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Taribavirin Sale

目录号 : GC37740

Taribavirin 是一种肌苷一磷酸脱氢酶抑制剂,具有抗多种病毒的活性,特别是丙型肝炎病毒和流感病毒。Taribavirin 是一种利巴韦林前药,旨在集中在肝脏内以靶向 HCV 感染的肝细胞,同时最小化红细胞 (RBC) 内的分布和溶血性贫血的发展。

Taribavirin Chemical Structure

Cas No.:119567-79-2

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产品描述

Taribavirin is an inosine monophosphate dehydrogenase inhibitor, has activity against a wide range of viruses, especially the hepatitis C virus and influenza virus[1].Taribavirin, is a ribavirin prodrug, is designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the development of hemolytic anemia[2].

Taribavirin (0-2 μM; 24 hours) significantly induces MCF-7 cell death, recording half inhibitory effect (IC50) of 0.756 μM in MCF-7 cells[1]. Cell Viability Assay[1] Cell Line: MCF-7 cells

[1]. Abd-Rabou AA, et al. Taribavirin and 5-Fluorouracil-Loaded Pegylated-Lipid Nanoparticle Synthesis, p38 Docking, and Antiproliferative Effects on MCF-7 Breast Cancer. Pharm Res. 2018 Feb 27;35(4):76. [2]. Deming P, et al. Taribavirin in the treatment of hepatitis C. Expert Opin Investig Drugs. 2011 Oct;20(10):1435-43.

Chemical Properties

Cas No. 119567-79-2 SDF
Canonical SMILES N=C(C1=NN([C@H]2[C@@H]([C@@H]([C@@H](CO)O2)O)O)C=N1)N
分子式 C8H13N5O4 分子量 243.22
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 4.1115 mL 20.5575 mL 41.115 mL
5 mM 0.8223 mL 4.1115 mL 8.223 mL
10 mM 0.4112 mL 2.0558 mL 4.1115 mL
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Research Update

Taribavirin in the treatment of hepatitis C

Expert Opin Investig Drugs 2011 Oct;20(10):1435-43.PMID:21854301DOI:10.1517/13543784.2011.606214.

Introduction: Treatment of chronic hepatitis C virus (HCV) is limited by substantial side effects including ribavirin-induced hemolytic anemia. Taribavirin, a ribavirin prodrug, was designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the subsequent development of hemolytic anemia. Areas covered: The objective of the review is to evaluate the efficacy and safety of Taribavirin as compared with ribavirin in the treatment of chronic HCV infections. A PubMed search was performed using the following key words: viramidine, Taribavirin and ribavirin analog. Additional sources included press releases on preliminary results of clinical trials of Taribavirin and abstracts presented at international meetings. The literature suggests that weight-based dosing of Taribavirin at 25 mg/kg demonstrates lower rates of hemolytic anemia with comparable rates of sustained virologic response (SVR) and is the optimum dose for further studies comparing the efficacy of Taribavirin with weight-based dosing of ribavirin. Expert opinion: Failure to eradicate HCV may be associated with extrahepatic viral replication. The dosing strategy of Taribavirin favors concentration within the liver to reduce treatment-limiting rates of anemia but may be insufficient to prevent virologic relapse.

Taribavirin for the treatment of chronic hepatitis C

Expert Opin Pharmacother 2008 Dec;9(18):3243-9.PMID:19040344DOI:10.1517/14656560802594459.

Background: The current standard therapy for chronic hepatitis C virus (HCV), combination therapy with pegylated interferon and ribavirin, is plagued by a number of side effects, most notably anemia. This anemia is typically managed with a reduction of ribavirin dosing, which may lead to reduced efficacy. Taribavirin, an oral prodrug of ribavirin, which has been shown to induce a lesser degree of anemia, is being investigated for the treatment of chronic HCV. Objective: To summarize the clinical trials involving Taribavirin and its potential role in the treatment of chronic HCV. Methods: Information was obtained via searches for data related to Taribavirin, as well as other current and investigational therapies for chronic HCV. Press releases discussing otherwise unpublished trial outcomes were obtained from the website of Valeant Pharmaceuticals, the producer of Viramidine (Taribavirin). Conclusion: Taribavirin may increase adherence to therapy for chronic HCV by reducing the need for dose reduction due to anemia. A recent Phase II trial investigating early and sustained virological response showed no statistically significant differences between ribavirin 1000/1200 mg and Taribavirin at 800-, 1200-, or 1600-mg dosing, while illustrating a lesser degree of anemia in 800- and 1200-mg dosing of Taribavirin. Ongoing studies will continue to examine the efficacy of combination therapy with Taribavirin in the place of ribavirin.

