ClevudineCAS# 163252-36-6 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 163252-36-6 | SDF | Download SDF |
| PubChem ID | 73115 | Appearance | Powder |
| Formula | C10H13FN2O5 | M.Wt | 260.22 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 50 mg/mL (192.15 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 1-[(2S,3R,4S,5S)-3-fluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione | ||
| SMILES | CC1=CN(C(=O)NC1=O)C2C(C(C(O2)CO)O)F | ||
| Standard InChIKey | GBBJCSTXCAQSSJ-XQXXSGGOSA-N | ||
| Standard InChI | InChI=1S/C10H13FN2O5/c1-4-2-13(10(17)12-8(4)16)9-6(11)7(15)5(3-14)18-9/h2,5-7,9,14-15H,3H2,1H3,(H,12,16,17)/t5-,6+,7-,9-/m0/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Clevudine is an antiviral drug for the treatment of hepatitis B.
Target: HBV
Clevudine is a nucleoside analog with an unnatural beta-L configuration. Clevudine showed potent antiviral activity during therapy and induced a sustained posttreatment antiviral effect for 6 months after a 12-week treatment period, and this was associated with a sustained normalization of ALT levels [1]. Clevudine showed a potent antiviral response, and its effect was higher in HBeAg-negative patients, with rapid viral load reduction after therapy. However, long-term therapy for more than 1 year resulted in the development of considerable resistance and myopathy. Therefore, we should consider alternative antiviral agents if clevudine resistance or clevudine-induced myopathy is developed in patients on clevudine for the treatment of CHB [2]. References: | |||||
Clevudine Dilution Calculator
Clevudine Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.8429 mL | 19.2145 mL | 38.429 mL | 76.858 mL | 96.0726 mL |
| 5 mM | 0.7686 mL | 3.8429 mL | 7.6858 mL | 15.3716 mL | 19.2145 mL |
| 10 mM | 0.3843 mL | 1.9215 mL | 3.8429 mL | 7.6858 mL | 9.6073 mL |
| 50 mM | 0.0769 mL | 0.3843 mL | 0.7686 mL | 1.5372 mL | 1.9215 mL |
| 100 mM | 0.0384 mL | 0.1921 mL | 0.3843 mL | 0.7686 mL | 0.9607 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Virological Response and Muscular Adverse Events during Long-Term Clevudine Therapy in Chronic Hepatitis B Patients.[Pubmed:23805155]
Hepat Mon. 2013 Apr 1;13(4):e6056.
BACKGROUND: Recently, several reports issued Clevudine induced myopathy in the long term use. OBJECTIVES: The aim of this study was to investigate antiviral effects and adverse events of Clevudine monotherapy in patients with chronic hepatitis B (CHB). PATIENTS AND METHODS: The subjects were 110 treatment-naive CHB patients. They were treated with 30 mg Clevudine/day for more than six months. Virological and biochemical tests, including that for serum creatine kinase (CK), were monitored at baseline and at 3-month intervals during treatment period. RESULTS: In HBeAg-positive patients, the cumulative rates of virological response were 74.0 %, 68.5 %, and 67.3 % after one, two, and three years of Clevudine treatment, respectively. Cumulative rates of HBeAg loss or seroconversion were 17.8 %, 30 %, and 31.5 % after one, two and, three years of Clevudine treatment, respectively. In HBeAg-negative patients, the cumulative rates of virological response were 97.3 %, 100 %, and 94.6 %, respectively. Virological breakthrough occurred in 27 patients. The rtM204I mutation in HBV polymerase was predominantly detected. Muscular adverse events were observed in 15 patients. All patients with myopathy recovered after the cessation of Clevudine monotherapy. Fluctuations in CK level during the Clevudine treatment period were frequently observed irrespective of development of myopathy. Multiple episodes of CK elevation were significantly related to the development of myopathy. CONCLUSIONS: Long-term Clevudine monotherapy is effective for suppression of serum HBV DNA level and normalization of serum alanine amino transaminase levels, but associated with occurrence of rtM204I mutation. Clevudine-induced muscular adverse events are not uncommon, although they are totally reversible after cessation of the treatment. Muscular adverse events and serum CK level should be carefully monitored during long-term treatment with Clevudine.
Noncompetitive inhibition of hepatitis B virus reverse transcriptase protein priming and DNA synthesis by the nucleoside analog clevudine.[Pubmed:23774432]
Antimicrob Agents Chemother. 2013 Sep;57(9):4181-9.
