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Lopinavir (ABT-378) is an antiretroviral of the protease inhibitor class. Lopinavir potently inhibited wild-type and mutant HIV protease (Ki = 1.3 to 3.6 pM). Lopinavir (ABT-378) also produced negligible or weak inhibition of human CYP1A2, 2B6, 2C9, 2C19 and 2D6. Lopinavir (ABT-378) blocked the replication of laboratory and clinical strains of HIV type 1 (50% effective concentration [EC50], 0.006 to 0.017 microM), and maintained high potency against mutant HIV selected by ritonavir in vivo (EC50, 50-fold after 8 h.
| Molecular Weight | 628.8 |
| Formula | C37H48N4O5 |
| CAS Number | 192725-17-0 |
| Solubility (25°C) | DMSO 110 mg/mL Ethanol 100 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.
| Related HIV Protease Products |
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Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM. |
| WAY-300700
WAY-300700 is a HIV-1 non-nucleoside reverse transcriptase inhibitor. |
| WAY-613473
WAY-613473 has inhibition of HIV-I replication |
| Cabotegravir
Cabotegravir, also known as S/GSK1265744 or GSK744, is potent HIV integrase inhibitor. |
| Tenofovir hydrate
Tenofovir hydrate is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B. |
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