Dosing & Uses
Dosage Forms & Strengths
tablet
- 86mg
- 345mg
Breast Cancer
Indicated for men or postmenopausal women with estrogen receptor positive (ER+), HER2-negative, ESR1-mutated advanced or metastatic breast cancer with disease progression following at least 1 line of endocrine therapy
345 mg PO qDay with food until disease progression or unacceptable toxicity
Dosage Modifications
Dose reduction recommendations for adverse reactions
- First dose reduction: 258 mg qDay
- Second dose reduction: 172 mg qDay
- Permanently discontinue if dose reduction <172 mg/day required
Modifications for adverse reactions
- Grade 1: Continue at current dose level
- Grade 2: Consider dose interruption until recovery to Grade ≤1 or baseline, then resume at same dose
-
Grade 3
- Interrupt dose until recovery to Grade ≤1 or baseline, then resume at next lower dose
- If Grade 3 toxicity recurs, interrupt until recovery to Grade ≤1 or baseline, then resume elacestrant reduced by another dose level
-
Grade 4
- Interrupt dose until recovery to Grade ≤1 or baseline, then resume at next lower dose
- Permanently discontinue if Grade 4 or intolerable adverse reaction recurs
Hepatic impairment
- Mild (Child-Pugh A): No dosage adjustment recommended
- Moderate (Child-Pugh B): Reduce dose to 258 mg qDay
- Severe (Child-Pugh C): Avoid use; not studied
Dosing Considerations
Select patients for treatment based on presence of ESR1 mutation(s) in plasma specimen using an FDA-approved test; see information on FDA-approved tests for detection of ESR1 mutations in breast cancer
Verify pregnancy status of females of reproductive potential before initiating
Obtain baseline lipid profile before initiating
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (110)
- adagrasib
adagrasib will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- amiodarone
amiodarone will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- amobarbital
amobarbital will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- apalutamide
apalutamide will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- aprepitant
aprepitant will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- armodafinil
armodafinil will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- atazanavir
atazanavir will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- belzutifan
belzutifan will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- bexarotene
bexarotene will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- bicalutamide
bicalutamide will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- bosentan
bosentan will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- butabarbital
butabarbital will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- butalbital
butalbital will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- carbamazepine
carbamazepine will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- cenobamate
cenobamate will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ceritinib
ceritinib will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- chloramphenicol
chloramphenicol will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- clarithromycin
clarithromycin will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- cobicistat
cobicistat will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- conivaptan
conivaptan will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- crizotinib
crizotinib will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- cyclosporine
cyclosporine will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- dabrafenib
dabrafenib will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- darunavir
darunavir will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- diltiazem
diltiazem will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- doxycycline
doxycycline will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- dronedarone
dronedarone will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- efavirenz
efavirenz will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- elagolix
elagolix will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
elvitegravir/cobicistat/emtricitabine/tenofovir DF will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- encorafenib
encorafenib, elacestrant. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Encorafenib inhibits and induces CYP3A4. Avoid with sensitive CYP3A4 substrates.
- entacapone
entacapone will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- enzalutamide
enzalutamide will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- erythromycin base
erythromycin base will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- erythromycin ethylsuccinate
erythromycin ethylsuccinate will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- erythromycin lactobionate
erythromycin lactobionate will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- erythromycin stearate
erythromycin stearate will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- etravirine
etravirine will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- fedratinib
fedratinib will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- fexinidazole
fexinidazole will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- fluconazole
fluconazole will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- fluvoxamine
fluvoxamine will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- fosamprenavir
fosamprenavir will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- fosaprepitant
fosaprepitant will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- fosphenytoin
fosphenytoin will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- fostamatinib
fostamatinib will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- grapefruit
grapefruit will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- haloperidol
haloperidol will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ibrexafungerp
ibrexafungerp will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- idelalisib
idelalisib will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- iloperidone
iloperidone will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- imatinib
imatinib will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- indinavir
indinavir will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- isavuconazonium sulfate
isavuconazonium sulfate will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- isoniazid
isoniazid will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- itraconazole
itraconazole will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ivacaftor
ivacaftor will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ivosidenib
ivosidenib will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ketoconazole
ketoconazole will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- lapatinib
lapatinib will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- larotrectinib
larotrectinib will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- lefamulin
lefamulin will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- lenacapavir
lenacapavir will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- letermovir
letermovir will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- levoketoconazole
levoketoconazole will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- lonafarnib
lonafarnib will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- lopinavir
lopinavir will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- lorlatinib
lorlatinib will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- lumacaftor/ivacaftor
lumacaftor/ivacaftor will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- mavacamten
mavacamten will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- metronidazole
metronidazole will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- mifepristone
mifepristone will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- mitapivat
mitapivat will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- mitotane
mitotane will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- mobocertinib
mobocertinib will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- modafinil
modafinil will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- nafcillin
nafcillin will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- nefazodone
nefazodone will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- nelfinavir
nelfinavir will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- netupitant/palonosetron
netupitant/palonosetron will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- nirmatrelvir/ritonavir
nirmatrelvir/ritonavir will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- olutasidenib
olutasidenib will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- pentobarbital
pentobarbital will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- pexidartinib
pexidartinib will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- phenobarbital
phenobarbital will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- phenytoin
phenytoin will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- posaconazole
posaconazole will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- primidone
primidone will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- quinupristin/dalfopristin
quinupristin/dalfopristin will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ribociclib
ribociclib will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rifabutin
rifabutin will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rifampin
rifampin will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rifapentine
rifapentine will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rimegepant
elacestrant will increase the level or effect of rimegepant by Other (see comment). Avoid or Use Alternate Drug.
