s unknown (see section 4.4).
Changes in serum creatinine
Bictegravir has been shown to increase serum creatinine due to inhibition of tubular secretion of creatinine, however these changes are not considered to be clinically relevant since they do not reflect a change in glomerular filtration rate. Increases in serum creatinine occurred by Week 4 of treatment and remained stable through Week 48. In Studies GS-US-380-1489 and GS-US-380-1490, median (Q1, Q3) serum creatinine increased by 0.10 (0.03, 0.17) mg/dL, 0.11 (0.03, 0.18) mg/dL, and 0.11 (0.04, 0.19) mg/dL from baseline to Week 48 in the Biktarvy, abacavir/dolutegravir/lamivudine, and dolutegravir+emtricitabine/tenofovir alafenamide groups, respectively. There were no discontinuations due to renal adverse events through Week 48 in Biktarvy clinical studies.
Changes in bilirubin
In Studies GS-US-380-1489 and GS-US-380-1490, total bilirubin increases were observed in 12% of treatment-naïve patients administered Biktarvy through Week 48. Increases were primarily Grade 1 (9%) and Grade 2 (3%) (1.0 to 2.5 x Upper Limit of Normal [ULN]), and were not associated with hepatic adverse reactions or other liver related laboratory abnormalities. There were no discontinuations due to hepatic adverse events through Week 48 in Biktarvy clinical studies.
Other special populations
Patients co-infected with hepatitis B
In 16 HIV/HBV co-infected adults administered Biktarvy (8 HIV/HBV treatment-naïve adults in Study GS-US-380-1490; 8 HIV/HBV suppressed adults in Study GS-US-380-1878), the safety profile of Biktarvy was similar to that in patients with HIV-1 monoinfection (see section 5.1).
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the national reporting system:
United Kingdom
Yellow Card Scheme
Website: www.mhra.gov.uk/yellowcard
or search for MHRA Yellow Card in the Google Play or Apple App Store
Ireland
HPRA Pharmacovigilance
Earlsfort Terrace
IRL - Dublin 2
Tel: +353 1 6764971
Fax: +353 1 6762517
Website: www.hpra.ie
e-mail: medsafety@hpra.ie
Malta
ADR Reporting
Website: www.medicinesauthority.gov.mt/adrportal
4.9 Overdose
If overdose occurs the patient must be monitored for evidence of toxicity (see section 4.8). Treatment of overdose with Biktarvy consists of general supportive measures including monitoring of vital signs as well as observation of the clinical status of the patient.
There is no specific antidote for overdose with Biktarvy. As bictegravir is highly bound to plasma proteins, it is unlikely that it will be significantly removed by hemodialysis or peritoneal dialysis. Emtricitabine can be removed by hemodialysis, which removes approximately 30% of the emtricitabine dose over a 3 hour dialysis period starting within 1.5 hours of emtricitabine dosing. Tenofovir is efficiently removed by hemodialysis with an extraction coefficient of approximately 54%. It is not known whether emtricitabine or tenofovir can be removed by peritoneal dialysis.
5. Pharmacological properties
5.1 Pharmacodynamic properties
Pharmacotherapeutic group: Antiviral for systemic use; antivirals for treatment of HIV infections, combinations, ATC code: J05AR20
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