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It is currently under development for the treatment of drug-susceptible and drug-resistant tuberculosis. A first-in-human trial of TBAJ-587, including single and multiple ascending oral doses and a dedicated food-effect cohort, was conducted in 92 healthy adults. Plasma exposures of TBAJ-587 were generally linear for AUC\n                      <jats:sub>tau<\/jats:sub>\n                      and slightly subproportional for\n                      <jats:italic toggle=\"yes\">C<\/jats:italic>\n                      <jats:sub>max<\/jats:sub>\n                      , with the major circulating active metabolite, M3, remaining low relative to the parent. A high-fat meal increased the mean\n                      <jats:italic toggle=\"yes\">C<\/jats:italic>\n                      <jats:sub>max<\/jats:sub>\n                      and AUC\n                      <jats:sub>last<\/jats:sub>\n                      3.46- and 2.26-fold, respectively. TBAJ-587 accumulated with multiple dosing over the 28-day period, with mean accumulation ratios across the three tested doses ranging from 1.69 to 2.32 for\n                      <jats:italic toggle=\"yes\">C<\/jats:italic>\n                      <jats:sub>max<\/jats:sub>\n                      and from 2.74 to 3.73 for AUC\n                      <jats:sub>tau<\/jats:sub>\n                      . However, steady-state conditions were not yet reached on day 28. Mean terminal half-lives after 28-day dosing of TBAJ-587 ranged from approximately 80 to 111 days. There were no deaths or serious adverse events, and TBAJ-587 was generally safe and well tolerated at single doses of 25\u2013800 mg under fasting conditions and multiple doses of 50\u2013200 mg once daily for 28 days after a standard breakfast. In addition, no dose- or time-dependent effects were noted for any of the other safety and tolerability parameters, including no clinically significant effects on the QTc interval. These results support further investigation of TBAJ-587 for the treatment of tuberculosis.\n                    <\/jats:p>\n                    <jats:sec>\n                      <jats:title>CLINICAL TRIALS<\/jats:title>\n                      <jats:p>\n                        This study is registered with ClinicalTrials.gov as\n                        <jats:related-object xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" document-id=\"NCT04890535\" document-id-type=\"clinical-trial-number\" source-id=\"ClinicalTrials.gov\" source-id-type=\"registry-name\" source-type=\"clinical-trials-registry\" xlink:href=\"https:\/\/clinicaltrials.gov\/study\/NCT04890535\">NCT04890535<\/jats:related-object>\n                        <jats:related-object xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" document-id=\".\" document-id-type=\"clinical-trial-number\" source-id=\"ClinicalTrials.gov\" source-id-type=\"registry-name\" source-type=\"clinical-trials-registry\" xlink:href=\"https:\/\/clinicaltrials.gov\/study\/NCT04890535\">.<\/jats:related-object>\n                      <\/jats:p>\n                    <\/jats:sec>\n                  <\/jats:sec>","DOI":"10.1128\/aac.01930-25","type":"journal-article","created":{"date-parts":[[2026,7,28]],"date-time":"2026-07-28T18:41:17Z","timestamp":1785264077000},"update-policy":"https:\/\/doi.org\/10.1128\/asmj-crossmark-policy-page","source":"Crossref","is-referenced-by-count":1,"title":["Pharmacokinetics and safety of TBAJ-587, a novel antimycobacterial diarylquinoline, in healthy participants"],"prefix":"10.1128","volume":"70","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-0205-522X","authenticated-orcid":true,"given":"Jerry","family":"Nedelman","sequence":"first","affiliation":[{"id":[{"id":"https:\/\/ror.org\/03ms7cf36","id-type":"ROR","asserted-by":"publisher"}],"name":"Global Alliance for TB Drug Development","place":["New York, USA"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Almari","family":"Conradie","sequence":"additional","affiliation":[{"id":[{"id":"https:\/\/ror.org\/03ms7cf36","id-type":"ROR","asserted-by":"publisher"}],"name":"Global Alliance for TB Drug Development","place":["New York, USA"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0009-0001-7383-2495","authenticated-orcid":true,"given":"Antonio","family":"Lombardi","sequence":"additional","affiliation":[{"id":[{"id":"https:\/\/ror.org\/03ms7cf36","id-type":"ROR","asserted-by":"publisher"}],"name":"Global Alliance for TB Drug Development","place":["New York, USA"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0009-0003-6761-9764","authenticated-orcid":true,"given":"Dean","family":"Hickman","sequence":"additional","affiliation":[{"id":[{"id":"https:\/\/ror.org\/03ms7cf36","id-type":"ROR","asserted-by":"publisher"}],"name":"Global Alliance for TB Drug Development","place":["New York, USA"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Khalid","family":"Abd-Elaziz","sequence":"additional","affiliation":[{"name":"QPS Netherlands BV","place":["Groningen, the Netherlands"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Peter","family":"Dogterom","sequence":"additional","affiliation":[{"name":"QPS Netherlands BV","place":["Groningen, the Netherlands"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Paul","family":"Bruinenberg","sequence":"additional","affiliation":[{"name":"Vast Therapeutics","place":["Morrisville, USA"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Antonio J. 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