- ritonavir
ritonavir will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rucaparib
rucaparib will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- saquinavir
saquinavir will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- schisandra
schisandra will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- secobarbital
secobarbital will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- sertraline
sertraline will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- sotorasib
sotorasib will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- St John's Wort
St John's Wort will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- stiripentol
stiripentol, elacestrant. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Stiripentol inhibits and induces CYP3A4. Avoid with sensitive CYP3A4 substrates.
- telotristat ethyl
telotristat ethyl will decrease the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- tetracycline
tetracycline will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- tucatinib
tucatinib will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- verapamil
verapamil will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- voriconazole
voriconazole will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- voxelotor
voxelotor will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
Monitor Closely (12)
- atorvastatin
elacestrant will increase the level or effect of atorvastatin by Other (see comment). Modify Therapy/Monitor Closely. Elacestrant (a BCRP inhibitor) may increase plasma concentrations of sensitive BCRP substrates, which may increase risk of adverse reactions related to these substrates. Refer to prescribing information for sensitive BCRP substrates for dosing recommendations.
- clonidine
elacestrant will increase the level or effect of clonidine by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Reduce dose of P-gp substrates per their Prescribing Information when minimal concentration changes may lead to serious or life-threatening adverse reactions.
- colchicine
elacestrant will increase the level or effect of colchicine by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Reduce dose of P-gp substrates per their Prescribing Information when minimal concentration changes may lead to serious or life-threatening adverse reactions.
- digoxin
elacestrant will increase the level or effect of digoxin by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Reduce dose of P-gp substrates per their Prescribing Information when minimal concentration changes may lead to serious or life-threatening adverse reactions.
- irinotecan
elacestrant will increase the level or effect of irinotecan by Other (see comment). Modify Therapy/Monitor Closely. Elacestrant (a BCRP inhibitor) may increase plasma concentrations of sensitive BCRP substrates, which may increase risk of adverse reactions related to these substrates. Refer to prescribing information for sensitive BCRP substrates for dosing recommendations.
- methotrexate
elacestrant will increase the level or effect of methotrexate by Other (see comment). Modify Therapy/Monitor Closely. Elacestrant (a BCRP inhibitor) may increase plasma concentrations of sensitive BCRP substrates, which may increase risk of adverse reactions related to these substrates. Refer to prescribing information for sensitive BCRP substrates for dosing recommendations.
- sirolimus
elacestrant will increase the level or effect of sirolimus by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Reduce dose of P-gp substrates per their Prescribing Information when minimal concentration changes may lead to serious or life-threatening adverse reactions.
- tacrolimus
elacestrant will increase the level or effect of tacrolimus by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Reduce dose of P-gp substrates per their Prescribing Information when minimal concentration changes may lead to serious or life-threatening adverse reactions.
- tazemetostat
elacestrant will increase the level or effect of tazemetostat by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Reduce dose of P-gp substrates per their Prescribing Information when minimal concentration changes may lead to serious or life-threatening adverse reactions.
- temsirolimus
elacestrant will increase the level or effect of temsirolimus by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Reduce dose of P-gp substrates per their Prescribing Information when minimal concentration changes may lead to serious or life-threatening adverse reactions.
- topotecan
elacestrant will increase the level or effect of topotecan by Other (see comment). Modify Therapy/Monitor Closely. Elacestrant (a BCRP inhibitor) may increase plasma concentrations of sensitive BCRP substrates, which may increase risk of adverse reactions related to these substrates. Refer to prescribing information for sensitive BCRP substrates for dosing recommendations.
- ubrogepant
elacestrant will increase the level or effect of ubrogepant by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Ubrogepant is a P-gp and BCRP substrate. Elacestrant (a BCRP and P-gp inhibitor) may increase levels of ubrogepant, which may lead to serious or life-threatening adverse reactions. Reduce dose of ubrogepant as per its prescribing information.
