Adverse Reactions & Discontinuations

An Established 5-Year Long-term Safety Profile^1-3

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Adverse Reactions in Treatment-Naïve Adults
Adverse Reactions in Virologically Suppressed Participants
Discontinuations in Treatment-Naïve Adults
Discontinuations in Virologically Suppressed Participants

Adverse Reactions in Treatment-Naïve Adults

Studies 1489 and 1490: Proven long-term safety and tolerability profile in treatment-naïve adults who received BIKTARVY® through Week 144^1,4

Study 1489

Adverse Reactions (ARs)
(All Grades) Reported in ≥2% of Adults Who Received BIKTARVY*

BIKTARVY (n=314)

ABC/DTG/3TC (n=315)

Nausea, %

Diarrhea, %

Headache, %

Fatigue, %

Abnormal dreams, %

Dizziness, %

Insomnia, %

Abdominal distension, %

Study 1490

ARs (All Grades) Reported in ≥ 2% of Adults Who Received BIKTARVY*

BIKTARVY (n=320)

DTG+FTC/TAF (n=325)

Nausea, %

Diarrhea, %

Headache, %

Fatigue, %

Abnormal dreams, %

Dizziness, %

Insomnia, %

Abdominal distension, %

*Frequencies of ARs are based on all adverse events attributed to trial drugs by the investigator. No ARs of Grade 2 or higher occurred in >1% of participants treated with BIKTARVY.

The majority (84%) of AEs associated with BIKTARVY were Grade 1²

Studies 1489 and 1490: Proven long-term safety and tolerability profile through Week 240 in adults initially randomized to BIKTARVY or switched to BIKTARVY at Week 144^2,3,5

Study 1489

ARs (All Grades) Reported in ≥2% of Adults Who Received BIKTARVY

BIKTARVY (Baseline-W240) (n=314)

Switched from ABC/ DTG/3TC to BIKTARVY (W144-240) (n=254)

Headache, %

Diarrhea, %

Nausea, %

Fatigue, %

Abnormal dreams, %

Dizziness, %

Insomnia, %

Proteinuria, %

Study 1490

ARs (All Grades) Reported in ≥2% of Adults Who Received BIKTARVY

BIKTARVY (Baseline-W240) (n=320)

Switched from DTG+FTC/TAF to BIKTARVY (W144-240) (n=265)

Headache, %

Diarrhea, %

Nausea, %

Fatigue, %

Abnormal dreams, %

Dizziness, %

Insomnia, %

Proteinura, %

Weight change through Week 144

Study 1489^1,2

In Study 1489, no adults discontinued BIKTARVY due to weight-related AEs through Week 144^1,2

In Study 1489, an AE of weight increase was reported for BIKTARVY (2.9%), ABC/DTG/3TC (4.1%), and weight decrease for BIKTARVY (1.9%), ABC/DTG/3TC (1.6%)²

Study 1490^1,2

In Study 1490, no adults discontinued BIKTARVY due to weight-related AEs through Week 144^1,2

In Study 1490, an AE of weight increase was reported for BIKTARVY (2.5%), DTG+FTC/TAF (3.1%), and weight decrease for BIKTARVY (0.9%), DTG+FTC/TAF (0.9%)²

Weight change through Week 240^3-5

In the OLE through Week 240, 3 study participants discontinued due to a weight-related adverse event attributed to study drug.^3-5
Median cumulative weight gain from baseline to Week 240, including the OLE, was 6.1 kg for participants initially randomized to BIKTARVY³
Cumulative median weight changes at Week 240 were numerically similar for all treatment groups⁴
At Week 144, significantly lower median weight changes were observed in participants treated with DTG/ABC/3TC vs DTG+FTC/TAF: 3.5 kg vs 5.0 kg (P = 0.02)^4,5
In the OLE from Week 144 to Week 240, greater median weight changes were observed in participants who switched to BIKTARVY from DTG/ABC/3TC vs those who switched from DTG+FTC/TAF: 2.4 kg vs 1.3 kg (P = 0.01)^4,5

3TC, lamivudine; ABC, abacavir; AE, adverse event; DTG, dolutegravir; FTC, emtricitabine; OLE, open-label extension; TAF, tenofovir alafenamide.

References: 1. Orkin C, DeJesus E, Sax PE, et al. Fixed-dose combination bictegravir, emtricitabine, and tenofovir alafenamide versus dolutegravir-containing regimens for initial treatment of HIV-1 infection: week 144 results from two randomised, double-blind, multicentre, Phase 3, non-inferiority trials. Lancet HIV. 2020;7(6):e389-e400. 2. Data on file. Gilead Sciences, Inc. 3. Wohl DA, Pozniak A, Workowski K, et al. B/F/TAF five-year outcomes in treatment-naïve adults. Poster presented at: Conference on Retroviruses and Opportunistic Infections; February 12-16, 2022; Virtual. Poster 494. 4. Orkin C, Antinori A, Rockstroh J, et al. Outcomes after switching from 144 weeks of blinded DTG/ABC/3TC or DTG+F/TAF to 96 weeks of open-label B/F/TAF. Poster presented at: HIV Glasgow 2022; October 23-26, 2022; Glasgow UK. Poster P088. 5. Orkin C, Antinori A, Rockstroh J, et al. Switch to bictegravir/emtricitabine/tenofovir alafenamide from dolutegravir-based therapy. AIDS. 2024;38:983-991.

