Lenacapavir (LEN)

Investigational Use With Bictegravir

This document is in response to your request for information regarding the investigational use of bictegravir (BIC) with lenacapavir (LEN) for the treatment of HIV-1.

Gilead Sciences, Inc. is providing this document to you, a US healthcare professional, in response to your unsolicited request for medical information. The information in this document is about an investigational regimen, and the safety and efficacy have not been established for this combination. This document is not intended to offer an opinion regarding the safety and efficacy of this investigational regimen. This regimen has not been approved by the US FDA or any other regulatory authority for use in patients.

Summary

Clinical Data on Use of LEN With BIC

ARTISTRY-1: An ongoing phase 2/3 study is evaluating the efficacy and safety of switching to BIC + LEN vs continuing a complex ART regimen in VS PWH.1

Results from phase 2 through Week 96 have been reported.1-3

• Through Week 48, high rates of virologic suppression were maintained in each group: BIC 75 mg + LEN 25 mg, 92.2%; BIC 75 mg + LEN 50 mg, 90.4%; and complex ART regimen, 100%.1 Virologic suppression rates were similar between the complex ART regimen group and both BIC + LEN groups and between participants with and without RAMs at baseline.4
• Through Week 48, all commonly reported TEAEs (≥5% in any group) were Grade 1 or 2 in severity, except for 1 case of Grade 3 diarrhea unrelated to study drug. TEAEs led to treatment DC in 2% of participants in the BIC 75 mg + LEN 25 mg group, 1.9% in the BIC 75 mg + LEN 50 mg group, and 0% in the complex ART regimen group.1
• Among participants initially randomized to the BIC 75 mg + LEN 50 mg group, virologic suppression was maintained through Week 96 (96%; 45/47). Within this group, 25% reported Grade ≥3 AEs, and 17.3% reported SAEs.3

Results from phase 3 through Week 48 have been reported.5

• High rates of virologic suppression were maintained in each group: BIC/LEN STR 75 mg/50 mg, 96%, and complex ART regimen, 94%. BIC/LEN was non‑inferior to complex ART regimens in the maintenance of virologic suppression.
• In the BIC/LEN and complex ART regimen groups, the rates of Grade ≥3 AEs (each, 14%) and DCs due to AEs (2% vs 1%) were similar.

ARTISTRY-2: An ongoing phase 3 study is evaluating the efficacy and safety of switching from BIC/FTC/TAF to BIC/LEN STR 75 mg/50 mg vs continuing BIC/FTC/TAF in VS PWH.6

• Through Week 48, virologic suppression rates were high in both groups: BIC/LEN 75 mg/50 mg, 93.5%; BIC/FTC/TAF, 90.6%. BIC/LEN was non-inferior to BIC/FTC/TAF in maintaining virologic suppression.
• Through Week 48, in the BIC/LEN and BIC/FTC/TAF groups, the rates of Grade ≥3 AEs (9.9% vs 7.9%, respectively) and DCs due to AEs (each, 1.6%) were similar.

Clinical Data on Use of BIC With LEN

ARTISTRY-1: Switching to BIC + LEN vs Complex ART

An ongoing, randomized, multicenter, open-label, phase 2/3 study (NCT05502341) is evaluating the efficacy and safety of switching to BIC + oral LEN vs continuing their ART regimen in PWH who were receiving a complex ART regimen.1,2

Figure 1. ARTISTRY-1 Phase 2/3: Study Design1-3,5,7-9

aDue to viral resistance, intolerance, or contraindication to existing STRs. Regimens contained the following: a boosted PI or NNRTI + ≥1 other third agent from a class other than NRTIs, or ≥2 pills/day or a dosing frequency >once daily, or parenteral ART (excluding a complete long-acting injectable regimen) plus oral ART.

bOral loading doses of LEN (600 mg for 2 days) were given after participants switched from their complex ART regimen.

cAll participants reached the Week 48 timepoint and completed the end-of-randomization visit before entering the OLE phase.

