Alternative Regimens for Switching from Dolutegravir in Virologically Suppressed Patients

Preferred Integrase‑Backbone Alternative

Bictegravir / emtricitabine / tenofovir alafenamide (BIC/FTC/TAF) is the preferred regimen when dolutegravir must be stopped because of contraindication, intolerance, or drug‑drug interaction; it preserves the integrase‑inhibitor backbone and shows efficacy and tolerability comparable to dolutegravir‑based therapy. [1][2]

Efavirenz 600 mg once daily plus two NRTIs (tenofovir + emtricitabine or lamivudine) is the preferred alternative because no dose adjustment is required with rifampin. [1][3]
Raltegravir 800 mg twice daily plus two NRTIs is an acceptable integrase‑inhibitor option compatible with rifampin. [1][3]
Boosted protease‑inhibitor regimens (e.g., darunavir/cobicistat) should be reserved for patients in whom efavirenz or raltegravir cannot be used; rifampin must be replaced by rifabutin 150 mg daily to avoid a severe interaction. [1][3]
Bictegravir cannot be co‑administered with rifampin because of a severe drug‑drug interaction. 1
Dolutegravir / lamivudine (dual‑drug regimen) is also contraindicated with rifampin. 4

BIC/FTC/TAF maintains viral suppression in > 90 % of patients switching from other integrase‑inhibitor regimens. [2][5]
Dolutegravir / rilpivirine provides durable virologic suppression for at least 2 years and is associated with improvements in bone mineral density and renal function. 6
Darunavir / cobicistat / emtricitabine / tenofovir alafenamide is an option for patients requiring a boosted protease‑inhibitor backbone. 2

BIC/FTC/TAF can be used despite likely prior NRTI resistance, provided integrase‑inhibitor resistance is absent. 5
Dolutegravir + tenofovir / emtricitabine remains effective even with NRTI‑resistance mutations, but closer virologic monitoring is advised. 5
Switching to NNRTI‑based or first‑generation integrase‑inhibitor regimens (raltegravir or elvitegravir) plus two NRTIs is discouraged because of a higher risk of virologic failure in the setting of NRTI resistance. 5
Monitoring: patients with NRTI resistance who switch to dual‑NRTI + dolutegravir or bictegravir should have HIV‑1 RNA measured at 1 month and every 3 months during the first year. 5

Dolutegravir / lamivudine maintains suppression in patients without prior virologic failure, NRTI resistance, or hepatitis B co‑infection. [1][6]
Long‑acting cabotegravir + rilpivirine (monthly or every 8 weeks) is non‑inferior to continued oral therapy, achieving viral suppression rates of ≈ 95 %. [6][5]
Adherence requirement: missed injections lead to prolonged sub‑therapeutic drug levels and potential resistance; strict adherence to the injection schedule is essential. 6
Hepatitis B co‑infection: long‑acting cabotegravir / rilpivirine should not be used unless separate HBV therapy is continued. 5

With rifampin: bictegravir, dolutegravir / lamivudine, doravirine, elvitegravir / cobicistat, long‑acting cabotegravir / rilpivirine, and any regimen containing rilpivirine should not be used. 4
During pregnancy: cobicistat‑boosted regimens (including darunavir / cobicistat) achieve inadequate plasma concentrations and should be avoided. 7
With hepatitis B co‑infection: tenofovir‑sparing regimens (dolutegravir / lamivudine, dolutegravir / rilpivirine, long‑acting cabotegravir / rilpivirine) are contraindicated unless HBV treatment is provided separately. 5

HIV‑1 RNA should be measured at 1 month after the switch to confirm continued suppression. 5
Viral load thereafter every 3 months during the first year, and at least every 6 months if the patient remains stable. 8
Renal function (serum creatinine, eGFR) should be assessed at baseline and periodically, especially when tenofovir‑containing regimens are used. 8
Comprehensive ART history must be reviewed before switching to identify any prior virologic failures or resistance findings. 5

Assuming all integrase inhibitors behave the same with rifampin: dolutegravir requires twice‑daily dosing, raltegravir requires 800 mg twice daily, and bictegravir cannot be used at all. 1
Overlooking hepatitis B status: switching to tenofovir‑sparing regimens without addressing HBV can precipitate hepatitis flares. 5
Switching in the presence of documented integrase‑inhibitor resistance: both dolutegravir and bictegravir rely on intact integrase susceptibility; resistance limits alternative options. 8
Using standard once‑daily dolutegravir dosing with rifampin: this results in sub‑therapeutic exposure; a 50 mg twice‑daily regimen is required. 1