Kaletra

Lopinavir/ritonavir tablets
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.