Study 1489: Changes in hip BMD through Week 144¹

BMD declines of ≥7% at the total hip were experienced in 1% of BIKTARVY participants and 2% of ABC/DTG/3TC participants at Week 48, in 2% of BIKTARVY participants and 3% of ABC/DTG/3TC participants at Week 96, and in 5% of BIKTARVY participants and 4% of ABC/DTG/3TC participants at Week 144²

– Analysis was conducted in a subset of the study population (n=597)²

In the OLE:

A mean change of −0.3% was observed from baseline at Week 240 (n=197)³
BMD declines of ≥7% at the total hip were experienced in 8% of participants (n=15/197) at Week 240²
Includes only participants initially randomized to BIKTARVY at Week 0, as these participants took BIKTARVY for 240 weeks³

The long-term clinical significance of changes in BMD is not known.

BMD was assessed at baseline, Week 24, Week 48, Week 96, Week 144, Week 192, and Week 240 by dual-energy x-ray absorptiometry (DXA) scans^2,3

Study 1489: Changes in lumbar spine BMD through Week 144¹

BMD declines of ≥5% at the lumbar spine were experienced in 10% of BIKTARVY participants and 6% of ABC/DTG/3TC participants at Week 48, in 12% of BIKTARVY participants and 6% of ABC/DTG/3TC participants at Week 96, and in 12% of BIKTARVY participants and 8% of ABC/DTG/3TC participants at Week 144²

– Analysis was conducted in a subset of the study population (n=603)²

In the OLE:

A mean change of −0.2% was observed from baseline at Week 240 (n=201)³
BMD declines of ≥5% at the lumbar spine were experienced in 20% of participants (n=41/201) at Week 240²
Includes only participants initially randomized to BIKTARVY at Week 0, as these participants took BIKTARVY for 240 weeks³

The long-term clinical significance of changes in BMD is not known.

BMD was assessed at baseline, Week 24, Week 48, Week 96, Week 144, Week 192, and Week 240 by dual-energy x-ray absorptiometry (DXA) scans^2,3

BMD was measured only in Study 1489

BMD, bone mineral density; CI, confidence interval; FTC, emtricitabine; OLE, open-label extension.

Changes in eGFR_CG and serum creatinine through Week 144

Study 1489^1-3

Median serum creatinine increased by 0.1 mg/dL in the BIKTARVY arm and by 0.11 mg/dL in the ABC/DTG/3TC arm from baseline¹

In the OLE for Study 1489 in participants who were initially randomized to BIKTARVY at Week 0 and continued through Week 240:

A median eGFR change of −8.2 mL/min from baseline was observed at Week 240 (n=213)^4,5
Median serum creatinine increased by 0.11 mg/dL in participants from baseline through Week 240⁵

In participants who switched from ABC/DTG/3TC to BIKTARVY at Week 144 through Week 240:

A median eGFR change of +2.0 mL/min from Week 144 was observed at Week 240 (n=217)⁶

The long-term clinical significance of changes in eGFR is not known.

Study 1490^1,7,8

Median serum creatinine increased by 0.11 mg/dL in the BIKTARVY arm and by 0.12 mg/dL in the DTG+FTC/TAF arm from baseline¹

In the OLE for Study 1490 in participants who were initially randomized to BIKTARVY at Week 0 and continued through Week 240:

A median eGFR change of -8.5 mL/min from baseline was observed at Week 240 (n=217)^4,5
Median serum creatinine increased by 0.11 mg/dL in patients from baseline through Week 240⁵

In participants who switched from DTG+FTC/TAF to BIKTARVY at Week 144 through Week 240:

A median eGFR change of +1.3 mL/min from Week 144 was observed at Week 240 (n=233)⁶

The long-term clinical significance of changes in eGFR is not known.

3TC, lamivudine; ABC, abacavir; DTG, dolutegravir; eGFR_CG, estimated glomerular filtration rate (Cockcroft-Gault); FTC, emtricitabine; OLE, open-label extension; TAF, tenofovir alafenamide.

Median change in fasting lipids from baseline through Week 144

Study 1489¹

BIKTARVY Baseline: (n=305) Week 144: (n=247)

ABC/ DTG/3TC Baseline: (n=305) Week 144: (n=256*)

Total-C (mg/dL)

+14

+10

LDL-C (mg/dL)

+21

+14

HDL-C (mg/dL)

Triglycerides (mg/dL)

Total-C:HDL-C ratio

-0.1

-0.3

Study 1490¹

BIKTARVY Baseline: (n=314) Week 144: (n=256)

DTG+ FTC/TAF Baseline: (n=321) Week 144: (n=274)

Total-C (mg/dL)

+12

LDL-C (mg/dL)

+19

HDL-C (mg/dL)

Triglycerides (mg/dL)

Total-C:HDL-C ratio

0.0

-0.1

*Except for triglycerides, which are (n=255) at Week 144.

In the OLE for Study 1489:

In participants who were initially randomized to BIKTARVY at Week 0 and continued through Week 240, median changes in fasting lipids from baseline were as follows (n=202): Total-C: +20 mg/dL, LDL-C: +22 mg/dL, HDL-C: +5 mg/dL, Triglycerides: +11 mg/dL, Total-C:HDL-C ratio: 0.0²
In participants who switched from ABC/DTG/3TC to BIKTARVY at Week 144 through Week 240, median changes in fasting lipids from baseline were as follows (n=215)^†: Total-C: +7 mg/dL, LDL-C: +2 mg/dL, HDL-C: 0.0 mg/dL, Triglycerides: -3 mg/dL, Total-C:HDL-C ratio: +0.1²

^†Except for triglycerides, which are (n=213) at Week 240.

