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Tazverik
tazemetostat
Adult Dosing .
Dosage forms: TAB: 200 mg
Withdrawn from US Market
- [March 2026]
- Info: risk of secondary hematologic malignancies outweighed potential benefits
Peds Dosing .
- Dosage forms: TAB: 200 mg
Withdrawn from US Market
- [March 2026]
- Info: the risk of secondary hematologic malignancies outweighed the potential benefits
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- avoid: breastfeeding during tx and x1wk after D/C
- caution: patients of childbearing potential
- caution: male patients of reproductive potential
Drug Interactions .
Overview
tazemetostat
methyltransferase inhibitor
- CYP3A4 substrate
- CYP2C8 inhibitor, weak
- CYP3A4 inducer, weak
- myelosuppressive oncologic agent
- prolongs QT interval (conditional)
- Withdrawn from US Market
Contraindicated
- pimozide
- ranolazine
- thioridazine
Avoid/Use Alternative
- adagrasib
- apalutamide
- aprepitant
- arsenic trioxide
- atazanavir
- avacopan
- bedaquiline
- berotralstat
- bosentan
- butalbital
- carbamazepine
- cenobamate
- ceritinib
- chloramphenicol
- ciprofloxacin
- cladribine oral
- clarithromycin
- clofazimine
- cobicistat
- codeine
- conivaptan
- crizotinib
- cyclosporine
- dabrafenib
- danazol
- darunavir
- deferiprone
- desogestrel (contraceptive)
- dexrazoxane
- dienogest (contraceptive)
- diltiazem
- dolutegravir
- domperidone
- dronedarone
- drospirenone (contraceptive)
- duvelisib
- efavirenz
- elagolix
- encorafenib
- enzalutamide
- ephedra
- erythromycin
- estradiol (contraceptive)
- ethinyl estradiol (contraceptive)
- ethynodiol (contraceptive)
- etonogestrel (contraceptive)
- etravirine
- fedratinib
- fentanyl
- fexinidazole
- fluconazole
- fosamprenavir
- fosfomycin injection
- fosphenytoin
- ganciclovir
- grapefruit
- hydroxychloroquine
- idelalisib
- imatinib
- isavuconazonium
- itraconazole
- ivosidenib
- ketoconazole
- lefamulin
- lenacapavir
- letermovir
- levoketoconazole
- levonorgestrel (contraceptive)
- levonorgestrel (post-coital contraceptive)
- lonafarnib
- lopinavir/ritonavir
- lorlatinib
- lumacaftor/ivacaftor
- lumateperone
- mavacamten
- medroxyprogesterone (contraceptive)
- meperidine
- mifepristone
- mitapivat
- mitotane
- mobocertinib
- modafinil
- nafcillin
- nefazodone
- nelfinavir
- netupitant
- nilotinib
- nirogacestat
- norelgestromin (contraceptive)
- norethindrone (contraceptive)
- norgestimate (contraceptive)
- norgestrel (contraceptive)
- oliceridine
- oxycodone
- pacritinib
- palifermin
- penicillamine
- pentamidine
- pentobarbital
- pexidartinib
- phenobarbital
- phenytoin
- posaconazole
- primaquine
- primidone
- quizartinib
- radium Ra 223 dichloride
- relacorilant
- repotrectinib
- ribociclib
- rifabutin
- rifampin
- rifapentine
- rilzabrutinib
- ritonavir
- ropeginterferon alfa-2b
- segesterone (contraceptive)
- sotalol
- sotorasib
- St. John's wort
- tipranavir
- toremifene
- tramadol
- tucatinib
- ulipristal (post-coital contraceptive)
- valganciclovir
- vandetanib
- verapamil
- voriconazole
- ziprasidone
- zuranolone
Monitor/Modify Tx
- aficamten
- albendazole
- alemtuzumab
- allopurinol
- amiodarone
- amlodipine
- anagrelide
- anti-thymocyte globulin
- apomorphine
- artemether/lumefantrine
- asenapine
- atidarsagene autotemcel
- atogepant
- auranofin
- azathioprine
- azithromycin
- balsalazide
- baricitinib
- benznidazole
- betibeglogene autotemcel
- buprenorphine
- cabozantinib
- chloroquine
- cidofovir
- citalopram
- clozapine
- colchicine
- copper histidinate
- cyclophosphamide
- dapsone
- deferasirox
- degarelix
- desflurane
- desipramine
- deuruxolitinib
- dexmedetomidine
- dexmedetomidine injection
- disopyramide
- dofetilide
- donepezil
- dordaviprone
- droperidol
- efbemalenograstim alfa
- eflapegrastim (G-CSF)
- elivaldogene autotemcel
- epirubicin
- eribulin
- etuvetidigene autotemcel
- everolimus
- exagamglogene autotemcel
- filgrastim (G-CSF)
- flecainide
- flucytosine
- fluorouracil
- fluphenazine
- foscarnet
- fostamatinib
- gilteritinib
- givinostat
- glasdegib
- goserelin
- haloperidol
- histrelin
- hydroxyurea
- hydroxyzine
- ibutilide
- ifosfamide
- inotuzumab ozogamicin
- interferon beta 1a
- interferon beta 1b
- interferon gamma 1b
- isoflurane
- isradipine
- leflunomide
- leuprolide
- levofloxacin
- linezolid
- lofexidine
- lovotibeglogene autotemcel
- lymphocyte immune globulin, anti-thymocyte globulin
- macimorelin
- marnetegragene autotemcel
- mercaptopurine
- mesalamine
