BIKTARVY Prescribing
Information DESCOVY Prescribing Information Important Safety
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BIKTARVY logo.BIKTARVY logo.
Safety & Tolerability Contraindications & DDIs Warnings & Precautions Adverse Reactions Discontinuations

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 history of treatment failure and no known resistance to any component of BIKTARVY.

Please see below for Important Safety Information for BIKTARVY.

Few Contraindications and Drug-Drug Interactions1

BIKTARVY® is contraindicated with two medications: dofetilide and rifampin

Established and Potentially Significant* Drug Interactions:
Alteration in Regimen May Be Recommended


Concomitant Drug Class: Drug Name Clinical Comment
Antiarrhythmics:
  • Dofetilide
 Coadministration is contraindicated due to the potential for serious and/or life-threatening events associated with dofetilide therapy.
Anticonvulsants:
  • Carbamazepine†
  • Oxcarbazepine
  • Phenobarbital
  • Phenytoin
 Coadministration with alternative anticonvulsants should be considered.
Antimycobacterials:
  • Rifabutin†
  • Rifampin†‡
  • Rifapentine
 Coadministration with rifampin is contraindicated due to the effect of rifampin on the BIC component of BIKTARVY.

Coadministration with rifabutin or rifapentine is not recommended.
Herbal products:
  • St. John’s wort§
 Coadministration with St. John’s wort is not recommended.
Medications or oral supplements containing polyvalent cations (e.g., Mg, Al, Ca, Fe):
  • Calcium or iron supplements†
  • Cation-containing antacids or laxatives†
  • Sucralfate
  • Buffered medications
Antacids containing Al/Mg:BIKTARVY can be taken at least 2 hours before or 6 hours after taking antacids containing Al/Mg.

Routine administration of BIKTARVY together with, or 2 hours after, antacids containing Al/Mg is not recommended.

Supplements or antacids containing Calcium or Iron: BIKTARVY and supplements or antacids containing calcium or iron can be taken together with food.

Routine administration of BIKTARVY under fasting conditions together with, or 2 hours after, supplements or antacids containing calcium or iron is not recommended.
Metformin Refer to the prescribing information of metformin for assessing the benefit and risk of concomitant use of BIKTARVY and metformin.
  • For an aging patient population, which may have comorbidities, the safety profile and drug-drug interactions of a treatment are important considerations when choosing a therapy2

*Table is not all-inclusive.

†Drug-drug interaction study was conducted with either BIKTARVY or its components as individual agents.

‡Strong inducer of CYP3A and P-gp, and inducer of UGT1A1.

§The induction potency of St. John’s wort may vary widely based on preparation.

No Known Dose Adjustments When BIKTARVY Is Coadministered With These Medications1

Drugs With No Clinically Significant Interactions With BIKTARVY

Drug Class Drug Within Class
Oral contraceptive Ethinyl estradiol, norgestimate
HCV antiviral Sofosbuvir, sofosbuvir/velpatasvir, ledipasvir/sofosbuvir, and sofosbuvir/velpatasvir/voxilaprevir
Benzodiazepine Midazolam
Selective serotonin reuptake inhibitor Sertraline

Warnings and Precautions1

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.

Established Safety Profile.

Demonstrated Long-Term Safety and Tolerability Profile in Treatment-Naïve Adults Through Week 1443,4

Study 1489
Adverse Reactions (ARs) (All Grades) Reported in ≥2% of Adults Who Received BIKTARVY

Study 1489

BIKTARVY(n=314)
ABC/
DTG/3TC(n=315)

Study 1490

BIKTARVY(n=320)
FTC/TAF
+DTG(n=325)
Nausea, % 6 18 3 5
Diarrhea, % 6 4 3 3
Headache, % 5 5 4 3
Fatigue, % 3 4 2 2
Abnormal dreams, % 3 3 <1 1
Dizziness, % 2 3 2 1
Insomnia, % 2 3 2 <1
Abdominal distension, % 2 2 1 2

Study 1490
Adverse Reactions (ARs) (All Grades) Reported in ≥2% of Adults Who Received BIKTARVY
BIKTARVY(n=320)
FTC/TAF
+DTG(n=325)
Nausea, % 3 5
Diarrhea, % 3 3
Headache, % 4 3
Fatigue, % 2 2
Abnormal dreams, % <1   <1
Dizziness, % 2 1
Insomnia, % 2 <1  
Abdominal distension, % 1 2

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.

