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Welireg
belzutifan
Black Box Warnings .
Embryo-Fetal Toxicity
exposure during pregnancy can cause embryo-fetal harm; verify pregnancy status prior to tx start; advise pts of risks and need for effective non-hormonal contraception; tx can render some hormonal contraceptives ineffective
Adult Dosing .
Dosage forms: TAB: 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
von Hippel-Lindau dz
- [120 mg PO qd]
- Info: for pts requiring tx but not requiring immediate surgery for associated renal cell carcinoma, CNS hemangioblastoma, or pancreatic neuroendocrine tumor; do not cut/crush/chew tab
renal cell CA, advanced
- [120 mg PO qd]
- Info: for pts w/ clear cell component who have received prior tx w/ PD-1/PD-L1 inhibitor and VEGF-TKI; do not cut/crush/chew tab
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 .
Peds dosing is currently unavailable or not applicable for this drug.
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- Hgb <9
- pulse oximeter <88% at rest
- avoid: breastfeeding during tx and x1wk after D/C
- caution: pulse oximeter <88% w/ exercise
- caution: UGT2B17 and CYP2C19 poor metabolizers, dual
- caution: pts of childbearing potential
- caution: male pts of reproductive potential
Drug Interactions .
Overview
belzutifan
hypoxia-inducible factor inhibitor
- CYP2C19 substrate
- UGT2B17 substrate
- CYP3A4 inducer, minor
Avoid/Use Alternative
- atogepant
- dolutegravir
- estradiol (contraceptive)
- etonogestrel (contraceptive)
- levonorgestrel (post-coital contraceptive)
- mavacamten
- norelgestromin (contraceptive)
- norgestimate (contraceptive)
- norgestrel (contraceptive)
- segesterone (contraceptive)
- zuranolone
Monitor/Modify Tx
- buprenorphine
- cannabidiol
- cannabis
- carbamazepine
- cyclophosphamide
- cyclosporine
- diltiazem
- disopyramide
- everolimus
- fedratinib
- fluconazole
- fluoxetine
- ifosfamide
- isradipine
- ketoconazole
- mitapivat
- nicardipine
- nimodipine
- nisoldipine
- oliceridine
- omeprazole
- perampanel
- quetiapine
- quinidine (antiarrhythmic)
- sirolimus
- stiripentol
- tacrolimus
- tiagabine
- voriconazole
Caution Advised
- abemaciclib
- acalabrutinib
- alfentanil
- alprazolam
- amiodarone
- aprepitant
- artemether/lumefantrine
- atorvastatin
- avacopan
- avapritinib
- axitinib
- bictegravir
- bosutinib
- brigatinib
- budesonide
- buspirone
- cabozantinib
- capivasertib
- capmatinib
- clarithromycin
- cobicistat
- cobimetinib
- codeine
- crizotinib
- daridorexant
- darunavir
- dasatinib
- deflazacort
- doravirine
- dronedarone
- elacestrant
- elbasvir
- elexacaftor/tezacaftor/ivacaftor
- eliglustat
- elvitegravir
- entrectinib
- erdafitinib
- erlotinib
- felodipine
- fentanyl
- finerenone
- fosaprepitant
- fostamatinib
- fruquintinib
- ganaxolone
- gepirone
- gilteritinib
- glasdegib
- glecaprevir
- grazoprevir
- guanfacine
- haloperidol
- hydrocortisone
- ibrutinib
- idelalisib
- imatinib
- infigratinib
- irinotecan
- isavuconazonium
- istradefylline
- itraconazole
- ivacaftor
- ixazomib
- lapatinib
- larotrectinib
- lazertinib
- lefamulin
- lenacapavir
- leniolisib
- letermovir
- levoketoconazole
- levonorgestrel intrauterine device (contraceptive)
- lonafarnib
- lorlatinib
- lurasidone
- macitentan
- maraviroc
- methadone
- midazolam
- midostaurin
- mobocertinib
- naldemedine
- naloxegol
- nefazodone
- nelfinavir
- neratinib
- netupitant
- nevirapine
- nifedipine
- nilotinib
- nirmatrelvir
- nirogacestat
- olaparib
- olutasidenib
- oxycodone
- palbociclib
- pemigatinib
- pimavanserin
- pirtobrutinib
- ponatinib
- praziquantel
- pretomanid
- quinine
- quizartinib
- repotrectinib
- ribociclib
- rilpivirine
- ripretinib
- ritonavir
- roflumilast
- rolapitant
- samidorphan
- selpercatinib
- selumetinib
- sildenafil
- simvastatin
- sirolimus albumin-bound
- sonidegib
- suzetrigine
- tadalafil
- tamoxifen
- tazemetostat
- temsirolimus
- tezacaftor/ivacaftor
- ticagrelor
- tipranavir
- tofacitinib
- tolvaptan
- toremifene
- tramadol
- vanzacaftor/tezacaftor/deutivacaftor
- velpatasvir
- venetoclax
- verapamil
- vinblastine
- vincristine
- vinorelbine
- voclosporin
- vonoprazan
- voxelotor
- voxilaprevir
- zanubrutinib
Adverse Reactions .
Serious Reactions
- anemia
- hypoxia
- anaphylaxis
- retinal detachment
- central retinal vein occlusion
Common Reactions
- fatigue
- myalgia
- nausea
- edema
- dyspnea
- headache
- dizziness
- constipation
- hypoxia
- appetite decr.
- abdominal pain
- vomiting
- diarrhea
- visual impairment
- hemorrhage
- HTN
- rash
- weight incr.
- URI
- arthralgia
- Hgb decr.
- Cr incr.
- ALT or AST incr.
- lymphocytes decr.
- sodium decr.
- potassium incr.
Safety/Monitoring .
Monitoring Parameters
pregnancy test at baseline; Hgb, oxygen saturation at baseline, then periodically during tx
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy; no human data available; risk of skeletal malformations and decr. body wt based on animal data at 0.2x or greater systemic exposure; risk of embryo-fetal death at 1x systemic exposure
Individuals of Reproductive Potential
obtain pregnancy test before tx start; avoid pregnancy by using effective non-hormonal contraception during tx and x1wk after D/C in female pts and using effective contraception during tx and x1wk after D/C in male 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: liver; CYP450: 2C19 (primary), 3A4 substrate; UGT: 2B17 (primary) substrate
Excretion: feces 51.7%, urine 49.6%; Half-life: 14h; Half-life: 14h
Subclass: Hypoxia-Inducible Factor-2 Alpha (HIF-2a) Inhibitors
Mechanism of Action
inhibits hypoxia-inducible factor (HIF)-2 alpha, blocking formation of HIF-2 alpha-HIF-1 beta transcriptional complex, reducing expression of downstream genes assoc. w/ cellular proliferation, angiogenesis, and tumor growth
Formulary .
No Formulary Selected
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