In the OLE for Study 1490:

In participants who were initially randomized to BIKTARVY at Week 0 and continued through Week 240, median changes in fasting lipids from baseline were as follows (n=208): Total-C: +22 mg/dL, LDL-C: +17 mg/dL, HDL-C: +4 mg/dL, Triglycerides: +10 mg/dL, Total-C:HDL-C ratio: +0.1²
In participants who switched from DTG+FTC/TAF to BIKTARVY at Week 144 through Week 240, median changes in fasting lipids from baseline were as follows (n=225): Total-C: +5 mg/dL, LDL-C: -2 mg/dL, HDL-C: +1 mg/dL, Triglycerides: +2 mg/dL, Total-C:HDL-C ratio: -0.1²

Lab abnormalities were observed with both BIKTARVY and comparators through Week 144

Study 1489^1,3

Reported in ≥2% (Grades 3-4) of Treatment‐Naïve Adults Who Received BIKTARVY

BIKTARVY (n=314)

ABC/ DTG/ 3TC (n=315)

Amylase (>2.0 x ULN)

ALT (>5.0 x ULN)

AST (>5.0 x ULN)

Creatine kinase (≥10.0 x ULN)

Neutrophils (<750 mm³)

LDL-cholesterol (fasted) (>190 mg/dL)

Lipase (>3.0 x ULN)^‡

GGT (>5.0 x ULN)

Study 1490^1,3

Reported in ≥2% (Grades 3-4) of Treatment‐Naïve Adults Who Received BIKTARVY

BIKTARVY (n=320)

DTG+FTC/TAF (n=325)

Amylase (>2.0 x ULN)

ALT (>5.0 x ULN)

AST (>5.0 x ULN)

Creatine kinase (≥10.0 x ULN)

Neutrophils (<750 mm³)

LDL-cholesterol (fasted) (>190 mg/dL)

Lipase (>3.0 x ULN)^‡

<1%

GGT (>5.0 x ULN)

Lab abnormalities through Week 240

Study 1489²

Reported in ≥2% (Grades 3-4) of Treatment-Naïve Adults Initially Randomized at Week 0 and Continued Through Week 240

BIKTARVY (n=314)

Amylase (increased)

ALT (increased)

AST (increased)

Creatine kinase (increased)

12%

Lipase (increased)^‡

20%

Neutrophils (decreased)

Serum glucose (fasting, hyperglycemia)

Serum glucose (nonfasting, hyperglycemia)

Total cholesterol (fasting, hypercholesterolemia)

LDL cholesterol (fasting, increased)

Urine glucose (glycosuria)

Urine RBC (hematuria, quantitative or dipstick)

Study 1490²

Reported in ≥2% (Grades 3-4) of Treatment-Naïve Adults Initially Randomized at Week 0 and Continued Through Week 240

BIKTARVY (n=320)

Amylase (increased)

ALT (increased)

AST (increased)

Creatine kinase

10%

Lipase (increased)^‡

Neutrophils (decreased)

Serum glucose (fasting, hyperglycemia)

Serum glucose (nonfasting, hyperglycemia)

Total cholesterol (fasting, hypercholesterolemia)

LDL cholesterol (fasting, increased)

Urine glucose (glycosuria)

Urine RBC (hematuria, quantitative or dipstick)

Study 1489^2,4,5

Reported in ≥2% (Grades 3-4) of Adults Switched to BIKTARVY at Week 144 Through Week 240

ABC/DTG/ 3TC switched to BIKTARVY (n=254)

Amylase (increased)

AST (increased)

Creatine kinase (increased)

Lipase (increased)^‡

11%

Serum glucose (fasting, hyperglycemia)

Serum glucose (nonfasting, hyperglycemia)

LDL cholesterol (fasting, increased)

Urine glucose (glycosuria)

Study 1490^2,4,5

Reported in ≥2% (Grades 3-4) of Adults Switched to BIKTARVY at Week 144 Through Week 240

DTG+ FTC/TAF switched to BIKTARVY (n=265)

Amylase (increased)

AST (increased)

Creatine kinase (increased)

Lipase (increased)^‡

21%

Serum glucose (fasting, hyperglycemia)

Serum glucose (nonfasting, hyperglycemia)

LDL cholesterol (fasting, increased)

Urine glucose (glycosuria)

ALT (increased)

Triglycerides (increased)

<1%

^‡Lipase test performed only in participants with serum amylase > 1.5 x ULN.

BIKTARVY is not recommended in patients with severe hepatic impairment (Child-Pugh Class C). For patients weighing ≥25 kg, BIKTARVY is not recommended in patients with severe renal impairment (estimated CrCl <30 mL/min) except in virologically suppressed patients with CrCl <15 mL/min on chronic hemodialysis. BIKTARVY is not recommended for patients weighing ≥14 kg to <25 kg with CrCl <30 mL/min.

ALT, alanine aminotransferase; AST, aspartate aminotransferase; CrCl, creatinine clearance; GGT, gamma-glutamyl transferase; HDL, high-density lipoprotein; LDL, low-density lipoprotein; OLE, open-label extension; ULN, upper limit of normal.

References: 1. Orkin C, DeJesus E, Sax PE, et al. Fixed-dose combination bictegravir, emtricitabine, and tenofovir alafenamide versus dolutegravir-containing regimens for initial treatment of HIV-1 infection: week 144 results from two randomised, double-blind, multicentre, Phase 3, non-inferiority trials. Lancet HIV. 2020;7(6):e389-e400. 2. Data on file. Gilead Sciences, Inc. 3. BIKTARVY. Prescribing information. Gilead Sciences, Inc.; 2024. 4. Orkin C, Antinori A, Rockstroh J, et al. Outcomes after switching from 144 weeks of blinded DTG/ABC/3TC or DTG+F/TAF to 96 weeks of open-label B/F/TAF. Poster presented at: HIV Glasgow 2022; October 23-26, 2022; Glasgow UK. Poster P088. 5. Orkin C, Antinori A, Rockstroh J, et al. Switch to bictegravir/emtricitabine/tenofovir alafenamide from dolutegravir-based therapy. AIDS. 2024;38(suppl):983-991.

