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[CAS NO. 3424-98-4] Telbivudine

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Catalog:	HY-B0017
Brand:	MCE
CAS:	3424-98-4

Overview

MDL	MFCD02683612
Molecular Weight	242.23
Molecular Formula	C10H14N2O5
SMILES	O=C(N1)N([C@@H]2C[C@@H](O)[C@H](CO)O2)C=C(C)C1=O

For research use only. We do not sell to patients.

Summary

Telbivudine (Epavudine), an orally active thymidine nucleoside analog, is a potent antiviral inhibitor of hepatitis B virus (HBV) replication ^[1] .

In Vitro

Telbivudine reverses B19V-induced dysregulation of BIRC3, thus, intervening in the apoptosis pathway and protecting susceptible cells from cell death ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00537537	Novartis Pharmaceuticals\|Novartis	Hepatitis B, Chronic	August 2007	Phase 4
NCT00962533	Nanfang Hospital of Southern Medical University\|Major Science and Technology Special Project of China Eleventh Five-year\|Novartis	Hepatitis B, Chronic	August 2009	Phase 4
NCT00076336	Novartis Pharmaceuticals\|Novartis	Hepatitis\|Hepatitis B, Chronic\|Cirrhosis	December 2003	Phase 3
NCT02447705	Chang Gung Memorial Hospital	Disorder Related to Transplantation\|Virus Diseases\|Injury Due to Exposure to External Cause	June 2013	Phase 2\|Phase 3
NCT00115245	Novartis\|Novartis Pharmaceuticals	Chronic Hepatitis B	November 2004	Phase 3
NCT00646503	Novartis	Hepatitis B, Chronic	March 2008	Phase 4
NCT00640588	Novartis Pharmaceuticals\|Novartis	Hepatitis B, Chronic	March 2008	Phase 3
NCT02774837	Seng Gee Lim\|National Medical Research Council (NMRC), Singapore\|Singapore Clinical Research Institute\|National University Health System, Singapore	Chronic Hepatitis B	April 2016	Phase 4
NCT02049736	Chinese University of Hong Kong	Chronic Hepatitis B	December 2013	Not Applicable
NCT01588912	Pusan National University Yangsan Hospital	Chronic Hepatitis B	April 2012	Phase 4
NCT00128544	Novartis\|Novartis Pharmaceuticals	Hepatitis B	May 2005	Phase 2
NCT00939068	Southeast University, China	Chronic Hepatitis B, Gestation	February 2008	Phase 4
NCT00907894	Novartis Pharmaceuticals\|Novartis	Chronic Hepatitis B	February 2009	Phase 1
NCT01337791	Southeast University, China	Chronic Hepatitis B\|Pregnancy Complications\|High Viral Load\|Elevated Alanine Aminotransferase Levels	August 2008	Phase 4
NCT01380951	The Fifth People´s Hospital of Suzhou	Liver Cirrhosis\|Chronic Hepatitis B	May 2011	Phase 4
NCT00376259	Novartis	Hepatitis B	January 2007	Phase 3
NCT01637844	Yi-Hua Zhou\|Taixing People´s Hospital\|Fourth People´s Hospital of Zhenjiang, China\|Wuxi Maternal and Child Health Hospital\|Kunshan First People Hospital\|The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School	HBV	April 2012	Phase 4
NCT01799486	Lin Bingliang\|Novartis\|Sun Yat-sen University	HBV-related Liver Cirrhosis	February 2013	Phase 4
NCT02338674	Fuzhou General Hospital	Hepatitis B, Chronic	October 2014	Phase 1\|Phase 2
NCT00970216	Chang Gung Memorial Hospital	Chronic Hepatitis B	February 2009
NCT00710216	University of Ulm\|Novartis	Hepatitis B, Chronic		Phase 4
NCT02301650	Beijing Ditan Hospital	the Safety of Anti-viral Drugs Used in Late Pregnancy	October 2014
NCT00412529	Novartis Pharmaceuticals\|Novartis	Hepatitis B\|Chronic Hepatitis B	December 2006	Phase 3
NCT00412750	Novartis	Hepatitis B	December 2006	Phase 3
NCT00131742	Novartis\|Novartis Pharmaceuticals	Chronic Hepatitis B	July 2004	Phase 3
NCT01732224	Institute of Liver and Biliary Sciences, India	Spontaneous Reactivation of Hepatitis B	November 2012	Not Applicable
NCT01379508	Novartis Pharmaceuticals\|Novartis	Chronic Hepatitis B	March 21, 2011	Phase 4
NCT00132652	Novartis\|Novartis Pharmaceuticals	Chronic Hepatitis B	February 2005	Phase 3
NCT00606099	Novartis	Chronic Hepatitis B	November 2007	Phase 4
NCT00781105	Novartis Pharmaceuticals\|Novartis	Chronic Hepatitis B	August 1, 2008	Phase 4
NCT01804387	Korea University	Chronic Hepatitis B	May 2011	Phase 4
NCT00805675	Novartis Pharmaceuticals\|Novartis	Hepatitis B Virus	November 2008	Phase 3
NCT02253485	Beijing Ditan Hospital	Immune Globulin, Prophylaxis, Telbuvidine, Vaccine	August 2012
NCT00804622	The University of Hong Kong\|Novartis Pharmaceuticals	Chronic Hepatitis B	December 2008	Phase 2
NCT00051090	National Institute of Allergy and Infectious Diseases (NIAID)	HIV Infections\|Hepatitis B		Not Applicable
NCT02826070	Nanfang Hospital of Southern Medical University\|Major Science and Technology Special Project of China Twelfth-Five-Year Project\|Novartis	Hepatitis B, Chronic	April 2015	Phase 4
NCT01102335	Fudan University	Hepatocellular Carcinoma	April 2010	Phase 4
NCT01595685	Asan Medical Center	Chronic Viral Hepatitis B Without Delta-agent	May 2012	Phase 3
NCT01005238	University Hospital, Basel, Switzerland	Hepatitis, Chronic	September 2009	Phase 4
NCT00124241	Novartis\|Novartis Pharmaceuticals	Hepatitis B		Phase 2
NCT02058108	Novartis Pharmaceuticals\|Novartis	Chronic Hepatitis B	October 31, 2014	Phase 3
NCT03778567	The University of Hong Kong	Hepatitis B, Chronic\|Chronic Kidney Diseases	August 1, 2013	Phase 4
NCT02894554	National Taiwan University Hospital	HBsAg-positive Renal Allograft Recipients	July 2014	Phase 4
NCT01743079	Beijing YouAn Hospital\|New Discovery LLC	Chronic Hepatitis B\|Late Pregnancy\|Transmission\|Complication	January 2009	Phase 4
NCT00275652	Mayo Clinic\|Merck Sharp & Dohme LLC	Hepatitis B\|Cirrhosis	June 2004	Phase 3
NCT00142298	Novartis Pharmaceuticals\|Merck Sharp & Dohme LLC\|Novartis	Chronic Hepatitis B	March 2005	Phase 3
NCT01260610	Institute of Liver and Biliary Sciences, India	Chronic Hepatitis B	June 2011	Not Applicable
NCT01529255	Nanfang Hospital of Southern Medical University\|Major Science and Technology Special Project of China Eleventh Five-year\|Novartis	Hepatitis B, Chronic	August 2011	Phase 4
NCT03468907	Third Affiliated Hospital, Sun Yat-Sen University	Hepatitis B, Chronic	June 1, 2015	Phase 4
NCT00467545	Novartis Pharmaceuticals\|Novartis	Chronic Hepatitis B	April 2007	Phase 4
NCT01480492	Cz Li\|Changhai Hospital	HBeAg Positive Chronic Hepatitis B Infection	January 2010	Not Applicable
NCT00810524	Sun Yat-sen University	Hepatitis B, Chronic	January 2007	Phase 4
NCT02615639	Third Affiliated Hospital, Sun Yat-Sen University\|Shanghai Jiao Tong University School of Medicine	Chronic Hepatitis B	November 2015	Phase 1\|Phase 2
NCT01788371	Hua Zhang\|Icahn School of Medicine at Mount Sinai\|Beijing YouAn Hospital	Hepatitis B Infection\|Chronic Infection\|Viremia	March 2009	Phase 4
NCT00409019	Novartis Pharmaceuticals\|Novartis	Chronic Hepatitis B		Phase 4
NCT01270165	Yonsei University	Chronic Hepatitis B	June 2010	Phase 3
NCT00057265	Novartis\|Novartis Pharmaceuticals	Chronic Hepatitis B	February 2003	Phase 3