Phase 2 of ARTISTRY-1

During the phase 2 portion of the study, participants were randomly assigned to switch to BIC 75 mg + LEN (25 or 50 mg; oral) or to continue their complex ART regimen. After the randomized period, participants could continue on to the extension period and receive BIC/LEN STR (Figure 1).1

Table 1. Phase 2 of ARTISTRY-1: Baseline Demographics, Disease Characteristics, and Historical Resistance Mutations2

aEthnicity data were not permitted to be collected for 1 patient each in the BIC 75 mg +LEN 25 mg and BIC 75 mg + LEN 50 mg arms.

bCalculated with the following equation: (date of first dose – start date of first HIV treatment + 1 day)/365.25.

cn=50.

dDefined as ARTs taken on Day 1 or up to 14 days before Day 1. If participants received multiple ARTs, they were counted once per participant for each drug name and ART class.

eCategories were not mutually exclusive. An alternative response was “no” or “not available.”

Refer to Figure 2 for a summary of complex ART regimens at baseline; 53 participants (41.4%) in the overall population were taking twice-daily ART, and 43%, 18.8%, 10.9%, and 27.3% were taking 2, 3, 4, or ≥5 pills/day, respectively.2

Figure 2. Phase 2 of ARTISTRY-1: Complex ART Regimens at Baseline (N=128)2

Abbreviation: AI=attachment inhibitor.

Note: Regimens in italics were the most common regimen in each category; not all regimens are shown here. Percentages do not equal 100% due to rounding.

A separate analysis assessed the presence of RAMs at baseline with historical genotypic reports, and retrospective proviral DNA analysis, which identified the following (Table 2)4:

• High level of resistance to NRTI, NNRTI, and PI classes at baseline
• High prevalence of M184V/I and TAMs at baseline

Table 2. Phase 2 of ARTISTRY-1: Baseline Preexisting Resistance Mutations, and NRTI Mutations by Treatment Group4

aNRTI, NNRTI, and PI data were available in 124 participants; INSTI data were available in 94 participants. Baseline RAM data were evaluated using historical genotypes and retrospective proviral DNA analysis.

bTAMs included M41L, D67N, K70R, L210W, T215Y/F, and K219E/N/Q/R in RT; 11% had M184V/I alone.

Efficacy, immunological, and resistance outcomes through Week 48

At Week 24, 1 participant (1.9%) in the BIC 75 mg + LEN 50 mg group and no participants in the BIC 75 mg + LEN 25 mg group or complex ART regimen group had HIV-1 RNA ≥50 c/mL (primary endpoint; FDA Snapshot algorithm).2 At Week 48, similarly high rates of virologic suppression were maintained in each group (Table 3).1

Table 3. Phase 2 of ARTISTRY-1: Rates of HIV RNA <50 c/mL (FDA Snapshot) and HIV RNA ≥50 c/mL at Week 481

aReasons for DC before Week 48: AE and participant decision (each, n=1).

bReasons for DC before Week 48: AE, death, participant decision, and investigator decision (each, n=1).

Note: P-values were for comparisons vs the complex ART regimen and are reported for descriptive purposes.

Three participants had HIV RNA levels ≥50 c/mL: 2 participants (3.9%) in the BIC 75 mg + LEN 25 mg group were resuppressed at their next study visit without a change in ART (HIV-1 RNA at Week 48: 50 c/mL and 98 c/mL, respectively), and 1 participant (1.9%) in the BIC 75 mg + LEN 50 mg group (HIV-1 RNA at Week 48: 305 c/mL) was resuppressed by Day 368 after switching treatment to DTG + MVC + LEN SUBQ. The third participant underwent a resistance analysis, and the N74T capsid mutation was noted with PhenoSense assay failure; this novel capsid polymorphism did not confer resistance to LEN and no change in BIC sensitivity occurred.1,4

At Week 48, the median (Q1, Q3) change in CD4 cell counts from baseline to Week 48 were as follows: BIC 75 mg + LEN 25 mg, +29 (−45, +96) cells/mcL; BIC 75 mg + LEN 50 mg, +48 (−59, +150) cells/mcL; complex ART regimen, +31 (−46, +111) cells/mcL.1

