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Biktarvy
bictegravir/ emtricitabine/ tenofovir alafenamide
Black Box Warnings .
Hepatitis B Exacerbation
severe acute HBV exacerbations in HBV/HIV co-infected patients when D/C products containing emtricitabine or tenofovir; monitor hepatic function closely for at least several months in HBV/HIV co-infected patients who D/C bictegravir/emtricitabine/tenofovir alafenamide; initiate anti-HBV tx if needed
Adult Dosing .
Dosage forms: TAB: 50 mg/200 mg/25 mg
HIV infection
- [50 mg/200 mg/25 mg PO qd]
- Info: do not crush/chew tab, but may split tab
HIV post-exposure prophylaxis (off-label)
- [50 mg/200 mg/25 mg PO qd]
- Info: do not crush/chew tab, but may split tab; refer to HIV Post-Exposure Prophylaxis, Occupational and HIV Post-Exposure Prophylaxis, Nonoccupational tables
renal dosing
- [tx-naive patients]
- CrCl <30: avoid use, dose adjustment not possible with fixed-dose combo
- HD: avoid use; PD: not defined
- [virologically-suppressed patients]
- CrCl <30: avoid use, dose adjustment not possible with fixed-dose combo
- HD: no adjustment, on dialysis days administer after dialysis; supplement not defined; PD: not defined
hepatic dosing
- [see below]
- Child-Pugh Class C: avoid use
Peds Dosing .
- Dosage forms: TAB: 30 mg/120 mg/15 mg, 50 mg/200 mg/25 mg
HIV infection
- [14-24 kg]
- Dose: 30 mg/120 mg/15 mg PO qd; Info: do not crush/chew tab, but may split tab
- [>25 kg]
- Dose: 50 mg/200 mg/25 mg PO qd; Info: do not crush/chew tab, but may split tab
HIV post-exposure prophylaxis, nonoccupational (off-label)
- [14-24 kg]
- Dose: 30 mg/120 mg/15 mg PO qd; Info: do not crush/chew tab, but may split tab; refer to HIV Post-Exposure Prophylaxis, Nonoccupational table
- [>25 kg]
- Dose: 50 mg/200 mg/25 mg PO qd; Info: do not crush/chew tab, but may split tab refer to HIV Post-Exposure Prophylaxis, Nonoccupational table
renal dosing
- [tx-naive patients]
- CrCl <30: avoid use, dose adjustment not possible with fixed-dose combo
- HD: avoid use; PD: not defined
- [virologically-suppressed patients]
- CrCl <30: avoid use, dose adjustment not possible with fixed-dose combo
- HD: not defined, consider adult renal dosing for guidance; PD: not defined
hepatic dosing
- [see below]
- Child-Pugh Class C: avoid use
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- hemodialysis (tx-naive patients)
- hepatic impairment, Child-Pugh Class C
- avoid: breastfeeding (patients with non-virological suppression throughout 3rd trimester)
- avoid: breastfeeding (patients with non-virological suppression postpartum)
- avoid: breastfeeding (patients with cracked nipple or bleeding nipple)
- avoid: breastfeeding (patients with mastitis)
- caution: nephrotoxic agent use, concurrent
- caution: nephrotoxic agent use, recent
- caution: renal impairment
- caution: renal disease risk
- caution: hepatic disease risk
- caution: HIV infection and HBV infection, concurrent
- caution: nucleoside tx, long-term
- caution: obesity
- caution: psychiatric disorder
Drug Interactions .
