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Inluriyo
imlunestrant
Adult Dosing .
Dosage forms: TAB: 200 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
ER-positive HER2-negative, ESR1-mutated breast CA, advanced or metastatic
- [400 mg PO qd]
- Info: for patients w/ disease progression following endocrine tx; give w/ LHRH agonist in pre/perimenopausal patients or male patients; give at least 2h before or 1h after food; do not cut/crush/chew tab
renal dosing
- [see below]
- eGFR >30: no adjustment; eGFR <30: not defined
- HD/PD: not defined
hepatic dosing
- [adjust dose amount]
- Child-Pugh Class B or C: 200 mg qd
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: male patients of reproductive potential
- caution: hepatic impairment, Child-Pugh Class B-C
Drug Interactions .
Overview
imlunestrant
estrogen antagonist
- CYP3A4 substrate
- BCRP inhibitor
- P-gp inhibitor, weak
- estrogen modulator
Contraindicated
- colchicine
Avoid/Use Alternative
- adagrasib
- alpelisib
- apalutamide
- apixaban
- atazanavir
- butalbital
- carbamazepine
- ceritinib
- chloramphenicol
- cladribine oral
- clarithromycin
- cobicistat
- dabigatran
- encorafenib
- ensartinib
- enzalutamide
- fosphenytoin
- futibatinib
- idelalisib
- itraconazole
- ivosidenib
- ketoconazole
- levoketoconazole
- lonafarnib
- lopinavir/ritonavir
- lumacaftor/ivacaftor
- mifepristone
- mitotane
- nefazodone
- nelfinavir
- neratinib
- pazopanib
- pentobarbital
- phenobarbital
- phenytoin
- posaconazole
- pralsetinib
- primidone
- relugolix
- repotrectinib
- ribociclib
- rifabutin
- rifampin
- ritonavir
- rivaroxaban
- sirolimus albumin-bound
- St. John's wort
- tipranavir
- topotecan
- tucatinib
- venetoclax
- voriconazole
Monitor/Modify Tx
- afatinib
- atorvastatin
- cyclosporine
- digoxin
- edoxaban
- enfortumab vedotin
- everolimus
- fluvastatin
- imatinib
- irinotecan
- lapatinib
- mavorixafor
- methotrexate
- mitoxantrone
- morphine
- pitavastatin
- pravastatin
- quinidine (antiarrhythmic)
- ranolazine
- riociguat
- rosuvastatin
- simvastatin
- sirolimus
- tacrolimus
- talazoparib
- tenofovir alafenamide
- tenofovir disoproxil
- ubrogepant
Caution Advised
- aprepitant
- avacopan
- berotralstat
- bosentan
- cenobamate
- ciprofloxacin
- clofazimine
- conivaptan
- crizotinib
- dabrafenib
- danazol
- darolutamide
- darunavir
- diltiazem
- dronedarone
- duvelisib
- efavirenz
- erythromycin
- estetrol (contraceptive)
- estradiol (contraceptive)
- estradiol (hormone replacement)
- estrogens, conjugated (hormone replacement)
- estrogens, esterified (hormone replacement)
- ethinyl estradiol (contraceptive)
- ethinyl estradiol (hormone replacement)
- etravirine
- fedratinib
- fexinidazole
- fluconazole
- fosamprenavir
- glecaprevir
- grapefruit
- isavuconazonium
- lefamulin
- lenacapavir
- letermovir
- lorlatinib
- mavacamten
- mitapivat
- modafinil
- nafcillin
- naldemedine
- netupitant
- nilotinib
- nirogacestat
- pacritinib
- pexidartinib
- pibrentasvir
- rifapentine
- rilzabrutinib
- seladelpar
- sotorasib
- sulfasalazine
- verapamil
Adverse Reactions .
Serious Reactions
- pleural effusion
Common Reactions
- musculoskeletal pain
- fatigue
- diarrhea
- nausea
- constipation
- abdominal pain
- vomiting
- headache
- cough
- appetite decr.
- hot flashes
- pruritus
- dyspepsia
- stomatitis
- Hgb decr.
- neutrophils decr.
- calcium decr.
- ALT or AST incr.
- triglycerides incr.
Safety/Monitoring .
Monitoring Parameters
pregnancy test at baseline; lipid profile at baseline, then periodically
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy; no human data available; risk of fetal harm, incl. teratogenicity and embryo-fetal death based on animal data at 0.1-1x 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 and 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: unknown; CYP450: 3A4 substrate; UGT: 1A1, 1A3, 1A8, 1A9, 1A10 substrate
Excretion: feces 97% (62% unchanged), urine 0.3%; Half-life: 30h
Subclass: Hormonal Oncologics, Antiestrogens
Mechanism of Action
binds to estrogen receptor-alpha and induces estrogen receptor-alpha protein degradation in breast cancer cells, inhibiting 17-beta estradiol-mediated cell proliferation
Formulary .
No Formulary Selected
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