Studies 1489 and 1490: Proven long-term safety and tolerability profile in a post hoc analysis of participants with high baseline viral load and low CD4 cell count through Week 240⁶

ARs (All Grades) Reported in ≥2% of Adults Initially Randomized to BIKTARVY

VL 100,000-400,000 copies/mL (n=99)

VL >400,000 copies/mL (n=20)

CD4 >200 cells/µL (n=80)

VL ≥100,000 copies/mL & CD4 <200 cells/µL (n=39)

Headache, %

Diarrhea, %

Nausea, %

Fatigue, %

Dizziness, %

Insomnia, %

Study drug-related SAE, %

Leading to premature study drug discontinuation, %

Study drug-related, %

5 cases of IRIS were reported: all had BL VL <100,000 copies/mL, 2 had CD4 <200 cells/µL, and all occurred within the first 48 weeks and resolved with treatment⁶
The most common study drug-related AEs were nausea, headache, and diarrhea; there were no drug-related serious adverse events in the high viral load or low CD4 subgroups⁶

Adverse Reactions in Virologically Suppressed Participants

Studies 1844 and 1878: Proven safety and tolerability profile in virologically suppressed adults through Week 48^4,7,8

Study 1844

ARs (All Grades) Reported in ≥ 2% of Adults Who Received BIKTARVY^†

BIKTARVY (n=282)

ABC/ DTG/3TC (n=281)

Headache, %

Flatulence, %

Nausea, %

Diarrhea, %

Study 1878

ARs (All Grades) Reported in ≥ 2% of Adults Who Received BIKTARVY*

BIKTARVY (n=290)

ATV- or
DRV-based
Regimen (n=287)

Headache, %

Flatulence, %

Nausea, %

Diarrhea, %

^†Frequencies of ARs are based on all adverse events attributed to trial drugs by the investigator. No ARs of Grade 2 or higher occurred in >1% of participants treated with BIKTARVY.²

The majority of ARs associated with BIKTARVY were Grade 1 in Study 1844 (58%) and in Study 1878 (76%)²
The safety profile of BIKTARVY in the extension phases through Week 96 and Week 168 was similar to that in the randomized phases of Studies 1878 and 1844, respectively^9,10
Overall, the safety profile of BIKTARVY in virologically suppressed adults was similar to that in treatment-naïve adults⁴
The most common ARs (incidence ≥5%; all grades) in clinical trials of treatment-naïve adults who received BIKTARVY were diarrhea, nausea, and headache⁴

Weight change through Week 48¹

Weight change through Week 120^1,†,‡

In Study 1844, no adults discontinued BIKTARVY due to weight-related adverse events through Week 168^1,2

In participants who continued on or switched to BIKTARVY during OLE, changes from baseline in body weight were consistent with changes reported through Week 48¹

*Shown for reference.

^†Low participant numbers out to Week 168 (n=12); median change at Week 168: +2.1 kg.

^‡This analysis includes participants initially randomized to BIKTARVY and participants who switched to BIKTARVY during the OLE.

3TC, lamivudine; ABC, abacavir; DTG, dolutegravir; IQR, interquartile range; OLE, open-label extension.

References: 1. Brar I, Ruane P, Ward D, et al. Long-term follow-up after a switch to bictegravir, emtricitabine, and tenofovir alafenamide from dolutegravir, abacavir, and lamivudine. Poster presented at: IDWeek; October 21-25, 2020; Virtual. Poster 1028. 2. Molina J-M, Ward D, Brar I, et al. Switching to fixed-dose bictegravir, emtricitabine, and tenofovir alafenamide from dolutegravir plus abacavir and lamivudine in virologically suppressed adults with HIV-1: 48 week results of a randomised, double-blind, multicentre, active-controlled, Phase 3, non-inferiority trial. Lancet HIV. 2018;5(7):e357-e365.

Weight change through Week 48^1,2

Weight change through Week 96^1,*

In Study 1878, no adults discontinued BIKTARVY due to weight-related adverse events through Week 96^1,3

In participants who continued on or switched to BIKTARVY during the extension phase, changes from baseline in body weight were consistent with changes reported through Week 48¹

*This analysis includes participants initially randomized to BIKTARVY and participants who switched to BIKTARVY during the extension phase.

IQR, interquartile range; SBR, stayed on baseline regimen.

References: 1. Rockstroh J, Molina J-M, Post F, et al. Long-term follow-up after a switch to bictegravir, emtricitabine, tenofovir alafenamide (B/F/TAF) from a boosted protease inhibitor-based regimen. Poster presented at: HIV Drug Therapy Glasgow 2020; October 5-8, 2020; Virtual. Poster P036. 2. Data on file. Gilead Sciences, Inc. 3. Daar ES, DeJesus E, Ruane P, et al. Efficacy and safety of switching to fixed-dose bictegravir, emtricitabine, and tenofovir alafenamide from boosted protease inhibitor-based regimens in virologically suppressed adults with HIV-1: 48 week results of a randomised, open-label, multicentre, Phase 3, non-inferiority trial. Lancet HIV. 2018;5(7):e347-e356.

