| Bioactivity | Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS[1][2]. | ||||||||||||
| Invitro | Lamivudine (1 μM) is potent inhibitor of hepatitis B virus (HBV) replication, shows antiviral activity in primary duck hepatocyte (PDH) cultures derived from ducklings congenitally infected with the duck hepatitis B virus (DHBV)[1].Lamivudine (0-20 μM; 2, 4, 9 d) inhibits DHBV replication with 50% inhibitory concentration of 0.55 μM[1].Lamivudine, combinded with penciclovir (9-[2-hydroxy-1-(hydroxymethyl)ethoxymethyl]guanine [PCV]), (1 μM; 2, 4, 9 d) shows synergistic effect, acts potent function in reducing the normally recalcitrant viral covalently closed circular (CCC) DNA form of DHBV[1]. | ||||||||||||
| In Vivo | Lamivudine (20-500 mg/kg/d; p.o.; 15 or 45 d) causes oxidative stress and is toxic to rat liver[2].Lamivudine (50 mg/kg; i.p.; single dose) penetrates well in CNS and localizes in brain regions susceptible to HIV neurodegeneration in rat[3]. Pharmacokinetic Parameters of Lamivudine in HIV-infected Rats[3]Parameter | ||||||||||||
| Name | Lamivudine | ||||||||||||
| CAS | 134678-17-4 | ||||||||||||
| Formula | C8H11N3O3S | ||||||||||||
| Molar Mass | 229.26 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Colledge D, et al. Synergistic inhibition of hepadnaviral replication by lamivudine in combination with penciclovir in vitro. Hepatology. 1997 Jul;26(1):216-25. [2]. Olaniyan LW, et al. Lamivudine-Induced Liver Injury. Open Access Maced J Med Sci. 2015 Dec 15;3(4):545-50. [3]. Mdanda S, et al. Zidovudine and Lamivudine as Potential Agents to Combat HIV-Associated Neurocognitive Disorder. Assay Drug Dev Technol. 2019 Oct;17(7):322-329. |