Overview
bictegravir
HIV integrase inhibitor
- CYP3A4 substrate
- UGT1A1 substrate
- MATE1 inhibitor
- OCT2 inhibitor
- affected by altered fat absorption
- binds to polyvalent cations
- interferes w/ gene therapy
emtricitabine
NRTI
- intracellular phosphorylation inhibitor
- affected by altered fat absorption
- interferes w/ gene therapy
tenofovir alafenamide
NRTI
- BCRP substrate
- P-gp substrate
- intracellular phosphorylation inhibitor
- affected by altered fat absorption
- interferes w/ gene therapy
- nephrotoxicity
- tenofovir alafenamide (prodrug) converted to tenofovir
Contraindicated
- carbamazepine
- cidofovir
- dofetilide
- fosphenytoin
- phenobarbital
- phenytoin
- rifampin
- St. John's wort
Avoid/Use Alternative
- adefovir dipivoxil
- aldesleukin
- amikacin
- amikacin inhaled
- apalutamide
- atazanavir
- atidarsagene autotemcel
- betibeglogene autotemcel
- bosentan
- bumetanide
- butalbital
- cenobamate
- cladribine oral
- clofarabine
- cobicistat
- dabrafenib
- danshen
- dicloxacillin
- efavirenz
- elivaldogene autotemcel
- encorafenib
- enzalutamide
- eslicarbazepine acetate
- etravirine
- fexinidazole
- fosamprenavir
- foscarnet
- ganciclovir
- gentamicin
- ivosidenib
- lamivudine
- lopinavir/ritonavir
- lorlatinib
- lovotibeglogene autotemcel
- lumacaftor/ivacaftor
- mannitol
- mavacamten
- methotrexate
- mitapivat
- mitotane
- modafinil
- nafcillin
- nevirapine
- oxaliplatin
- oxcarbazepine
- pacritinib
- pentamidine
- pentobarbital
- pexidartinib
- polymyxin B
- primidone
- repotrectinib
- rifabutin
- rifapentine
- sotorasib
- streptomycin
- streptozocin
- tenofovir disoproxil
- tipranavir
- tobramycin
- tobramycin inhaled
- turmeric
- valganciclovir
Monitor/Modify Tx
- abrocitinib
- acalabrutinib
- acyclovir
- adagrasib
- aficamten
- alectinib
- aliskiren
- aluminum hydroxide
- amiloride
- amiodarone
- amphotericin
- anthrax immune globulin
- asciminib
- aspirin
- auranofin
- axitinib
- azilsartan medoxomil
- azithromycin
- balsalazide
- belumosudil
- benazepril
- berotralstat
- bevacizumab
- bisoprolol
- bleomycin
- botulism immune globulin
- brigatinib
- cabozantinib
- calcium acetate
- calcium carbonate
- calcium citrate
- calcium gluconate
- canagliflozin
- candesartan cilexetil
- cannabidiol
- capecitabine
- capmatinib
- captopril
- carboplatin
- carfilzomib
- carvedilol
- celecoxib
- chlorothiazide
- chlorthalidone
- chromium
- cimetidine
- cisplatin
- clarithromycin
- clindamycin
- colistimethate
- copper histidinate
- creatine
- crizotinib
- cyclophosphamide
- cyclosporine
- cytomegalovirus immune globulin
- danicopan
- daridorexant
- darolutamide
- deferasirox
- deferoxamine
- diclofenac
- diclofenac topical
- diflunisal
- diltiazem
- diosmin
- dronedarone
- elacestrant
- elagolix
- elbasvir
- elexacaftor/tezacaftor/ivacaftor
- eliglustat
- eltrombopag
- eluxadoline
- enalapril
- enalaprilat
- enasidenib
- entrectinib
- erdafitinib
- erythromycin
- ethacrynic acid
- etodolac
- etuvetidigene autotemcel
- everolimus
- febuxostat
- felodipine
- fenoprofen
- ferric citrate
- ferric maltol
- ferrous fumarate
- ferrous gluconate
- ferrous sulfate
- flibanserin
- flucytosine
- flurbiprofen
- fluvoxamine
- fosinopril
- fostamatinib
- fostemsavir
- furosemide
- gilteritinib
- ginkgo
- grazoprevir
- hydrochlorothiazide
- hydroxocobalamin IV
- ibrutinib