Study 4030: Proven safety and tolerability profile in virologically suppressed adults, including those with preexisting M184V/I resistance mutation through Week 48²

Study 4030

ARs (All Grades) Reported in ≥2% of Virologically Suppressed Adults

BIKTARVY (n=284)

DTG+FTC/TAF (n=281)

Abnormal dreams, %

Weight increased, %

Diarrhea, %

Headache, %

Weight change from baseline through Week 48¹

Weight changes were similar through Week 48 (P = 0.46) in adults who were randomized to BIKTARVY and those who were randomized to DTG+FTC/TAF. In Study 4030, significantly more weight gain was observed at Week 48 (P < 0.001) in participants switching from TDF-based regimens (+2.2 kg) compared with those remaining on TAF-based regimens (+0.6 kg).²

References: 1. Data on file. Gilead Sciences, Inc. 2. Sax PE, Rockstroh JK, Luetkemeyer AF, et al; GS-US-380-4030 Investigators. Switching to bictegravir, emtricitabine, and tenofovir alafenamide in virologically suppressed adults with human immunodeficiency virus. Clin Infect Dis. 2021;73 2):e485-e493.

Changes in eGFR_CG through Week 48¹

In Study 4030, median changes from baseline in eGFR were similar between groups at Week 48 (P=0.38).

There were no discontinuations due to renal-related adverse events and no cases of proximal renal tubulopathy.²

The long-term clinical significance of changes in eGFR is not known.

BIKTARVY is not recommended in patients with severe hepatic impairment (Child-Pugh Class C). For patients weighing ≥25 kg, BIKTARVY is not recommended in patients with severe renal impairment (estimated CrCl <30 mL/min) except in virologically suppressed patients with CrCl <15 mL/min on chronic hemodialysis. BIKTARVY is not recommended for patients weighing ≥14 kg to <25 kg with CrCl <30 mL/min.³

Median changes in fasting lipids from baseline through Week 48¹

Study 4030

BIKTARVY Baseline (n=280) Week 48 (n=252)

DTG+FTC/TAF Baseline (n=278) Week 48 (n=249)

Total cholesterol (mg/dL)

-1

Direct LDL (mg/dL)

HDL (mg/dL)

Total cholesterol to HDL ratio

-0.1

0.0

Triglycerides (mg/dL)

Lab abnormalities were observed with both BIKTARVY and comparators through Week 48¹

Study 4030

Reported in ≥2% (Grades 3-4) of Participants in Either Group

BIKTARVY (n=284)

DTG+FTC/TAF (n=281)

Amylase (increased)

Creatine kinase (increased)

LDL (fasting increased)

Lipase (increased)*

17%

20%

Glycosuria^†

*Lipase test performed only in participants with serum amylase >1.5 x ULN.

^†Glycosuria abnormalities were all reported in the setting of hyperglycemia.

Reference: 1. Sax PE, Rockstroh JK, Luetkemeyer AF, et al; GS-US-380-4030 Investigators. Switching to bictegravir, emtricitabine, and tenofovir alafenamide in virologically suppressed adults with human immunodeficiency virus. Clin Infect Dis. 2021;73(2):e485-e493.

Study 1961: Proven safety and tolerability profile in virologically suppressed adult women through Week 48^2,11

Study 1961

ARs (All Grades) Reported in >1 Virologically Suppressed Adult Woman Who Received BIKTARVY

BIKTARVY (n=234)

INSTI- or PI- based Regimen (n=236)

Iron deficiency anemia, %

Nausea, %

Vomiting, %

Through Week 48, no woman discontinued due to AEs in either treatment arm¹¹

The safety profile of BIKTARVY in the extension phase through Week 96 was similar to that in the randomized phase of Study 1961¹²

Study 4449: Proven safety and tolerability profile in virologically suppressed adults aged ≥65 years through Week 96^2,13,14

Study 4449

ARs (All Grades) Reported in ≥1% of Virologically Suppressed Adults Aged ≥65 Years Through Week 96^§

BIKTARVY (N=86)

Abdominal discomfort, %

1.2

Abnormal feces, %

1.2

Constipation, %

1.2

Dizziness, %

1.2

Gamma-glutamyl transferase increased, %

1.2

Headache, %

1.2

Insomnia, %

1.2

Irritability, %

1.2

Myalgia, %

1.2

Pruritus, %

1.2

Sleep disorder, %

1.2

Tendonitis, %

1.2

Weight increased, %

1.2

^§ Frequencies of ARs are based on all adverse events attributed to trial drugs by the investigator.

Through Week 96, there were 2 (2.3%) Grade 3 study drug-related AEs in adults aged ≥65 years¹⁴

Study 1474: Proven safety and tolerability profile in virologically suppressed children and adolescents^2,15-17

Study 1474: Cohorts 1 and 2 Through Week 96

ARs (All Grades) Reported in >1 Participant

Aged ≥6 to
<18 Years
Weighing ≥25 kg (n=100)

Abdominal discomfort, %

Neutropenia, %

Study 1474: Cohort 3 Through Week 48

ARs (All Grades) Reported in >1 Participant

Aged ≥2 Years
Weighing ≥14 kg
to <25 kg (n=22)

Abdominal discomfort, %

Neutropenia, %

The other ARs that occurred in single participants were similar to those seen in adults.^4,16,17

BRAAVE: Proven safety and tolerability profile in virologically suppressed Black American Adults through Week 72^2,18

ARs at Week 24 (All Grades) Reported in ≥1% of Adults Who Switched to BIKTARVY²

BIKTARVY (n=330)