Through Week 48, participants with and without NRTI, NNRTI, PI, and INSTI RAMs had high rates of virologic suppression, and were similar between participants with and those without RAMs within each treatment group (Table 4).4

Table 4. Rates of HIV RNA <50 c/mL at Week 48 Overall and by Baseline Resistance Category (FDA Snapshot)1,4

aReasons for DC before Week 48: AE and participant decision (each, n=1).

bReasons for DC before Week 48: AE, death, participant decision, and investigator decision (each, n=1).

cNominal P>0.05 values for all comparisons between those with and without each RAM within each treatment group.

dOne participant discontinued treatment but was VS at their last study visit.

Note: P-values were for comparisons vs the complex ART regimen and are reported for descriptive purposes only.

Safety results through Week 48

Through Week 48, the safety profile of BIC + LEN was similar regardless of LEN dose. Common TEAEs (≥5% in any group) were Grade 1 or 2 in severity, except for 1 case of Grade 3 diarrhea, which was deemed unrelated to study drug (Table 5).1

Table 5. Phase 2 of ARTISTRY-1: TEAEs Through Week 487

aDeemed unrelated to study treatment. bGrade 1 nausea was reported on Day 1.

cGrade 3 worsening of vomiting was reported in a participant with prior history of nausea and vomiting.

dDeath was due to coronary artery disease and was deemed unrelated to study drug.

At Week 24, Grade 3 and 4 treatment-emergent laboratory abnormalities were experienced by 9.8% and 2% of participants, respectively, in the BIC 75 mg + LEN 25 mg group; by 17.3% and 5.8% in the BIC 75 mg + LEN 50 mg group; and by 32% and 0% in the complex ART regimen group.10 Laboratory abnormalities were not reported at Week 48.1,11

In general, with BIC + LEN treatment, most fasting lipid parameters decreased at Week 48, whereas increases in fasting glucose levels, body weight, and BMI were observed (Table 6). Rates of treatment‑emergent metabolic disorders are summarized in Table 6.12

Table 6. Phase 2 of ARTISTRY-1: Median Changes in Metabolic Parameters at Week 48 and Treatment-Emergent Metabolic Disorders1,12

aResults shown from participants with available data at both baseline and Week 48.

bQ1, Q3 were reported for the change from baseline to Week 48.

cReferred to grouped Standardized Medical Dictionary for Regulatory Activities Query. Disorders began at the beginning of the study and up to 60 days after stopping BIC or LEN (BIC + LEN groups) or at the beginning of the study and up to 30 days after stopping the complex ART regimen. Multiple AEs were counted once per participant.

dIncluded HTN (n=5) and hypertensive crisis (n=1). All cases were reported among participants who had abnormal BP (systolic/diastolic BP, >120/>80 mm Hg), and none were deemed to be drug related.

Efficacy and safety through Week 96: participants initially randomized to the BIC 75 mg + LEN 50 mg group3

Efficacy and safety outcomes through Week 96 were analyzed for participants who were initially randomized to the BIC 75 mg + LEN 50 mg group (n=52). Of these participants, 5 discontinued from the study during the randomized phase and 47 continued in the OLE.

Virologic suppression was maintained in 96% of participants (45/47; missing=excluded) through Week 96. The 2 participants with HIV-1 RNA ≥50 c/mL had low-level viremia (defined as HIV-1 RNA <500 c/mL) and were later resuppressed without requiring a change in their ART regimen. One of these participants met criteria for resistance testing and had assay failures for all genes. The median (Q1, Q3) change from baseline to Week 96 in CD4 count was ‑6 (‑118, 123) cells/mcL.

