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Terlipressin Sale

(Synonyms: 特利加压素) 目录号 : GC32463

A prodrug form of lysipressin

Terlipressin Chemical Structure

Cas No.:14636-12-5

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10mM (in 1mL DMSO)
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5mg
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10mg
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50mg
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100mg
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产品描述

Terlipressin is a prodrug form of the vasopressin peptide lysipressin and a partial agonist of the vasopressin V1A receptor (Ki = 0.85 ?M).1 It is also an agonist of vasopressin V1B and V2 receptors (Kis = 1.11 and 1.58 ?M, respectively). It increases mean arterial pressure (MAP) and decreases mortality in a rat model of uncontrolled hemorrhagic shock when administered at a dose of 15 ?g/kg.2 Terlipressin (2.6 ?g/kg per hour), in combination with norepinephrine, improves vascular reactivity and increases survival time in a rat model of cecal ligation and puncture-induced septic shock and a rabbit model of LPS-induced septic shock.3 It also increases MAP in a rat model of liver cirrhosis with portal hypertension, arterial hypotension, high cardiac output, and low systemic vascular resistance.4

1.Colson, P.H., Virsolvy, A., Gaudard, P., et al.Terlipressin, a vasoactive prodrug recommended in hepatorenal syndrome, is an agonist of human V1, V2 and V1B receptors: Implications for its safety profilePharmacol. Res.113(Pt A)257-264(2016) 2.Lee, C.C., Lee, M.T., Chang, S.S., et al.A comparison of vasopressin, terlipressin, and lactated ringers for resuscitation of uncontrolled hemorrhagic shock in an animal modelPLoS One9(4)e95821(2014) 3.Xiao, X., Zhu, Y., Zhen, D., et al.Beneficial and side effects of arginine vasopressin and terlipressin for septic shockJ. Surg. Res.195(2)568-579(2015) 4.Fernández-Varo, G., Oró, D., Cable, E.E., et al.Vasopressin 1a receptor partial agonism increases sodium excretion and reduces portal hypertension and ascites in cirrhotic ratsHepatology63(1)207-216(2016)

Chemical Properties

Cas No. 14636-12-5 SDF
别名 特利加压素
Canonical SMILES Gly-Gly-Gly-Cys-Tyr-Phe-Gln-Asn-Cys-Pro-Lys-Gly-NH2 (Disulfide bridge: Cys4-Cys9)
分子式 C52H74N16O15S2 分子量 1227.37
溶解度 DMSO : ≥ 12.3 mg/mL (10.02 mM) 储存条件 Store at -20°C
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1 mM 0.8148 mL 4.0738 mL 8.1475 mL
5 mM 0.163 mL 0.8148 mL 1.6295 mL
10 mM 0.0815 mL 0.4074 mL 0.8148 mL
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Research Update

Terlipressin plus Albumin for the Treatment of Type 1 Hepatorenal Syndrome

N Engl J Med 2021 Mar 4;384(9):818-828.PMID:33657294DOI:10.1056/NEJMoa2008290.