Weight Change Data in Studies 1489 and 1490

Study 1489 and 1490: Weight Change Through Week 144

Study 14893,4

Chart of weight change data in 1489 study through week 144. Chart of weight change data in 1489 study through week 144.

In Study 1489, no adults discontinued BIKTARVY due to weight-related AEs through Week 1443-5

  • 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%)

Study 14903,4

Chart of weight change data in study 1490 through week 144. Chart of weight change data in study 1490 through week 144.

In Study 1490, no adults discontinued BIKTARVY due to weight-related AEs through Week 1443-5

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

In the OLEs through Week 240, 1 participant initially randomized to BIKTARVY discontinued due to obesity, which was considered to be related to the study drug by the investigator5

Median cumulative weight gain from baseline to Week 240, including the OLE, was 6.1 kg for participants initially randomized to BIKTARVY5

IMPORTANT SAFETY INFORMATION

Contraindications

  • Coadministration: Do not use BIKTARVY with dofetilide or rifampin.

3TC, lamivudine; ABC, abacavir; AE, adverse event; DTG, dolutegravir; FTC, emtricitabine; TAF, tenofovir alafenamide.

Bone Data in Study 1489

Study 1489: Changes in Hip BMD Through Week 1444

Chart of hip BMD data in 1489 study through week 144.
  • BMD declines of ≥7% at the total hip were experienced in 1% of BIKTARVY patients and 2% of ABC/DTG/3TC patients at Week 48, in 2% of BIKTARVY patients and 3% of ABC/DTG/3TC patients at Week 96, and in 5% of BIKTARVY patients and 4% of ABC/DTG/3TC patients at Week 1443
    • Analysis was conducted in a subset of the study population (n=597)3

In the OLE:

  • A mean change of −0.3% was observed from baseline at Week 240 (n=197)5
  • BMD declines of ≥7% at the total hip were experienced in 8% of patients (n=15/197) at Week 2403,5
  • Includes only participants initially randomized to BIKTARVY at Week 0, as these participants took BIKTARVY for 240 weeks5

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) scans3,5

Study 1489: Changes in Lumbar Spine BMD Through Week 1444

Chart of lumbar spine BMD data in 1489 study through week 144.
  • BMD declines of ≥5% at the lumbar spine were experienced in 10% of BIKTARVY patients and 6% of ABC/DTG/3TC patients at Week 48, in 12% of BIKTARVY patients and 6% of ABC/DTG/3TC patients at Week 96, and in 12% of BIKTARVY patients and 8% of ABC/DTG/3TC patients at Week 1443
    • Analysis was conducted in a subset of the study population (n=603)3

In the OLE:

  • A mean change of −0.2% was observed from baseline at Week 240 (n=201)5
  • BMD declines of ≥5% at the lumbar spine were experienced in 20% of patients (n=41/201) at Week 2403,5
  • Includes only participants initially randomized to BIKTARVY at Week 0, as these participants took BIKTARVY for 240 weeks5

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) scans3,5

BMD was measured only in Study 1489

IMPORTANT SAFETY INFORMATION (cont’d)

Drug Interactions

  • Prescribing information: Consult the full prescribing information for BIKTARVY for more information on Contraindications, Warnings, and potentially significant drug interactions, including clinical comments.
  • Drugs affecting renal function: Coadministration of BIKTARVY with drugs that reduce renal function or compete for active tubular secretion may increase concentrations of FTC and tenofovir and the risk of adverse reactions.

