Telbivudine

Structural formula
General
Non-proprietary name	Telbivudine
other names	L- thymidine 1- (2- Deoxy- β - L -erythro-pentofuranosyl) -thymine 1 - [(2 S , 4 R , 5 S ) -4-hydroxy-5- (hydroxymethyl) oxolan-2-yl] -5-methylpyrimidin-2,4-dione
Molecular formula	C 10 H 14 N 2 O 5
External identifiers / databases
CAS number 3424-98-4 EC number 608-961-3 ECHA InfoCard 100.125.511 PubChem 159269 DrugBank DB01265 Wikidata Q413621
Drug information
ATC code	J05 AF11
Drug class	Antiviral
properties
Molar mass	242,23 g · mol -1
Physical state	firmly
Melting point	186 ° C
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed GHS labeling of hazardous substances Caution H and P phrases H: 302 P: ?
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Telbivudine or L-thymidine (trade name: Sebivo ^® , manufacturer: Novartis ) is the L - enantiomer of the nucleoside thymidine . It is used in adult patients as a drug for the treatment of chronic hepatitis B in the virus replication stage .

Mechanism of action

Telbivudine is phosphorylated to the active triphosphate form by host cell kinases . Telbivudine 5'-triphosphate inhibits HBV DNA polymerase (reverse transcriptase) because it is incorporated into the virus DNA instead of the natural substrate thymidine 5'-triphosphate. The attachment of further nucleotides is structurally not possible and the result is a DNA chain break, the HBV replication is stopped.

Side effects

Side effects are u. a. Muscle disorders , worsening kidney function , upper respiratory tract infections , fatigue and malaise, abdominal pain , nasopharyngitis , headache , blood CPK increase , cough , nausea and vomiting , flu and flu-like symptoms, post-operative pain, diarrhea and misshapen stool, and pharyngolaryngeal joints Pain indicated. In February 2008, clinical studies with a combination therapy of telbivudine and interferon had to be discontinued because 8 of 48 (16.6 percent) patients developed peripheral neuropathy , five of them severe. With telbivudine monotherapy, a frequency of this side effect of 0.6 percent was observed and occurred after approximately two to six months of therapy.

Development and marketing

Telbivudine was approved across Europe by the EU Commission in April 2007 and came onto the market in Germany in May 2007. In one study, telbivudine was more effective than the standard drug lamivudine after one year and there was less resistance-related loss of effectiveness. Telbivudine selects the same resistant mutants as lamivudine and is significantly more expensive.

Individual evidence

1. ^ The Merck Index . An Encyclopaedia of Chemicals, Drugs and Biologicals. 14th edition, 2006, pp. 1567-1568, ISBN 978-0-911910-00-1 .
2. ↑ There is not yet a harmonized classification for this substance . A labeling of 2,4 (1H, 3H) -pyrimidinedione, 1- (2-deoxy-β-L-erythro-pentofuranosyl) -5-methyl- in the Classification and Labeling Inventory of the European Chemicals Agency is shown, which is derived from a self-classification by the distributor (ECHA), accessed on July 12, 2020.
3. ^ Journal of Chemotherapy. Born in 2007, No. 4 ..
4. ↑ Lai, Ching-Lung et al. (2007): Telbivudine versus lamivudine in patients with chronic hepatitis B. In: N. Engl. J. Med. Vol. 357, pp. 2576-2588, PMID 18094378 .
5. ↑ Deutsches Ärzteblatt: Peripheral neuropathy in telbivudine ( Memento from August 12, 2011 in the Internet Archive ).

This article is about a health issue. It is not used for self-diagnosis and does not replace a diagnosis by a doctor. Please note the information on health issues !