Background: The vasoconstrictor Terlipressin is used for type 1 hepatorenal syndrome (HRS-1) in many parts of the world and is part of the clinical practice guidelines in Europe. Methods: We conducted a phase 3 trial to confirm the efficacy and safety of Terlipressin plus albumin in adults with HRS-1. The patients were randomly assigned in a 2:1 ratio to receive Terlipressin or placebo for up to 14 days; in both groups, concomitant use of albumin was strongly recommended. The primary end point was verified reversal of HRS, defined as two consecutive serum creatinine measurements of 1.5 mg per deciliter or less at least 2 hours apart and survival without renal-replacement therapy for at least 10 days after the completion of treatment. Four prespecified secondary end points were analyzed with the Hochberg procedure to account for multiple comparisons. Results: A total of 300 patients underwent randomization - 199 were assigned to the Terlipressin group and 101 to the placebo group. Verified reversal of HRS was reported in 63 patients (32%) in the Terlipressin group and 17 patients (17%) in the placebo group (P = 0.006). With respect to the prespecified secondary end points, HRS reversal, defined as any serum creatinine level of 1.5 mg per deciliter or less during the first 14 days, was reported in 78 patients (39%) in the Terlipressin group and 18 (18%) in the placebo group (P<0.001); HRS reversal without renal-replacement therapy by day 30, in 68 (34%) and 17 (17%), respectively (P = 0.001); HRS reversal among patients with systemic inflammatory response syndrome (84 patients in the Terlipressin group and 48 patients in the placebo group), in 31 (37%) and 3 (6%), respectively (P<0.001); and verified reversal of HRS without recurrence by day 30, in 52 (26%) and 17 (17%), respectively (P = 0.08). At day 90, liver transplantations had been performed in 46 patients (23%) in the Terlipressin group and 29 patients (29%) in the placebo group, and death occurred in 101 (51%) and 45 (45%), respectively. More adverse events, including abdominal pain, nausea, diarrhea, and respiratory failure, occurred with Terlipressin than with placebo. Death within 90 days due to respiratory disorders occurred in 22 patients (11%) in the Terlipressin group and 2 patients (2%) in the placebo group. Conclusions: In this trial involving adults with cirrhosis and HRS-1, Terlipressin was more effective than placebo in improving renal function but was associated with serious adverse events, including respiratory failure. (Funded by Mallinckrodt Pharmaceuticals; CONFIRM ClinicalTrials.gov number, NCT02770716.).

Terlipressin in the treatment of hepatorenal syndrome: A systematic review and meta-analysis

Medicine (Baltimore) 2018 Apr;97(16):e0431.PMID:29668606DOI:10.1097/MD.0000000000010431.

Background: Hepatorenal syndrome is a fatal complication of advanced cirrhosis. Terlipressin is the most widely used treatment method, however, the therapy effects remain inconsonant. We aim to systematically assess the safety and efficacy of Terlipressin for hepatorenal syndrome. Methods: We conducted a systematic review and meta-analysis. Randomized controlled trials involving Terlipressin for hepatorenal syndrome were included in a systematic literature search. Two authors independently assessed the studies for inclusion and extracted the data. A meta-analysis was conducted to estimate the safety and efficacy of Terlipressin for hepatorenal syndrome. Results: A total of 18 randomized controlled trials including 1011 patients were included. Hepatorenal syndrome reverse rate was 42.0% in the Terlipressin group and 26.2% in the non-terlipressin group. Terlipressin had greater hepatorenal syndrome reverse rate and renal function improvement rate than placebo and octreotide in the management of HRS. Comparing to norepinephrine, Terlipressin had similar efficacy, but with more adverse events. No significant difference of the efficacy was found between Terlipressin and dopamine treatment. The subgroup analysis for type 1 HRS had the above same results, except that the adverse events were not significant different between norepinephrine group and Terlipressin group. Conclusions: Terlipressin was superior to placebo and octreotide for reversal of hepatorenal syndrome and improving renal function, but it had no superiority comparing to norepinephrine.

Terlipressin and the Treatment of Hepatorenal Syndrome: How the CONFIRM Trial Moves the Story Forward

Am J Kidney Dis 2022 May;79(5):737-745.PMID:34606933DOI:10.1053/j.ajkd.2021.08.016.

Hepatorenal syndrome (HRS) is a form of acute kidney injury (AKI) occurring in patients with advanced cirrhosis and is associated with significant morbidity and mortality. The pathophysiology underlying HRS begins with increasing portal pressures leading to the release of vasodilatory substances that result in pooling blood in the splanchnic system and a corresponding reduction in effective circulating volume. Compensatory activation of the sympathetic nervous system and the renin-angiotensin-aldosterone system and release of arginine vasopressin serve to defend mean arterial pressure but at the cost of severe constriction of the renal vasculature, leading to a progressive, often fulminant form of AKI. There are no approved treatments for HRS in the United States, but multiple countries, including much of Europe, use Terlipressin, a synthetic vasopressin analogue, as a first-line therapy. CONFIRM (A Multi-Center, Randomized, Placebo Controlled, Double-Blind Study to Confirm Efficacy and Safety of Terlipressin in Subjects With Hepatorenal Syndrome Type 1), the third randomized trial based in North America evaluating Terlipressin, met its primary end point of showing greater rates of HRS reversal in the Terlipressin arm. However, due to concerns about the apparent increased rates of respiratory adverse events and a lack of evidence for mortality benefit, Terlipressin was not approved by the Food and Drug Administration (FDA). We explore the history of regulatory approval for Terlipressin in the United States, examine the results from CONFIRM and the concerns they raised, and consider the future role of Terlipressin in this critical clinical area of continued unmet need.