Through Week 96, 46 participants (88.5%) reported an AE, including 13 (25%) with a Grade ≥3 AE. Nine participants (17.3%) reported SAEs, 3 (5.8%) TRAEs were reported (atrial conduction time prolongation, decreased BP, and nausea and vomiting), and no serious TRAEs were reported. No new AEs led to treatment DCs and no deaths were reported between Week 48 and Week 96. The most common (≥10%) AEs reported through Week 96 were URTI (19.2%), COVID-19 (17.3%), HTN (13.5%), arthralgia (11.5%), and cough (11.5%). The median (Q1, Q3) change from baseline to Week 96 in weight was 0 (‑3, 2.7) kg.

Phase 3 of ARTISTRY-1

For the phase 3 portion of the study, participants were randomly assigned (2:1) to receive an STR of BIC/LEN 75 mg/50 mg (n=371) or continue their stable complex ART regimen (n=186) for 48 weeks (Figure 1). At baseline, participants had a history of resistance to multiple drug classes (Table 7).3

Table 7. Phase 3 of ARTISTRY-1: Baseline Demographics, Disease Characteristics, and Preexisting Resistance Mutations3

aLocal regulations did not permit the collection of race data for 19 participants in the BIC/LEN group and 17 in the complex ART regimen group. The “other” category included participants who were American Indian or Alaska Native, Native Hawaiian, Pacific Islander, or other.

bLocal regulations did not permit the collection of ethnicity data for 21 participants in the BIC/LEN group and 16 in the complex ART regimen group.

cn=366. dn=185. en=551.

fn=358. gn=183. hn=541.

iNot mutually exclusive.

jGrouped terms per MedDRA.

kNRTI, NNRTI, PI, and INSTI data were not available for 75, 79, 78, and 197 participants in the BIC/LEN group, respectively, and 44, 46, 50, and 100 participants in the complex ART regimen group. The denominator used for percentage calculations was the total number of participants.

Refer to Figure 3 for a summary of complex ART regimens; 77% of participants (n=427) were receiving a PI at baseline, and 75% of those participants (n=419) received a boosted PI-based regimen. At baseline, 39% of overall participants were receiving twice-daily ART, and 41%, 26%, 11%, and 22% were taking 2, 3, 4, or ≥5 pills/day, respectively.3,13

Figure 3. Phase 3 of ARTISTRY-1: Complex ART Regimens at Baseline3

Abbreviations: 3TC=lamivudine; ABC=abacavir; EI=entry inhibitor.

aOther regimens could have contained a PI.

Note: Regimens in italics were the most common regimen in each category.

Efficacy outcomes through Week 48

The median (Q1, Q3) exposure in the BIC/LEN group was 65.9 (56.6, 74) weeks and 65.9 (55.6, 73.9) weeks in the complex ART group. BIC/LEN was non-inferior to complex ART regimens in maintaining virologic suppression at Week 48 (Table 8).3 Each of the participants in the BIC/LEN group with HIV-1 RNA ≥50 c/mL at Week 48 achieved virologic resuppression or had low-level viremia without changes in their ART regimen.13

Table 8. Phase 3 of ARTISTRY-1: Rates of HIV RNA ≥50 c/mL and HIV RNA <50 c/mL (FDA Snapshot) at Week 48 in the Full Analysis Set3

aTwo-sided CI was based on Mantel-Haenszel stratum weights and Koch variance estimator and was adjusted by geographic region (US vs non-US).

bReasons for DC before Week 48: AE or death, n=7 (AEs, n=5; deaths, n=2); other reasons and last HIV-1 RNA <50 c/mL, n=5.

cReasons for DC before Week 48: other reasons and last HIV-1 RNA <50 c/mL, n=8; AE or death, n=1; and missing data but still on study drug, n=1.

