YUTREPIA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for YUTREPIA (YUTREPIA).
YUTREPIA (treprostinil) is a prostacyclin analog that directly vasodilates pulmonary and systemic arterial beds and inhibits platelet aggregation. It binds to prostacyclin receptor (IP receptor), increasing cAMP in vascular smooth muscle cells, leading to vasodilation.
| Metabolism | Primarily hepatic metabolism via cytochrome P450 (CYP) 2C8 and, to a lesser extent, CYP2C9. Treprostinil is extensively metabolized to inactive metabolites. |
| Excretion | Renal: 80% as unchanged drug; fecal: 15% as metabolites; biliary: <5%. |
| Half-life | Terminal elimination half-life: 12-15 hours (range 11-18 h) in adults; prolonged in renal impairment (CrCl <30 mL/min: up to 30 h). |
| Protein binding | 98% bound to albumin (primarily) and alpha-1-acid glycoprotein. |
| Volume of Distribution | 1.2-1.5 L/kg (total body water). Indicates extensive tissue distribution. |
| Bioavailability | Oral: 70-80% (first-pass metabolism reduces from ~90% absorbed). |
| Onset of Action | Oral: 30-45 minutes; IV: 5-10 minutes. |
| Duration of Action | Oral: 6-8 hours; IV: 4-6 hours. Clinical effects may persist longer due to active metabolite. |
| Molecular Weight | 141850 |
0.6 mg/kg intravenously over 15 minutes every 3 weeks until disease progression or unacceptable toxicity.
| Dosage form | POWDER |
| Renal impairment | No dose adjustment recommended for mild to moderate renal impairment (CrCl ≥30 mL/min). For severe renal impairment (CrCl <30 mL/min) or end-stage renal disease, data not available; use with caution. |
| Liver impairment | No dose adjustment recommended for mild hepatic impairment (Child-Pugh A). For moderate or severe hepatic impairment (Child-Pugh B or C), not studied; use with caution. |
| Pediatric use | Safety and efficacy not established in pediatric patients; no recommended dose. |
| Geriatric use | No specific dose adjustment recommended; however, elderly patients may have increased sensitivity. Monitor renal function and overall status. |
| 1st trimester | No adequate human data; animal studies show no risk. Use only if clearly needed. |
| 2nd trimester | No known teratogenic risk; limited human data. Use only if potential benefit justifies risk. |
| 3rd trimester | Avoid near term due to potential uterine relaxation and risk of postpartum hemorrhage. |
Clinical note
Comprehensive clinical and safety monograph for YUTREPIA (YUTREPIA).
| Placental transfer | Minimal due to high molecular weight; active transport by P-glycoprotein. Low transplacental transfer expected. |
| Breastfeeding | Excretion into human milk unknown; due to high molecular weight, unlikely to reach significant levels in infant. Caution if breastfeeding. |
| Lactation Rating |
■ FDA Black Box Warning
YUTREPIA must be administered via continuous infusion (subcutaneous or intravenous) using an infusion pump. Abrupt withdrawal or sudden dose reduction may lead to worsening of pulmonary hypertension, which may be fatal. The infusion device must be carefully monitored to avoid delivery interruptions.
| Serious Effects |
Hypersensitivity to treprostinil or any componentSevere hepatic impairment (Child-Pugh class C)
| Precautions | Risk of infection due to intravenous catheter use; chronic intravenous infusions may be associated with bloodstream infections and sepsis. Subcutaneous infusion site reactions (pain, erythema, induration) are common. Patients with hepatic impairment require dose adjustment. Patients with concurrent use of anticoagulants or antiplatelet agents may have increased bleeding risk. Monitor for signs of pulmonary edema if used in patients with pulmonary veno-occlusive disease. |
| Food/Dietary | No specific food interactions have been reported. Maintain a balanced diet; avoid grapefruit juice as it may theoretically affect CYP2C8 metabolism of treprostinil, though clinical significance is unknown. |
Loading safety data…
| L3 - Moderate Risk |
| Teratogenic Risk | YUTREPIA (treprostinil) is a prostacyclin analog. Based on animal studies and limited human data, treprostinil is not expected to increase the risk of major birth defects. However, due to its vasodilatory effects, there is a potential for reduced uterine blood flow, which could theoretically affect fetal growth. No trimester-specific risks have been identified in humans; the drug should be used during pregnancy only if clearly needed. |
| Fetal Monitoring | Maternal: Monitor blood pressure, heart rate, and signs of bleeding (treprostinil inhibits platelet aggregation). Fetal: Standard prenatal monitoring including ultrasound for fetal growth and amniotic fluid volume, as vasodilation may affect placental perfusion. Frequent fetal heart rate monitoring should be considered in pregnant women on treprostinil. |
| Fertility Effects | In animal studies, treprostinil did not impair fertility at doses up to 25 times the human exposure. No human data are available. There is no known effect on human fertility; however, underlying pulmonary arterial hypertension may itself impact fertility. |
| Clinical Pearls | YUTREPIA (treprostinil) is a prostacyclin analogue administered via subcutaneous infusion. Monitor infusion site reactions closely; rotate sites every 3 days to minimize pain and erythema. Dose titration should be based on clinical response and tolerability; abrupt discontinuation may cause rebound pulmonary hypertension. Use with caution in patients with hepatic impairment due to reduced clearance. Inhaled treprostinil is available for pulmonary arterial hypertension (PAH) maintenance therapy. |
| Patient Advice | YUTREPIA is given as a continuous infusion under the skin; do not stop suddenly without talking to your doctor. · Rotate infusion sites every 3 days to reduce skin reactions. Report signs of infection, severe pain, or bruising at the site. · Common side effects include headache, nausea, and jaw pain. These may improve with dose adjustments. · Carry an emergency supply of medication and spare infusion sets when traveling. · Do not mix YUTREPIA with other medications in the infusion pump unless instructed by your healthcare provider. |