{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,4,25]],"date-time":"2026-04-25T10:00:05Z","timestamp":1777111205862,"version":"3.51.4"},"reference-count":27,"publisher":"Wiley","issue":"4","license":[{"start":{"date-parts":[[2020,8,9]],"date-time":"2020-08-09T00:00:00Z","timestamp":1596931200000},"content-version":"vor","delay-in-days":8,"URL":"http:\/\/creativecommons.org\/licenses\/by-nc-nd\/4.0\/"}],"content-domain":{"domain":["bpspubs.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Pharmacology Res &amp; Perspec"],"published-print":{"date-parts":[[2020,8]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>A single\u2010dose oral granule formulation of secnidazole 2\u00a0g (SOLOSEC<jats:sup>\u2122<\/jats:sup>) has been approved in the US as a treatment for bacterial vaginosis. Available data on the likelihood of in vitro drug\u2010drug and alcohol\u2010drug interactions are limited. Secnidazole was incubated with cultured human hepatocytes over a range of concentrations (0\u201010\u00a0000\u00a0\u03bcmol\/L) to assess metabolic profiling. Cytochrome P450 (CYP) and aldehyde dehydrogenase inhibition over a similar concentration range were evaluated in human liver microsomes (HLMs) or recombinant enzymes using competition or time\u2010dependent inactivation assays. Secnidazole exhibited very low metabolism in HLMs at concentrations up to 6400\u00a0\u00b5mol\/L. Secnidazole was found to be metabolized to a limited extent predominantly by CYP3A4 and CYP3A5 among a panel of cDNA\u2010expressed enzymes. Secnidazole inhibited CYP2C19 and CYP3A4, with IC<jats:sub>50<\/jats:sub> values of 3873 and 3722\u00a0\u00b5mol\/L, respectively. Secnidazole did not exhibit time\u2010dependent inhibition. There was no inhibition (IC<jats:sub>50<\/jats:sub> value &gt;5000\u00a0\u00b5mol\/L) observed for any other CYP enzyme or with human recombinant aldehyde dehydrogenase 2 (ALDH2). These results are the first reported observation of the metabolism and drug\u2010drug interaction profile for secnidazole and demonstrate that the agent has minimal to no potential drug interactions of concern.<\/jats:p>","DOI":"10.1002\/prp2.634","type":"journal-article","created":{"date-parts":[[2020,8,10]],"date-time":"2020-08-10T06:56:43Z","timestamp":1597042603000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":3,"title":["In vitro metabolic profile and drug\u2010drug interaction assessment of secnidazole, a high\u2010dose 5\u2010nitroimidazole antibiotic for the treatment of bacterial vaginosis"],"prefix":"10.1002","volume":"8","author":[{"given":"Helen S.","family":"Pentikis","sequence":"first","affiliation":[{"name":"SAJE Consulting Baltimore MD USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Nikki","family":"Adetoro","sequence":"additional","affiliation":[{"name":"Lupin Pharmaceuticals Baltimore MD USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Gregory","family":"Kaufman","sequence":"additional","affiliation":[{"name":"Lupin Pharmaceuticals Baltimore MD USA"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2020,8,9]]},"reference":[{"key":"e_1_2_8_2_1","doi-asserted-by":"publisher","DOI":"10.2165\/00003495-199651040-00007"},{"key":"e_1_2_8_3_1","doi-asserted-by":"crossref","unstructured":"PetrinaM CosentinoL RabeL HillierS.Susceptibility of bacterial vaginosis (BV)\u2010 associated bacteria to secnidazole metronidazole tinidazole and clindamycin. Presented at: Infectious Diseases Society of Obstetrics and Gynecology Annual Meeting; August 11\u201013 Annapolis MD. 2016.","DOI":"10.1016\/j.ajog.2016.09.041"},{"key":"e_1_2_8_4_1","article-title":"A phase 2 randomized, double\u2010blind, placebo\u2010controlled study to evaluate the effectiveness and safety of single, oral doses of SYM\u20101219, a granule formulation containing 1 and 2 gram doses of secnidazole, for the treatment of women with bacterial vaginosis","author":"Hillier S","year":"2015","journal-title":"Infect Dis Soc Obstet Gynecol."