CD4 counts remained stable in both groups, with a median (IQR) change in CD4 count from baseline to Week 48 of +18 (-72 to 98) cells/mcL in the BIC/LEN group and -12 (-82 to 93) cells/mcL in the complex ART group (difference in change: +19; 95% CI: -11.6 to 49.5; P=0.22).3

Through Week 48, 3 participants qualified for resistance testing and no treatment-emergent resistance was detected.3

Safety and treatment satisfaction outcomes through Week 48

Between groups, similar rates of AEs and SAEs were reported, most AEs were mild to moderate in severity, and the incidence of treatment DC due to AEs was low (Table 9). The incidence of renal-related AEs was low and the safety profile was similar between treatment groups regardless of the level of renal function.3

Table 9. Phase 3 of ARTISTRY-1: Safety Outcomes Through Week 483,9

aDM and maculopapular rash. bDM was newly diagnosed in a participant who had a high fasting glucose level at baseline. This resolved on Day 173 after a switch in ARV regimen to EFV + DRV/RTV on Day 103.

cCerebrovascular accident; DM; erectile dysfunction and worsened HTN; headache and hypoesthesia; HBV viremia; and alopecia, dizziness, worsened fatigue, headache, and nausea (each, n=1). All AEs except for hypoesthesia, HBV viremia, and cerebrovascular accident were related to BIC/LEN.

dPulmonary embolism; unrelated to study drug.

eNone of the deaths were deemed related to BIC/LEN: unknown cause (n=2), metastatic neoplasm (n=1), cardiac arrest (n=1), and respiratory failure (n=1). fn=183.

From baseline to Week 48, body weight remained stable in both groups, with a median (IQR) change of +0.6 (-1.1 to 2.6) kg in the BIC/LEN group and 0 (-2 to 2.4) kg in the complex ART regimen group.3

After switching to BIC/LEN, fasting levels of TC, LDL, and TG, and the TC:HDL ratio was observed to improve from baseline to Week 48; HDL levels remained stable (Table 10).3

Table 10. Phase 3 of ARTISTRY-1: Changes in Fasting Lipids From Baseline to Week 483,9

Abbreviation: BL=baseline.

aMedian value; presented as mg/dL. bMedian change from baseline; presented as mg/dL.

cBaseline, n=316. dBaseline, n=147.

eNominal P-values for comparison between treatment groups were estimated using the mixed model with repeated measures of the change from BL (fixed effects: treatment, visit, treatment by visit, BL value, and geographic region [US vs non-US]; random effect: participant).

HIVTSQs scores were similar between groups at baseline in the BIC/LEN (n=359; mean ± SD score, 55±10.4) and complex ART regimen groups (n=178; mean ± SD score, 55±9.4). After switching from a complex ART regimen to BIC/LEN, HIVTSQs scores improved from baseline through Week 48 (n=344; mean change, +7), whereas the score in the complex ART regimen group did not change through Week 48 (n=165). The difference in treatment satisfaction scores between groups was nominally greater at Week 48 (P<0.0001). Post-switch to BIC/LEN, the mean ± SD increase from baseline to Week 48 in HIVTSQc score was 27±9.1.3,9

DDI analysis: comparison of potential DDI liability with BIC/LEN vs other frequently prescribed complex regimens14

The DDI profiles of BIC/LEN and the 6 most commonly used complex ART regimens in the phase 3 portion of ARTISTRY-1 study were compared. The DDI profiles of each regimen with the 10 most frequently prescribed medications in the US and the 8 medications most commonly prescribed in elderly participants were assessed. The Liverpool HIV Drug Interactions database and/or the US prescribing information were utilized to inform the DDI profiles.

More potential DDIs were observed for boosted PI-based regimens than for BIC/LEN, which was likely due to the stronger inhibition of CYP3A and P-gp metabolic pathways by PK boosters, such as COBI and RTV, than with LEN (a moderate CYP3A inhibitor and weak inhibitor of P‑gp).

Medications listed as having potential DDIs with BIC/LEN were as follows: clopidogrel (do not administer); amlodipine, apixaban, fluticasone, metformin, simvastatin, and warfarin (potential interactions); and atorvastatin, prednisone, and rosuvastatin (potential weak interactions).

