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Bictegravir (BIC)

Antiretroviralprescriptionoral · predicted

Second-generation integrase strand transfer inhibitor (INSTI) with high barrier to resistance, co-formulated with TAF and FTC as Biktarvy. Not available as standalone. Plasma half-life ~18h supports once-daily dosing. Oral bioavailability ~70%; metabolized by CYP3A4 and UGT1A1. Unboosted (unlike elvitegravir) so fewer drug interactions than older INSTIs.

Projected serum levels — 50 mg, once daily

Bictegravir (BIC)
Bictegravir (BIC) modeled serum levels, 50 mg once daily over 15 days Population-based pharmacokinetic estimate. Steady state reached after approximately 3 days. 0 25 50 75 100 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule ≈ steady state · day 3
Bictegravir (BIC) modeled serum levels with a loading dose of 104 mg, then 50 mg once daily The first dose is larger so levels approach steady state faster. 0 25 50 75 100 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule

Maintenance schedule: 50 mg once daily (oral).

Loading schedule: 104 mg on day 1, then 50 mg once daily — reaching therapeutic levels sooner.

Modeled steady state after ~3 days: peak ≈ 63.5 mg, trough ≈ 40.2 mg body load. Population-based estimate over 15 days for a 50 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.

Key facts

Category
Antiretroviral
Route modeled
Oral
Model confidence
predicted
Half-life
17 h
Common dose
50 mg
Suggested maximum
50 mg/day
Reference dose range
25–50 mg (single dose)
Suggested cadence
once daily
Validated against
50 mg oral — Cmax 6.2 mg/L at 2 h

Documented interactions

  • contraindicated
    Efavirenz (Sustiva) + Bictegravir (BIC) CYP induction

    Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Bictegravir (BIC) AUC by ~0.20x

  • contraindicated
    Rifampin + Bictegravir (BIC) CYP induction

    Rifampin inducer of CYP3A4 predicted to change Bictegravir (BIC) AUC by ~0.20x

  • danger
    Carbamazepine (Tegretol) + Bictegravir (BIC) CYP induction

    Carbamazepine (Tegretol) inducer of CYP3A4 predicted to change Bictegravir (BIC) AUC by ~0.30x

  • danger
    Clarithromycin (Biaxin) + Bictegravir (BIC) CYP inhibition

    Clarithromycin (Biaxin) mechanism_based of CYP3A4 predicted to change Bictegravir (BIC) AUC by ~2.12x

  • danger
    Diltiazem + Bictegravir (BIC) CYP inhibition

    Diltiazem mechanism_based of CYP3A4 predicted to change Bictegravir (BIC) AUC by ~2.12x

  • danger
    Grapefruit (whole fruit) + Bictegravir (BIC) CYP inhibition

    Grapefruit (whole fruit) mechanism_based of CYP3A4 predicted to change Bictegravir (BIC) AUC by ~2.12x

Serum checks 231 modeled interaction pairings for bictegravir (bic) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.

Research behind this entry

  1. Antiviral activity, safety, and pharmacokinetics of bictegravir as 10-day monotherapy in HIV-1-infected adults Gallant JE et al. · Lancet HIV, 2017 DOI

    First-in-HIV-patients monotherapy PK/PD study establishing bictegravir's potent antiviral activity and PK supporting 50 mg once-daily dosing.

  2. Bictegravir: first global approval Deeks ED · Drugs, 2018 DOI

    Regulatory review summarizing bictegravir's pharmacology, PK, clinical efficacy, and approval as part of BIC/FTC/TAF (Biktarvy).

2 published studies referenced in the app, each with a plain-language summary.