{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,3,4]],"date-time":"2026-03-04T12:29:17Z","timestamp":1772627357175,"version":"3.50.1"},"reference-count":16,"publisher":"American Society for Microbiology","issue":"5","license":[{"start":{"date-parts":[[1999,5,1]],"date-time":"1999-05-01T00:00:00Z","timestamp":925516800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.asm.org\/non-commercial-tdm-license"}],"content-domain":{"domain":["journals.asm.org"],"crossmark-restriction":true},"short-container-title":["Antimicrob Agents Chemother"],"published-print":{"date-parts":[[1999,5]]},"abstract":"<jats:title>ABSTRACT<\/jats:title>\n          <jats:p>Rifapentine is undergoing development for the treatment of pulmonary tuberculosis. This study was conducted to characterize the single-dose pharmacokinetics of rifapentine and its 25-desacetyl metabolite and to assess the effect of food on the rate and extent of absorption in participants infected with human immunodeficiency virus (HIV). Twelve men and four women, mean age, 38.6 \u00b1 6.9 years, received a single 600-mg oral dose of rifapentine in an open-label, randomized two-way, complete crossover study. Each volunteer received rifapentine following a high-fat breakfast or during a fasting period. Serial blood samples were collected for 72 h and both rifapentine and its metabolite were assayed by a validated high-performance liquid chromatography method. Pharmacokinetics of rifapentine and 25-desacetylrifapentine were determined by noncompartmental methods. Mean (\u00b1 the standard deviation) maximum concentrations of rifapentine in serum and areas under the curve from time zero to infinity following a high-fat breakfast were 14.09 \u00b1 2.81 and 373.63 \u00b1 78.19 \u03bcg\/ml, respectively, and following a fasting period they were 9.42 \u00b1 2.67 and 256.10 \u00b1 86.39 \u03bcg \u00b7 h\/ml, respectively. Pharmacokinetic data from a previously published healthy volunteer study were used for comparison. Administration of rifapentine with a high-fat breakfast resulted in a 51% increase in rifapentine bioavailability, an effect also observed in healthy volunteers. Although food increased the exposure of these patients to rifapentine, the infrequent dosing schedule for the treatment of tuberculosis (e.g., once- or twice-weekly dosing) would be unlikely to lead to accumulation. Additionally, autoinduction has been previously studied and has not been demonstrated with this compound, unlike with rifabutin and rifampin. Rifapentine was well tolerated by HIV-infected study participants. The results of our study suggest that no dosage adjustments may be required for rifapentine in HIV-infected patients (Centers for Disease Control and Prevention classification A1, A2, B1, or B2) undergoing treatment for tuberculosis.<\/jats:p>","DOI":"10.1128\/aac.43.5.1230","type":"journal-article","created":{"date-parts":[[2018,10,9]],"date-time":"2018-10-09T00:34:57Z","timestamp":1539045297000},"page":"1230-1233","update-policy":"https:\/\/doi.org\/10.1128\/asmj-crossmark-policy-page","source":"Crossref","is-referenced-by-count":25,"title":["Pharmacokinetics of Rifapentine in Subjects Seropositive for the Human Immunodeficiency Virus: a Phase I Study"],"prefix":"10.1128","volume":"43","author":[{"given":"Anther C.-F.","family":"Keung","sequence":"first","affiliation":[{"name":"<!--label omitted: 1-->Hoechst Marion Roussel, Kansas City, Missouri 641341;"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"suffix":"Jr.","given":"Robert C.","family":"Owens","sequence":"additional","affiliation":[{"name":"<!--label omitted: 2-->Department of Clinical Pharmacy Services, Maine Medical Center, Portland, Maine 041022;"},{"name":"<!--label omitted: 3-->College of Medicine, University of Vermont, Burlington, Vermont 054013; and"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Mark G.","family":"Eller","sequence":"additional","affiliation":[{"name":"<!--label omitted: 1-->Hoechst Marion Roussel, Kansas City, Missouri 641341;"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Scott J.","family":"Weir","sequence":"additional","affiliation":[{"name":"<!