General Information

Complera is a single tablet fixed dose comprised of emtricitabine, tenofovir disoproxil fumarate and rilpivirine. Emtricitabine and tenofovir are nucleoside reverse transcriptase inhibitors and rilpivirine is a non-nucleoside reverse transcriptase inhibitor.

Complera is specifically approved for use as a complete regimen for the treatment of HIV-1 infection in patients weighing at least 35 kg:

• as initial therapy in those with no antiretroviral treatment history and with HIV-1 RNA less than or equal to 100,000 copies/mL at the start of therapy

OR

• to replace a stable antiretroviral regiment in those who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral regimen for at least 6 months with no treatment failure and no known substitutions associated with resistance to the individual components of Complera.

Complera is supplied as a tablet for oral administration. Each tablet contains 200 mg of emtricitabine, 27.5 mg of rilpivirine hydrochloride and 300 mg of tenofovir disoproxil fumarate. The recommended dose is one tablet taken orally once daily with a meal.

Mechanism of Action

Complera is a single tablet fixed dose comprised of emtricitabine, tenofovir disoproxil fumarate and rilpivirine. Emtricitabine and tenofovir are nucleoside reverse transcriptase inhibitors and rilpivirine is a non-nucleoside reverse transcriptase inhibitor.

Side Effects

Adverse events associated with the use of Complera may include, but are not limited to, the following:
rilpivirine

• insomnia
• headache

emtricitabine and tenofovir disoproxil fumarate

• diarrhea
• nausea
• fatigue
• headache
• dizziness
• depression
• insomnia
• abnormal dreams
• rash

Clinical Trial Results

The FDA approval of Complera was based on 48-week data from two phase III double-blind, active controlled, randomized studies (ECHO and THRIVE) conducted by Tibotec that evaluated the safety and efficacy of rilpivirine compared to efavirenz (EFV) among treatment-naïve HIV-1 infected adults. Both arms of the study were administered with a background regimen, in which the majority of subjects in the rilpivirine arm received Truvada. Both trials reached their primary objective, the non-inferiority of rilpivirine vs. EFV in the proportion of patients achieving an undetectable viral load (less than 50 copies/mL) at week 48 (with a maximum allowable difference of 12%). Results showed that 84.3% of patients in the rilpivirine group reached an undetectable viral load, compared with 82.3% of patients in the EFV group. The virologic failure rate was 9% in the rilpivirine group and 4.8% in the EFV group. The pooled analysis at 96 weeks showed that 78% of subjects achieved and sustained an undetectable plasma viral load. These data demonstrated non-inferiority (12% margin) of rilpivirine to EFV in lowering viral load in this population at 96 weeks. Subjects taking rilpivirine had a virologic failure rate of 14% compared to 8% experienced by subjects taking EFV, of which 3 percent and 2 percent occurred in the second year of treatment, respectively. A bioequivalence study, conducted by Gilead, demonstrated that the co-formulated single-tablet regimen achieved the same levels of medication in the blood as emtricitabine plus rilpivirine plus tenofovir disoproxil fumarate.