Telbivudine

• L- thymidine
• 1 - (2 -deoxy- β -L -erythro- pentofuranosyl ) thymine
• 1 - [( 2S, 4R, 5S )-4 -hydroxy- 5 - ( hydroxymethyl) oxolane -2-yl ] - 5 - methyl-pyrimidin- 2 ,4-dione

J05AF11

Virostatikum

186 ° C

Template: Infobox chemical / molecular formula search available

Telbivudine or L- thymidine (trade name: Sebivo ®, manufactured by 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 stage of viral replication ( viral replication ).

Mechanism of action

Telbivudine is phosphorylated by kinases of the host cell to the active triphosphate form. Telbivudine - 5'-triphosphate inhibits the HBV DNA polymerase ( reverse transcriptase) as it is fitted instead of the natural substrate, thymidine -5'- triphosphate into the viral DNA. The attachment of additional nucleotides is not structurally possible and it results in a DNA chain termination, HBV replication is stopped.

Side effects

Side effects are, inter alia, Muscle diseases, deterioration of renal function, infections of the upper respiratory tract, fatigue and malaise, abdominal pain, nasopharyngitis, headache, increase in CPK in the blood, coughing, nausea and vomiting, flu and flu-like symptoms, pain after the operation, diarrhea and loose stools, and pharyngolaryngeal pain specified. In February 2008, clinical trials of combination therapy of telbivudine and interferon had to be canceled because in 8 of 48 ( 16.6 percent ) patients occurred a peripheral neuropathy, including five severe cases. In monotherapy with telbivudine a frequency of this side effect of 0.6 percent was observed, which occurred about two to six months duration of therapy.

Development and marketing

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