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epoprostenol (Caripul)

✓ Approved

Actelion · PTGIR · 小分子

什么是 epoprostenol？

epoprostenol 是一种小分子，由Actelion研发。该药已获批，用于治疗相关适应症，给药途径：Injectable (Others)、Intravenous (IV)。

药物档案

商品名Caripul
公司Actelion
药物类别小分子
分子靶点PTGIR
给药途径Injectable (Others), Intravenous (IV)
状态Approved
来源： ClinicalTrials.gov, Actelion

作用机制

分子靶点

epoprostenol 作用于 1 个分子靶点：

PTGIRprostaglandin I2 receptor (IP, PRIPR)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

epoprostenol 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Respiratory, thoracic and mediastinal disordersPulmonary hypertension✓ Approved

相关研究文献

PubMedJournal of medicinal chemistry2026-07-27

Synthesis, Modeling, and Biological Properties of Fluoroprostacyclin Analogues: Potent Agonists for Prostanoid Receptors.

Jing Changcheng C, Perez-Powell Isabel I, Baars Hannah H, Mallah Shahida S et al.

Prostacyclin (PGI2, epoprostenol) and its more stable analogues iloprost and cicaprost are used in the treatment of pulmonary arterial hypertension (PAH) and other related diseases. Currently, PGI2 therapy is the most effective treatment for PAH, but is administered intravenously due to its instability under physiological conditions. We considered creating more chemically stable hybrids of PGI2 by merging essential features of iloprost/cicaprost with a more stable C-7 fluorinated PGI2, which maintained the cyclic enol ether. The synthesis employed our key bicyclic enal and furnished the required PGI2 analogues in just 7-8 steps, providing the most expedient route to this class of molecules. This led to the discovery of compound 9, a picomolar-potent, IP receptor-selective, and chemically stable PGI2 analogue that combined the ω-side chain of cicaprost with the C-7 difluorinated enol ether of PGI2. This compound provides the most potent PGI2 analogue tested to date.

PMID 42503823
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PubMedFrontiers in pharmacology2026-07-23

Pharmacovigilance assessment of gout: a real-world study using the FAERS database.

Ren Honghao H, Yao Nannan N, Ren Xiaodong X, Su Yani Y et al.

Drug intervention is a key method for preventing gout, various drugs have been implicated as potential risk factors in individual studies. This study aims to comprehensively identify drugs linked to the development of gout. Data were obtained from the FDA Adverse Event Reporting System (FAERS), and disproportionality analysis was employed to quantitatively assess the associations between drugs and gout. Four complementary signal detection methods-Reporting Odds Ratio (ROR), Proportional Reporting Ratio (PRR), Bayesian Confidence Propagation Neural Network (BCPNN), and Multi-item Gamma Poisson Shrinker (MGPS)-were utilized. To further delineate exposure-outcome relationships and identify influential predictors, least absolute shrinkage and selection operator (LASSO) logistic regression was implemented. Time-to-onset (TTO) analysis was conducted to examine the temporal dynamics between drug initiation and the occurrence of gout. Finally, a comprehensive assessment of the therapeutic indications of the drugs was performed. A total of 35 drugs were ultimately identified as potentially associated with the onset and progression of gout. Among these, several agents have been previously reported in the literature as having possible links to gout development. In addition, a number of novel candidates were detected for which evidence of an association with gout remains limited or has not been clearly established. These include Lenalidomide, Sacubitril valsartan, Ruxolitinib, Treprostinil, Octreotide, Selexipag, Rosuvastatin, Sitagliptin, Riociguat, Epoprostenol, Patiromer, Dasabuvir ombitasvir paritaprevir ritonavir, Tafamidis, Sparsentan, and Iloprost. Furthermore, TTO analysis suggested that approximately 75% of gout events occurred within 0.6 years following initiation of therapy. These pharmacotherapeutic agents are employed across diverse clinical settings, encompassing haematological malignancies, cardiovascular diseases, and pulmonary hypertension. These findings suggest the potential for targeted monitoring of drug-associated gout in clinical practice. When administering these medications, it may be crucial to regularly assess patients' uric acid levels and maintain heightened awareness for the possible onset of gout.

PMID 42488563
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PubMedJournal of burn care & research : official publication of the American Burn Association2026-07-08

A Protocolized Intravenous Epoprostenol Pathway for Frostbite: A Canadian Burn Centre Quality Improvement and Implementation Report.

Natanson Rimona R, Adibfar Alex A, Au Anita A, Tillman Bourke B et al.

Severe frostbite is a dynamic microvascular injury that can progress to delayed tissue loss despite appropriate initial care. Contemporary management emphasizes rapid rewarming, antithromboxane therapy, clinical grading, selective thrombolysis, and prostacyclin-based treatment. Iloprost is the prostacyclin analogue most often described, but access may be delayed in some Canadian settings. We developed and implemented a monitored intravenous epoprostenol pathway for Cauchy grade 2 to 4 frostbite and retrospectively evaluated 23 patients treated between December 2017 and November 2025. The pathway incorporated rapid rewarming, grading, topical and systemic antithromboxane therapy, eligibility criteria, dose titration, physiologic monitoring, dose modification, multidisciplinary care, and follow-up. Overall, 153 of 216 affected digits were preserved. Preservation varied by severity: 62 of 65 grade 2 digits, 74 of 100 grade 3 digits, and 7 of 41 grade 4 digits were preserved. Twelve patients avoided amputation altogether. Mean treatment duration was 3.8 days, and most patients reached 8 ng/kg/min at least once. Documented adverse effects or dose-limiting symptoms occurred in nine patients and were managed with dose reduction or temporary interruption. Available records did not identify thrombolytic therapy, permanent discontinuation for adverse reaction or grade 2 reassessment, or serious drug-attributed adverse events. Protocol-guided intravenous epoprostenol was feasible and generally well tolerated. Findings should be interpreted as descriptive and hypothesis-generating rather than evidence of treatment efficacy.

