose: 200 mg PO bid; Info: avoid food for at least 2h before and 1h after admin; 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: female pts of reproductive potential
- caution: electrolyte abnormalities
- caution: long QT syndrome, congenital
- caution: QT prolongation
- caution: QT prolongation family hx
- caution: torsades de pointes hx
- 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
- OATP1B1 inhibitor, weak
- OATP1B3 inhibitor, weak
- P-gp inhibitor, weak
- cardiotoxic effects
- hypertensive effects
- myelosuppressive oncologic agent
- prolongs QT interval (conditional)
- thrombogenic effects
Contraindicated
- cisapride
- colchicine
- deuruxolitinib
- grazoprevir
- pimozide
- thioridazine
Avoid/Use Alternative
- abrocitinib
- alpelisib
- alprazolam
- apixaban
- arsenic trioxide
- bedaquiline
- bosentan
- brincidofovir
- chloramphenicol
- cladribine oral
- codeine
- dabigatran
- deferiprone
- domperidone
- dronedarone
- elagolix
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- epirubicin
- erdafitinib
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- futibatinib
- ganciclovir
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- idarubicin
- itraconazole
- lefamulin
- lonafarnib
- macitentan
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- methadone
- midodrine
- mobocertinib
- neratinib
- ospemifene
- oxycodone
- pacritinib
- palifermin
- pazopanib
- penicillamine
- pentamidine
- pirfenidone
- pralsetinib
- primaquine
- propafenone
- quizartinib
- radium Ra 223 dichloride
- relugolix
- repotrectinib
- resmetirom
- rivaroxaban
- ropeginterferon alfa-2b
- simvastatin
- siponimod
- sirolimus albumin-bound
- sodium phenylbutyrate/taurursodiol
- sotalol
- topotecan
- toremifene
- tranexamic acid
- vaccinia immune globulin
- valganciclovir
- vandetanib
- venetoclax
- zavegepant
- ziprasidone
Monitor/Modify Tx
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- norepinephrine
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- oxytocin
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- phendimetrazine
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- phenylephrine
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- triazolam
- triclabendazole
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- trimethoprim
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- ubrogepant
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- valoctocogene roxaparvovec
- valproic acid
- valsartan
- vamorolone
- 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
- zidovudine
- ziv-aflibercept
- zolmitriptan
Caution Advised
- conivaptan
- daridorexant
- darolutamide
- glecaprevir
- naldemedine
- palovarotene
- pibrentasvir
- rifabutin
- rifampin
- roflumilast
- roflumilast topical
- seladelpar
- sirolimus topical
- voxilaprevir
Adverse Reactions .
Serious Reactions
- thrombocytopenia
- neutropenia
- anemia
- pancreatitis
- HTN
- hypersensitivity rxn
- cardiotoxicity
- cardiac failure
- arrhythmia
- QT prolongation
- female infertility (animal studies)
Common Reactions
- hypersensitivity rxn
- 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 hx; 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 female pts
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: unknown; CYP450: 3A4 substrate; UGT: 2B7, 2B17 substrate
Excretion: 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
binds BCR-ABL myristoyl pocket, inhibiting BCR-ABL tyrosine kinase, incl. both wild-type and T315I-mutated
Formulary .
No Formulary Selected
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