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 bictegravir/emtricitabine/tenofovir alafenamide.
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 bictegravir/emtricitabine/tenofovir alafenamide. If appropriate, anti-hepatitis B therapy may be warranted.
HIV-1 infection, treatment: One tablet (bictegravir 50 mg/emtricitabine 200 mg/tenofovir alafenamide 25 mg) once daily.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
CrCl ≥30 mL/minute: No dosage adjustment necessary.
CrCl <30 mL/minute: Use is not recommended.
End-stage renal disease on hemodialysis: One tablet (bictegravir 50 mg/emtricitabine 200 mg/tenofovir alafenamide 25 mg) once daily; administer after hemodialysis on dialysis days.
Mild to moderate impairment (Child-Pugh class A or B): No dosage adjustments necessary.
Severe impairment (Child-Pugh class C): Use is not recommended (has not been studied).
(For additional information see "Bictegravir, emtricitabine, and tenofovir alafenamide: Pediatric drug information")
Note: Multiple tablet strengths are available and contain different amounts of each component; use caution.
HIV-1 infection, treatment: Note: Gene mutation and antiretroviral resistance patterns should be evaluated (refer to https://www.iasusa.org for more information) when necessary.
Pediatric patients:
Weight 14 to <25 kg: Bictegravir 30 mg/emtricitabine 120 mg/tenofovir alafenamide 15 mg per tablet: Oral: One tablet once daily. Note: In clinical trials evaluating this dose, the youngest patients were 3 years of age.
Weight ≥25 kg: Bictegravir 50 mg/emtricitabine 200 mg/tenofovir alafenamide 25 mg per tablet: Oral: One tablet once daily.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Pediatric patients weighing ≥14 kg:
CrCl ≥30 mL/minute: No dosage adjustment necessary.
CrCl <30 mL/minute: Use is not recommended.
End-stage renal disease on hemodialysis: There are no dosage adjustments provided in the manufacturer's labeling; however, based on data in adults with end-stage renal disease, the standard dose is recommended, with administration after hemodialysis on dialysis days.
Pediatric patients weighing ≥14 kg:
Mild to moderate impairment (Child-Pugh class A or B): No dosage adjustment necessary.
Severe impairment (Child-Pugh class C): Use is not recommended (has not been studied).
Refer to adult dosing.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Biktarvy: Bictegravir 30 mg, emtricitabine 120 mg, and tenofovir alafenamide 15 mg, Bictegravir 50 mg, emtricitabine 200 mg, and tenofovir alafenamide 25 mg
No
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Biktarvy: Bictegravir 50 mg, emtricitabine 200 mg, and tenofovir alafenamide 25 mg
Oral: Administer with or without food. Administer 2 hours before or 6 hours after aluminum- or magnesium-containing antacids. Administer with food with concomitant calcium- or iron-containing supplements or antacids; coadministration with or 2 hours after calcium- or iron-containing supplements or antacids is not recommended under fasting conditions.
Oral: Administer with or without food.
Bictegravir 30 mg/emtricitabine 120 mg/tenofovir alafenamide 15 mg tablet (pediatric patients weighing 14 to <25 kg): If unable to swallow tablet whole, tablet may be split and each part swallowed separately; all parts should be swallowed within ~10 minutes.
HIV-1 infection, treatment: Treatment of HIV-1 infection (as a complete regimen) in adults and pediatric patients ≥14 kg as initial therapy in those with no antiretroviral treatment history; or to replace a stable antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA <50 copies/mL) with no history of treatment failure and no known substitutions associated with resistance to the individual components.
The tenofovir alafenamide fumarate (TAF) component of bictegravir, emtricitabine, tenofovir alafenamide (BIC/FTC/TAF) is associated with kidney impairment, acute kidney injury (AKI), and proximal tubular nephropathy. Cases of TAF-associated AKI and renal tubulopathy (RT) have been reported (Ref). Syndromes reported include Fanconi syndrome (FS) (Ref), FS (Ref) and FS with nephrogenic diabetes insipidus (Ref). AKI or RT resolution occurred immediately to 3 months after discontinuation (Ref). Renal function may not return to baseline (Ref). Incidence is lower than with tenofovir disoproxil fumarate (TDF) (Ref). TAF has been used safely in patients previously diagnosed with TDF-related FS/RT (Ref).
