Lamivudine (BCH-189) is a potent nucleoside analog reverse transcriptase inhibitor with an IC50 of 2.7 mM. The pH-driven uptake of TEA by BBMV (pHin = 6.0, pHout = 7.5) was inhibited by lamivudine. The IC50 value (concentration resulting in 50% inhibition) for the concentration-dependent effect of lamivudine on TEA uptake by BBMV after 30 s was 2668 uM whereas IC50 values for cimetidine and trimethoprim were < 2.5 uM and < 25 uM, respectively. The early uptake of TEA by BLMV was also reduced significantly by lamivudine. The IC50 value for the concentration-dependent effect of lamivudine on uptake of TEA by BLMV at 30 s was > 25 mM, whereas the IC50 values for cimetidine and trimethoprim were 2116 uM and 445uM, respectively.
| Molecular Weight | 229.26 |
| Formula | C8H11N3O3S |
| CAS Number | 134678-17-4 |
| Solubility (25°C) | Water 50 mg/mL DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Lesley J Scott. Dolutegravir/Lamivudine Single-Tablet Regimen: A Review in HIV-1 Infection
[3] Princy N Kumar, et al. Lamivudine for the treatment of HIV
[4] Tim Ibbotson, et al. Lamivudine/zidovudine/abacavir: triple combination tablet
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