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Record W4413940474 · doi:10.1002/bcp.70208

Plasma bictegravir/emtricitabine/tenofovir alafenamide concentrations in transgender women with HIV on oestrogen‐based gender‐affirming hormone therapy in comparison to cisgender women living with HIV

2025· article· en· W4413940474 on OpenAlexaff
Sumito Sunagawa, Mona Loutfy, Alice Tseng, Ashley Lacombe‐Duncan, Yasmeen Persad, R. Fung, I. Armstrong, Lawrence Chan, Quang Nguyen, Susan Hranilovic, David S.P. Tan, Roberta Halpenny, Nirubini Jeyarajah, James D. McCully, Kimberly K. Scarsi

Bibliographic record

VenueBritish Journal of Clinical Pharmacology · 2025
Typearticle
Languageen
FieldMedicine
TopicHIV-related health complications and treatments
Canadian institutionsWellesley InstituteSt. Michael's HospitalOntario Ministry of LabourToronto East General HospitalUniversity of TorontoToronto General HospitalMaple Leaf FoodsMaple Leaf Medical ClinicWomen's College Hospital
Fundersnot available
KeywordsTenofovir alafenamideEmtricitabineHuman immunodeficiency virus (HIV)Transgender womenMedicineSex hormone-binding globulinTenofovirTransgender PersonGynecologyInternal medicineHormonePharmacologyOncologyVirologyAntiretroviral therapyMen who have sex with menViral loadAndrogen

Abstract

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5 Background: Oestrogen-based gender-affirming hormone therapy (E-GAHT) typically consists of an oestrogen ± an anti-androgen and is essential for many transgender women. However, there is concern regarding drug–drug interactions (DDIs) between antiretroviral therapy (ART) and E-GAHT. This study's objective was to investigate the pharmacokinetics of bictegravir/emtricitabine/tenofovir alafenamide (BIC/FTC/TAF) in transgender women taking E-GAHT compared to pre-menopausal cisgender women. Methods: We conducted a parallel group study in adult transgender women with HIV taking ART (transgender group) and cisgender women with HIV taking ART (control group). All participants were on suppressive ART for at least 6 months prior to and either taking or switched to BIC/FTC/TAF at entry. All participants in the transgender group were taking at least 2 mg/day of oral estradiol and anti-androgen therapy and could not have any E-GAHT medication changes for at least 3 months prior to entry. At the Month 2 visit, blood samples were collected prior to ART and E-GAHT dosing (if applicable) and then at 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 24 h post-dose. BIC, FTC and TAF plasma concentrations were measured using a validated LC-MC/MS assay. Maximum (Cmax) and minimum (Cmin) concentrations were observed, and area under the concentration-time curve (AUC) over 24 h was calculated by non-compartmental methods. Data are presented as median (IQR) and compared between transgender and control groups by geometric mean ratio (GMR) with 90% confidence intervals (CI). Results: A total of 25 participants were enrolled, 10 transgender women and 15 cisgender women. E-GAHT consisted of a median estradiol dose of 4 mg (4, 4). Anti-androgen therapy included spironolactone (n = 6), cyproterone (n = 2), hypopituitarism (n = 1) and orchidectomy (n = 1). Median BIC Cmax, Cmin and AUC for the transgender group were 9.1 mcg/mL (8.1, 9.6), 2.6 mcg/mL (1.1, 3.1) and 119.5 h*mcg/mL (86.6, 141.2), respectively, compared to 7.2 mcg/mL (6.4, 9), 1.9 mcg/mL (1.4, 3.4) and 123.9 h*mcg/mL (79.7, 133.2), respectively, for the Control group. BIC PK parameters were similar between groups (GMR [90% CI]: 1.1 [0.9, 1.4], 1 [0.6, 1.7], and 1 [0.8, 1.3], respectively). Median FTC Cmax, Cmin and AUC for the transgender group were 2 mcg/mL (1.3, 2.5), 0.1 mcg/mL (0.1, 0.1) and 10.7 h*mcg/mL (8.7, 14), respectively, compared to 2 mcg/mL (1.6, 2.3), 0.1 mcg/mL (0.1, 0.1) and 11 h*mcg/mL (9.8, 15.6), respectively, for the control group. FTC PK parameters were similar between groups (GMR [90% CI]: 0.9 [0.8, 1.2], 1.1 [0.8, 1.5], and 1 [0.8, 1.2], respectively). Median TAF Cmax, Cmin and AUC for the transgender group were 164 ng/mL (90, 335), 0.5 ng/mL (0.5, 0.5) and 143 h*ng/mL (116, 320), respectively, compared to 250 ng/mL (132, 396), 0.5 ng/mL (0.5, 0.5) and 230 h*ng/mL (189, 394), respectively, for the control group. TAF PK parameters were similar between groups (GMR [90% CI]: 0.7 [0.4, 1.2], 1 [1, 1], and 0.7 [0.5, 1], respectively). All participants remained virally suppressed (HIV RNA < 200 copies/mL) throughout the study. Conclusion: BIC/FTC/TAF plasma pharmacokinetics were similar between groups, indicating no clinically significant effect of oral E-GAHT on BIC/FTC/TAF.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame machine prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. The Gemma side is a direct model label for every work in the frame, read from the title-only record. The Codex side is a classifier learned from the 10,348 direct Codex labels and calibrated to design-weighted sample rates; fields without enough sample support carry no Codex call. Candidate is the union of the two sides; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels.

metaresearch head score (Codex)0.000
metaresearch head score (Gemma)0.000
Version: metacan-v3-hybrid-931329e0061cValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Observational · Consensus signal: Observational
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.002
Threshold uncertainty score0.006

Distilled classifier scores by category (both heads)

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.000
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.000
Insufficient payload (model declined to judge)0.0020.000

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.056
GPT teacher head0.403
Teacher spread0.347 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one source (direct Gemma or distilled Codex), not a consensus.

The models applied no category: nothing in the taxonomy fit this work.
Study designObservational
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

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Published2025
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