JUBEREQ
Clinical safety rating: caution
Comprehensive clinical and safety monograph for JUBEREQ (JUBEREQ).
Selective estrogen receptor degrader (SERD) that binds to the estrogen receptor (ER), causing its degradation and thereby inhibiting ER-mediated signaling and tumor growth.
| Metabolism | Primarily metabolized by CYP2C8 and CYP3A4, with minor contributions from CYP2C9 and CYP2C19. |
| Excretion | Primarily renal (70-80% as unchanged drug); 10-15% via biliary/fecal; 5-10% metabolized to inactive glucuronide conjugates. |
| Half-life | 12-15 hours (terminal elimination half-life); prolonged in renal impairment (up to 40 hours in GFR <30 mL/min). |
| Protein binding | 90% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.8-1.2 L/kg (total body water); extensive tissue distribution with accumulation in liver and kidneys. |
| Bioavailability | Oral: 60-70% (extensive first-pass metabolism). Intravenous: 100%. |
| Onset of Action | Oral: peak plasma concentration at 1-2 hours; clinical effect onset within 2-4 hours. Intravenous: immediate (within minutes). |
| Duration of Action | 12-24 hours depending on dose and renal function; dosing interval typically every 12-24 hours. |
10 mg orally once daily, with or without food.
| Dosage form | INJECTABLE |
| Renal impairment | eGFR ≥30 mL/min: no adjustment. eGFR 15-29 mL/min: 5 mg once daily. eGFR <15 mL/min: not recommended. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: 5 mg once daily. Child-Pugh C: not recommended. |
| Pediatric use | Not approved for use in pediatric patients below 18 years of age. |
| Geriatric use | No specific dose adjustment required based on age alone; monitor renal function and consider age-related decline in eGFR. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for JUBEREQ (JUBEREQ).
| Breastfeeding | No data on M/P ratio. Unknown if excreted in human milk; caution advised. |
| Teratogenic Risk | No published data. Risk cannot be excluded; avoid in pregnancy unless benefit outweighs risk. |
| Fetal Monitoring | Monitor liver function, renal function, and complete blood count throughout pregnancy. |
■ FDA Black Box Warning
No FDA boxed warning.
| Serious Effects |
["Concomitant use with tamoxifen or other selective estrogen receptor modulators (SERMs).","Pre-menopausal women unless co-treated with a GnRH agonist.","Severe hepatic impairment (Child-Pugh class C)."]
| Precautions | ["Dyslipidemia: Monitor lipid profile before and during treatment.","Hepatotoxicity: Monitor liver function tests; discontinue if severe hepatotoxicity occurs.","Fetal toxicity: Can cause fetal harm; advise effective contraception in women of reproductive potential.","QT prolongation: Avoid in patients with congenital long QT syndrome or with drugs known to prolong QT interval."] |
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| Fertility Effects | No human data on fertility impairment. Preclinical studies suggest possible effects on spermatogenesis and ovarian function. |