Pharmacokinetics and Safety of Bictegravir in Pregnant and Postpartum Persons With HIV and Their Infants
Issued Date
2025-03-01
Resource Type
ISSN
15254135
eISSN
19447884
Scopus ID
2-s2.0-85210310258
Pubmed ID
39813286
Journal Title
Journal of Acquired Immune Deficiency Syndromes (1999)
Volume
98
Issue
3
Start Page
300
End Page
307
Rights Holder(s)
SCOPUS
Bibliographic Citation
Journal of Acquired Immune Deficiency Syndromes (1999) Vol.98 No.3 (2025) , 300-307
Suggested Citation
Powis K.M., Pinilla M., McMorrow F., Stek A., Brooks K.M., Shapiro D.E., Knowles K., Eke A.C., Greene E., Agwu A., Topete L., Browning R., Chakhtoura N., Arora P., Huang X., Best B.M., Mirochnick M., Momper J.D., Deville J.G., Carter M.F., Nielsen-Saines K., Floyd R., Thomas-Seaton L.T., Jordan-Thompson S., Moore R.M., Mills M., Rosenberg M.G., Haines A., Anderson T., Collinson-Streng A., Jao J., Lartey E., Cehic R., Gomez N., Alverez G.A., Mitchell C.D., Aziz M., Cejtin H., McNichols M., Rungmaitree S., Phatharadom P., Morales Y., Spector S.A., Deutsch K., Loughran M. Pharmacokinetics and Safety of Bictegravir in Pregnant and Postpartum Persons With HIV and Their Infants. Journal of Acquired Immune Deficiency Syndromes (1999) Vol.98 No.3 (2025) , 300-307. 307. doi:10.1097/QAI.0000000000003571 Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/105334
Title
Pharmacokinetics and Safety of Bictegravir in Pregnant and Postpartum Persons With HIV and Their Infants
Author(s)
Powis K.M.
Pinilla M.
McMorrow F.
Stek A.
Brooks K.M.
Shapiro D.E.
Knowles K.
Eke A.C.
Greene E.
Agwu A.
Topete L.
Browning R.
Chakhtoura N.
Arora P.
Huang X.
Best B.M.
Mirochnick M.
Momper J.D.
Deville J.G.
Carter M.F.
Nielsen-Saines K.
Floyd R.
Thomas-Seaton L.T.
Jordan-Thompson S.
Moore R.M.
Mills M.
Rosenberg M.G.
Haines A.
Anderson T.
Collinson-Streng A.
Jao J.
Lartey E.
Cehic R.
Gomez N.
Alverez G.A.
Mitchell C.D.
Aziz M.
Cejtin H.
McNichols M.
Rungmaitree S.
Phatharadom P.
Morales Y.
Spector S.A.
Deutsch K.
Loughran M.
Pinilla M.
McMorrow F.
Stek A.
Brooks K.M.
Shapiro D.E.
Knowles K.
Eke A.C.
Greene E.
Agwu A.
Topete L.
Browning R.
Chakhtoura N.
Arora P.
Huang X.
Best B.M.
Mirochnick M.
Momper J.D.
Deville J.G.
Carter M.F.
Nielsen-Saines K.
Floyd R.
Thomas-Seaton L.T.
Jordan-Thompson S.
Moore R.M.
Mills M.
Rosenberg M.G.
Haines A.
Anderson T.
Collinson-Streng A.
Jao J.
Lartey E.
Cehic R.
Gomez N.
Alverez G.A.
Mitchell C.D.
Aziz M.
Cejtin H.
McNichols M.
Rungmaitree S.
Phatharadom P.
Morales Y.
Spector S.A.
Deutsch K.
Loughran M.
Author's Affiliation
Siriraj Hospital
Skaggs School of Pharmacy & Pharmaceutical Sciences
Department of Pediatrics
FHI 360
Frontier Science & Technology Research Foundation, Inc.
Harvard T.H. Chan School of Public Health
University of California, San Diego
Massachusetts General Hospital
University of Southern California
University of Miami
University of Colorado Anschutz Medical Campus
Jacobi Medical Center
National Institute of Child Health and Human Development (NICHD)
National Institute of Allergy and Infectious Diseases (NIAID)
Keck School of Medicine of USC
Boston University Chobanian & Avedisian School of Medicine
Center for Biostatistics in AIDS Research
Johns Hopkins University
David Geffen School of Medicine at UCLA
Gilead Sciences Incorporated
Emory University School of Medicine
Rush University
Johns Hopkins University School of Medicine
Lurie Children’s Hospital
Skaggs School of Pharmacy & Pharmaceutical Sciences
Department of Pediatrics
FHI 360
Frontier Science & Technology Research Foundation, Inc.
Harvard T.H. Chan School of Public Health
University of California, San Diego
Massachusetts General Hospital
University of Southern California
University of Miami
University of Colorado Anschutz Medical Campus
Jacobi Medical Center
National Institute of Child Health and Human Development (NICHD)
National Institute of Allergy and Infectious Diseases (NIAID)
Keck School of Medicine of USC
Boston University Chobanian & Avedisian School of Medicine
Center for Biostatistics in AIDS Research
Johns Hopkins University
David Geffen School of Medicine at UCLA
Gilead Sciences Incorporated
Emory University School of Medicine
Rush University
Johns Hopkins University School of Medicine
Lurie Children’s Hospital
Corresponding Author(s)
Other Contributor(s)
Abstract
Background: Limited data exist on bictegravir pharmacokinetics in pregnancy among persons with HIV (PWH) and infant washout. Setting: Nonrandomized, open-label, multicenter phase-IV prospective study of bictegravir pharmacokinetics and safety in pregnant PWH and their infants. Methods: Steady-state 24-hour pharmacokinetic sampling of oral bictegravir 50 mg once daily (a component of fixed-dose combination bictegravir/emtricitabine/tenofovir alafenamide) during the second and third trimesters and postpartum was performed. Cord blood and infant washout samples were collected. Total and free bictegravir concentrations were measured by validated liquid chromatography with tandem mass spectrometry methods. Within-participant geometric mean ratios (GMR) with 90% confidence intervals (CI) were calculated to compare pharmacokinetics between second and third trimester versus postpartum. Infant HIV testing results were obtained. Results: Twenty-seven maternal–infant pairs were enrolled. Bictegravir area under the concentration–time curve from time 0 through 24 hours post-dose was 46% lower in the second trimester (n = 12; P = 0.002; GMR 0.54; 90% CI: 0.43 to 0.69) and 52% lower in the third trimester (n = 24; P, 0.0001; GMR 0.48; 90% CI: 0.43 to 0.55), compared with postpartum. C24 concentrations were above the estimated bictegravir protein-adjusted 95% effective concentration of 0.162 mg/mL. The median ratio of cord-to-maternal blood concentration was 1.38 (n = 17; quartiles: 1.17–1.63). Median T1/2 for infant bictegravir washout was 33.2 hours (quartiles: 25.7–45.9) with a Cmax of 2.06 mg/mL (quartiles: 1.37–2.72). Overall, 88%–92% of participants maintained suppression, 40 copies/mL throughout pregnancy and postpartum. All available infant HIV testing results were negative. The safety profile for pregnant PWH and infants was acceptable. Conclusions: Bictegravir exposure was lower during pregnancy compared with postpartum, yet C24 concentrations were greater than the bictegravir protein-adjusted 95% effective concentration.