https://interactions.guidetherapeutiquevih.com/en/interaction-details?id=19211

Bictegravir

Metformin

No clinically significant interactions were observed.

No pharmaceutical opinion available for this interaction.

Mechanism

Bictegravir can inhibit the renal transport (OCT2 and MATE 1) and increase plasma concentration of Metformin.

Bictegravir

Pharmacodynamic effects

–

Recommendations

–

Alternative solution(s)

–

Metformin

Pharmacodynamic effects

Interaction considered clinically non-significant according to the monograph.

Recommendations

No dosage adjustment is necessary.

Close monitoring of adverse effects should be considered in patients with moderate renal impairment.

Alternative solution(s)

–

Monitor

Adverse effects of metformin: gastrointestinal effects and symptoms related to hypoglycemia.

Monitor signs and symptoms of lactic acidosis: nausea, vomiting, stomach pain, weight loss, shortness of breath, and great fatigue.

Tests

Blood Sugar

Pharmacokinetic parameters
Parameters
Reference number
# patients
Dose
Frequency
Duration (days)
HIV
AUC
Cmax
Cmin
Bictegravir
3368
16
75 mg *
QD
4
-
 
 
 
Metformin
3368
16
850 mg/500 mg †
BID †
4
-
+ 39% °
+ 28% °
+ 36% °
Comment

Ref #3368 : * Given with emtricitabine/tenofovir alafenamide (200/25 mg).
† 850 mg metformin at 12 hours postdose of B/F/TAF or placebo and 500 mg BID after.
° When coadministered with B/F/TAF relative to placebo.
Metformin t1/2 was similar, renal clearance decreased approximately by 31% but importantly, clinically-relevant pharmacodynamics responses were not statistically different.

Comment
Reference
  • 3392
    Bictegravir/emtricitabine/tenofovir alafenamide (BIKTARVY), Gilead Sciences, Ontario, Canada, 14 avril 2023.
  • 3368
    Zhang H, West S, Vu A, Martin H, Graham H et al. Lack of Clinically Relevant Effect of Bictegravir on Metformin Pharmacokinetics and Pharmacodynamics. 18th International Workshop on Clinical Pharmacology of Antiviral Therapy. June 14-16, 2017, Chicago, USA, Abstract P_50.