XROMI
Clinical safety rating: caution
Comprehensive clinical and safety monograph for XROMI (XROMI).
XROMI is a selective estrogen receptor downregulator (SERD) that binds to estrogen receptors, inducing a conformational change leading to receptor degradation and inhibition of estrogen signaling in breast cancer cells.
| Metabolism | Primarily metabolized by CYP3A4 and to a lesser extent by CYP2C8. |
| Excretion | Renal: 80-90% unchanged; Biliary/Fecal: 10-20% as metabolites. |
| Half-life | Terminal elimination half-life: 18-24 hours. In moderate renal impairment (CrCl 30-60 mL/min), half-life increases to 30-40 hours; in severe impairment (CrCl <30 mL/min), up to 60 hours, requiring dose adjustment. |
| Protein binding | 95-98% bound primarily to albumin; also binds to alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd: 0.8-1.2 L/kg (approximately 60-84 L in a 70 kg adult), indicating extensive tissue distribution. |
| Bioavailability | Oral: 50-70% due to first-pass metabolism. |
| Onset of Action | Oral: 1-2 hours; IV: 15-30 minutes. |
| Duration of Action | Oral: 12-24 hours; IV: 6-12 hours. Duration may be prolonged in hepatic impairment due to reduced clearance. |
| Action Class | Proton pump inhibitors |
| Brand Substitutes | Kemopraz 20mg Capsule, Omee Capsule, Omecip Capsule, Omesec 20 Capsule, Rizole 40mg Capsule, Promisec 40mg Capsule, Estom 40mg Capsule, Zolcer 40mg Capsule, Ozol 40mg Capsule |
5 mg orally once daily.
| Dosage form | SOLUTION |
| Renal impairment | GFR 30-89 mL/min: no adjustment; GFR <30 mL/min: not recommended. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose to 2.5 mg once daily; Child-Pugh C: not recommended. |
| Pediatric use | Not established; use not recommended in patients <18 years. |
| Geriatric use | Initiate at 2.5 mg once daily; titrate based on tolerability. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for XROMI (XROMI).
| Breastfeeding | XROMI is excreted into human milk; M/P ratio is 1.2. Potential for serious adverse reactions in nursing infants, including renal impairment and electrolyte disturbances. Breastfeeding is not recommended during therapy and for 1 week after last dose. |
| Teratogenic Risk | XROMI is contraindicated in pregnancy. First trimester: Major congenital malformations including neural tube defects and cardiac anomalies. Second and third trimesters: Fetal growth restriction, oligohydramnios, neonatal nephrotoxicity, and persistent pulmonary hypertension. Risk is dose-dependent and increases with duration of exposure. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Hypersensitivity to XROMI or any component of the formulation","Pregnancy"]
| Precautions | ["Embryo-fetal toxicity: Can cause fetal harm; advise females of reproductive potential to use effective contraception.","Dyslipidemia: Monitor serum cholesterol levels during treatment.","Musculoskeletal pain: Arthralgia and myalgia common; manage symptomatically.","Hot flashes and night sweats: Common; manage symptomatically."] |
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| Fetal Monitoring | Monitor maternal renal function, serum electrolytes, and blood pressure weekly. Perform serial fetal ultrasounds for growth and amniotic fluid volume. Monitor for signs of fetal distress. After birth, monitor neonatal renal function and electrolytes. |
| Fertility Effects | XROMI may impair female fertility based on animal studies showing reduced implantation and increased pre- and post-implantation loss. Reversible upon discontinuation. Effects on male fertility unknown. |