Entecavir is mainly used to treat chronic hepatitis B infection in adults and children two years and older with active viral replication and evidence of active disease with elevations in liver enzymes.[2] It is also used to prevent hepatitis B virus reinfection after liver transplant[8] and to treat HIV patients infected with hepatitis B virus. Entecavir is weakly active against HIV, but is not recommended for use in HIV-HBV co-infected patients without a fully suppressive anti-HIV regimen[9] as it may select for resistance to lamivudine and emtricitabine in HIV.[10]
The efficacy of entecavir has been studied in several randomized, double-blind, multicentre trials. Entecavir by mouth is effective and generally well tolerated treatment.[11]
The majority of people who use entecavir have little to no side effects.[12] The most common side effects include headache, fatigue, dizziness, and nausea.[2] Less common effects includetrouble sleeping and gastrointestinal symptoms such as sour stomach, diarrhea, and vomiting.[13]
Entecavir is taken by mouth as a tablet or solution. Doses are based on a person's weight.[2] The solution is recommended for children more than 2 years old who weigh up to 30 kg. Entecavir is recommended on an empty stomach at least 2 hours before or after a meal, generally at the same time every day. It is not used in children less than 2 years old. Dose adjustments are also recommended for people with decreased kidney function.[2]
1992: SQ-34676 at Squibb as part of anti-herpes virus program[16]
1997: BMS 200475 developed at BMS pharmaceutical research institute as antiviral nucleoside analogue à Activity demonstrated against hepatitis B virus, HSV-1, HCMV, VZV in cell lines & no or little activity against HIV or influenza[17]
Superior activity observed against hepatitis B virus pushed research towards BMS 200475, its base analogues and its enantiomer against hepatitis B virus in HepG2.2.15 cell line[17]
Comparison to other NAs, proven more selective potent inhibitor of hepatitis B virus by virtue of being Guanine NA[18]
1998: Inhibition of hepadnaviral polymerases was demonstrated in vitro in comparison to a number of NAs-TP[19]
Metabolic studies showed more efficient phosphorylation to triphosphate active form[20]
3-year treatment of woodchuck model of CHB à sustained antiviral efficacy and prolonged life spans without detectable emergence of resistance[21]
Efficacy # LVD resistant hepatitis B virus replication in vitro[22]
Superior activity compared to LVD in vivo for both HBeAg+ & HBeAg− patients[23][24]
Bristol-Myers Squibb was the original patent holder for Baraclude, the brand name of entecavir in the US and Canada. The drug patent expiration for Baraclude was in 2015.[27][28]Entecavir patents were a subject of litigation in the US betweenBristol Myers Squibb (the patent owner) andTeva Pharmaceuticals USA (a generic manufacturer). The lawsuit resulted in a relatively rare in the pharmaceutical field patent invalidation forobviousness, which was affirmed in June 2014, by theUS Court of Appeals for the Federal Circuit (752 F.32d 967).
^World Health Organization (2023).The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023). Geneva: World Health Organization.hdl:10665/371090. WHO/MHP/HPS/EML/2023.02.
^Slusarchyk, WA, Field AK, Greytok JA, Taunk P, Tooumari AV, et al. (1992). "4-Hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl purines and pyrimidines, a new class of anti-herpesvirus agents".Antiviral Research.17: 98.doi:10.1016/0166-3542(92)90200-o.
^abBisacchi GS, Chao ST, Bachard C, Daris JP, Innaimo SF, Jacobs JA, et al. (1997). "BMS-200475, a novel carbocyclic 29-deoxyguanosine analog with potent and selective antihepatitis B virus activity in vitro".Bioorganic & Medicinal Chemistry Letters.7 (2):127–132.doi:10.1016/s0960-894x(96)00594-x.
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