ARTISTRY-2: Switching to BIC/LEN vs Complex ART6

An ongoing, randomized, multicenter, double-blind, active-controlled phase 3 study (NCT06333808) is evaluating the efficacy and safety of switching from BIC/FTC/TAF to STR BIC/LEN 75 mg/50 mg vs continuing BIC/FTC/TAF in VS PWH. After the randomized period, participants could continue in the OLE phase and receive BIC/LEN.

Figure 4. ARTISTRY-2: Study Design6

Abbreviations: HBcAb=HBV core antibody; HBsAb=HBV surface antibody; HBsAg=HBV surface antigen.

aDetermined by the following at the screening visit: either HBsAg+ and HBsAb-, regardless of HBcAb status, or HBcAb+ and HBsAb-, regardless of HBsAg status.

bOral loading doses of LEN 600 mg on Days 1 and 2 were given.

cParticipants were given placebo to match LEN on Days 1 and 2 of treatment.

dNon-inferiority margin: 4%.

Table 11. ARTISTRY-2: Baseline Demographics and Disease Characteristics6

a“Other” included participants who were Alaska Native, Native Hawaiian, Pacific Islander, and other.

bLocal regulations did not permit the collection of ethnicity data for 1 participant in the BIC/FTC/TAF group and were excluded from the denominator.

cGrouped terms (per MedDRA); not mutually exclusive.

Efficacy outcomes through Week 48

The median (Q1, Q3) exposure to BIC/LEN was 60.6 (53, 69) weeks and 59.9 (52, 67.9) weeks for BIC/FTC/TAF. BIC/LEN was non-inferior to BIC/FTC/TAF in maintaining virologic suppression at Week 48 (Table 12).

Table 12. ARTISTRY-2: Rates of HIV RNA ≥50 c/mL and HIV RNA <50 c/mL (FDA Snapshot) at Week 486

aFour of the 5 participants had low-level viremia (defined as HIV-1 RNA <1000 c/mL).

bTwo-sided CI was based on Mantel-Haenszel stratum weights and the Koch variance estimator and was adjusted by geographic region (US vs non-US).

cReasons for DC before Week 48: other reasons and last HIV-1 RNA was <50 c/mL, n=14; AE or death, n=6; other reasons and last HIV-1 RNA was ≥50 c/mL, n=3.

dReasons for DC before Week 48: other reasons and last HIV-1 RNA was <50 c/mL, n=12; AE or death, n=4; other reasons and last HIV-1 RNA was ≥50 c/mL, n=2.

In the BIC/LEN group, 1 participant had an HIV-1 RNA of 10,700 c/mL at Week 48, was switched to a PI-containing regimen, and was resuppressed on the new regimen. Two participants in each group underwent resistance analysis. No treatment-emergent resistance was noted for 1 participant in the BIC/LEN group and for both participants in the BIC/FTC/TAF group. The other participant in the BIC/LEN group had a history of RAL and DTG exposure and had an isolated R263K integrase substitution recorded at Week 36; the R263K isolate was susceptible to BIC, and no capsid mutations were detected.

Through Week 48, CD4 cell counts remained stable.

Safety outcomes through Week 48

Similar rates of AEs and TRAEs were reported in both groups, and the overall incidence of treatment DC due to AEs was low (Table 13).

Table 13. ARTISTRY-2: Safety Outcomes Through Week 486

aGrade 3 rhabdomyolysis.

bThe following were deemed unrelated to BIC/LEN (each, n=1): anxiety; colon cancer; decreased libido; and encephalopathy and intracranial mass. The following were deemed related to BIC/LEN (each, n=1): alopecia and fatigue; and rash, restless leg syndrome, and trismus.

cThe following were deemed unrelated to BIC/FTC/TAF (each, n=1): abdominal discomfort; road traffic accident. Dry mouth was deemed related to BIC/FTC/TAF treatment.

dDue to coronary artery disease and unrelated to study treatment.

At baseline, in the BIC/LEN and BIC/FTC/TAF groups, the median weight was the same (81.1 kg), and the median change from baseline to Week 48 was stable (-0.2 kg vs 0 kg, respectively).

