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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
pheochromocytoma or paraganglioma
- [120 mg PO qd]
- Info: for pts w/ locally advanced, unresectable, or metastatic dz; do not cut/crush/chew tab
renal dosing
- [see below]
- eGFR >30: no adjustment; eGFR <30: not defined, caution advised
- 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, caution advised
Peds 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
pheochromocytoma or paraganglioma
- [12 yo and older, <40 kg]
- Dose: 80 mg PO qd; Info: for pts w/ locally advanced, unresectable, or metastatic dz; do not cut/crush/chew tab
- [12 yo and older, >40 kg]
- Dose: 120 mg PO qd; Info: for pts w/ locally advanced, unresectable, or metastatic dz; do not cut/crush/chew tab
renal dosing
- [see below]
- eGFR >30: no adjustment; eGFR <30: not defined, caution advised
- 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, caution advised
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- Hgb <8
- pulse oximeter <88% at rest
- partial pressure of arterial oxygen <55 mmHg at rest
- avoid: breastfeeding during tx and x1wk after D/C
- caution: pulse oximeter <88% w/ exercise
- caution: partial pressure of arterial oxygen <55 mmHg w/ exercise
- caution: UGT2B17 and CYP2C19 poor metabolizers, dual
- caution: pts of childbearing potential
- caution: male pts of reproductive potential
- caution: eGFR <30
- caution: bilirubin >1.5x ULN
Drug Interactions .
Overview
belzutifan
hypoxia-inducible factor inhibitor
- CYP2C19 substrate
- UGT2B17 substrate
- CYP3A4 inducer, weak
- immunosuppressive effects
Avoid/Use Alternative
- adenovirus vaccine, live
- atazanavir
- atogepant
- chikungunya vaccine, live
- cholera vaccine, live
- codeine
- dengue vaccine, live
- desogestrel (contraceptive)
- dienogest (contraceptive)
- dolutegravir
- drospirenone (contraceptive)
- estradiol (contraceptive)
- ethinyl estradiol (contraceptive)
- ethynodiol (contraceptive)
- etonogestrel (contraceptive)
- fentanyl
- fosamprenavir
- influenza nasal vaccine, live
- levonorgestrel (contraceptive)
- levonorgestrel (post-coital contraceptive)
- lopinavir/ritonavir
- lumateperone
- mavacamten
- measles/mumps/rubella vaccine, live
- medroxyprogesterone (contraceptive)
- meperidine
- norelgestromin (contraceptive)
- norethindrone (contraceptive)
- norgestimate (contraceptive)
- norgestrel (contraceptive)
- rabies vaccine
- ranolazine
- rotavirus vaccine, live
- segesterone (contraceptive)
- smallpox vaccine, live
- tramadol
- typhoid vaccine, live
- ulipristal (post-coital contraceptive)
- varicella vaccine, live
- yellow fever vaccine, live
- zuranolone
Monitor/Modify Tx
- amlodipine
- anthrax vaccine
- buprenorphine
- cannabidiol
- cannabis
- carbamazepine
- cenobamate
- chikungunya vaccine
- COVID-19 vaccine
- cyclophosphamide
- cyclosporine
- diltiazem
- diphtheria/tetanus vaccine
- diphtheria/tetanus/pertussis vaccine
- disopyramide
- ebola vaccine, live
- efavirenz
- everolimus
- fedratinib
- fexinidazole
- fluconazole
- fluoxetine
- fluvoxamine
- Haemophilus b vaccine
- hepatitis A vaccine
- hepatitis B vaccine
- human papillomavirus vaccine
- ifosfamide
- influenza H5N1 vaccine
- influenza vaccine
- isradipine
- Japanese encephalitis vaccine
- ketoconazole
- meningococcal vaccine
- mitapivat
- nicardipine
- nimodipine
- nisoldipine
- oliceridine
- omeprazole
- perampanel
- pneumococcal vaccine
- poliovirus vaccine
- quetiapine
- quinidine (antiarrhythmic)
- respiratory syncytial virus vaccine
- sirolimus
- smallpox/mpox vaccine, live
- stiripentol
- tacrolimus
- tiagabine
- tick-borne encephalitis vaccine
- typhoid vaccine
- ubrogepant
- voriconazole
- warfarin
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
- crizotinib
- daridorexant
- darunavir
- dasatinib
- defactinib
- deflazacort
- doravirine
- dronedarone
- drospirenone (hormone replacement)
- elacestrant
- elbasvir
- elexacaftor/tezacaftor/ivacaftor
- eliglustat
- elvitegravir
- entrectinib
- erdafitinib
- erlotinib
- felodipine
- 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
- vanzacaftor/tezacaftor/deutivacaftor
- velpatasvir
- venetoclax
- verapamil
- vinblastine
- vincristine
- vinorelbine
- voclosporin
- vonoprazan
- voxelotor
- voxilaprevir
- zanubrutinib
Adverse Reactions .
Serious Reactions
- anemia
- hypoxia
- pleural effusion
- dyspnea
- hemorrhage
- anaphylaxis
- retinal detachment
- central retinal vein occlusion
- infection, serious
- HTN
Common Reactions
- fatigue
- myalgia
- nausea
- dyspnea
- edema
- headache
- dizziness
- constipation
- anemia
- hypoxia
- appetite decr.
- abdominal pain
- diarrhea
- vomiting
- HTN
- hemorrhage
- musculoskeletal pain
- weight incr.
- visual impairment
- rash
- URI
- arthralgia
- cough
- 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 pts of childbearing potential 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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