SBR (No Switch at Baseline) (n=165)

Diarrhea, %

Flatulence, %

Abnormal dreams, %

Headache, %

Nausea, %

The most common ARs reported (all grades) in ≥1% of participants on BIKTARVY through Week 48 (n=493) were weight increase (2%), flatulence (1%), abnormal dreams (1%), diarrhea (1%), headache (1%)²
The most common ARs in the extension through Week 72 were similar to those observed in participants who received BIKTARVY through Week 48²

Weight change from baseline through Week 72^1-3

Weight Change Through Week 24

Weight Change Through Week 72

Weight changes through Week 24 were similar between adults who were randomized to BIKTARVY and those who stayed on baseline regimen^1-3

In BRAAVE, no adults discontinued due to weight-related adverse events through Week 72³

*From 2-sided Wilcoxon rank-sum test comparing BIKTARVY vs SBR at Week 24.

SBR, stayed on baseline regimen.

References: 1. Hagins D, Kumar P, Saag M, et al. Switching to bictegravir/emtricitabine/tenofovir alafenamide in Black Americans with HIV-1: a randomized Phase 3b, multicenter, open-label study. J Acquir Immune Defic Syndr. 2021;88(1):86-95. 2. Hagins DP, Kumar PN, Saag M, et al. Randomized switch to B/F/TAF in African American adults with HIV. Abstract presented at: Conference on Retroviruses and Opportunistic Infections; March 8-11, 2020; Boston, MA. Abstract 36. 3. Kumar P, Stephens JL, Wurapa AK, et al. Week 72 outcomes and COVID-19 impact from the BRAAVE 2020 study: a randomized switch to B/F/TAF in Black American adults with HIV. Poster presented at: International AIDS Society Conference on HIV Science; July 18-21, 2021; Virtual. Poster PEB161.

Weight changes through Week 72¹

SBR vs BIKTARVY

Delayed Switch*

More weight gain was observed at Week 72 in participants switching from TDF- or ABC-based regimens compared with those remaining on a TAF-based regimen¹

*Baseline for delayed switch: time of first BIKTARVY dose.

^†From 2-sided Wilcoxon rank-sum test comparing baseline regimens containing TAF vs TDF.

^‡Comparing baseline regimens containing TAF vs ABC.

ABC, abacavir; NRTI, nucleoside reverse transcriptase inhibitor; SBR, stayed on baseline regimen; TAF, tenofovir alafenamide; TDF, tenofovir disoproxil fumarate.

Reference: 1. Kumar P, Stephens JL, Wurapa AK, et al. Week 72 outcomes and COVID-19 impact from the BRAAVE 2020 study: a randomized switch to B/F/TAF in Black American adults with HIV. Poster presented at: International AIDS Society Conference on HIV Science; July 18-21, 2021; Virtual. Poster PEB161.

Discontinuations In Treatment-Naïve Adults

Low rates of discontinuation due to adverse events in treatment-naïve adults^1-3,5

Treatment-Naïve Adults

Through Week 144¹

Study 1489

0.0^%

BIKTARVY
(n=314)

1.6^%

ABC/DTG/3TC
(n=315)

Study 1490

1.9^%

BIKTARVY
(n=320)

1.8^%

DTG+FTC/TAF
(n=325)

Through Week 240 (including OLE)
in participants initially randomized to BIKTARVY³

Study 1489

1.3^%

BIKTARVY
(n=314)

Study 1490

1.9^%

BIKTARVY
(n=320)

In participants who switched to BIKTARVY
at Week 144 through Week 240⁵

Study 1489

0.8^%

BIKTARVY
(n=254)

Study 1490

0.0^%

BIKTARVY
(n=265)

No treatment-naïve adults discontinued BIKTARVY due to renal-, hepatic-, or bone-related adverse events through Week 240^1,3,5

Prior to or when initiating BIKTARVY and during therapy, assess serum creatinine, estimated creatinine clearance, urine glucose, and urine protein in all patients as clinically appropriate. In patients with chronic kidney disease, assess serum phosphorus.⁴
BIKTARVY is not recommended in patients with severe hepatic impairment (Child-Pugh Class C). For patients weighing ≥25 kg, BIKTARVY is not recommended in patients with severe renal impairment (estimated CrCl <30 mL/min) except in virologically suppressed patients with CrCl <15 mL/min on chronic hemodialysis. BIKTARVY is not recommended for patients weighing ≥14 kg to <25 kg with CrCl <30 mL/min.⁴

Discontinuations In Virologically Suppressed Participants

Low rates of discontinuation due to adverse events in virologically suppressed participants^2,4,7-20

Virologically Suppressed Adults

Through Week 48^2,7,8

Study 1844

2.1^%

BIKTARVY
(n=282)

0.7^%

ABC/DTG/3TC
(n=281)

Study 1878

0.7^%

BIKTARVY
(n=290)

0.3^%

ATV- or DRV-based Regimen
(n=287)

Through Week 168
(including OLE)⁹

Study 1844

1.3^%

BIKTARVY
(n=547)

Through Week 96 (including Extension)¹⁰

Study 1878

1.1^%

BIKTARVY
(n=534)

Virologically Suppressed Adults, Including Those With Known or Suspected Preexisting M184V/I Resistance Mutation

Through Week 48¹⁹

Study 4030

2.1^%

BIKTARVY
(n=284)

2.1^%

DTG+FTC/TAF
(n=281)

No discontinuations due to renal-, hepatic-, bone-, or weight-related adverse events through Week 48.¹⁹

Virologically Suppressed Adult Women

Through Week 48¹¹

Study 1961

0.0^%

BIKTARVY
(n=234)