Terlipressin Is Superior to Noradrenaline in the Management of Acute Kidney Injury in Acute on Chronic Liver Failure

Hepatology 2020 Feb;71(2):600-610.PMID:30076614DOI:10.1002/hep.30208.

Hepatorenal syndrome (HRS) carries a high short-term mortality in patients with cirrhosis and acute on chronic liver failure (ACLF). Terlipressin and noradrenaline are routinely used in cirrhosis with HRS and have been found to be equally effective. There are no data comparing the efficacy of Terlipressin with noradrenaline in ACLF patients with HRS. In an open-label, randomized controlled trial (RCT), consecutive patients with ACLF diagnosed with HRS acute kidney injury (AKI) were randomized to albumin with infusion of Terlipressin (2-12 mg/day; n = 60) or noradrenaline (0.5-3.0 mg/h; n = 60). Response to treatment, course of AKI, and outcome were studied. Baseline characteristics, including AKI stage and sepsis-related HRS-AKI, were comparable between groups. Compared to noradrenaline, Terlipressin achieved greater day 4 (26.1% vs. 11.7%; P = 0.03) and day 7 (41.7% vs. 20%; P = 0.01) response. Reversal of HRS was also better with Terlipressin (40% vs. 16.7%; P = 0.004), with a significant reduction in the requirement of renal replacement therapy (RRT; 56.6% vs. 80%; P = 0.006) and improved 28-day survival (48.3% vs. 20%; P = 0.001). Adverse events limiting use of drugs were higher with Terlipressin than noradrenaline (23.3% vs. 8.3%; P = 0.02), but were reversible. On multivariate analysis, high Model for End-Stage Liver Disease (MELD; odds ratio [OR], 1.10; confidence interval [CI] = 1.009-1.20; P = 0.03) and noradrenaline compared to Terlipressin (OR, 3.05; CI = 1.27-7.33; P = 0.01) predicted nonresponse to therapy. Use of noradrenaline compared to Terlipressin was also predictive of higher mortality (hazard ratio [HR], 2.08; CI = 1.32-3.30; P = 0.002). Conclusion: AKI in ACLF carries a high mortality. Infusion of Terlipressin gives earlier and higher response than noradrenaline, with improved survival in ACLF patients with HRS-AKI.

Role of Terlipressin and Albumin for Hepatorenal Syndrome in Liver Transplantation

Liver Transpl 2020 Oct;26(10):1328-1336.PMID:32574418DOI:10.1002/lt.25834.

Hepatorenal syndrome (HRS) is one of the most ominous complications of portal hypertension in patients with decompensated cirrhosis and ascites. It is associated with very high mortality on the wait list. Liver transplantation (LT) is the most successful therapeutic option for patients with HRS. However, not all the LT candidates with HRS are able to receive a deceased donor allograft in a timely manner because it is a scarce resource and patients may need alternative best supportive treatment with systemic splanchnic vasoconstrictors and albumin as a bridge to transplant. The combination of Terlipressin and albumin is efficacious in the reversal of HRS and is used worldwide. More recently, the multicenter, randomized, placebo-controlled double-blind study to confirm efficacy and safety of Terlipressin in subjects with hepatorenal syndrome type 1 (the CONFIRM study) trial demonstrated the efficacy of Terlipressin and albumin in the reversal of HRS in a North American cohort. The aim of this article is to review the role of Terlipressin and albumin in LT candidates with HRS in the United States.