{"doi":"10.1093/jac/dkab155","title":"Antiretroviral drug exposure in urethral and glans surface sampling of the penis","abstract":"BACKGROUND: HIV exposure to penile tissues provides a risk of acquisition among men, yet studies evaluating penile antiretroviral (ARV) drug distribution have been lacking. We measured ARVs on urethral and glans surface swabs collected following a dose of tenofovir alafenamide, emtricitabine, elvitegravir, darunavir and cobicistat. METHODS: Thirty-five HIV-negative male participants provided urethral swabs, glans swabs, rectal swabs, blood and urine up to 96 h following a single dose of tenofovir alafenamide/emtricitabine/elvitegravir/cobicistat and darunavir. ARVs were measured by liquid chromatography-mass spectrometry with a lower limit of detection (LOD) of 1 ng/swab for swabs and 10 ng/mL for plasma and urine. Concentrations are reported as median and range. RESULTS: Urethral swab emtricitabine and darunavir concentrations peaked at 4 h for emtricitabine (36 ng/swab; 3-307 ng/swab) and 8 h for darunavir (25 ng/swab; 2-52 ng/swab). Glans swab emtricitabine and darunavir concentrations peaked 24 h after dosing (emtricitabine 14 ng/swab, <LOD-328 ng/swab; darunavir 6 ng/swab, <LOD-149 ng/swab). Estimated peak urethral secretion emtricitabine and darunavir concentrations are between 10 and 20 μg/mL, similar to rectal secretions, 4-fold greater than in plasma, but 2-fold lower than in urine. Tenofovir and elvitegravir were detected on less than 20% of urethral or glans swabs collected within 24 h of dosing. CONCLUSIONS: We document ARV dosing in the urethra and on the glans surface with high drug concentrations noted for emtricitabine and darunavir and lower tenofovir and elvitegravir concentrations. Data suggest a potential protective role of urethral emtricitabine or darunavir against penile HIV acquisition.","journal":"Journal of Antimicrobial Chemotherapy","year":2021,"id":202386,"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":6,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9027,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2021-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":782405,"name":"Jeffrey J. Fountain","orcid":"0000-0001-9473-7705","position":1,"is_corresponding":false},{"id":341005,"name":"Chuong Dinh","orcid":null,"position":2,"is_corresponding":false},{"id":783054,"name":"L. Davis Lupo","orcid":null,"position":3,"is_corresponding":false},{"id":327668,"name":"Amy Martin","orcid":null,"position":4,"is_corresponding":false},{"id":783055,"name":"Christopher Conway-Washington","orcid":null,"position":5,"is_corresponding":false},{"id":782406,"name":"LaShonda Hall","orcid":"0000-0002-1769-9888","position":6,"is_corresponding":false},{"id":340072,"name":"Colleen F. Kelley","orcid":"0000-0001-5611-0119","position":7,"is_corresponding":false},{"id":340074,"name":"J. Gerardo Garcı́a-Lerma","orcid":"0000-0001-6437-7745","position":8,"is_corresponding":false},{"id":340073,"name":"Walid Heneine","orcid":"0000-0003-3119-3565","position":9,"is_corresponding":false},{"id":326320,"name":"Richard E. Haaland","orcid":"0000-0001-8165-3879","position":0,"is_corresponding":true}],"reference_count":37,"raw_metadata":null,"created_at":"2026-07-18T23:51:10.291262Z","pmid":"34007982","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":[]}