Mechanism: Dose- and time-related; tenofovir inhibition of DNA polymerase-gamma results in mitochondrial DNA (mtDNA) depletion, mitochondrial dysfunction, and cell toxicity (Ref). Proximal tubule epithelial cells are susceptible due to active uptake of tenofovir by OAT-1 and OAT-3 and efflux by MDRP-4 (Ref). Although TAF is converted to tenofovir in target lymphoid cells and hepatocytes rather than in the plasma like TDF, the proportion of the dose reaching the kidneys is similar. Proximal tubule epithelial cell exposure to tenofovir from TAF is lower than TDF (Ref).
Onset: Varied; onset ranged from 1 day to 9 months, depending on associated risk factors, in reported AKI or RT cases (Ref). In some cases, patients have had prolonged prior use with TDF before initiation of TAF (Ref). AKI has been described with TDF years after TDF initiation (Ref).
Risk factors:
• Concurrent nephrotoxic medications (Ref)
• Concurrent pharmacologic boosters (eg, cobicistat) (Ref)
• Preexisting kidney disease or history of AKI (Ref)
• Preexisting liver disease (eg, hepatitis C coinfection) (Ref)
• HIV (especially low CD4 count) (Ref)
• Diabetes (Ref)
• Lower body weight (Ref)
• Older age (Ref)
• Previous exposure to TDF (Ref)
• Genetic polymorphisms (Ref)
Bictegravir, emtricitabine, and tenofovir alafenamide (BIC/FTC/TAF) is associated with weight gain (Ref). Median weight gain 96 weeks after initiation in antiretroviral-naïve individuals was 3.5 kg to 3.6 kg (Ref). Median weight gain at 144 weeks was 4.1 kg to 4.4 kg (Ref). Weight gain may also plateau (Ref). Weight increases with BIC/FTC/TAF are not significantly different from those after initiation of dolutegravir (DTG) + abacavir/lamivudine (ABC/3TC) or DTG + FTC/TAF (Ref), but may be larger than weight increases with darunavir, cobicistat, emtricitabine, tenofovir alafenamide (DRV/COBI/FTC/TAF) (Ref) or efavirenz/emtricitabine/tenofovir disoproxil fumarate (EFV/FTC/TDF) (Ref).
Switching to an integrase strand inhibitor (INSTI)-containing regimen from EFV/FTC/TDF may be associated with greater weight gain at 18 months than switching to a protease inhibitor (PI)-based regimen or remaining on EFV/FTC/TDF (Ref). Similarly, switching from a TDF to TAF may result in weight gain (Ref). Switching virally suppressed females to ABC/DTG/3TC resulted in greater weight gain than in those remaining on TDF/FTC + nonnucleoside reverse-transcriptase inhibitor (NNRTI) at 48 weeks (Ref).
INSTI-containing regimens may be associated with a greater increase in waist circumference in females (Ref) and patients of black race (Ref). Addition of or switch to an INSTI-containing regimen may be associated with increased risk of metabolic syndrome (including diabetes mellitus) in females (Ref) and an increased BMI class (Ref). INSTI-containing regimens may increase risk for obesity compared with non-INSTI-containing regimens (Ref). Some data suggest an association between weight gain and cardiovascular disease in INSTI-containing regimens (Ref).
Although there is a case report of a 13 kg/m2 BMI increase reversing over 2 years with a change from elvitegravir, cobicistat, emtricitabine, and tenofovir alafenamide fumarate back to EFV/FTC/TDF (Ref), it is unclear if this is generalizable (Ref).
Mechanism: Not clearly established; TAF may have less of a weight suppressive effect than other nucleos(t)ide reverse transcriptase inhibitors (NRTIs). Similarly, INSTIs such as BIC may have less of a weight suppressive effect than other anchor drugs and stimulate weight gain through effects on estrogen-mediated pathways, regulation of glucose and lipid metabolism, melanocortin stimulating system suppression, or insulin sensitivity by magnesium chelation (Ref).
Onset: Delayed; weight gain and BMI increases ≥5% have been observed after 12 weeks of treatment (Ref).
