This tablet formulation of lopinavir and ritonavir provides several advantages over the capsule formulation.
ABBOTTTablet formulation approved with reduced pill burden
This tablet formulation of lopinavir and ritonavir provides several advantages over the capsule formulation, including: a reduced pill burden of 4 tablets daily, dosing without a food requirement, and no need for refrigerated storage of the tablets. The tablet formulation of lopinavir/ritonavir was approved on October 28, 2005, in combination with other antiretroviral agents for the treatment of HIV infection.
Efficacy. The efficacy of lopinavir/ritonavir twice-daily in combination with stavudine and lamivudine was evaluated compared to nelfinavir 3-times-daily plus stavudine and lamivudine in 653 antiretroviral treatment-naïve patients. Through 48 weeks of therapy, there was a statistically significantly higher proportion of patients in the lopinavir/ritonavir arm with HIV RNA <400 copies/mL (75% vs 62%, respectively) and <50 copies/mL (67% vs 52%, respectively). Likewise, the efficacy of once-daily lopinavir/ritonavir in combination with tenofovir DF and emtricitabine was evaluated against lopinavir/ritonavir twice-daily in combination with tenofovir DF and emtricitabine in 190 antiretroviral treatment-naïve patients. Patients achieved and maintained HIV RNA <50 copies/mL at rates of 71% and 65% in the lopinavir/ritonavir once- and twice-daily groups, respectively (95% CI for the difference, –7.6%–19.5%). In a study of 288 single protease inhibitor-experienced, non-nucleoside reverse transcriptase inhibitor (NNRTI)-naïve patients, the efficacy of twice-daily lopinavir/ritonavir plus nevirapine and nucleoside reverse transcriptase inhibitors (NRTIs) was compared with an investigator-selected protease inhibitor(s) plus nevirapine and NRTIs. Patients achieved and maintained HIV RNA <400 copies/mL at rates of 57% and 33% in the lopinavir/ritonavir and investigator-selected protease inhibitor groups, respectively. In an ongoing study of lopinavir/ritonavir twice-daily at 3 dose levels (200/100 mg, 400/100 mg, and 400/200 mg) plus stavudine and lamivudine, 71% of patients achieved HIV RNA <400 copies/mL, while 70% of patients achieved HIV RNA <50 copies/mL through 204 weeks of study. In an ongoing study of lopinavir/ritonavir twice-daily at 2 dose levels (400/100 mg and 400/200 mg) plus nevirapine and NRTIs, 54% of patients achieved HIV RNA <400 copies/mL, while 50% of patients achieved HIV RNA <50 copies/mL through 144 weeks of study.
Dosing. In therapy-naïve patients, the recommended dose of lopinavir/ritonavir is 400/100 mg (2 tablets) twice-daily or 800/200 mg (4 tablets) once-daily with or without food. In therapy-experienced patients, the recommended dose of lopinavir/ritonavir is 400/100 mg (2 tablets) twice-daily taken with or without food. Once-daily administration of lopinavir/ritonavir is not recommended in therapy-experienced patients. Lopinavir/ritonavir 400/100-mg tablets can be administered twice daily in combination with efavirenz, nevirapine, fosamprenavir, or nelfinavir with no dose adjustment in antiretroviral-naïve patients. A dose increase of lopinavir/ritonavir tablets to 600/150 mg (3 tablets) twice-daily may be considered when the therapy is used in combination with efavirenz, nevirapine, fosamprenavir without ritonavir, or nelfinavir in treatment-experienced patients in which decreased susceptibility to lopinavir is clinically suspected.