0.0^%

INSTI- or PI-based Regimen
(n=236)

Through Week 96 (including Extension)¹²

Study 1961

0.2^%

BIKTARVY
(n=462)

Virologically Suppressed Adults Aged ≥65 Years

Through Week 96¹⁴

Study 4449

5.8^%

BIKTARVY
(n=86)

Virologically Suppressed Children and Adolescents

Cohorts 1 & 2 Through Week 96^15,16

Study 1474

0.0^%

Aged ≥12 to <18 years, ≥35 kg Cohort 1 (n=50)

2.0^%

Aged ≥6 to <12 years, ≥25 kg Cohort 2 (n=50)

Cohort 3 Through Week 48¹⁷

Study 1474

0.0^%

Aged ≥2 years, ≥14 kg to <25 kg Cohort 3 (n=22)

Virologically Suppressed Black Americans

Through Week 24²⁰

BRAAVE

2.1^%

BIKTARVY
(n=330)

0.0^%

SBR
(n=165)

Through Week 72 (including Extension)¹⁸

BRAAVE

2.4^%

BIKTARVY
(n=493)

No virologically suppressed participants discontinued BIKTARVY due to bone-related adverse events at any clinical trial time points^2,4,7-20

In Study 1961, 1 discontinuation occurred due to a hepatic-related adverse event found to be related to study drug^2,12
In BRAAVE, 1 discontinuation occurred due to a renal-related adverse event, which was not reported to be related to study drug¹⁸

Prior to or when initiating BIKTARVY and during therapy, assess serum creatinine, CrCl, urine glucose, and urine protein in all patients as clinically appropriate. In patients with chronic kidney disease, assess serum phosphorus.⁴

Contraindications & DDIs

Dosing & Administration

Please see full Prescribing Information for BIKTARVY^® and DESCOVY^®, including BOXED WARNINGS.

3TC, lamivudine; ABC, abacavir; AE, adverse event; ATV, atazanavir; BL, baseline; CD4, cluster of differentiation 4; CrCl, creatinine clearance; DRV, darunavir; DTG, dolutegravir; FTC, emtricitabine; INSTI, integrase strand transfer inhibitor; IRIS, immune reconstitution inflammatory syndrome; PI, protease inhibitor; SAE, serious adverse event; SBR, stayed on baseline regimen; TAF, tenofovir alafenamide; TDF, tenofovir disoproxil fumarate; VL, viral load.

References: 1. Orkin C, DeJesus E, Sax PE, et al. Fixed-dose combination bictegravir, emtricitabine, and tenofovir alafenamide versus dolutegravir-containing regimens for initial treatment of HIV-1 infection: week 144 results from two randomised, double-blind, multicentre, Phase 3, non-inferiority trials. Lancet HIV. 2020;7(6):e389-e400. 2. Data on file. Gilead Sciences, Inc. 3. Wohl DA, Pozniak A, Workowski K, et al. B/F/TAF five-year outcomes in treatment-naïve adults. Poster presented at: Conference on Retroviruses and Opportunistic Infections; February 12-16, 2022; Virtual. Poster 494. 4. BIKTARVY. Prescribing information. Gilead Sciences, Inc.; 2024. 5. Orkin C, Antinori A, Rockstroh J, et al. Outcomes after switching from 144 weeks of blinded DTG/ABC/3TC or DTG+F/TAF to 96 weeks of open-label B/F/TAF. Poster presented at: HIV Glasgow 2022; October 23-26, 2022; Glasgow UK. Poster P088. 6. Ramgopal M, Wurapa A, Baumgarten A, et al. 5-year outcomes of bictegravir/emtricitabine/tenofovir alafenamide as initial treatment of HIV-1 in adults with high baseline HIV-1 RNA and/or low CD4 count in two Phase 3 randomized clinical trials. Presented at: Infectious Disease Week 2022; October 19-23, 2022; Washington, DC. Poster 1251. 7. Molina J-M, Ward D, Brar I, et al. Switching to fixed-dose bictegravir, emtricitabine, and tenofovir alafenamide from dolutegravir plus abacavir and lamivudine in virologically suppressed adults with HIV-1: 48 week results of a randomised, double-blind, multicentre, active-controlled, Phase 3, non-inferiority trial. Lancet HIV. 2018;5(7):e357-e365. 8. Daar ES, DeJesus E, Ruane P, et al. Efficacy and safety of switching to fixed-dose bictegravir, emtricitabine, and tenofovir alafenamide from boosted protease inhibitor-based regimens in virologically suppressed adults with HIV-1: 48 week results of a randomised, open-label, multicentre, Phase 3, non-inferiority trial. Lancet HIV. 2018;5(7):e347-e356. 9. Brar I, Ruane P, Ward D, et al. Long-term follow-up after a switch to bictegravir, emtricitabine, and tenofovir alafenamide from dolutegravir, abacavir, and lamivudine. Poster presented at: IDWeek; October 21-25, 2020; Virtual. Poster 1028. 10. Rockstroh J, Molina J-M, Post F, et al. Long-term follow-up after a switch to bictegravir, emtricitabine, tenofovir alafenamide (B/F/TAF) from a boosted protease inhibitor-based regimen. Poster presented at: HIV Drug Therapy Glasgow 2020; October 5-8, 2020; Virtual. Poster P036. 11. Kityo C, Hagins D, Koenig E, et al. Switching to fixed-dose bictegravir, emtricitabine, and tenofovir alafenamide (B/F/TAF) in virologically suppressed HIV-1 infected women: a randomized, open-label, multicenter, active-controlled, Phase 3, noninferiority trial. J Acquir Immune Defic Syndr. 2019;82(3):321-328. 12. Kityo C, Hagins D, Koenig E, et al. Longer-term (96-week) efficacy and safety of switching to bictegravir, emtricitabine, and tenofovir alafenamide (B/F/TAF) in women. Oral presentation at: International AIDS Society Conference on HIV Science 2019; July 21-24, 2019; Mexico City, Mexico. Abstract MOAB0106. 13. Maggiolo F, Rizzardini G, Molina J-M, et al. Bictegravir/emtricitabine/tenofovir alafenamide in virologically suppressed people with HIV aged ≥65 years: week 48 results of a Phase 3b, open-label trial. Infect Dis Ther. 2021;10(2):775-788. 14. Maggiolo F, Rizzardini G, Molina J-M, et al. Bictegravir/emtricitabine/tenofovir alafenamide in older individuals with HIV: Results of a 96-week, Phase 3b, open- label, switch trial in virologically suppressed people ≥65 years of age. HIV Med. 2023;24(1):27-36. 15. Gaur AH, Cotton MF, Rodriguez CA, et al. Fixed-dose combination bictegravir, emtricitabine, and tenofovir alafenamide in adolescents and children with HIV: week 48 results of a single-arm, open-label, multicentre, phase 2/3 trial. Lancet Child Adolesc Health. 2021;5(9):642-651. 16. Natukunda E, Rodriguez CA, McGrath EJ, et al. B/F/TAF in virologically suppressed adolescents and children: two-year outcomes in 6 to <18 year olds and six-month outcomes in toddlers. Abstract presented at: International Workshop on HIV & Pediatrics. July 16-17, 2021; Virtual. Abstract 2. 17. Rodriguez CA. Strehlau R, Chokephaibulkit K, et al. One year outcome of bictegravir/emtricitabine/tenofovir alafenamide (B/F/TAF) in virologically suppressed children ≥ 2 years weighing 14 to < 25 kg. Oral presentation at: International Workshop on HIV & Pediatrics 2022; July 27-28, 2022; Montreal, Quebec, Canada. Oral 2. 18. Kumar P, Stephens JL, Wurapa AK, et al. Week 72 outcomes and COVID-19 impact from the BRAAVE 2020 study: a randomized switch to B/F/TAF in Black American adults with HIV. Poster presented at: International AIDS Society Conference on HIV Science; July 18-21, 2021; Virtual. Poster PEB161. 19. Sax PE, Rockstroh JK, Luetkemeyer AF, et al; GS-US-380-4030 Investigators. Switching to bictegravir, emtricitabine, and tenofovir alafenamide in virologically suppressed adults with human immunodeficiency virus. Clin Infect Dis. 2021;73(2):e485-e493. 20. Hagins D, Kumar P, Saag M, et al. Switching to bictegravir/emtricitabine/tenofovir alafenamide in Black Americans with HIV-1: a randomized Phase 3b, multicenter, open-label study. J Acquir Immune Defic Syndr. 2021;88(1):86-95.