Risk factors:
• Females (Ref)
• Black or Hispanic race (Ref)
• Older age (Ref)
• Pre-treatment obesity (adolescents) (Ref)
• Lower pre-treatment BMI (adults) (Ref)
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Also see individual agents.
>10%: Hepatic: Increased serum bilirubin (17%)
1% to 10%:
Cardiovascular: Increased serum creatine kinase (6% to 8%)
Dermatologic: Skin rash (<2%)
Endocrine & metabolic: Increased LDL cholesterol (4% to 5%)
Gastrointestinal: Abdominal distention (1% to 2%), abdominal pain (<2%), diarrhea (3% to 6%), dyspepsia (<2%), flatulence (<2%), increased serum amylase (3%), increased serum lipase (≤2%), nausea (3% to 6%), vomiting (<2%)
Hematologic & oncologic: Decreased neutrophils (3%)
Hepatic: Increased gamma-glutamyl transferase (1% to 2%), increased serum alanine aminotransferase (2% to 3%), increased serum aspartate aminotransferase (2% to 5%)
Nervous system: Abnormal dreams (≤3%), depression (<2%), dizziness (2%), fatigue (2% to 3%), headache (4% to 5%), insomnia (2%), suicidal ideation (2%), suicidal tendencies (2%)
Frequency not defined: Renal: Increased serum creatinine
Postmarketing:
Dermatologic: Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria (Sax 2017)
Endocrine & metabolic: Gynecomastia (Biagi 2020), weight gain (Orkin 2020)
Gastrointestinal: Pancreatitis (Simeni Njonnou 2020)
Hypersensitivity: Angioedema
Infection: Reactivation of HBV (following discontinuation in coinfected HIV-1 and HBV patients)
Neuromuscular & skeletal: Rhabdomyolysis (Simeni Njonnou 2020)
Renal: Acute kidney injury (Ueaphongsukkit 2021), Fanconi syndrome (Bahr 2019), proximal tubular nephropathy (Ueaphongsukkit 2021), renal tubular necrosis
Coadministration with dofetilide, rifampin
Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to bictegravir, emtricitabine , tenofovir alafenamide, or any component of the formulation; coadministration with St John’s wort
Concerns related to adverse effects:
• Immune reconstitution syndrome: Patients may develop immune reconstitution syndrome, resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection during initial HIV treatment or activation of autoimmune disorders (eg, Graves disease, polymyositis, Guillain-Barré syndrome, autoimmune hepatitis) later in therapy; further evaluation and treatment may be required.
• Lactic acidosis/hepatomegaly: Lactic acidosis and severe hepatomegaly with steatosis, sometimes fatal, have been reported with the use of nucleoside analogs, alone or in combination with other antiretrovirals. Suspend treatment in any patient who develops clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity (marked transaminase elevation may/may not accompany hepatomegaly and steatosis).
Disease-related concerns:
• Hepatic impairment: Use with caution in hepatic impairment; see "Dosing: Hepatic Impairment" for additional information.
• Renal impairment: Use with caution in renal impairment; see "Dosing: Altered Kidney Function" for additional information.
Emtricitabine-associated hyperpigmentation may occur at a higher frequency in pediatric patients compared to adults (children: 32%; adults: 2% to 6%). Bictegravir may increase SCr via inhibition of tubular secretion; it does not affect glomerular filtration.
Through disruption in vitamin D metabolism, decreases in bone mineral density (BMD) have been observed with tenofovir alafenamide (TAF) after 48 weeks of treatment; however, the incidence and negative impact on BMD is less than that observed with tenofovir disoproxil fumarate (TDF). Additionally, TAF is associated with less renal toxicity than TDF but equal antiviral efficacy. A higher incidence of dyslipidemia has been reported with TAF than TDF. TAF is preferred over TDF whenever possible; do not use TAF and TDF concomitantly (HHS [pediatric] 2021).