All currently approved antiviral drugs for the treatment of chronic hepatitis B virus (HBV) infection are nucleos(t)ide reverse transcriptase inhibitors (NRTI), which inhibit the DNA synthesis activity of the HBV polymerase. The polymerase is a unique reverse transcriptase (RT) that has a novel protein priming activity in which HP initiates viral DNA synthesis using itself as a protein primer. We have determined the ability of NRTI-triphosphates (TP) to inhibit HBV protein priming and their mechanisms of action. While entecavir-TP (a dGTP analog) inhibited protein priming initiated specifically with dGTP, Clevudine-TP (a TTP analog) was able to inhibit protein priming independently of the deoxynucleoside triphosphate (dNTP) substrate and without being incorporated into DNA. We next investigated the effect of NRTIs on the second stage of protein priming, wherein two dAMP nucleotides are added to the initial deoxyguanosine nucleotide. The obtained results indicated that Clevudine-TP as well as tenofovir DF-DP strongly inhibited the second stage of protein priming. Tenofovir DF-DP was incorporated into the viral DNA primer, whereas Clevudine-TP inhibited the second stage of priming without being incorporated. Finally, kinetic analyses using the HBV endogenous polymerase assay revealed that Clevudine-TP inhibited DNA chain elongation by HP in a noncompetitive manner. Thus, Clevudine-TP appears to have the unique ability to inhibit HBV RT via binding to and distorting the HP active site, sharing properties with both NRTIs and nonnucleoside RT inhibitors.
Management of Clevudine-Resistant Chronic Hepatitis B: A Multicenter Cohort Study.[Pubmed:27538443]
Gut Liver. 2017 Jan 15;11(1):129-135.
Background/Aims: Data are lacking regarding the management of chronic hepatitis B (CHB) with resistance to Clevudine (CLV). This study evaluated the efficacy of different rescue therapies for CLV-resistant CHB. Methods: Patients with CLV-resistant CHB were enrolled in the cohort, and all patients developed virologic breakthrough during CLV therapy and had confirmed-genotypic resistance to CLV (rtM204I mutation) before enrollment. Results: Of the 107 patients, 12 received adefovir (ADV), 21 received a CLV plus ADV combination (CLV+ADV), 34 received a lamivudine plus ADV combination (LAM+ADV), and 40 received entecavir (ETV) therapy for 48 weeks. The CLV+ADV group had the lowest hepatitis B virus (HBV) DNA level (p<0.0001) and showed the greatest reduction of HBV DNA levels from baseline compared to all other groups (p=0.004) at week 48. HBV DNA was undetectable (<70 IU/mL) in 0%, 57.1%, 21.2%, and 27.5% (p=0.003) of the patients in each group, respectively, at week 48. At the end of the study, the mean alanine transaminase (ALT) level, rate of ALT normalization, and rate of hepatitis B envelope antigen loss or seroconversion did not differ between groups. Conclusions: CLV+ADV combination therapy in patients with CLV-resistant CHB more effectively suppresses HBV replication than ETV, ADV, or LAM+ADV therapy.
A randomized, open-label study comparing low-dose clevudine plus adefovir combination therapy with clevudine monotherapy in naive chronic hepatitis B patients.[Pubmed:25101150]
Hepatol Int. 2014 May 25;8(3):375-81.
PURPOSE: Clevudine 30 mg showed potent antiviral activity with a marked post-treatment antiviral effect. However, long-term treatment with Clevudine monotherapy induced resistance and myopathy in some cases. The objective of this study is to evaluate the preliminary efficacy and safety of the combination of Clevudine 20 mg and adefovir compared to Clevudine monotherapy. METHODS: Seventy-four patients were randomized to either a combination of Clevudine 20 mg and adefovir or Clevudine 20 or 30 mg and were treated for 2 years. The viral kinetics for 24 weeks, virological response [VR; hepatitis B virus (HBV) DNA less than 300 copies/ml], and the biochemical response [BR; normal alanine aminotransferase (ALT)] were assessed. RESULTS: There was no difference in baseline characteristics among the three groups. Viral kinetics study showed no statistically significant difference among them during 24 weeks. The combination group showed 95 % virological response with a statistically significant difference compared to the Clevudine 30 mg (67 %) and 20 mg (71 %) groups (p = 0.0376). Biochemical response rates were similar in all groups (78-94 %). No resistance was reported in the combination group, while 20 % of patients treated with Clevudine 30 mg or 20 mg reported resistance during 2 years. Muscle-related symptoms such as myalgia (1 in Clevudine 30 mg, 1 in the combination group) and muscle weakness (1 in Clevudine 30 mg, 2 in Clevudine 20 mg) were reported in five patients (7 %); of these, three patients discontinued the study. CONCLUSION: We concluded that the combination of Clevudine 20 mg and adefovir produced a potent antiviral response together with a good resistance profile compared to Clevudine monotherapy at 96 weeks in this pilot study.