INDICATION

BIKTARVY® is indicated as a complete regimen for the treatment of HIV-1 infection in adult and pediatric patients weighing ≥14 kg who have no antiretroviral (ARV) treatment history or to replace the current ARV regimen in those who are virologically suppressed (HIV-1 RNA <50 copies per mL) on a stable ARV regimen with no known or suspected substitutions associated with resistance to bictegravir or tenofovir.

INDICATION

Important Safety Information

BOXED WARNING: POST TREATMENT ACUTE EXACERBATION OF HEPATITIS B

Severe acute exacerbations of hepatitis B have been reported in patients who are coinfected with HIV-1 and HBV and have discontinued products containing emtricitabine (FTC) and/or tenofovir disoproxil fumarate (TDF), and may occur with discontinuation of BIKTARVY. Closely monitor hepatic function with both clinical and laboratory follow-up for at least several months in patients who are coinfected with HIV-1 and HBV and discontinue BIKTARVY. If appropriate, anti-hepatitis B therapy may be warranted.

Contraindications

Coadministration: Do not use BIKTARVY with dofetilide or rifampin.

Warnings and precautions

Drug interactions: See Contraindications and Drug Interactions sections. Consider the potential for drug interactions prior to and during BIKTARVY therapy and monitor for adverse reactions.
Immune reconstitution syndrome, including the occurrence of autoimmune disorders with variable time to onset, has been reported.
New onset or worsening renal impairment: Postmarketing cases of renal impairment, including acute renal failure, proximal renal tubulopathy (PRT), and Fanconi syndrome have been reported with tenofovir alafenamide (TAF)–containing products. Do not initiate BIKTARVY in patients with estimated creatinine clearance (CrCl) <30 mL/min except in virologically suppressed adults <15 mL/min who are receiving chronic hemodialysis. Patients with impaired renal function and/or taking nephrotoxic agents (including NSAIDs) are at increased risk of renal-related adverse reactions. Discontinue BIKTARVY in patients who develop clinically significant decreases in renal function or evidence of Fanconi syndrome.
Renal monitoring: Prior to or when initiating BIKTARVY and during therapy, assess serum creatinine, CrCl, urine glucose, and urine protein in all patients as clinically appropriate. In patients with chronic kidney disease, assess serum phosphorus.
Lactic acidosis and severe hepatomegaly with steatosis: Fatal cases have been reported with the use of nucleoside analogs, including FTC and TDF. Discontinue BIKTARVY if clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity develop, including hepatomegaly and steatosis in the absence of marked transaminase elevations.