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

Renal Data in Studies 1489 and 1490

Study 1489 and 1490: Changes in eGFR and Serum Creatine Through Week 144

Study 14894-7

Chart of eGFR in 1489 study through week 144. Chart of eGFR in 1489 study through week 144.
  • Median serum creatine increased by 0.1 mg/dL in the BIKTARVY arm and by 0.11 mg/dL in the ABC/DTG/3TC arm from baseline4

In the OLE:

  • A median eGFR change of −8.2mL/min from baseline was observed at Week 240 (n=213)3,5
  • Median serum creatine increased by 0.11 mg/dL in patients from baseline through Week 2403
  • Includes only participants initially randomized to BIKTARVY at Week 0, as these participants took BIKTARVY for 240 weeks5

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

Study 14904,8,9

Chart of eGFR in study 1490 through week 144. Chart of eGFR in study 1490 through week 144.
  • Median serum creatine increased by 0.11 mg/dL in the BIKTARVY arm and by 0.12 mg/dL in the FTC/TAF+DTG arm from baseline4

In the OLE:

  • A median eGFR change of -8.5mL/min from baseline was observed at Week 240 (n=217)3,5
  • Median serum creatine increased by 0.11mg/dL in patients from baseline through Week 240 (n=217)3
  • Includes only participants initially randomized to BIKTARVY at Week 0, as these participants took BIKTARVY for 240 weeks5

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

IMPORTANT SAFETY INFORMATION (cont’d)

Warnings and Precautions

  • 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 orevidence 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.

eGFR, estimated glomerular filtration rate; OLE, open-label extension.

Lipid Data in Studies 1489 and 1490

Study 1489 and 1490: Median Change in Fasting Lipids from Baseline Through Week 144

Study 14894

Chart of median change in fasting lipids in study 1489 through week 144. Chart of median change in fasting lipids in study 1489 through week 144.
  • In the OLE at 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: +5mg/DL, Triglycerides: +11mg/dL, Total-C:HDL-C ratio: 0.03
  • Includes only participants initially randomized to BIKTARVY at Week 0, as these participants took BIKTARVY for 240 weeks

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

Median Change in Fasting Lipids from Baseline

Study 14904

Chart of median change in fasting lipids in study 1490 through week 144. Chart of median change in fasting lipids in study 1490 through week 144.
  • In the OLE at Week 240, median changes in fasting lipids from baseline were as follows (n=208): Total-C:+22mg/dL, LDL-C: +17mg/dL, HDL-C: +4mg/DL, Triglycerides: +10mg/dL, Total-C:HDL-C ratio:0.13
  • Includes only participants initially randomized to BIKTARVY at Week 0, as these participants took BIKTARVY for 240 weeks

BIKTARVY® Had Similar Incidence of Laboratory Abnormalities to Comparators

Study 14894

Chart of weight change data in 1489 study. Chart of weight change data in 1489 study.

Study 14904

Chart of weight change data in 1490 study. Chart of weight change data in 1490 study.

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 with CrCl <30 mL/min.

IMPORTANT SAFETY INFORMATION (cont’d)

Pregnancy and lactation

  • Pregnancy: There is insufficient human data on the use of BIKTARVY during pregnancy. Dolutegravir, another integrase inhibitor, has been associated with neural tube defects. Discuss the benefit-risk of using BIKTARVY during pregnancy and conception. An Antiretroviral Pregnancy Registry (APR) has been established. Available data from the APR for FTC shows no difference in the rates of birth defects compared with a US reference population.
  • Lactation:Women infected with HIV-1 should be instructed not to breastfeed, due to the potential for HIV-1 transmission.

ALT, alanine aminotransferase; AST, aspartate aminotransferase; CrCl, creatine clearance; LDL, low-density lipoprotein; OLE, open-label extension; ULN, upper limit of normal.