Minor (0)
Adverse Effects
>10%
All grades
- Musculoskeletal pain (41%)
- Nausea (35%)
- Cholesterol increased (30%)
- AST increased (29%)
- Triglycerides increased (27%)
- Fatigue (26%)
- Hemoglobin decreased (26%)
- Vomiting (19%)
- ALT increased (17%)
- Sodium decreased (16%)
- Creatinine increased (16%)
- Decreased appetite (15%)
- Diarrhea (13%)
- Constipation (12%)
- Headache (12%)
- Abdominal pain (11%)
- Hot flush (11%)
1-10%
All grades
- Dyspepsia (10%)
Grade 3 or 4
- Musculoskeletal pain (7%)
- Nausea (2.5%)
- Fatigue (2%)
- Headache (2%)
- Triglycerides increased (2%)
- Cholesterol increased (1%)
- Sodium decreased (1%)
- Hemoglobin decreased (1%)
<1%
Grade 3 or 4
- Vomiting (0.8%)
- Decreased appetite (0.8%)
Warnings
Contraindications
None
Cautions
Hypercholesterolemia and hypertriglyceridemia reported; monitor lipid profile before initiating and periodically during treatment
Based on findings in animals and its mechanism of action, elacestrant can cause fetal harm when administered to pregnant females
Drug interaction overview
- Substrate of CYP3A4 (major), CYP2A6 (minor), and CYP2C9 (minor)
- Inhibitor of P-gp and BCRP
-
Strong or moderate CYP3A4 inducers
- Avoid coadministration
- Strong or moderate CYP3A4 inducers decrease elacestrant systemic exposure, which may decrease effectiveness
-
Strong or moderate CYP3A4 inhibitors
- Avoid coadministration
- Strong or moderate CYP3A4 inhibitors increase elacestrant systemic exposure, which may increase risk for adverse effects
-
P-gp substrates
- Modify dose and monitor
- Reduce dose of P-gp substrates per their prescribing information when minimal concentration changes may lead to serious or life-threatening adverse reactions
-
BCRP substrates
- Modify dose and monitor
- Reduce dose of BCRP substrates per their prescribing information when minimal concentration changes may lead to serious or life-threatening adverse reactions
Pregnancy & Lactation
Pregnancy
Based on animal studies and its mechanism of action, elacestrant can cause fetal harm when administered to pregnant females
Verify pregnancy status of females of reproductive potential before initiating
Animal studies
- Oral administration of elacestrant to pregnant rats during organogenesis caused embryo-fetal mortality and structural abnormalities at maternal exposures below the recommended dose based on AUC
Contraception
- Advise females of reproductive potential (including partners of men being treated with elacestrant) to use effective contraception during treatment and for 1 week after last dose
Infertility
- Based on findings from animal studies, may impair fertility in females and males of reproductive potential
Lactation
Data are unavailable on presence of drug in human milk, effects on milk production, or breastfed children
Advise lactating females to not breastfeed during treatment and for 1 week after last dose
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Estrogen receptor antagonist that binds to estrogen receptor-alpha (ERα)
In ER-positive (ER+) HER2-negative (HER2-) breast cancer cells, elacestrant inhibited 17β-estradiol mediated cell proliferation at concentrations inducing degradation of ERα protein mediated through proteasomal pathway
Elacestrant demonstrated in vitro and in vivo antitumor activity including in ER+ HER2- breast cancer models resistant to fulvestrant and cyclin-dependent kinase 4/6 inhibitors and those harboring estrogen receptor 1 gene (ESR1) mutations
Absorption
Bioavailability: ~10%
Peak plasma time: 1-4 hr
Peak plasma concentration: 119 ng/mL
AUC: 2240 ng⋅h/mL
Steady-state reached by Day 6
Effect of food
- Taking 345 mg with a high-fat meal (800-1000 calories, 50% fat) increased Cmax by 42% and AUC by 22% compared with fasted administration
Distribution
Protein bound: >99%
Vd: 5800 L
Metabolism
Primarily metabolized by CYP3A4 and to lesser extent by CYP2A6 and CYP2C9
Elimination
Half-life: 30-50 hr
Clearance: 186 L/hr
Renal clearance: ≤0.14 L/hr
Excretion: Feces 82% (34% unchanged); urine 7.5% (<1% unchanged)
Administration
Oral Administration
Take with food to reduce nausea and vomiting
Take at approximately the same time each day
Swallow tablet whole; do not chew, crush, or split
Do not take tablets that are broken, cracked, or look damaged
Missed dose
- If dose is missed for >6 hr or vomiting occurs, skip dose and take next dose the following day at regularly scheduled time
Storage
Store at 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)
Images
Formulary
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