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No pharmacokinetic, efficacy, or safety data of the 1200\u00a0mg q.d. regimen have been reported in pregnant women to date as it is challenging to collect these clinical data. This study aimed to develop a population pharmacokinetic (PopPK) model to predict the pharmacokinetic profile of raltegravir 1200\u00a0mg q.d. in pregnant women and to discuss the expected pharmacodynamic properties of raltegravir 1200\u00a0mg q.d. during pregnancy based on previously reported concentration\u2010effect relationships. Data from 11 pharmacokinetic studies were pooled (<jats:italic>n<\/jats:italic>\u00a0=\u00a0221). A two\u2010compartment model with first\u2010order elimination and absorption through three sequential transit compartments best described the data. We assessed that the bio\u2010availability of the 600\u00a0mg tablets was 21% higher as the 400\u00a0mg tablets, and the bio\u2010availability in pregnant women was 49% lower. Monte\u2013Carlo simulations were performed to predict the pharmacokinetic profile of 1200\u00a0mg q.d. in pregnant and nonpregnant women. The primary criteria for efficacy were that the lower bound of the 90% confidence interval (CI) of the concentration before next dose administration (C<jats:sub>trough<\/jats:sub>) geometric mean ratio (GMR) of simulated pregnant\/nonpregnant women had to be greater than 0.75. The simulated raltegravir C<jats:sub>trough<\/jats:sub> GMR (90% CI) was 0.51 (0.41\u20130.63), hence not meeting the primary target for efficacy. Clinical data from two pregnant women using 1200\u00a0mg q.d. raltegravir showed a similar C<jats:sub>trough<\/jats:sub> ratio pregnant\/nonpregnant. Our pharmacokinetic results support the current recommendation of not using the raltegravir 1200\u00a0mg q.d. regimen during pregnancy until more data on the exposure\u2010response relationship becomes available.<\/jats:p>","DOI":"10.1002\/psp4.12586","type":"journal-article","created":{"date-parts":[[2020,12,26]],"date-time":"2020-12-26T03:12:06Z","timestamp":1608952326000},"page":"161-172","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":7,"title":["A population pharmacokinetics analysis assessing the exposure of raltegravir once\u2010daily 1200\u00a0mg in pregnant women living with HIV"],"prefix":"10.1002","volume":"10","author":[{"given":"Vera E.","family":"Bukkems","sequence":"first","affiliation":[{"name":"Department of Pharmacy Radboud Institute for Health Sciences (RIHS) Radboud University Medical Center Nijmegen The Netherlands"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Teun M.","family":"Post","sequence":"additional","affiliation":[{"name":"Leiden Experts on Advanced Pharmacokinetics and Pharmacodynamics (LAP&amp;P) Leiden The Netherlands"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Angela P.","family":"Colbers","sequence":"additional","affiliation":[{"name":"Department of Pharmacy Radboud Institute for Health Sciences (RIHS) Radboud University Medical Center Nijmegen The Netherlands"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"David M.","family":"Burger","sequence":"additional","affiliation":[{"name":"Department of Pharmacy Radboud Institute for Health Sciences (RIHS) Radboud University Medical Center Nijmegen The Netherlands"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Elin M.","family":"Svensson","sequence":"additional","affiliation":[{"name":"Department of Pharmacy Radboud Institute for Health Sciences (RIHS) Radboud University Medical Center Nijmegen The Netherlands"},{"name":"Department of Pharmacy Uppsala University Uppsala Sweden"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2021,1,25]]},"reference":[{"key":"e_1_2_9_2_1","unstructured":"DHHS.Recommendations for the use of antiretroviral drugs in pregnant women with HIV infection and interventions to reduce perinatal HIV transmission in the United States.https:\/\/files.aidsinfo.nih.gov\/contentfiles\/lvguidelines\/PerinatalGL.pdf.2020. 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