- mesalamine rectal
- methadone
- methotrexate
- moxifloxacin
- mycophenolate mofetil
- mycophenolic acid
- nicardipine
- nimodipine
- nisoldipine
- olsalazine
- ondansetron
- osimertinib
- paclitaxel
- paliperidone
- palonosetron
- pasireotide
- pegfilgrastim (G-CSF)
- peginterferon alfa 2a
- peginterferon beta 1a
- procainamide
- proguanil
- propafenone
- pyrimethamine
- quinidine (antiarrhythmic)
- quinidine (CYP2D6 inhibitor)
- quinine
- repaglinide
- revumenib
- ribavirin
- rituximab
- romidepsin
- rucaparib
- ruxolitinib topical
- sargramostim (GM-CSF)
- sarilumab
- satralizumab
- selpercatinib
- sevoflurane
- sirolimus
- stiripentol
- succimer
- sulfasalazine
- tacrolimus
- taletrectinib
- telavancin
- teplizumab
- teriflunomide
- tetrabenazine
- thalidomide
- tiagabine
- tocilizumab
- tofacitinib
- triclabendazole
- trifluridine
- trimethoprim
- triptorelin
- ubrogepant
- upadacitinib
- valproic acid
- vancomycin
- vemurafenib
- warfarin
- zidovudine
- ziftomenib
Caution Advised
- abemaciclib
- acalabrutinib
- alfentanil
- alprazolam
- armodafinil
- atorvastatin
- avapritinib
- axitinib
- belzutifan
- bexarotene
- bictegravir
- bosutinib
- brigatinib
- budesonide
- buspirone
- capivasertib
- capmatinib
- clobazam
- cobimetinib
- danshen
- daridorexant
- darolutamide
- dasatinib
- defactinib
- deflazacort
- dexamethasone
- dicloxacillin
- doravirine
- drospirenone (hormone replacement)
- echinacea
- elacestrant
- elafibranor
- elbasvir
- elexacaftor/tezacaftor/ivacaftor
- eliglustat
- elvitegravir
- enasidenib
- entrectinib
- erdafitinib
- erlotinib
- eslicarbazepine acetate
- felbamate
- felodipine
- finerenone
- fosaprepitant
- fruquintinib
- garlic
- gepirone
- ginkgo
- ginseng, Asian
- glecaprevir
- glycerol phenylbutyrate
- grazoprevir
- griseofulvin
- guanfacine
- hydrocortisone
- ibrutinib
- irinotecan
- istradefylline
- ivacaftor
- lapatinib
- larotrectinib
- lazertinib
- leniolisib
- levonorgestrel intrauterine device (contraceptive)
- lurasidone
- macitentan
- maraviroc
- meropenem
- midazolam
- midostaurin
- naldemedine
- naloxegol
- neratinib
- nevirapine
- nifedipine
- nirmatrelvir
- odevixibat
- olaparib
- olutasidenib
- omaveloxolone
- oxcarbazepine
- palbociclib
- pemigatinib
- perampanel
- pimavanserin
- pioglitazone
- pirtobrutinib
- ponatinib
- praziquantel
- prednisone
- pretomanid
- quetiapine
- rilpivirine
- ripretinib
- roflumilast
- rolapitant
- rufinamide
- samidorphan
- sebetralstat
- selumetinib
- simvastatin
- sirolimus albumin-bound
- sonidegib
- sunvozertinib
- suzetrigine
- tadalafil
- tamoxifen
- tasimelteon
- tecovirimat
- telotristat ethyl
- temsirolimus
- tezacaftor/ivacaftor
- ticagrelor
- tolvaptan
- topiramate
- tovorafenib
- vaborbactam
- vamorolone
- vanzacaftor/tezacaftor/deutivacaftor
- velpatasvir
- venetoclax
- vinblastine
- voclosporin
- vonoprazan
- vorasidenib
- voxilaprevir
- zanubrutinib
Adverse Reactions .
Serious Reactions
- secondary malignancy
- anemia
- hemorrhage
- pleural effusion
- respiratory distress
- pneumonia
- sepsis
- herpes zoster
Common Reactions
- fatigue
- nausea
- pain
- respiratory infection
- cough
- abdominal pain
- diarrhea
- vomiting
- headache
- musculoskeletal pain
- alopecia
- appetite decr.
- rash
- constipation
- hemorrhage
- UTI
- dyspnea
- weight decr.
- fever
- Hgb decr.
- lymphocytes decr.
- glucose incr.
- platelets decr.
- WBC decr.
- ALT or AST incr.
- alk phos incr.
Safety/Monitoring .
Withdrawn from US Market
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy; risk of skeletal variations based on animal data at 1.5x and 2x systemic exposure; risk of teratogenicity and embryo-fetal death at 7x and 14x systemic exposure
Individuals of Reproductive Potential
obtain pregnancy test before tx start; avoid pregnancy by using effective non-hormonal contraception during tx and x6mo after D/C in patients of childbearing potential and during tx and for at least 3mo after D/C in male patients
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 tazemetostat: unknown; CYP450: 3A4 substrate
Excretion: for tazemetostat: feces 79%, urine 15%; Half-life: 3.1h
Subclass: Epigenetic Modifiers, Histone Methyltransferase (HMT) Inhibitors
Mechanism of Action
for tazemetostat: inhibits methyltransferase EZH2, preventing methylation of histone H3 lysine 27, leading to decreased tumor cell proliferation in EZH2 mutated cancer cells
Formulary .
No Formulary Selected
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