{"doi":"10.1093/cid/ciaa1416","title":"Dynamics of the Decay of Human Immunodeficiency Virus (HIV) RNA and Distribution of Bictegravir in the Genital Tract and Rectum in Antiretroviral-naive Adults Living With HIV–1 Treated With Bictegravir/Emtricitabine/Tenofovir Alafenamide (Spanish HIV/AIDS Research Network, PreEC/RIS 58)","abstract":"BACKGROUND: The pharmacokinetics of bictegravir (BIC) and its association with the decay of human immunodeficiency virus (HIV)-1 RNA in genital fluids and the rectum have not yet been addressed. METHODS: We conducted a prospective, multicenter study of antiretroviral-naive people living with HIV-1 and initiating BIC/emtricitabine (FTC)/tenofovir alafenamide (TAF). HIV-1 RNA was measured (limit of quantification, 40 copies/mL) in blood plasma (BP), seminal plasma (SP), rectal fluid (RF), and cervicovaginal fluid (CVF) at baseline; Days 3, 7, 14, and 28; and Weeks 12 and 24. Total and protein-unbound BIC concentrations at 24 hours postdose (C24h) were quantified in BP, SP, CVF and rectal tissue (RT) on Day 28 and Week 12 using a validated liquid chromatography-tandem mass spectrometry assay. RESULTS: The study population comprised 15 males and 8 females. In SP, RF, and CVF, the baseline HIV-1 RNA was >40 copies/mL in 12/15, 13/15, and 4/8 individuals, respectively, with medians of 3.54 (2.41-3.79), 4.19 (2.98-4.70), and 2.56 (1.61-3.56) log10 copies/mL, respectively. The initial decay slope was significantly lower in SP than in RF and BP. The time to undetectable HIV-1 RNA was significantly shorter in SP and RF than in BP. All women achieved undetectable HIV-1 RNA in CVF at Day 14. The median total BIC concentrations in SP, RT, and CVF were 65.5 (20.1-923) ng/mL, 74.1 (6.0-478.5) ng/g, and 61.6 (14.4-1760.2) ng/mL, respectively, representing 2.7%, 2.6%, and 2.8% of the BP concentration, respectively, while the protein-unbound fractions were 51.1%, 44.6%, and 42.6%, respectively. CONCLUSIONS: BIC/FTC/TAF led to rapid decay of HIV-1 RNA in genital and rectal fluids. Protein-unbound BIC concentrations in SP, RT, and CVF highly exceeded the half-maximal effective concentration (EC50) value (1.1 ng/mL). CLINICAL TRIALS REGISTRATION: EudraCT 2018-002310-12.","journal":"Clinical Infectious Diseases","year":2020,"id":69982,"datarank":0.0,"base_score":0.0,"endowment":0.0,"self_citation_contribution":0.0,"citation_network_contribution":0.0,"self_endowment_contribution":0.0,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":20,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.8745,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2020-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":370686,"name":"Juan Tiraboschi","orcid":"0000-0002-0073-873X","position":1,"is_corresponding":false},{"id":370687,"name":"Jordí Niubó","orcid":"0000-0001-9511-0138","position":2,"is_corresponding":false},{"id":31314,"name":"Javier Martínez‐Picado","orcid":"0000-0002-4916-2129","position":3,"is_corresponding":false},{"id":370688,"name":"Mackenzie L. Cottrell","orcid":"0000-0002-0291-5111","position":4,"is_corresponding":false},{"id":370689,"name":"Peré Domingo","orcid":"0000-0003-1138-5770","position":5,"is_corresponding":false},{"id":370690,"name":"Iván Chivite","orcid":"0000-0002-1959-246X","position":6,"is_corresponding":false},{"id":97915,"name":"Eugènia Negredo","orcid":"0000-0001-5298-1734","position":7,"is_corresponding":false},{"id":370691,"name":"Amanda P. Schauer","orcid":"0000-0002-7026-7224","position":8,"is_corresponding":false},{"id":372555,"name":"Brian Van Horne","orcid":null,"position":9,"is_corresponding":false},{"id":372556,"name":"Sandra Morenilla","orcid":null,"position":10,"is_corresponding":false},{"id":369701,"name":"Víctor Urrea","orcid":"0000-0002-2577-856X","position":11,"is_corresponding":false},{"id":370692,"name":"Ana Silva‐Klug","orcid":"0000-0003-4660-534X","position":12,"is_corresponding":false},{"id":370693,"name":"Sofía Scévola","orcid":"0000-0003-3578-5031","position":13,"is_corresponding":false},{"id":370694,"name":"Benito García","orcid":"0000-0003-1320-5227","position":14,"is_corresponding":false},{"id":370695,"name":"Angela D. M. Kashuba","orcid":"0000-0002-9171-8493","position":15,"is_corresponding":false},{"id":372557,"name":"Daniel Podzamczer","orcid":null,"position":16,"is_corresponding":false},{"id":370685,"name":"Arkaitz Imaz","orcid":"0000-0001-8411-1952","position":0,"is_corresponding":true}],"reference_count":31,"raw_metadata":null,"created_at":"2026-07-18T21:43:11.119231Z","pmid":"32945851","pmcid":null,"fwci":null,"citation_percentile":null,"influential_citations":0,"oa_status":null,"license":null,"views":0,"total_file_size_bytes":0,"version_count":0,"fair_f":null,"fair_a":null,"fair_i":null,"fair_r":null,"fair_zscore":null,"fair_rationale":null,"fair_model":null,"fair_agent_version":null,"fair_fulltext_source":null,"fair_has_llm":null,"fair_computed_at":null,"clinical_trials":[],"software_tools":[],"db_accessions":[],"linked_datasets":[],"topics":[]}