Taribavirin and 5-Fluorouracil-Loaded Pegylated-Lipid Nanoparticle Synthesis, p38 Docking, and Antiproliferative Effects on MCF-7 Breast Cancer

Pharm Res 2018 Feb 27;35(4):76.PMID:29488022DOI:10.1007/s11095-017-2283-3.

Purpose: Breast cancer is the second most common cause of mortality in women in the United States. Targeted delivery of antitumor breast cancer drugs as a drug-delivery strategy may allow direct delivery into the tumor. Currently, chemotherapy is one of the principle strategies for cancer treatment, but it can have toxic side effects. Nanotechnology attempts to resolve these challenges by loading drugs in nanoparticles, such as solid lipid nanoparticles (SLN). In response to the breast cancer drug 5-fluorouracil (5-FU), p38MAPK signaling has been investigated since the 1990s. Ribavirin, a nucleotide derivative, inhibits p38MAPK in infected hepatocytes. A ribavirin prodrug, Taribavirin (TBV), was recently synthesized to concentrate in the liver and have minimal concentration in red blood cells. Methods: In this study, TBV and 5-FU-pegylated SLNs were prepared and characterized. The in vitro cytotoxicity was evaluated against MCF-7 breast cancer cells. Using molecular docking experiments, 5-FU and TBV were docked on p38MAPK protein. Results: The TBV nanoformulation had the highest cytotoxic effects, achieving IC50 = 0.690 μM after 24 h, compared with free TBV, which also achieved a good cytotoxic effect (IC50 = 0.756 μM). However, there was a detectable cytotoxic effect and an undetectable IC50 of 5-FU nanoparticles and free 5-FU on MCF-7 cells. Conclusions: The effect of TBV nanoparticles on MCF-7 cells may be due to its inhibitory effect against p38MAPK protein, where it fits inside the active pocket site of the p38 protein molecular surface, with a minimum binding affinity of -5.5 kcal/mol (rmsd of 1.07), and it formed strong hydrogen bonds with amino acids ASP'168, ILE'166, HIS'148, and ILE'147. Further studies are warranted to investigate the mechanistic details of the proposed approach.

Ribavirin analogs

Clin Liver Dis 2009 Aug;13(3):419-27.PMID:19628158DOI:10.1016/j.cld.2009.05.006.

Ribavirin is ineffective against hepatitis C virus as mono-therapy but is critical in attaining both early virologic response and sustained virologic response when combined with pegylated interferon. Ribavirin has significant dose-limiting toxicities, the most important of which is hemolytic anemia. Taribavirin is a ribavirin pro-drug, which targets the liver and has less incidence of anemia, and it may be a promising alternative to ribavirin in the future.

Virological response and safety outcomes in therapy-nai ve patients treated for chronic hepatitis C with Taribavirin or ribavirin in combination with pegylated interferon alfa-2a: a randomized, phase 2 study

J Hepatol 2007 Jul;47(1):51-9.PMID:17470380DOI:10.1016/j.jhep.2007.02.018.

Background/aims: Pegylated interferon plus ribavirin can cause dose-limiting anemia. Taribavirin, a ribavirin prodrug, has shown a lower incidence of anemia. We sought to determine the efficacy and safety of Taribavirin vs. ribavirin combined with pegylated interferon in patients with chronic hepatitis C (CHC). Methods: This phase 2 open-label study randomized 180 patients with CHC to receive pegylated interferon alfa-2a 180 microg/week plus Taribavirin 800, 1200 or 1600 mg QD or ribavirin 1000 or 1200 mg QD. Efficacy variables included proportions of patients with undetectable serum HCV RNA levels at end of treatment and after a 24-week follow-up. Results: The proportions of patients with undetectable HCV RNA at 12 weeks did not differ significantly between Taribavirin (38%, 42%, and 49% for the 800, 1200, and 1600 mg groups) and ribavirin (49%). The highest proportion of patients with undetectable HCV RNA at end of treatment and at follow-up occurred in both the Taribavirin 1200mg QD (63% and 37%) and ribavirin groups (62% and 44%). SVR rates were 23%, 37% and 29% for Taribavirin and 44% for ribavirin. Fewer patients on any dose of Taribavirin had severe anemia (hemoglobin <10 g/dL) than on ribavirin (6/135 [4%] vs. 12/45 [27%]). Conclusions: Given with interferon, Taribavirin produced SVR rates comparable to those of ribavirin, with a lower occurrence of anemia.