The majority (84%) of ARs associated with BIKTARVY were Grade 13

Demonstrated Safety and Tolerability Profile in Virologically Suppressed Adults Through Week 481,3,10,11

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

Study 1844

BIKTARVY(n=282)
ABC/
DTG/3TC(n=281)

Study 1878

BIKTARVY(n=290)
ATV- or DRV-Based Regimen(n=287)
Headache, % 2 3 5 0
Flatulence, % 0 2 2 0
Nausea, % 0 2 2 0
Diarrhea, % 1 1 2 0
Adverse Reactions (ARs) (All Grades) Reported in ≥2% of Adults Who Switched to BIKTARVY

Study 1878

BIKTARVY(n=290)
ATV- or DRV-Based
Regimen(n=287)
Headache, % 5 0
Flatulence, % 2 0
Nausea, % 2 0
Diarrhea, % 2 0

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


  • The majority of adverse reactions associated with BIKTARVY were Grade 1 in Study 1878 (76%) and in Study 1844 (58%)
  • The most common ARs (incidence ≥5%; all grades) in clinical trials of treatment-naïve adults who received BIKTARVY were diarrhea, nausea, and headache
  • Overall, the safety profile of BIKTARVY in virologically suppressed adults was similar to that in treatment-naïve adults
Weight Change Data in Study 1844

Study 184410,12

Chart of weight change data in 1844 study through week 48.
Chart of weight change data in 1844 study through week 120.

In Study 1844, no adults discontinued BIKTARVY due to weight-related adverse events through Week 48

  • In participants who continued on or switched to BIKTARVY during OLE, changes from baseline in body weight were consistent with changes reported through Week 48
  • *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.

IMPORTANT SAFETY INFORMATION (cont’d)

Contraindications

  • Coadministration: Do not use BIKTARVY with dofetilide or rifampin.

AE, adverse event; DTG, dolutegravir; FTC, emtricitabine; TAF, tenofovir alafenamide.

Weight Change Data in Study 1878

Study 18782,11,13

Chart of weight change data in 1878 study through week 48.
Chart of weight change data in 1878 study through week 96.

In Study 1878, no adults discontinued BIKTARVY due to weight-related adverse events through Week 48

  • 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 48
  • *This analysis includes participants initially randomized to BIKTARVY and participants who switched to BIKTARVY during the extension phase.

IMPORTANT SAFETY INFORMATION (cont’d)

Contraindications

  • Coadministration: Do not use BIKTARVY with dofetilide or rifampin.

AE, adverse event; DTG, dolutegravir; FTC, emtricitabine; TAF, tenofovir alafenamide.

Demonstrated Safety and Tolerability Profile in Virologically Suppressed Adult Women Through Week 483

Adverse Reactions (ARs) (All Grades) Reported in >1 Adult Women Who Switched to BIKTARVY

Study 1961

BIKTARVY(n=234)
INSTI- or PI-
Based Regimen(n=236)
Iron deficiency anemia, % 0.9 0
Nausea, % 0.9 0
Vomiting, % 0.9 0

Through Week 48, no woman discontinued due to AEs in either treatment arm14

Demonstrated Safety and Tolerability Profile in Virologically Suppressed Adults Aged ≥65 Years Through Week 963,15,16

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

Study 4449

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. No ARs of grade 3 or 4 occurred with BIKTARVY.

At Week 96, there were 2 (2.3%) Grade 3-4 study drug-related AEs in adults aged ≥65 years

Demonstrated Safety and Tolerability Profile in Virologically Suppressed Children and Adolescents17,18

Adverse Reactions (ARs) (All Grades) Reported in >1 Participant

Study 1474: Cohorts 1 and 2 through Week 96

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

Study 1474: Cohort 3 through Week 24

Ages ≥2 Years Weighing
≥14 to <25 kg (n=22)
Abdominal discomfort, % 3 0
Neutropenia, % 1 5
Adverse Reactions (All Grades) Reported in 10% of Virologically Suppressed Pediatric and Adolescent Patients

Study 1474: Cohorts 1 and 2

Ages ≥6 to <18 Years
Weighing ≥25 kg (n=100)
Abdominal discomfort, % 3
Neutropenia, % 1
Adverse Reactions (All Grades) Reported in 10% of Virologically Suppressed Pediatric and Adolescent Patients

Study 1474: Cohort 3

Ages >2 Years Weighing
≥14 to <25 kg (n=22)
Abdominal discomfort, % 0
Neutropenia, % 5