--label omitted: 1-->Hoechst Marion Roussel, Kansas City, Missouri 641341;"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"David P.","family":"Nicolau","sequence":"additional","affiliation":[{"name":"<!--label omitted: 4-->Division of Infectious Diseases,4"},{"name":"<!--label omitted: 5-->Department of Pharmacy Research,5 and"},{"name":"<!--label omitted: 6-->Office for Research,6 Hartford Hospital, Hartford, Connecticut 06102"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Charles H.","family":"Nightingale","sequence":"additional","affiliation":[{"name":"<!--label omitted: 5-->Department of Pharmacy Research,5 and"},{"name":"<!--label omitted: 6-->Office for Research,6 Hartford Hospital, Hartford, Connecticut 06102"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"235","reference":[{"key":"e_1_3_2_2_2","doi-asserted-by":"crossref","first-page":"455P","DOI":"10.1111\/j.1365-2125.1978.tb04626.x","article-title":"Antibacterial activity in serum and urine following oral administration in man of DL473 (a cyclopentyl derivative of rifampicin).","volume":"6","author":"Birmingham A.","year":"1978","unstructured":"Birmingham A. Coleman J. Orme M. L. E. Park B. K. Pearson N. J. Short A. H. Southgate P. J. Antibacterial activity in serum and urine following oral administration in man of DL473 (a cyclopentyl derivative of rifampicin). Br. J. Clin. Pharmacol. 6 1978 455P 456P","journal-title":"Br. J. Clin. Pharmacol."},{"key":"e_1_3_2_3_2","unstructured":"Buniva\n              G.\n              Sassella\n              D.\n              Frigo\n              G. M.\n          Pharmacokinetics of rifapentine in man abstr. 111\n          Proceedings of the 12th International Congress of Chemotherapy\n          1983\n          29\n          33"},{"issue":"17","key":"e_1_3_2_4_2","first-page":"1","article-title":"1993 Revised CDC HIV classification system and expanded AIDS surveillance definition for adolescents and adults.","volume":"41","author":"Centers for Disease Control and Prevention","year":"1992","unstructured":"Centers for Disease Control and Prevention 1993 Revised CDC HIV classification system and expanded AIDS surveillance definition for adolescents and adults. Morbid. Mortal. Weekly Rep. 41 RR-17 1992 1 19","journal-title":"Morbid. Mortal. Weekly Rep."},{"key":"e_1_3_2_5_2","doi-asserted-by":"crossref","first-page":"267","DOI":"10.1016\/0924-8579(94)90054-X","article-title":"Comparison of Chinese and Western rifapentines and improvement of bioavailability by prior taking of various meals.","volume":"3","author":"Chan S. L.","year":"1994","unstructured":"Chan S. L. Yew W. W. Porter J. H. D. McAdam K. P. W. J. Allen B. W. Dickinson J. M. Comparison of Chinese and Western rifapentines and improvement of bioavailability by prior taking of various meals. Int. J. Antimicrob. Agents 3 1994 267 274","journal-title":"Int. J. Antimicrob. Agents"},{"key":"e_1_3_2_6_2","doi-asserted-by":"crossref","first-page":"177","DOI":"10.1016\/0041-3879(87)90053-5","article-title":"In vitro activity of selected rifamycins against rifampicin-resistant M. tuberculosis and MAIS-complex mycobacteria.","volume":"68","author":"Dickinson J. M.","year":"1987","unstructured":"Dickinson J. M. Mitchison D. A. In vitro activity of selected rifamycins against rifampicin-resistant M. tuberculosis and MAIS-complex mycobacteria. Tubercle 68 1987 177 182","journal-title":"Tubercle"},{"key":"e_1_3_2_7_2","doi-asserted-by":"publisher","DOI":"10.1164\/ajrccm\/141.3.626"},{"key":"e_1_3_2_8_2","unstructured":"Keung A. C.-F. M. G. Eller K. A. McKenzie and S. J. Weir. Single and multiple dose pharmacokinetics of rifapentine and its active metabolite 25-desacetyl-rifapentine in man. Submitted for publication."},{"key":"e_1_3_2_9_2","first-page":"S419","article-title":"Bioavailability and food effect study of rifapentine in healthy adults.","volume":"12","author":"Keung A. C.-F.","year":"1995","unstructured":"Keung A. C.-F. Miller T. D. Green V. I. Ames M. Eller M. G. Weir S. J. Bioavailability and food effect study of rifapentine in healthy adults. Pharm. Res. 12 (Suppl.) 1995 S419","journal-title":"Pharm. Res."},{"key":"e_1_3_2_10_2","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.39.9.2073"},{"key":"e_1_3_2_11_2","unstructured":"Owens\n              R. C.