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Dolutegravir (DTG / Tivicay)

Antiretroviralprescriptionoral · inferred

Second-generation INSTI with high genetic barrier to resistance, forming the backbone of many WHO-recommended first-line regimens (DTG/3TC/TDF, DTG/3TC, Triumeq, Dovato). Plasma half-life ~14h; metabolized primarily by UGT1A1 and CYP3A4. Effective once-daily unboosted dosing. Oral bioavailability high. Known to increase neural tube defect signal watched in early pregnancy (initial Tsepamo signal largely attenuated with follow-up).

Projected serum levels — 50 mg, once daily

Dolutegravir (DTG / Tivicay)
Dolutegravir (DTG / Tivicay) modeled serum levels, 50 mg once daily over 15 days Population-based pharmacokinetic estimate. Steady state reached after approximately 1 days. 0 25 50 75 100 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule ≈ steady state · day 1
Dolutegravir (DTG / Tivicay) modeled serum levels with a loading dose of 67.7 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: 67.7 mg on day 1, then 50 mg once daily — reaching therapeutic levels sooner.

Modeled steady state after ~1 days: peak ≈ 51.7 mg, trough ≈ 15.0 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
inferred
Half-life
14 h
Common dose
50 mg
Suggested maximum
100 mg/day
Reference dose range
25–100 mg (single dose)
Suggested cadence
once daily
Validated against
50 mg oral — Cmax 3.7 mg/L at 2 h

Documented interactions

  • danger
    Carbamazepine (Tegretol) + Dolutegravir (DTG / Tivicay) CYP induction

    Carbamazepine (Tegretol) inducer of CYP3A4 predicted to change Dolutegravir (DTG / Tivicay) AUC by ~0.44x

  • danger
    Efavirenz (Sustiva) + Dolutegravir (DTG / Tivicay) CYP induction

    Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Dolutegravir (DTG / Tivicay) AUC by ~0.31x

  • danger
    Levothyroxine (Synthroid) + Dolutegravir (DTG / Tivicay) Protein binding

    Dolutegravir (DTG / Tivicay) may displace Levothyroxine (Synthroid) from plasma protein binding sites, transiently raising free drug concentration. This drug has a narrow therapeutic index; free…

  • danger
    Rifampin + Dolutegravir (DTG / Tivicay) CYP induction

    Rifampin inducer of CYP3A4 predicted to change Dolutegravir (DTG / Tivicay) AUC by ~0.31x

  • danger
    Tacrolimus (Prograf) + Dolutegravir (DTG / Tivicay) Protein binding

    Dolutegravir (DTG / Tivicay) may displace Tacrolimus (Prograf) from plasma protein binding sites, transiently raising free drug concentration. This drug has a narrow therapeutic index; free…

  • danger
    Warfarin (Coumadin) + Dolutegravir (DTG / Tivicay) Protein binding

    Dolutegravir (DTG / Tivicay) may displace Warfarin (Coumadin) from plasma protein binding sites, transiently raising free drug concentration. This drug has a narrow therapeutic index; free…

Serum checks 242 modeled interaction pairings for dolutegravir (dtg / tivicay) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.

Research behind this entry

  1. Pharmacokinetics and safety of dolutegravir (S/GSK1349572) in HIV-1-infected individuals Min S et al. · AIDS, 2011 DOI

    First-in-HIV-patients study establishing dolutegravir's pharmacokinetic profile and dose-response, supporting 50 mg once-daily development.

  2. Once-daily dolutegravir versus raltegravir in antiretroviral-naive adults with HIV-1 infection: 48 week results from the randomised, double-blind, non-inferiority SPRING-2 study Raffi F et al. · Lancet, 2013 DOI

    SPRING-2 trial establishing dolutegravir non-inferior to raltegravir with convenient once-daily dosing and favorable resistance profile.

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