  • No one discontinued due to adverse events in cohort 1 (ages 12 to ‹18 years)
  • 1 patient discontinued due to adverse events in cohort 2 (ages 6 to ‹12 years)
  • No one discontinued due to adverse events in cohort 3 (ages 2 and up)

Minimal Discontinuations Due to Adverse Events in Treatment-Naïve Adults3-5

Treatment-Naïve Adults4,5
Through Week 144

Study 1489

0.0%

BIKTARVY(n=314)

1.6%

ABC/DTG/3TC(n=315)

Study 1490

1.9%

BIKTARVY(n=320)

1.8%

FTC/TAF+DTG(n=325)

Through Week 240 (including OLE)5 in participants initially randomized to BIKTARVY

Study 1489

1.3%

BIKTARVY(n=314)

Study 1490

1.9%

BIKTARVY(n=320)

No treatment-naïve adults discontinued BIKTARVY due to renal-, hepatic-, or bone-related adverse events through Week 240. One adult discontinued due to a weight-related AE through Week 240, which was evaluated by the investigator to be related to study drug.4,5

  • 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 with CrCl <30 mL/min.1

Minimal Discontinuations Due to Adverse Events in Virologically Suppressed Patients1,3,10-19

Virologically Suppressed Adults3,10-13
Through Week 48

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)

Study 1844

1.3%

BIKTARVY(n=547)

Through Week 96 (including Extension)

Study 1878

1.1%

BIKTARVY(n=534)

Virologically Suppressed Adult Women14,19

Through Week 48

Study 1961

0.0%

BIKTARVY(n=234)

0.0%

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

Through Week 96 (including Extension)

Study 1961

0.2%

BIKTARVY(n=462)

Virologically Suppressed Adults Aged ≥65 Years16

Through Week 96

Study 4449

5.8%

BIKTARVY(N=86)

Virologically Suppressed Children and Adolescents1,17,18

Through Week 96

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)

Through Week 24

Study 1474

0.0%

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

No virologically suppressed patients discontinued BIKTARVY due to renal-or bone-related adverse events at any clinical trial timepoints. One virologically suppressed patient discontinued due to a hepatic-related adverse event (Study 1961) and 1 virologically suppressed patient discontinued due to a weight-related adverse event (Study 4449); both were found to be related to study drug.3,10-19

  • 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


Please see below for Important Safety Information for BIKTARVY.

LEARN MORE ABOUT BIKTARVY DOSING

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 history of treatment failure and no known resistance to any component of BIKTARVY.

Please see below for Important Safety Information for BIKTARVY.

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.

Adverse reactions

  • Most common adverse reactions (incidence ≥5%; all grades) in clinical studies through week 144 were diarrhea (6%), nausea (6%), and headache (5%).

Drug interactions

  • Prescribing information: Consult the full prescribing information for BIKTARVY for more information on Contraindications, Warnings, and potentially significant drug interactions, including clinical comments.
  • Enzymes/transporters: Drugs that induce P-gp or induce both CYP3A and UGT1A1 can substantially decrease the concentration of components of BIKTARVY. Drugs that inhibit P-gp, BCRP, or inhibit both CYP3A and UGT1A1 may significantly increase the concentrations of components of BIKTARVY. BIKTARVY can increase the concentration of drugs that are substrates of OCT2 or MATE1.
  • Drugs affecting renal function: Coadministration of BIKTARVY with drugs that reduce renal function or compete for active tubular secretion may increase concentrations of FTC and tenofovir and the risk of adverse reactions.

