Biktarvy is Effective for HIV-1 Infection Regardless of Genotype
Biktarvy (bictegravir, emtricitabine, and tenofovir alafenamide) is highly effective for treating HIV-1 infection across all genotypes and is recommended as a first-line treatment option due to its high genetic barrier to resistance and potent viral suppression. 1
Efficacy and Mechanism of Action
- Biktarvy is a complete three-drug regimen containing bictegravir (an integrase strand transfer inhibitor or INSTI), emtricitabine and tenofovir alafenamide (both nucleoside/nucleotide reverse transcriptase inhibitors) 1
- It is specifically indicated for treatment of HIV-1 infection in patients who have no antiretroviral treatment history or to replace current regimens in virologically suppressed patients 1
- Bictegravir is a second-generation INSTI with high resilience to INSTI-resistance mutations, providing effectiveness across HIV-1 genotypes 2
- Clinical trials have demonstrated that Biktarvy is non-inferior to other leading HIV regimens, including dolutegravir-based therapies, with consistently high rates of viral suppression (>84% at 96 weeks) 3
Clinical Recommendations and Guidelines
- The International Antiviral Society-USA Panel lists Biktarvy (bictegravir/TAF/emtricitabine) as a generally recommended initial regimen for HIV-1 treatment (evidence rating AIa) 4
- Biktarvy maintains its effectiveness regardless of HIV-1 genotype due to its high genetic barrier to resistance, with no resistance emerging to any of the antiretrovirals in the single-tablet regimen during clinical trials 5
- In patients who acquire HIV-1 while taking PrEP (TXF/XTC), bictegravir in combination with TXF/XTC can be started before resistance testing results are available 4
- For patients with viral suppression and previous treatment failure with archived resistance mutations, Biktarvy may be effective even in the presence of M184V/I mutations 4
Special Populations and Considerations
- Biktarvy is suitable for patients co-infected with hepatitis B virus (HBV) as it contains tenofovir alafenamide and emtricitabine, both of which are active against HBV 5
- It can be used in patients with renal impairment with creatinine clearance ≥30 mL/min, making it the first non-pharmacologically boosted, INSTI-based triple-combination suitable for these patients 5
- Biktarvy is not currently recommended with rifampin due to drug-drug interactions and inadequate data (evidence rating: AIII) 4
- Biktarvy should not be used during pregnancy due to inadequate data to support its use (evidence rating: AIII) 4
Safety Profile and Tolerability
- Biktarvy is generally well-tolerated with the most common adverse reactions (incidence ≥5%) being diarrhea, nausea, and headache 1
- It has minimal drug-drug interactions compared to other antiretroviral classes, making it a preferred option when co-administered with other medications 6
- No HLA-B*5701 testing is required before starting Biktarvy, making it suitable for "rapid start" treatment 5
- Treatment discontinuation due to adverse events is rare, with only 2% of patients discontinuing in clinical trials through 96 weeks 3
Important Clinical Considerations
- Prior to starting Biktarvy, testing for hepatitis B virus infection is recommended as severe acute exacerbations of hepatitis B have been reported in patients who discontinued products containing emtricitabine and/or tenofovir 1
- Regular monitoring of HIV viral load is essential to ensure continued virological suppression 6
- Biktarvy can be taken once daily with or without food, improving convenience and adherence 7
- The high genetic barrier to resistance development makes Biktarvy a durable treatment option with sustained efficacy over time 2
Biktarvy represents an important advancement in HIV treatment with its combination of potent efficacy across HIV-1 genotypes, high barrier to resistance, favorable safety profile, and convenient single-tablet, once-daily dosing.