Refer to individual components.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Acyclovir-Valacyclovir: May increase the serum concentration of Tenofovir Products. Tenofovir Products may increase the serum concentration of Acyclovir-Valacyclovir. Risk C: Monitor therapy
Adefovir: May diminish the therapeutic effect of Tenofovir Products. Adefovir may increase the serum concentration of Tenofovir Products. Tenofovir Products may increase the serum concentration of Adefovir. Risk X: Avoid combination
Aminoglycosides: May increase the serum concentration of Tenofovir Products. Tenofovir Products may increase the serum concentration of Aminoglycosides. Risk C: Monitor therapy
Antihepaciviral Combination Products: May increase the serum concentration of Bictegravir. Risk C: Monitor therapy
Atazanavir: May increase the serum concentration of Bictegravir. Risk C: Monitor therapy
Betibeglogene Autotemcel: Antiretroviral Agents may diminish the therapeutic effect of Betibeglogene Autotemcel. Risk X: Avoid combination
Cabozantinib: MRP2 Inhibitors may increase the serum concentration of Cabozantinib. Risk C: Monitor therapy
Calcium Salts: May decrease the serum concentration of Bictegravir. Management: Bictegravir, emtricitabine, and tenofovir alafenamide can be administered with calcium salts under fed conditions, but coadministration with or 2 hours after a calcium salt is not recommended under fasting conditions. Risk D: Consider therapy modification
CarBAMazepine: May decrease the serum concentration of Tenofovir Alafenamide. Risk X: Avoid combination
Cidofovir: May increase the serum concentration of Tenofovir Products. Tenofovir Products may increase the serum concentration of Cidofovir. Risk C: Monitor therapy
Cladribine: Agents that Undergo Intracellular Phosphorylation may diminish the therapeutic effect of Cladribine. Risk X: Avoid combination
Clofarabine: OCT2 Inhibitors may increase the serum concentration of Clofarabine. Risk C: Monitor therapy
Cobicistat: May increase the serum concentration of Tenofovir Alafenamide. Risk C: Monitor therapy
CYP3A4 Inducers (Strong): May decrease the serum concentration of Bictegravir. Risk C: Monitor therapy
Dalfampridine: OCT2 Inhibitors may increase the serum concentration of Dalfampridine. Management: Consider alternatives to this combination. Carefully weigh the risk of seizures against the benefit of combining OCT2 inhibitors with dalfampridine. Risk D: Consider therapy modification
Dofetilide: Bictegravir may increase the serum concentration of Dofetilide. Risk X: Avoid combination
Elivaldogene Autotemcel: Antiretroviral Agents may diminish the therapeutic effect of Elivaldogene Autotemcel. Management: Avoid use of antiretroviral medications for at least one month, or for the amount of time required for elimination of the retroviral medication, prior to stem cell mobilization and until the all apheresis cycles are finished Risk X: Avoid combination
Fosphenytoin-Phenytoin: May decrease the serum concentration of Tenofovir Alafenamide. Risk X: Avoid combination
Ganciclovir-Valganciclovir: Tenofovir Products may increase the serum concentration of Ganciclovir-Valganciclovir. Ganciclovir-Valganciclovir may increase the serum concentration of Tenofovir Products. Risk C: Monitor therapy
Iron Preparations: May decrease the serum concentration of Bictegravir. Management: Bictegravir, emtricitabine, and tenofovir alafenamide can be administered with iron preparations under fed conditions, but coadministration with or 2 hours after an iron preparation is not recommended under fasting conditions. Risk D: Consider therapy modification
Lumacaftor and Ivacaftor: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (High risk with Inhibitors or Inducers). Lumacaftor and Ivacaftor may decrease the serum concentration of P-glycoprotein/ABCB1 Substrates (High risk with Inhibitors or Inducers). Risk C: Monitor therapy
MetFORMIN: MATE1/2-K Inhibitors may increase the serum concentration of MetFORMIN. Risk C: Monitor therapy
Mitapivat: May decrease the serum concentration of UGT1A1 Substrates. Risk C: Monitor therapy
Nirmatrelvir and Ritonavir: May increase the serum concentration of Tenofovir Alafenamide. Risk C: Monitor therapy
Nonsteroidal Anti-Inflammatory Agents: May enhance the nephrotoxic effect of Tenofovir Products. Management: Seek alternatives to these combinations whenever possible. Avoid use of tenofovir with multiple NSAIDs or any NSAID given at a high dose due to a potential risk of acute renal failure. Diclofenac appears to confer the most risk. Risk D: Consider therapy modification
Nonsteroidal Anti-Inflammatory Agents (Topical): May enhance the nephrotoxic effect of Tenofovir Products. Risk C: Monitor therapy