- ibuprofen
- ibuprofen lysine
- ifosfamide
- imatinib
- imlunestrant
- immune globulin
- indapamide
- indomethacin
- iodixanol
- iohexol
- iomeprol
- iopamidol
- iopromide
- iothalamate meglumine
- ioversol
- irbesartan
- isavuconazonium
- istradefylline
- itraconazole
- ivacaftor
- ketoconazole
- ketoprofen
- ketorolac
- lanthanum
- lapatinib
- lazertinib
- ledipasvir
- leflunomide
- leniolisib
- lenvatinib
- levacetylleucine
- levoketoconazole
- lifileucel
- lisinopril
- lithium
- lomitapide
- lomustine
- lonafarnib
- losartan
- lutetium Lu 177 vipivotide tetraxetan
- magnesium carbonate
- magnesium citrate
- magnesium hydroxide
- magnesium oxide
- magnesium salicylate
- magnesium supplement
- maribavir
- mavorixafor
- meclofenamate
- mefenamic acid
- meloxicam
- mesalamine
- mesalamine rectal
- metformin
- metolazone
- midostaurin
- mifepristone
- milk thistle
- mirabegron
- mitomycin
- moexipril
- molindone
- momelotinib
- nabumetone
- naproxen
- nefazodone
- nelfinavir
- neomycin
- neratinib
- nifedipine
- nusinersen
- olmesartan medoxomil
- olsalazine
- orlistat
- osimertinib
- oteseconazole
- oxaprozin
- pamidronate
- paromomycin
- paroxetine
- pazopanib
- pemetrexed
- penicillamine
- pentostatin
- perindopril
- pindolol
- piroxicam
- pirtobrutinib
- plazomicin
- polyethylene glycol
- polyethylene glycol/electrolytes
- ponatinib
- posaconazole
- pretomanid
- primaquine
- procainamide
- propafenone
- quercetin
- quinapril
- quinidine (antiarrhythmic)
- quinidine (CYP2D6 inhibitor)
- quinine
- ramipril
- ramucirumab
- ranolazine
- regorafenib
- remibrutinib
- resmetirom
- Rho(D) immune globulin
- rilzabrutinib
- ritonavir
- rituximab
- rolapitant
- ropeginterferon alfa-2b
- rucaparib
- salsalate
- sarecycline
- selpercatinib
- sevabertinib
- sirolimus
- sitagliptin
- sorafenib
- sotagliflozin
- sparsentan
- spironolactone
- stiripentol
- sucralfate
- sucroferric oxyhydroxide
- sulfate bowel prep
- sulindac
- sunitinib
- sunvozertinib
- suvorexant
- tacrolimus
- tafamidis
- tedizolid
- telavancin
- telmisartan
- temsirolimus
- tepotinib
- teriflunomide
- tezacaftor/ivacaftor
- ticagrelor
- tiopronin
- tivozanib
- tolmetin
- tolvaptan
- torsemide
- trandolapril
- trazodone
- triamterene
- trimethoprim
- trofinetide
- tucatinib
- uridine triacetate
- vaccinia immune globulin
- vadadustat
- valacyclovir
- valbenazine
- valsartan
- vancomycin
- vandetanib
- vanzacaftor/tezacaftor/deutivacaftor
- vemurafenib
- venetoclax
- verapamil
- vimseltinib
- voclosporin
- willow bark
- xanomeline
- zinc oral
- ziv-aflibercept
- zoledronic acid
- zongertinib
- zonisamide
Caution Advised
- armodafinil
- artemether/lumefantrine
- belzutifan
- bexarotene
- capivasertib
- ceritinib
- chloramphenicol
- clobazam
- dalfampridine
- dexamethasone
- echinacea
- elafibranor
- felbamate
- garlic
- gemfibrozil
- ginseng, Asian
- glycerol phenylbutyrate
- griseofulvin
- idelalisib
- memantine
- meropenem
- mobocertinib
- odevixibat
- olutasidenib
- omaveloxolone
- perampanel
- pioglitazone
- pramipexole
- prednisone
- probenecid
- ribociclib
- rufinamide
- sarilumab
- suzetrigine
- tazemetostat
- tecovirimat
- telotristat ethyl
- tocilizumab
- topiramate
- tovorafenib
- vaborbactam
- valproic acid
- vamorolone
- vinblastine
- vorasidenib
- voriconazole
- zanubrutinib
Adverse Reactions .
