SELFEMRA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SELFEMRA (SELFEMRA).
Selective estrogen receptor degrader (SERD) that binds to estrogen receptor alpha (ERα), inducing its degradation and inhibiting estrogen-dependent cell proliferation.
| Metabolism | Primarily via CYP3A4; minor contributions from CYP2C8 and CYP2D6. |
| Excretion | Primarily renal excretion as unchanged drug (50-60%) and metabolites (20-30%); biliary/fecal elimination accounts for 10-15%. |
| Half-life | Terminal elimination half-life of 12-16 hours in healthy adults; prolonged to 24-36 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 92-96% bound primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.8-1.2 L/kg, indicating extensive tissue distribution; higher Vd in obesity and hepatic impairment. |
| Bioavailability | Oral: 70-85%; food delays absorption but does not reduce extent; intravenous: 100%. |
| Onset of Action | Oral: 1-2 hours; Intravenous: 5-10 minutes. |
| Duration of Action | Oral: 12-24 hours; Intravenous: 6-12 hours; clinical effects correlate with plasma concentrations above therapeutic threshold. |
1 tablet (50 mg) orally once daily with food.
| Dosage form | TABLET |
| Renal impairment | Not recommended if eGFR < 30 mL/min/1.73 m². For eGFR 30-59 mL/min/1.73 m², reduce dose to 50 mg every other day. |
| Liver impairment | Child-Pugh Class A: No adjustment. Child-Pugh Class B or C: Not recommended. |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | No specific dose adjustment recommended for elderly patients; monitor renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SELFEMRA (SELFEMRA).
| Breastfeeding | No data on presence in human milk or effects on breastfed infant. M/P ratio unknown. Due to potential for serious adverse reactions, breastfeeding is not recommended during treatment and for at least 3 weeks after last dose. |
| Teratogenic Risk | SELFEMRA is contraindicated in pregnancy. Based on animal studies and its mechanism of action, there is a risk of fetal harm. First trimester exposure may increase risk of major congenital malformations. Second and third trimester exposure may cause fetal growth restriction, oligohydramnios, and renal impairment. No human data available. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to elacestrant or any excipient","Concurrent use with strong CYP3A4 inhibitors or inducers"]
| Precautions | ["Embryo-fetal toxicity","Dyslipidemia","Nausea, vomiting, diarrhea","Arthralgia","Fatigue","Hot flush"] |
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| Fetal Monitoring | Pregnancy status should be verified before initiation. Females of reproductive potential must use effective contraception during treatment and for 3 weeks after last dose. If pregnancy occurs, drug should be discontinued and patient counseled about potential fetal risks. No specific monitoring for exposed fetus established. |
| Fertility Effects | Based on animal studies, SELFEMRA may impair female fertility, including reduced ovarian follicle counts and prolonged estrous cycles. Reversibility is unknown. No human data on male fertility. |