Orlistat: May decrease the serum concentration of Antiretroviral Agents. Risk C: Monitor therapy
OXcarbazepine: May decrease the serum concentration of Tenofovir Alafenamide. Risk X: Avoid combination
P-glycoprotein/ABCB1 Inducers: May decrease the serum concentration of Tenofovir Alafenamide. Management: Consider alternatives to the use of P-gp inducers with tenofovir alafenamide. If combined, monitor for reduced tenofovir alafenamide concentrations and efficacy, and for the development of resistance. Risk D: Consider therapy modification
PHENobarbital: May decrease the serum concentration of Tenofovir Alafenamide. Risk X: Avoid combination
Polyvalent Cation Containing Products: May decrease the serum concentration of Bictegravir. Management: Administer bictegravir under fasting conditions at least 2 hours before or 6 hours after polyvalent cation containing products. Coadministration of bictegravir with or 2 hours after most polyvalent cation products is not recommended. Risk D: Consider therapy modification
Primidone: May decrease the serum concentration of Tenofovir Alafenamide. Risk X: Avoid combination
Rifabutin: May decrease the serum concentration of Tenofovir Alafenamide. Risk X: Avoid combination
Rifabutin: May decrease the serum concentration of Bictegravir. Risk X: Avoid combination
RifAMPin: May decrease the serum concentration of Tenofovir Alafenamide. Risk X: Avoid combination
RifAMPin: May decrease the serum concentration of Bictegravir. Risk X: Avoid combination
Rifapentine: May decrease the serum concentration of Tenofovir Alafenamide. Risk X: Avoid combination
Rifapentine: May decrease the serum concentration of Bictegravir. Risk X: Avoid combination
Ritonavir: May increase the serum concentration of Tenofovir Alafenamide. Risk C: Monitor therapy
St John's Wort: May decrease the serum concentration of Tenofovir Alafenamide. Risk X: Avoid combination
St John's Wort: May decrease the serum concentration of Bictegravir. Risk X: Avoid combination
Tipranavir: May decrease the serum concentration of Tenofovir Alafenamide. Risk X: Avoid combination
UGT1A1 Inducers: May decrease the serum concentration of Bictegravir. Risk C: Monitor therapy
The Health and Human Services (HHS) perinatal HIV guidelines note data are insufficient to recommend this fixed-dose combination for patients with HIV infection who are not yet pregnant but are trying to conceive.
Viral suppression sustained below the limits of detection with antiretroviral therapy (ART) and modification of therapy (if needed) is recommended in all patients with HIV infection who are planning a pregnancy. Optimization of the health of the person who will become pregnant and a discussion of the potential risks and benefits of ART during pregnancy is also recommended prior to conception. In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender diverse people assigned female sex at birth.
Health care providers caring for couples planning a pregnancy when one or both partners are diagnosed with HIV infection may contact the National Perinatal HIV Hotline (1-888-448-8765) for clinical consultation (HHS [perinatal] 2021).
Also refer to the emtricitabine and tenofovir alafenamide monographs for additional information specific to these components.
Bictegravir crosses the placenta.
Data collected by the antiretroviral registry related to the use of bictegravir in pregnancy are insufficient to evaluate teratogenicity. Refer to the emtricitabine and tenofovir alafenamide monographs for additional information specific to these components.
The Health and Human Services (HHS) perinatal HIV guidelines note data are insufficient to recommend this fixed-dose combination for pregnant patients with HIV infection who are antiretroviral-naive, who have had antiretroviral therapy (ART) in the past but are restarting, who require a new ART regimen (due to poor tolerance or poor virologic response of current regimen), or who become pregnant during therapy.
Pharmacokinetic studies of bictegravir are insufficient to make dosing recommendations for pregnant patients.
ART is recommended for all pregnant people with HIV infection to maximize their health, maintain the viral load below the limit of detection, and reduce the risk of perinatal transmission. Therapy should be individualized following a discussion of the potential risks and benefits of treatment during pregnancy. Patients on fully suppressive regimens prior to pregnancy generally may continue the same regimen considering known pregnancy outcomes and pharmacokinetic data. Monitoring of patients who are pregnant is more frequent than in patients who are not pregnant. ART initiated during pregnancy can be modified after delivery. In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender diverse people assigned female sex at birth.