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 206.42 mM ; Need ultrasonic)

H ₂ O : 33.33 mg/mL ( 137.60 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.1283 mL	20.6415 mL	41.2831 mL
5 mM	0.8257 mL	4.1283 mL	8.2566 mL
10 mM	0.4128 mL	2.0642 mL	4.1283 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 10 mg/mL (41.28 mM); Clear solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 3.25 mg/mL (13.42 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 3.25 mg/mL (13.42 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 3.25 mg/mL (13.42 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Kim JW, et al. Telbivudine: a novel nucleoside analog for chronic hepatitis B. Ann Pharmacother. 2006;40(3):472-478.
[2] Zobel T, et al. Telbivudine Reduces Parvovirus B19-Induced Apoptosis in Circulating Angiogenic Cells. Viruses. 2019;11(3):227. Published 2019 Mar 6.

Synonyms

2,4(1H,3H)-Pyrimidinedione, 1-(2-deoxy-β-L-erythro-pentofuranosyl)-5-methyl-

Thymine, 1-(2-deoxy-β-L-erythro-pentofuranosyl)-

1-(2-Deoxy-β-L-erythro-pentofuranosyl)-5-methyl-2,4(1H,3H)-pyrimidinedione

2′-Deoxy-L-thymidine

L-Thymidine

β-L-Thymidine

Epavudine

NV 02B

Telbivudine

Sebivo

L-Deoxythymidine

Tyzeka

32: PN: WO2016077321 SEQID: 32 claimed sequence

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