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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 including toxicity-related dose adjustments
ER-positive HER2-negative, ESR1-mutated breast CA, advanced or metastatic
- [400 mg PO qd]
- Info: for patients with disease progression following endocrine tx; use as monotherapy or with abemaciclib; 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 receptor degrader
- CYP3A4 substrate
- BCRP inhibitor
- P-gp inhibitor, weak
- estrogen modulator
Contraindicated
Avoid/Use Alternative
Monitor/Modify Tx
Caution Advised
Adverse Reactions .
Serious Reactions
- pleural effusion
- pneumonia
- renal failure
- arrhythmia
- venous thromboembolism
- interstitial lung disease
- pneumonitis
Common Reactions
- musculoskeletal pain
- fatigue
- diarrhea
- nausea
- constipation
- abdominal pain
- vomiting
- rash
- headache
- cough
- weight decr.
- appetite decr.
- hot flashes
- pruritus
- dyspepsia
- stomatitis
- fever
- UTI
- dizziness
- insomnia
- arrhythmia
- alopecia
- back pain
- venous thromboembolism
- interstitial lung disease
- pneumonitis
- Hgb decr.
- neutrophils decr.
- lymphocytes decr.
- calcium decr.
- triglycerides incr.
- ALT or AST incr.
- Cr incr.
- Plt decr.
- cholesterol 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, including 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: for imlunestrant: unknown; CYP450: 3A4 substrate; UGT: 1A1, 1A3, 1A8, 1A9, 1A10 substrate
Excretion: for imlunestrant: feces 97% (62% unchanged), urine 0.3%; Half-life: 30h
Subclass: Estrogen Receptor Degraders ; Hormonal Oncologics, Antiestrogens
Mechanism of Action
for imlunestrant: 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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