BIKTARVY Prescribing
Information DESCOVY Prescribing Information Important Safety
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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 ≥25 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: Cases of acute renal failure and Fanconi syndrome have been reported with the use of tenofovir prodrugs. In clinical trials of BIKTARVY, there have been no cases of Fanconi syndrome or proximal renal tubulopathy (PRT). Do not initiate BIKTARVY in patients with estimated creatinine clearance (CrCl) <30 mL/min. 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.

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


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 3 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 subjects treated with BIKTARVY.

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

Demonstrated Safety and Tolerability Profile in Virologically Suppressed Adults Through Week 481,3-5


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. No ARs of Grade 2 or higher occurred in ≥1% of subjects treated with BIKTARVY.


  • The majority of adverse events 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 of treatment-naïve adults


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

Adverse Reactions (ARs) (All Grades) Reported in ≥0.5% of 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

Overall, 1% of Treatment-Naïve Adults Discontinued BIKTARVY Due to AEs Through Week 1443


Discontinuation Rates Due to AEs


  BIKTARVY(n=314) ABC/DTG/
3TC(n=315)
Study 1489
Treatment-Naïve
Adults		 0.0% 1.6%

  BIKTARVY(n=320) FTC/TAF
+DTG(n=325)
Study 1490
Treatment-Naïve
Adults		 1.9% 1.8%

No adults discontinued BIKTARVY due to renal-, hepatic-, bone-, or weight-related adverse events3
  • BIKTARVY is not recommended in patients with severe renal impairment (estimated CrCl <30 mL /min) or severe hepatic impairment (Child-Pugh Class C)

Overall, 1% of Virologically Suppressed Adults Discontinued BIKTARVY Due to AEs Through Week 483-6


Discontinuation Rates Due to AEs

 
BIKTARVY(n=282)		 ABC/DTG/3TC(n=281)
Study 1844
Virologically Suppressed
Adults		 2.1% 0.7%

 
BIKTARVY(n=290)		 ATV- or DRV-
Based Regimen(n=287)
Study 1878
Virologically Suppressed
Adults		 0.7% 0.3%

 
BIKTARVY(n=234)		 INSTI- or PI-
Based Regimen(n=236)
Study 1961
Virologically Suppressed
Adult Women		 0.0% 0.0%

No adults discontinued BIKTARVY due to renal-, hepatic-, or bone-related adverse events3,4,6
  • 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 Starting Appropriate Patients on BIKTARVY

INDICATION

BIKTARVY® is indicated as a complete regimen for the treatment of HIV-1 infection in adult and pediatric patients weighing ≥25 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.

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: Cases of acute renal failure and Fanconi syndrome have been reported with the use of tenofovir prodrugs. In clinical trials of BIKTARVY, there have been no cases of Fanconi syndrome or proximal renal tubulopathy (PRT). Do not initiate BIKTARVY in patients with estimated creatinine clearance (CrCl) <30 mL/min. 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: Patients weighing ≥25 kg: 1 tablet taken once daily with or without food.
  • Renal impairment: 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]. Foster City, CA: Gilead Sciences, Inc.; 2019. 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. Gilead Sciences, Inc. 4. 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. 5. 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. 6. Kityo C, Hagins D, Koenig E, et al. Switching to bictegravir/emtricitabine/tenofovir alafenamide in women. Poster presented at: Conference on Retroviruses and Opportunistic Infections; March 4-7, 2018; Boston, MA.