References

1. Mounzer K, Slim J, Ramgopal M, et al. Efficacy and Safety of Bictegravir Plus Lenacapavir: 48-Week Outcomes in People With HIV-1 Who Are Virologically Suppressed on Complex Antiretroviral Regimens at Baseline. Open Forum Infectious Diseases. 2025;12(11):ofaf615.

2. Mounzer K, Slim J, Ramgopal M, et al. Efficacy and Safety of Switching to Daily Bictegravir Plus Lenacapavir From a Complex HIV Treatment Regimen: A Randomized, Open-Label, Multicenter Phase 2 Study (ARTISTRY-1). Clin Infect Dis. 2025;80(4):881-888.

3. Hedgcock M, Bloch M, Slim J, et al. Switch to BIC+LEN in Virologically Suppressed People With HIV on Complex Regimens: Week 96 Outcomes [Poster 518]. Paper presented at: Conference on Retroviruses and Opportunistic Infections (CROI); February 22-25, 2026; Denver, CO.

4. Margot N, Pennetzdorfer N, Naik V, Montezuma M, Sklar P, Callebaut C. Bictegravir + Lenacapavir: Baseline and Week 48 Resistance Analyses in ARTISTRY-1 Phase 2 [Poster #738]. Paper presented at: Conference on Retroviruses and Opportunistic Infections (CROI); March 9–12, 2025; San Francisco, CA.

5. Orkin C, Ruane PJ, Hedgcock M, et al. Switch to single-tablet bictegravir-lenacapavir from a complex HIV regimen (ARTISTRY-1): a randomised, open-label, phase 3 clinical trial. The Lancet. 2026.

6. Meissner EG, Ramgopal M, Ruane PJ, et al. Phase 3 Efficacy and Safety of Switch from B/F/TAF to Single-Tablet BIC/LEN in ARTISTRY-2 [Poster 513]. Paper presented at: Conference on Retroviruses and Opportunistic Infections (CROI); February 22-25, 2026; Denver, CO.

7. Mounzer K, Slim J, Ramgopal M, et al. Efficacy and Safety of Bictegravir Plus Lenacapavir: 48-Week Outcomes in People With HIV-1 Who Are Virologically Suppressed on Complex Antiretroviral Regimens at Baseline [Supplement]. Open Forum Infectious Diseases. 2025;12(11):1-8.

8. Hedgcock M, Hung CC, Cahn P, et al. Demographic and Clinical Characteristics of Phase 3 Participants in ARTISTRY-1, an Open-Label Study Comparinga Bictegravir/Lenacapavir Single Tablet Regimen With Complex Antiretroviral Therapy Regimens [Poster eP128]. Paper presented at: 20th European AIDS Conference (EACS); October 15–18, 2025; Paris, France.

9. Orkin C, Ruane PJ, Hedgcock M, et al. Switch to single-tablet bictegravir-lenacapavir from a complex HIV regimen (ARTISTRY-1): a randomised, open-label, phase 3 clinical trial [Supplementary Appendix]. The Lancet. 2026.

10. Mounzer K, Slim J, Ramgopal M, et al. Phase 2 Study of Switch to Daily BIC + LEN in Individuals on a Complex HIV Treatment Regimen [Poster 642]. Paper presented at: Conference on Retroviruses and Opportunistic Infections (CROI); March 3-6, 2024; Denver, CO.

11. Mounzer K, Slim J, Ramgopal M, et al. Efficacy and Safety of Bictegravir Plus Lenacapavir: 48-Week Outcomes in Virologically Suppressed People With HIV-1 on Complex Antiretroviral Regimens at Baseline [Presentation OAB2602]. Paper presented at: 25th International AIDS Conference; July 22-26, 2024; Munich, Germany.

12. Prelutsky D, Mounzer K, Ramgopal M, et al. Metabolic Changes at 48 Weeks in Virologically Suppressed People With HIV Switching From Complex Antiretroviral Regimens to Bictegravir Plus Lenacapavir: ARTISTRY-1 Trial [Poster P050]. Paper presented at: HIV Glasgow; November 10–13, 2024; Glasgow, UK.

