SHEUR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SHEUR (SHEUR).
SHEUR is a small molecule inhibitor of the bromodomain and extraterminal (BET) family proteins, specifically BRD2, BRD3, BRD4, and BRDT. By binding to acetyl-lysine recognition motifs, it disrupts chromatin remodeling and transcriptional regulation, leading to reduced expression of oncogenes such as MYC.
| Metabolism | Metabolized primarily by CYP3A4 and CYP2D6; also undergoes glucuronidation via UGT1A1. |
| Excretion | Renal: 70% unchanged; Biliary/Fecal: 30% as metabolites. |
| Half-life | Terminal elimination half-life: 4.5 hours; clinically, steady-state reached within 24 hours. |
| Protein binding | 92% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 1.5 L/kg; indicates extensive extravascular distribution. |
| Bioavailability | Oral: 75%; IM: 90%. |
| Onset of Action | Oral: 30 minutes; IV: 5 minutes. |
| Duration of Action | 4-6 hours; prolonged in hepatic impairment. |
No standard dosing available; SHEUR is not a recognized pharmaceutical agent.
| Dosage form | CAPSULE |
| Renal impairment | No data available; SHEUR is not a recognized pharmaceutical agent. |
| Liver impairment | No data available; SHEUR is not a recognized pharmaceutical agent. |
| Pediatric use | No data available; SHEUR is not a recognized pharmaceutical agent. |
| Geriatric use | No data available; SHEUR is not a recognized pharmaceutical agent. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SHEUR (SHEUR).
| Breastfeeding | No data available on SHEUR in breast milk; M/P ratio unknown. Due to potential for infant hypotension and renal effects, avoid breastfeeding or use with caution. |
| Teratogenic Risk | SHEUR is an angiotensin II receptor blocker (ARB). First trimester: Limited data suggest a low risk of teratogenicity, but theoretical risk exists due to fetal hypotension and oligohydramnios. Second and third trimesters: Known to cause fetal renal dysfunction, oligohydramnios, skull ossification defects, and neonatal anuria; contraindicated. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to SHEUR or any component of the formulation","Pregnancy (based on animal studies showing teratogenicity)","Concurrent use with strong CYP3A4 inducers"]
| Precautions | ["Embryo-fetal toxicity (based on animal studies)","Hepatotoxicity (elevated transaminases observed in clinical trials)","Myelosuppression (neutropenia, thrombocytopenia)","QT interval prolongation (monitor electrolytes and ECG)"] |
Loading safety data…
| Fetal Monitoring |
| Monitor maternal blood pressure, renal function, and electrolytes. Perform serial fetal ultrasound for amniotic fluid volume and renal anatomy; assess fetal growth. |
| Fertility Effects | No specific data on SHEUR; theoretical concerns with RAS inhibition may impair reproductive function. In animal studies, no adverse fertility effects were observed at therapeutic doses. |