Clinical Pharmacology in Drug Development最新文献

{"title":"Pharmacokinetic Study and Bioequivalence Evaluation of Two Sustained-Release Tablets of Tamsulosin in Healthy Chinese Subjects Under Fasting and Postprandial Conditions.","authors":"Jie Wang, Fang Yao, Pan Lu, Yafang Xie, Xiuwen Li, Qiangwei Liu, Yang Liu, Dan Cao, Jun Liang, Ming Zhou","doi":"10.1002/cpdd.1589","DOIUrl":"https://doi.org/10.1002/cpdd.1589","url":null,"abstract":"<p><p>Tamsulosin is a highly selective α1A adrenergic receptor antagonist that can relax smooth muscles in the urethra, bladder neck, and prostate and improve urinary disorders. It is therefore widely used to treat lower urinary tract symptoms caused by benign prostatic hyperplasia. The aim of this study is to evaluate the pharmacokinetic (PK) characteristics and bioequivalence of 2 different formulations (tamsulosin sustained-release tablets and tamsulosin sustained-release capsules) in healthy Chinese subjects. This study was a single-center, randomized, open label, 2-formulation, single-administration, 2-cycle, double-crossover fasting/postprandial bioequivalence trial that included 56 healthy volunteers (28 fasting and 28 postprandial). Blood samples were collected from volunteers after oral administration, plasma concentrations of tamsulosin were determined by liquid chromatography-tandem mass spectrometry for PK analysis, and the safety and tolerability of the drug were monitored. Under fasting and postprandial conditions, the 90% confidence intervals for maximum observed concentration (C_max) and area under the plasma concentration-time curve from time 0 to the last sampling time (AUC_0-t) of the test and reference formulations were within an acceptable range (80%-125%). All adverse events (AEs) were mild and no serious AEs were observed in the study. The subject formulation of tamsulosin extended-release tablets was safe and well tolerated in healthy Chinese Volunteers.</p>","PeriodicalId":10495,"journal":{"name":"Clinical Pharmacology in Drug Development","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-09-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145022938","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Phenobarbital Bioequivalence in Chinese Population: Considering the Role of Food on Pharmacokinetics.","authors":"Wang Xinman, Liu Yuan, Sun Ying, Wang Yiyun","doi":"10.1002/cpdd.1604","DOIUrl":"https://doi.org/10.1002/cpdd.1604","url":null,"abstract":"<p><p>Epilepsy is one of the most severe neurological disorders in the world, which might seriously endanger the lives of patients. Phenobarbital is an important medicine clinically used for the treatment of epilepsy, and it is irreplaceable in the treatment of generalized tonic-clonic seizures, focal seizures, status epilepticus, and pediatric epilepsy. However, the original research medicine of phenobarbital has not been launched in China. Therefore, an economical and effective generic medicine is of great significance to patients. In this study, a single-center, randomized, open-label, single-dose, two-formulation, two-period, two-sequence crossover design and parallel design were adopted. The phenobarbital tablets produced by Shandong Xinhua Pharmaceutical Co., Ltd. were used as the test formulation, and Phenobal produced by Fujinaga Pharmaceutical Co., Ltd. was used as the reference formulation for a bioequivalence study. Additionally, the influence of food on the pharmacokinetic parameters al was investigated. The results showed that the test formulation and the reference formulation were bioequivalent, and food might reduce the C_max (maximum concentration) and exposure of phenobarbital. This study provides data support for the marketing of generic phenobarbital medicines and offers a theoretical basis for the rational administration of phenobarbital. The clinical trial was registered in Chinese Clinical Trial Registry (Registration numbers: CTR20242404 and CTR20244155).</p>","PeriodicalId":10495,"journal":{"name":"Clinical Pharmacology in Drug Development","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-09-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145005953","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"2025 CPDD Abstract Booklet","authors":"","doi":"10.1002/cpdd.1588","DOIUrl":"10.1002/cpdd.1588","url":null,"abstract":"<p><b>DATE: September 14, 2025</b></p><p><b>TIME: 5:00 – 7:00 PM</b></p><p><b>DATE: September 15, 2025</b></p><p><b>TIME: 5:00 – 7:00 PM</b></p>","PeriodicalId":10495,"journal":{"name":"Clinical Pharmacology in Drug Development","volume":"14 S1","pages":"1-140"},"PeriodicalIF":1.8,"publicationDate":"2025-09-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://accp1.onlinelibrary.wiley.com/doi/epdf/10.1002/cpdd.1588","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144998839","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Safety