},{"key":"e_1_2_8_5_1","doi-asserted-by":"publisher","DOI":"10.1155\/2010\/705692"},{"key":"e_1_2_8_6_1","doi-asserted-by":"publisher","DOI":"10.1093\/jac\/31.1.9"},{"key":"e_1_2_8_7_1","doi-asserted-by":"publisher","DOI":"10.2165\/00003088-199936050-00004"},{"key":"e_1_2_8_8_1","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.28.4.561"},{"key":"e_1_2_8_9_1","doi-asserted-by":"publisher","DOI":"10.1046\/j.1439-0442.1999.00245.x"},{"key":"e_1_2_8_10_1","first-page":"285","article-title":"Mechanisms of selective toxicity of metronidazole and other nitroimidazole drugs","volume":"56","author":"Edwards D","year":"1980","journal-title":"Br J Vener Dis"},{"key":"e_1_2_8_11_1","doi-asserted-by":"publisher","DOI":"10.4155\/fmc.11.90"},{"key":"e_1_2_8_12_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1600-051X.1993.tb00398.x"},{"key":"e_1_2_8_13_1","first-page":"391","article-title":"The effect of cytochrome P450 metabolism on drug response, interactions, and adverse effects","volume":"76","author":"Lynch T","year":"2007","journal-title":"Am Fam Physician"},{"key":"e_1_2_8_14_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1530-0277.1980.tb04785.x"},{"key":"e_1_2_8_15_1","unstructured":"Metronidazole package insert.G.D. Searle LLC a subsidiary of Pharmacia Corporation Chicago IL 60680.2003."},{"key":"e_1_2_8_16_1","doi-asserted-by":"publisher","DOI":"10.1080\/00498250802638155"},{"key":"e_1_2_8_17_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.cbi.2011.02.018"},{"key":"e_1_2_8_18_1","doi-asserted-by":"publisher","DOI":"10.1096\/fasebj.6.2.1371482"},{"key":"e_1_2_8_19_1","unstructured":"FrydmanA LemarLRM.A review of the pharmacokinetics of secnidazole in man. In: Secnidazole: a new approach in 5\u2010nitroimidazole therapy Proceedings from the 16th International Congress of Chemotherapy 1989 June 12; Jerusalem Amsterdam: Excerpta Medica.1989:12\u201026."},{"key":"e_1_2_8_20_1","doi-asserted-by":"publisher","DOI":"10.1080\/004982598238886"},{"key":"e_1_2_8_21_1","doi-asserted-by":"publisher","DOI":"10.1080\/10915810701583010"},{"key":"e_1_2_8_22_1","first-page":"40","article-title":"Alcohol and medication interactions","volume":"23","author":"Weathermon R","year":"1999","journal-title":"Alcohol Res Heal"},{"key":"e_1_2_8_23_1","doi-asserted-by":"publisher","DOI":"10.1155\/1999\/539376"},{"key":"e_1_2_8_24_1","doi-asserted-by":"publisher","DOI":"10.1056\/NEJM198312153092412"},{"key":"e_1_2_8_25_1","doi-asserted-by":"publisher","DOI":"10.1007\/s12325-016-0411-9"},{"key":"e_1_2_8_26_1","doi-asserted-by":"publisher","DOI":"10.1089\/jwh.2017.6500"},{"key":"e_1_2_8_27_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ajog.2017.08.017"},{"key":"e_1_2_8_28_1","doi-asserted-by":"publisher","DOI":"10.1097\/AOG.0000000000002135"}],"container-title":["Pharmacology Research &amp; Perspectives"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/onlinelibrary.wiley.com\/doi\/pdf\/10.1002\/prp2.634","content-type":"application\/pdf","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/onlinelibrary.wiley.com\/doi\/full-xml\/10.1002\/prp2.634","content-type":"application\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/bpspubs.onlinelibrary.wiley.com\/doi\/pdf\/10.1002\/prp2.634","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2023,9,5]],"date-time":"2023-09-05T09:49:57Z","timestamp":1693907397000},"score":1,"resource":{"primary":{"URL":"https:\/\/bpspubs.onlinelibrary.wiley.com\/doi\/10.1002\/prp2.634"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2020,8]]},"references-count":27,"journal-issue":{"issue":"4","published-print":{"date-parts":[[2020,8]]}},"alternative-id":["10.1002\/prp2.634"],"URL":"https:\/\/doi.org\/10.1002\/prp2.634","archive":["Portico"],"relation":{},"ISSN":["2052-1707","2052-1707"],"issn-type":[{"value":"2052-1707","type":"print"},{"value":"2052-1707","type":"electronic"}],"subject":[],"published":{"date-parts":[[2020,8]]},"assertion":[{"value":"2020-04-21","order":0,"name":"received","label":"Received","group":{"name":"publication_history","label":"Publication History"}},{"value":"2020-06-30","order":1,"name":"accepted","label":"Accepted","group":{"name":"publication_history","label":"Publication History"}},{"value":"2020-08-09","order":2,"name":"published","label":"Published","group":{"name":"publication_history","label":"Publication History"}}],"article-number":"e00634"}}