Serious Reactions
- lactic acidosis
- hepatomegaly with steatosis
- hepatotoxicity
- HBV exacerbation, post-tx (HBV co-infected patients)
- pancreatitis
- nephrotoxicity
- neutropenia
- immune reconstitution syndrome
- autoimmune disorder
- suicidality
- angioedema
- Stevens-Johnson syndrome
- toxic epidermal necrolysis
Common Reactions
- diarrhea
- headache
- fatigue
- hyperbilirubinemia
- CK elevated
- abnormal dreams
- dizziness
- insomnia
- hypercholesterolemia
- hyperamylasemia
- neutropenia
- LFTs elevated
- nausea
- vomiting
- depression
- rash
- dyspepsia
- abdominal pain
- asthenia
- Cr incr.
- bone density loss
- arthralgia
- myalgia
- cough
- paresthesia
- peripheral neuropathy
- palmar-plantar hyperpigmentation
- hypertriglyceridemia
- hematuria
- hyperglycemia
- glycosuria
- rhinitis
- flatulence
- weight gain
Safety/Monitoring .
Monitoring Parameters
hepatitis B serology including HBsAg at baseline; Cr at baseline, 2-8wk after tx start or change, then q3-6mo; urinalysis at baseline if renal impairment or risk, then at least q6mo; LFTs at baseline, 2-8wk after tx start or change, then q3-6mo, then if HBV co-infection, continue for several mo after D/C; phosphorus if chronic kidney disease
Pregnancy/Lactation .
Pregnancy
Clinical Summary
bictegravir: may use during pregnancy; no known risk of fetal harm based on limited human data and animal data at 0.6x and 36x recommended human dose
emtricitabine: benefits outweigh risks during pregnancy; no known risk of fetal harm based on limited human data and animal data at 60x and 120x recommended human dose
tenofovir alafenamide: may use during pregnancy; no known risk of fetal harm based on limited human data and animal data at >51x recommended human dose; possible risk of low birth wt based on conflicting animal data with tenofovir disoproxil
Pregnancy Registry
enroll patients in Antiretroviral Pregnancy Registry at 1-800-258-4263; additional info at www.apregistry.com
Lactation
Clinical Summary
weigh risk/benefit if virologically suppressed throughout 3rd trimester and at delivery, otherwise avoid breastfeeding; avoid breastfeeding if mastitis or nipples cracked or bleeding; give infant antiretroviral prophylaxis with zidovudine or nevirapine; risk of postnatal HIV transmission if non-virologically suppressed based on human data; risk of postnatal HIV transmission low if virologically suppressed based on human data; inadequate human data available with bictegravir, though possible risk of infant harm based on drug excretion into milk; no known risk of infant harm with emtricitabine based on human data; inadequate human data available with tenofovir alafenamide, though possible risk of infant diarrhea based on limited human data with tenofovir disoproxil; no human data available to assess effects on milk production
Pharmacology .
Metabolism: for bictegravir: liver; CYP450: 3A substrate; UGT: 1A1 substrate; for emtricitabine: oxidation; CYP450: none; UGT: substrate (enzymes not defined); for tenofovir alafenamide: intracellular; CYP450: minimal; 3A substrate
Excretion: for bictegravir: feces 60.3%, urine 35%; Half-life: 17.3h; for emtricitabine: urine 70%, feces 14%; Half-life: 10h; for tenofovir alafenamide: feces 31.7%; urine <1%; Half-life: 30min
Subclass: HIV: Integrase Strand Transfer Inhibitors (INSTIs) ; HIV: Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs)
Mechanism of Action
for bictegravir: inhibits HIV integrase, preventing viral DNA insertion into host cell DNA; for emtricitabine: inhibits reverse transcriptase and incorporates into viral DNA, resulting in DNA chain termination; for tenofovir alefanamide: prodrug converted to tenofovir, which inhibits reverse transcriptase and incorporates into viral DNA, resulting in DNA chain termination
Formulary .
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