Data collection to monitor pregnancy and infant outcomes following exposure to ART is ongoing. Health care providers are encouraged to enroll patients who are pregnant exposed to antiretroviral medications as early in pregnancy as possible in the Antiretroviral Pregnancy Registry (1-800-258-4263 or www.APRegistry.com).
Health care providers caring for pregnant patients with HIV infection and their infants may contact the National Perinatal HIV Hotline (1-888-448-8765) for clinical consultation (HHS [perinatal] 2021).
Emtricitabine is present in breast milk; excretion of bictegravir and tenofovir alafenamide are unknown.
This combination is recommended when acute HIV infection is detected in patients who are breastfeeding. Breastfeeding should be interrupted when acute HIV infection is suspected and not continued if infection is confirmed. Milk may be expressed and stored while waiting for confirmation.
Maternal or infant antiretroviral therapy does not completely eliminate the risk of postnatal HIV transmission. In addition, multiclass-resistant virus has been detected in breastfeeding infants despite maternal therapy. In the United States, where formula is usually accessible, affordable, safe, and sustainable, and the risk of infant mortality due to diarrhea and respiratory infections is low, the Health and Human Services (HHS) perinatal HIV guidelines do not recommend breastfeeding for patients with HIV infection when safer infant feeding options are available.
Information is available for counseling and managing patients with HIV infection who are considering breastfeeding (1-888-448-8765). In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender diverse people assigned female sex at birth (HHS [perinatal] 2021).
Also refer to the emtricitabine and tenofovir alafenamide monographs for additional information.
CD4 count, HIV RNA plasma levels; serum creatinine, estimated CrCl, urine glucose, urine protein (prior to initiation and as clinically indicated during therapy); serum phosphorus in patients with chronic kidney disease; hepatic function tests, bone density (patients with a history of bone fracture or have risk factors for bone loss); testing for hepatitis B virus (HBV) is recommended prior to the initiation of antiretroviral therapy. If used as therapy replacement in virologically suppressed patients meeting criteria, additional HIV-1 RNA and regimen tolerability monitoring is recommended to assess potential virologic failure or rebound. Patients with HIV and HBV coinfection should be monitored for several months following therapy discontinuation.
Bictegravir, an integrase inhibitor, inhibits HIV integrase by binding to the integrase-active site and blocking the strand transfer step of DNA integration. Emtricitabine is a cytidine analogue and tenofovir alafenamide is converted intracellularly to tenofovir (adenosine nucleotide analog) and subsequently phosphorylated by cellular kinases to the active moiety, tenofovir diphosphate. Emtricitabine and tenofovir alafenamide interfere with HIV viral RNA-dependent DNA polymerase activities resulting in inhibition of viral replication.
Protein binding: Bictegravir: >99%; Emtricitabine <4%; Tenofovir alafenamide ~80%
Metabolism:
Bictegravir: By CYP3A enzymes and hepatic glucuronidation mediated by UGT1A1
Emtricitabine: Not significantly metabolized
Tenofovir alafenamide: Converted intracellulary by hydrolysis (non-CYP enzymes) to tenofovir then phosphorylated by cellular kinases to the active moiety, tenofovir diphosphate; minimal extent by CYP3A
Half-life elimination: Bictegravir: 17.3 hours; Emtricitabine: 10.4 hours; Tenofovir alafenamide: 0.51 hours (active metabolite, tenofovir diphosphate: 150 to 180 hours [intracellular])
Time to peak: Bictegravir: 2 to 4 hours; Emtricitabine: 1.5 to 2 hours; Tenofovir alafenamide: 0.5 to 2 hours
Excretion: Bictegravir: Feces (60.3%), urine (35%); Emtricitabine: Feces (13.7%), urine (70%); Tenofovir alafenamide: Feces (31.7%), urine (<1%)
Pediatric: Exposures to all three components were higher in pediatric patients 3 to <12 years of age as compared to adults and trough concentrations of bictegravir were lower in pediatric patients 12 to <18 years as compared to adults; differences are not considered clinically significant.
Tablets (Biktarvy Oral)
30-120-15 mg (per each): $143.35
50-200-25 mg (per each): $143.35
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