PMID 42417809
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PubMedThe journal of vascular access2026-06-24

Outcomes of long-term central venous access devices in pulmonary arterial hypertension: A 10-year case series.

Gómez-Sandoval Juan J, Correa-Martinez Valeria V, Amaya-Nieto Javier J, Conde-Camacho Rafael R et al.

Continuous prostacyclin infusion is the standard of care for pulmonary arterial hypertension, requiring central venous access devices where dwell time is critical but associated with complications. Retrospective 10-year case series of 18 adult pulmonary arterial hypertension patients managed through central venous access devices by a specialized multidisciplinary team. Sixty-nine catheters were analyzed across 18 patients; median catheter survival estimated by the Kaplan-Meier method was 9.3 months (95% confidence interval (8.1-12)). Occlusion was the most frequent complication (1.20 per 1,000 catheter-days) and the leading removal reason across all device types. Catheter-related bloodstream infections occurred in four instances (0.22 per 1,000 catheter-days), with methicillin-susceptible Staphylococcus aureus as the only isolated pathogen. Catheter-related thrombosis was documented in two cases. Three catheters fractured, one of each device type. Evidence on central venous access device outcomes in pulmonary arterial hypertension remains scarce in middle-income countries. The median dwell time observed in this series was shorter than that reported in high-income country cohorts, while catheter-related bloodstream infection and thrombosis rates were numerically lower than those documented in comparable series. In this descriptive 10-year case series from a middle-income country, long-term central venous access devices for continuous epoprostenol infusion in pulmonary arterial hypertension were associated with a prolonged dwell time and low complication rates under a structured multidisciplinary follow-up model. Larger multicenter studies are needed to confirm generalizability and identify determinants of catheter longevity.

PMID 42338134
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PubMedRespiratory medicine case reports2026-06-19

Delayed-onset portopulmonary hypertension following liver transplantation with near hemodynamic normalization on triple therapy.

Abdullah Maie M, Roche Stephen S, Mwangi John J, Arnold Liam L

Portopulmonary hypertension (PoPH) is a distinct subtype of pulmonary arterial hypertension (PAH) occurring in the setting of portal hypertension. Although liver transplantation (LT) may relieve portal pressure, pulmonary vascular remodeling can persist or, rarely, develop de novo after transplantation, posing diagnostic and therapeutic challenges. Delayed-onset PoPH after LT remains poorly characterized, with limited data to guide recognition and management. We describe a case of a 67-year-old male who developed severe PoPH three years after orthotopic LT for end-stage liver disease secondary to alcohol use and metabolic dysfunction- associated steatotic liver disease (MASLD). He presented with hypoxic respiratory failure, dyspnea, and volume overload. Echocardiography and right-heart catheterization (RHC) confirmed severe precapillary pulmonary hypertension. Combination therapy with intravenous epoprostenol, macitentan, and sildenafil resulted in marked hemodynamic and clinical improvement. He was subsequently transitioned from intravenous epoprostenol to oral selexipag and has maintained near-normal pulmonary pressures for two years. This case highlights delayed post-LT PoPH and demonstrates that even late-presenting disease may achieve substantial hemodynamic improvement with aggressive, guideline-directed PAH therapy.

PMID 42317786
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PubMedThe International journal of artificial organs2026-06-17

Antithrombin and 20% albumin as treatment of oxygenator high pressures excursion during cardiopulmonary bypass in cardiac surgery: A case report.

Mandarano Raffaele R, Pedevilla Silvia S, Annese Flavia F, Pessetti Luca L et al.

High-pressure excursions (HPE) during cardiopulmonary bypass (CPB) are rare but potentially life-threatening events linked to coagulation activation, inflammation. Known risk factors include male sex, large body surface area (BSA), elevated hematocrit (Htc), prior stroke and urgent surgery. Recommended management follows a stepwise approach involving haemodilution, heparin and antithrombin (AT), albumin or epoprostenol depending on Htc and pressure thresholds. We report a 69-year-old man undergoing urgent complex cardiac surgery who developed rising pre-oxygenator pressures 10 min after CPB initiation. Despite initial haemodilution and AT, pressures improved only partially. Administration of 100 mL of 20% albumin led to rapid normalization of pre-oxygenator and delta pressures, allowing safe continuation of CPB. The postoperative course was uneventful. Subsequent review of the oxygenator transmembrane resistance (R) showed a progressive decline following the administration of AT and albumin. This case suggests that AT, administered alongside albumin, may reduce blood viscosity and improve oxygenator performance. Further research is needed to clarify mechanisms and standardize management of HPE during CPB.

PMID 42304810
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