and Pharmacokinetics of Long-Acting Monoclonal Antibodies Tixagevimab and Cilgavimab (AZD7442) in a China Phase 2 Study and Evaluation of Asian Race Effect.","authors":"Jing Zhang, Huixia Zhang, Yajuan Zhang, Shuyuan Liu, Xiaoyun Ge, Haiyue Zhang, Yunfei Li, Cecil Chi-Keung Chen, Oleg Stepanov, Weifeng Tang, Wenhong Zhang","doi":"10.1002/cpdd.1586","DOIUrl":"https://doi.org/10.1002/cpdd.1586","url":null,"abstract":"<p><p>Safety, pharmacokinetics, and impact of race of pharmacokinetics on monoclonal antibodies tixagevimab and cilgavimab (AZD7442) were assessed in Chinese adult participants in a Phase 2, randomized, double-blind, placebo-controlled trial. In total, 272 participants were randomized 3:1 to a single intravenous dose of 600 mg AZD7442 or placebo and followed for 451 days. Mean participant age was 34.2 years, 5.9% were aged greater than 60 years, and 69.1% were male. Adverse events (AEs) occurred in 72.8% and 80.0% of participants with AZD7442 and placebo, respectively; most were mild or moderate in severity. Serious AEs were reported in 3.0% and 4.3% of participants with AZD7442 and placebo, respectively. No AEs of special interest, infusion-related reactions, or deaths occurred. Maximum serum concentrations of tixagevimab and cilgavimab were rapidly achieved following infusion, then declined through Day 361. Mean half-lives were 85 days for tixagevimab and 80 days for cilgavimab. AZD7442 recipients exhibited greater than 4-fold neutralizing antibody titer increases versus baseline at Day 8, which then declined through Day 361. Among AZD7442 recipients, 20.8% were treatment-emergent antidrug antibody positive. Asian race had no clinically significant impact on AZD7442 pharmacokinetics. Overall, intravenous 600 mg AZD7442 was well tolerated in Chinese adult participants. AZD7442 pharmacokinetics were similar in Asian and non-Asian participants. ClinicalTrials.gov identifier: NCT05184062.</p>","PeriodicalId":10495,"journal":{"name":"Clinical Pharmacology in Drug Development","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-09-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144999795","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Relative Bioavailability, Food Effect, and Bioequivalence Studies to Assess a New Zanubrutinib 160-mg Tablet: Results From 2 Phase 1 Studies in Healthy Volunteers.","authors":"Bilal Tariq, Chester Lin, Vaibhav Mundra, Yang Gao, Dan Zhang, Ying C Ou","doi":"10.1002/cpdd.1584","DOIUrl":"https://doi.org/10.1002/cpdd.1584","url":null,"abstract":"<p><p>Zanubrutinib is a next-generation Bruton tyrosine kinase inhibitor approved for treating B-cell malignancies. Two phase 1 studies evaluated a new 160-mg zanubrutinib tablet versus 80-mg capsules. In study BGB-3111-115 (n = 43), a randomized 3-period crossover trial, relative bioavailability and food effects were assessed. Under fasted conditions, systemic exposure (area under the concentration-time curve [AUC]) was comparable between tablets and capsules at both 160- and 320-mg doses. A high-fat meal increased tablet maximum plasma concentration (C_max) by 47%-79% but had minimal effect on AUC (<18%), supporting administration with or without food. Study BGB-3111-114 (n = 58) was a randomized, replicate crossover study that evaluated bioequivalence (BE) under fasted conditions. Geometric mean ratios of AUC_0-t and AUC_0-∞ (tablets vs capsules) were 1.00 (90% confidence interval [CI] 0.95-1.05) and 0.99 (90% CI 0.94-1.04), meeting BE criteria. Tablet C_max was modestly higher (geometric mean ratio 1.22, 90% CI 1.14-1.30), with no expected clinical impact based on established zanubrutinib exposure-response relationships. Both formulations were well tolerated, with no serious adverse events. In vitro testing showed tablets readily dispersed into a stable suspension suitable for nasogastric tube administration. Together, these results supported zanubrutinib tablets as a flexible alternative to capsules, with the potential to reduce pill burden (4 capsules vs 2 tablets) and improve long-term adherence.</p>","PeriodicalId":10495,"journal":{"name":"Clinical Pharmacology in Drug Development","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-09-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144945467","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pharma's AI Inflection Point: What Does It Mean for Early Phase Clinical Development?","authors":"Amalia M. Issa","doi":"10.1002/cpdd.1596","DOIUrl":"10.1002/cpdd.1596","url":null,"abstract":"&lt;p&gt;If you attended or will soon attend any clinical pharmacology or drug development conference this year, you would have noticed that artificial intelligence (AI) is a major focus everywhere. Headlines, plenaries, and panels all speak to AI's rapid ascendance. Yet, this trend is much more than media hype or marketing spin—it marks a true inflection point for the pharmaceutical industry.