{"doi":"10.17615/8ym0-mf79","title":"A Modified Grapefruit Juice Eliminates Two Compound Classes as Major Mediators of the Grapefruit Juice-Fexofenadine Interaction: An In Vitro-In Vivo “Connect”: The Journal of Clinical Pharmacology","abstract":"The grapefruit juice-fexofenadine interaction involves inhibition of intestinal organic anion transporting polypeptide (OATP)-mediated uptake. Only naringin has been shown clinically to inhibit intestinal OATP; other constituents have not been evaluated. The effects of a modified grapefruit juice devoid of furanocoumarins (~99%) and polymethoxyflavones (~90%) on fexofenadine disposition were compared to effects of the original juice. Extracts of both juices inhibited estrone 3-sulfate and fexofenadine uptake by similar extents in OATP-transfected cells (~50% and ~25%, respectively). Healthy volunteers (n=18) were administered fexofenadine (120 mg) with water, grapefruit juice, or modified grapefruit juice (240 ml) by randomized, three-way crossover design. Compared to water, both juices decreased fexofenadine geometric mean AUC and Cmax by ~25% (p≤0.008 and p≤0.011, respectively), with no effect on terminal half-life (p=0.11). Similar effects by both juices on fexofenadine pharmacokinetics indicate furanocoumarins and polymethoxyflavones are not major mediators of the grapefruit juice-fexofenadine interaction.","journal":"UNC Libraries","year":2020,"id":137019,"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":0,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9584,"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":596218,"name":"Paul A. Dawson","orcid":"0000-0002-7318-4985","position":1,"is_corresponding":false},{"id":596219,"name":"Tian Lan","orcid":"0000-0001-7713-5411","position":2,"is_corresponding":false},{"id":255429,"name":"Mary F. Paine","orcid":"0000-0002-3331-1839","position":3,"is_corresponding":false},{"id":596909,"name":"Wilbur Widmer","orcid":null,"position":4,"is_corresponding":false},{"id":596910,"name":"Yolanda V. Scarlett","orcid":null,"position":5,"is_corresponding":false},{"id":596220,"name":"Karen M. VanderMolen","orcid":"0000-0002-1637-8660","position":6,"is_corresponding":false},{"id":593850,"name":"Christina S. Won","orcid":null,"position":7,"is_corresponding":false},{"id":267276,"name":"Nicholas H. Oberlies","orcid":"0000-0002-0354-8464","position":0,"is_corresponding":true}],"reference_count":0,"raw_metadata":null,"created_at":"2026-07-18T23:16:52.487376Z","pmid":null,"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":[]}