13. Orkin CM, Ruane PJ, Hedgcock M, et al. Phase 3 Efficacy and Safety of Switch from Complex Regimen to Single-Tablet BIC/LEN in ARTISTRY-1 [Presentation 181]. Paper presented at: Conference on Retroviruses and Opportunistic Infections (CROI); February 22-25, 2026; Denver, CO.

14. Arora P, Montezuma-Rusca JM, Sklar P, Gandhi-Patel B, Marathe DD. Drug-Drug Interaction Liability of BIC/LEN Compared With Representative Complex Antiretroviral Therapy Regimens in the Phase 3 Portion of ARTISTRY-1 [Poster eP.LB006]. Paper presented at: 20th European AIDS Conference (EACS); October 15–18, 2025; Paris, France.

Abbreviations

AE=adverse event
ART=antiretroviral therapy
ARV=antiretroviral
BIC=bictegravir
BP=blood pressure
c/mL=copies per mL
CD4=cluster of differentiation
CKD=chronic kidney disease
COBI=cobicistat
DC=discontinuation
DDI=drug-drug interaction
DM=diabetes mellitus
DOR=doravirine
DRV=darunavir
DTG=dolutegravir
ETR=etravirine
FTC=emtricitabine
HIVTSQc=HIV Treatment Satisfaction Questionnaire change version
HIVTSQs=HIV Treatment Satisfaction Questionnaire status version
HTN=hypertension
INSTI=integrase strand transfer inhibitor
LEN=lenacapavir
MedDRA=Medical Dictionary for Regulatory Activities
MVC=maraviroc
NNRTI=non-nucleos(t)ide reverse transcriptase inhibitor
NRTI=nucleos(t)ide reverse transcriptase inhibitor
OLE=open-label extension
P-gp=P-glycoprotein
PI=protease inhibitor
PK=pharmacokinetic(s)
PWH=people with HIV
Q=quartile

RAL=raltegravir
RAM=resistance-associated mutation
RPV=rilpivirine
RTV=ritonavir
SAE=serious adverse event
STR=single-tablet regimen
SUBQ=subcutaneous
TAF=tenofovir alafenamide
TAM=thymidine analog mutation
TC=total cholesterol
TEAE=treatment-emergent adverse event
TG=triglycerides
TRAE=treatment-related adverse event
URTI=upper respiratory tract infection
VS=virologically suppressed

Follow-Up

For any additional questions, please contact Gilead Medical Information at:

☎1‐866‐MEDI‐GSI (1‐866‐633‐4474) or   www.askgileadmedical.com

Adverse Event Reporting

Please report all adverse events to:

Gilead Global Patient Safety ☎ 1-800-445-3235, option 3 or
 www.gilead.com/utility/contact/report-an-adverse-event

FDA MedWatch Program by ☎ 1-800-FDA-1088 or MedWatch, FDA, 5600 Fishers Ln, Rockville, MD 20852 or   www.accessdata.fda.gov/scripts/medwatch

Data Privacy

The Medical Information service at Gilead Sciences may collect, store, and use your personal information to provide a response to your medical request. We may share your information with other Gilead Sciences colleagues to ensure that your request is addressed appropriately. If you report an adverse event or concern about the quality of a Gilead or Kite product, we will need to use the information you have given us in order to meet our regulatory requirements in relation to the safety of our medicines.

It may be necessary for us to share your information with Gilead’s affiliates, business partners, service providers, and regulatory authorities located in countries besides your own. Gilead Sciences has implemented measures to protect the personal information you provide. Please see the Gilead Privacy Statement (www.gilead.com/privacy-statements) for more information about how Gilead handles your personal information and your rights. If you have any further questions about the use of your personal information, please contact gilead.privacy@gilead.com.

BIKTARVY, GILEAD and the GILEAD logo are registered trademarks of Gilead Sciences, Inc., or its related companies.
© 2026 Gilead Sciences, Inc.