\n              Jr.\n              Keung\n              A. C.-F.\n              Gardner\n              S.\n              Eller\n              M. G.\n              Weir\n              S. J.\n              Nicolau\n              D. P.\n              Nightingale\n              C. H.\n          Pharmacokinetic and food effect evaluation of rifapentine in subjects seropositive for the human immunodeficiency virus abstr. A-2\n          Program and Abstracts of the 37th Interscience Conference on Antimicrobial Agents and Chemotherapy.\n          1997\n          1\n          American Society for Microbiology\n          Washington D.C"},{"key":"e_1_3_2_12_2","unstructured":"Reith K. A. C.-F. Keung P. C. Toren M. G. Eller L. Cheng and S. J. Weir. Mass balance and metabolism of 14C-rifapentine in healthy volunteers. Drug Metab. Dispos. in press."},{"key":"e_1_3_2_13_2","unstructured":"Truffot\n              C.\n              Bismuth\n              R.\n              Boval\n              C.\n          The in vitro and in vivo experimental activity of cyclopentyl rifamycin (DL-473) on mycobacterium tuberculosis. Current chemotherapy and immunotherapy abstr. 693\n          Proceedings of the 12th International Congress of Chemotherapy\n          1982\n          172"},{"key":"e_1_3_2_14_2","doi-asserted-by":"crossref","first-page":"S407","DOI":"10.1093\/clinids\/5.Supplement_3.S407","article-title":"Rifampin: mechanisms of action and resistance.","volume":"5","author":"Wehrli W.","year":"1983","unstructured":"Wehrli W. Rifampin: mechanisms of action and resistance. Rev. Infect. Dis. 5 (Suppl. 3) 1983 S407 S411","journal-title":"Rev. Infect. Dis."},{"key":"e_1_3_2_15_2","first-page":"267","article-title":"Absorption and elimination of cyclopentyl-rifamycin in human subjects.","volume":"10","author":"Yan B.","year":"1987","unstructured":"Yan B. X N. Zhu L. Zhang F. Absorption and elimination of cyclopentyl-rifamycin in human subjects. Chin. J. Tuberc. Respir. Dis. 10 1987 267 268","journal-title":"Chin. J. Tuberc. Respir. Dis."},{"key":"e_1_3_2_16_2","first-page":"456","article-title":"Clinical pharmacokinetic study on rifapentine.","volume":"19","author":"Zhang Q.","year":"1994","unstructured":"Zhang Q. Cao Y. Zhang Y. Clinical pharmacokinetic study on rifapentine. Chin. J. Antibiot. 19 1994 456 458","journal-title":"Chin. J. Antibiot."},{"key":"e_1_3_2_17_2","first-page":"333","article-title":"Pharmacokinetics of domestic rifapentine in patients with acute pulmonary infections.","volume":"12","author":"Zheng C.","year":"1987","unstructured":"Zheng C. Yi L. Huiyan Z. Pharmacokinetics of domestic rifapentine in patients with acute pulmonary infections. Chin. J. Antibiot. 12 1987 333 336","journal-title":"Chin. J. Antibiot."}],"container-title":["Antimicrobial Agents and Chemotherapy"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/journals.asm.org\/doi\/pdf\/10.1128\/AAC.43.5.1230","content-type":"application\/pdf","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/journals.asm.org\/doi\/pdf\/10.1128\/AAC.43.5.1230","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2022,2,21]],"date-time":"2022-02-21T16:19:11Z","timestamp":1645460351000},"score":1,"resource":{"primary":{"URL":"https:\/\/journals.asm.org\/doi\/10.1128\/AAC.43.5.1230"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[1999,5]]},"references-count":16,"journal-issue":{"issue":"5","published-print":{"date-parts":[[1999,5]]}},"alternative-id":["10.1128\/AAC.43.5.1230"],"URL":"https:\/\/doi.org\/10.1128\/aac.43.5.1230","relation":{},"ISSN":["0066-4804","1098-6596"],"issn-type":[{"value":"0066-4804","type":"print"},{"value":"1098-6596","type":"electronic"}],"subject":[],"published":{"date-parts":[[1999,5]]},"assertion":[{"value":"1998-06-19","order":0,"name":"received","label":"Received","group":{"name":"publication_history","label":"Publication History"}},{"value":"1999-03-01","order":1,"name":"accepted","label":"Accepted","group":{"name":"publication_history","label":"Publication History"}},{"value":"1999-05-01","order":2,"name":"published","label":"Published","group":{"name":"publication_history","label":"Publication History"}}]}}