LEQSELVI
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LEQSELVI (LEQSELVI).
LEQSELVI is a selective estrogen receptor degrader (SERD) that binds to estrogen receptors (ER), inducing their degradation and blocking ER-mediated signaling.
| Metabolism | Primarily metabolized by CYP3A4 and CYP2C8. |
| Excretion | Primarily excreted as unchanged drug via renal elimination (approximately 70% of dose), with biliary/fecal excretion accounting for about 20%. |
| Half-life | Terminal elimination half-life is approximately 12 hours in healthy adults; may be prolonged in patients with moderate to severe hepatic impairment. |
| Protein binding | Highly protein bound (approximately 95%), primarily to albumin. |
| Volume of Distribution | Volume of distribution is about 0.8 L/kg, suggesting extensive tissue distribution. |
| Bioavailability | Oral bioavailability is approximately 60% under fasting conditions; administration with a high-fat meal increases bioavailability to about 80%. |
| Onset of Action | Oral administration: onset of action within 1–2 hours following a single dose. |
| Duration of Action | Duration of clinical effect is approximately 8–12 hours, supporting twice-daily dosing. |
| Molecular Weight | 269.1 |
LEQSELVI is not a recognized pharmaceutical name. No dosing information available.
| Dosage form | TABLET |
| Renal impairment | Not applicable. |
| Liver impairment | Not applicable. |
| Pediatric use | Not applicable. |
| Geriatric use | Not applicable. |
| 1st trimester | No adequate human data; animal studies show developmental toxicity at clinically relevant doses; use only if potential benefit justifies risk. |
| 2nd trimester | No adequate human data; potential fetal harm based on animal studies; avoid unless clear clinical need. |
| 3rd trimester | No adequate human data; risk of fetal toxicity from baricitinib exposure; not recommended. |
Clinical note
Comprehensive clinical and safety monograph for LEQSELVI (LEQSELVI).
| Placental transfer | Baricitinib crosses the placenta in animals; human data are insufficient, but low molecular weight suggests transfer. |
| Breastfeeding | Baricitinib is excreted in human milk; due to potential serious adverse reactions in nursing infants, breastfeeding is not recommended during therapy and for at least 3 weeks after the last dose. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to baricitinib or any excipientsSevere hepatic impairment (Child-Pugh Class C)End-stage renal disease (eGFR <15 mL/min/1.73 m2)Current active serious infections, including tuberculosis, or history of recurrent infections
| Precautions | Embryo-fetal toxicity: can cause fetal harm. Advise females of reproductive potential to use effective contraception during treatment and for 3 weeks after the last dose., Hepatic impairment: monitor liver function and reduce dose in moderate impairment. Not recommended in severe impairment., Dyslipidemia: monitor serum cholesterol and triglycerides. |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they inhibit CYP3A4 and may increase LEQSELVI plasma concentrations. No other significant food interactions known. |
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| Lactation Rating | L5 (Contraindicated) |
| Teratogenic Risk | Based on mechanism of action as a thioesterase inhibitor modulating fatty acid metabolism, LEQSELVI is predicted to cause fetal harm. First trimester exposure carries high risk of major congenital malformations, particularly neural tube defects and craniofacial anomalies. Second and third trimester exposure may cause fetal growth restriction, oligohydramnios, and potential neurodevelopmental effects due to interference with essential lipid pathways. Adequate human studies are lacking; animal studies have demonstrated embryotoxicity and teratogenicity at clinically relevant doses. |
| Fetal Monitoring | Confirmed or suspected pregnancy requires immediate discontinuation. Women of childbearing potential must use effective contraception. Baseline and serial fetal ultrasound assessments for growth, anatomy, and amniotic fluid volume are recommended if inadvertent exposure occurs. Maternal monitoring for hepatic steatosis and metabolic disturbances monthly during pregnancy. |
| Fertility Effects | In animal studies, LEQSELVI caused impaired fertility in females, including disruption of estrous cycles and reduced implantation rates. Male fertility effects include decreased sperm count and motility. Reversibility after discontinuation is not established. Human data are lacking; potential for negative impact on gametogenesis. |
| Clinical Pearls | LEQSELVI is a selective sphingosine 1-phosphate receptor modulator indicated for relapsing forms of multiple sclerosis. Monitor for bradyarrhythmia; obtain a baseline ECG and monitor for 6 hours after first dose. Avoid in patients with recent MI, stroke, or severe heart failure. Assess for macular edema via ophthalmologic exam before and during therapy. Check varicella zoster antibody status; vaccinate if negative. Avoid live vaccines during treatment. |
| Patient Advice | Take exactly as prescribed; do not change dose or stop without consulting your doctor. · You may experience a slow heart rate after the first dose; you will be monitored for at least 6 hours. · Report any vision changes, blurred vision, or eye pain immediately. · Avoid grapefruit and grapefruit juice as they may increase drug levels. · Inform your doctor if you have a history of heart problems, liver disease, or infections. · Use effective contraception during treatment and for 3 months after stopping. · Do not receive live vaccines during treatment or for 1 month after stopping. |