Dosage and administration

  • Dosage: Adult and pediatric patients weighing ≥25 kg: 1 tablet containing 50 mg bictegravir (BIC), 200 mg emtricitabine (FTC), and 25 mg tenofovir alafenamide (TAF) taken once daily with or without food. Pediatric patients weighing ≥14 kg to <25 kg: 1 tablet containing 30 mg BIC, 120 mg FTC, and 15 mg TAF taken once daily with or without food. For these pediatric patients, who are unable to swallow a whole tablet, the tablet can be split and each part taken separately as long as all parts are ingested within approximately 10 minutes.
  • Renal impairment: For patients weighing ≥25 kg, not recommended in patients with CrCl 15 to <30 mL/min, or <15 mL/min who are not receiving chronic hemodialysis, or <15 mL/min who are receiving chronic hemodialysis and have no antiretroviral treatment history. For patients weighing ≥14 kg to <25 kg, not recommended in patients with CrCl <30 mL/min.
  • Hepatic impairment: Not recommended in patients with severe hepatic impairment.
  • Prior to or when initiating: Test patients for HBV infection.
  • Prior to or when initiating, and during treatment: As clinically appropriate, assess serum creatinine, CrCl, urine glucose, and urine protein in all patients. In patients with chronic kidney disease, assess serum phosphorus.

Pregnancy and lactation

  • Pregnancy: There is insufficient human data on the use of BIKTARVY during pregnancy. Dolutegravir, another integrase inhibitor, has been associated with neural tube defects. Discuss the benefit-risk of using BIKTARVY during pregnancy and conception. An Antiretroviral Pregnancy Registry (APR) has been established. Available data from the APR for FTC shows no difference in the rates of birth defects compared with a US reference population.
  • Lactation: Women infected with HIV-1 should be instructed not to breastfeed, due to the potential for HIV-1 transmission.

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

3TC, lamivudine; ABC, abacavir; AE, adverse event; Al, aluminum; ATV, atazanavir; BIC, bictegravir; Ca, calcium; CrCl, creatinine clearance; DRV, darunavir; DTG, dolutegravir; Fe, iron; FTC, emtricitabine; HCV, hepatitis C virus; INSTI, integrase strand transfer inhibitor; Mg, magnesium; NSAIDs, nonsteroidal anti-inflammatory drugs; PI, protease inhibitor; TAF, tenofovir alafenamide; TDF, tenofovir disoproxil fumarate.

References: 1. BIKTARVY. Package insert. Gilead Sciences, Inc.; 2021. 2. Burgess MJ, Zeuli JD, Kasten MJ. Management of HIV/AIDS in older patients-drug/drug interactions and adherence to antiretroviral therapy. HIV/AIDS (Auckl). 2015;7:251-264. 3. Data on file. Gliead Sciences, Inc. 4. 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. 5. 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. 6. Wohl DA, Yazdanpanah Y, Baumgarten A, et al. Bictegravir combined with emtricitabine and tenofovir alafenamide versus dolutegravir, abacavir, and lamivudine for initial treatment of HIV-1 infection: week 96 results from a randomised, double-blind, multicentre, phase 3, non-inferiority trial. Lancet HIV. 2019;6(6):e355-e363. 7. Gallant J, Lazzarin A, Mills A, et al. Bictegravir, emtricitabine, and tenofovir alafenamide versus dolutegravir, abacavir, and lamivudine for initial treatment of HIV-1 infection (GS-US-380-1489): a double-blind, multicentre, phase 3, randomised controlled non-inferiority trial. Lancet. 2017;390(10107):2063-2072. 8. Stellbrink H-J, Arribas JR, Stephens JL, et al. Co-formulated bictegravir, emtricitabine, and tenofovir alafenamide versus dolutegravir with emtricitabine and tenofovir alafenamide for initial treatment of HIV-1 infection: week 96 results from a randomised, double-blind, multicentre, phase 3, non-inferiority trial. Lancet HIV. 2019;6(6):e364-e372. 9. Sax PE, Pozniak A, Montes ML, et al. Coformulated bictegravir, emtricitabine, and tenofovir alafenamide versus dolutegravir with emtricitabine and tenofovir alafenamide, for initial treatment of HIV-1 infection (GS-US-380-1490): a randomised, double-blind, multicentre, phase 3, non-inferiority trial. Lancet. 2017;390(10107):2073-2082. 10. Molina JM, 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. 11. 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. 12. 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; Washington, DC. Poster 1028. 13. 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. 14. 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. 15. Maggiolo F, Rizzardini G, Molina J-M, et al. 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Abstract presented at: International Workshop on HIV & Pediatrics. July 16-17, 2021; Virtual. Abstract 2. 19. 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.