&lt;/p&gt;&lt;p&gt;A report&lt;span&gt;&lt;sup&gt;1&lt;/sup&gt;&lt;/span&gt; published this summer offers a timely snapshot into the current state of AI in the pharmaceutical industry. Based on interviews and survey data from senior C-suite executives at more than 40 organizations, including most of the top 20 pharmaceutical companies, the report highlights that AI has reached a critical tipping point. AI is no longer an experimental curiosity but a core strategic priority across drug R&amp;D, clinical development, and commercialization. Leaders from Big Pharma, major tech companies, and innovative startups concur that we are entering a pivotal phase for AI. The next 12 to 24 months will likely determine whether AI becomes a foundational technology or remains an incremental tool in pharmaceutical R&amp;D. As a result, strategies and investments are shifting away from cautious experimentation and pilot projects toward enterprise-wide adoption.&lt;/p&gt;&lt;p&gt;As clinical pharmacologists and drug development experts, we must ask: What does this strategic shift mean for early phase studies, where rigor and innovation are non-negotiable?&lt;/p&gt;&lt;p&gt;Enterprise-level AI initiatives are being championed at the C-suite, with leadership aligning budgets, governance structures, and strategic priorities&lt;span&gt;&lt;sup&gt;1&lt;/sup&gt;&lt;/span&gt; to achieve measurable gains in speed, efficiency, and scientific innovation. For early-phase clinical studies, these priorities could not be more aligned. Phase I/II trials stand to benefit immensely from AI in several domains.&lt;/p&gt;&lt;p&gt;Emerging scientific literature demonstrates that generative AI,&lt;span&gt;&lt;sup&gt;2&lt;/sup&gt;&lt;/span&gt; multi-omics modeling,&lt;span&gt;&lt;sup&gt;3&lt;/sup&gt;&lt;/span&gt; and federated learning&lt;span&gt;&lt;sup&gt;4&lt;/sup&gt;&lt;/span&gt; can uncover novel drug targets, optimize biomarker-driven trial designs, and identify subtle signals of efficacy and safety that may otherwise go undetected, especially in smaller, early-phase cohorts. This evolution of AI in clinical trials opens real opportunities for clinical pharmacologists to contribute to innovative, data-driven approaches to drug development.&lt;/p&gt;&lt;p&gt;The report highlights an ongoing transition: whereas pharma previously sought to build AI tools internally for reasons of data ownership and trust, there is a notable rise in hybrid and partnership models.&lt;span&gt;&lt;sup&gt;1&lt;/sup&gt;&lt;/span&gt; Pharma is increasingly open to leveraging foundational models from big tech and specialized startups, provided that solutions are transparent, validated, and regulatory-ready. Similar sentiments are echoed by Brumfeld et al.,&lt;span&gt;&lt;sup&gt;14&lt;/sup&gt;&lt;/span&gt; who found that consortium approaches and publi","PeriodicalId":10495,"journal":{"name":"Clinical Pharmacology in Drug Development","volume":"14 9","pages":"646-648"},"PeriodicalIF":1.8,"publicationDate":"2025-09-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://accp1.onlinelibrary.wiley.com/doi/epdf/10.1002/cpdd.1596","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144927483","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Disposition and Absolute Bioavailability of Orally Administered Orforglipron in Healthy Participants.","authors":"Bridget L Morse, Shobha Bhattachar, Xiaosu Ma, David E Coutant, Boris Czeskis, Clare Nicoll, Kenneth C Cassidy","doi":"10.1002/cpdd.1594","DOIUrl":"https://doi.org/10.1002/cpdd.1594","url":null,"abstract":"<p><p>Orforglipron is a non-peptide, oral glucagon-like peptide 1 receptor agonist under development for glycemic control in adults with type 2 diabetes and weight management in people with obesity. Two phase 1, open-label studies evaluated the disposition and absolute bioavailability of orforglipron in healthy adults. Study A participants (N = 10) received a 1-mg orforglipron oral capsule while fasting and an intravenous dose of ∼21 µg of [14C]-orforglipron. Study B participants (N = 6) received an oral solution of 3 mg of orforglipron with ∼200 µCi of [14C]-orforglipron while fasting. In study A, total plasma radioactivity and [14C]-orforglipron were measured by accelerator mass spectrometry (AMS) and high-performance liquid chromatography (HPLC)/AMS, while orforglipron was measured by HPLC/MS. The mean absolute oral bioavailability of orforglipron was 79.1% ± 16.8%. In study B, urine and feces were analyzed for total radioactivity. Metabolic radioprofiling was performed on selected plasma and fecal samples by HPLC/high-resolution MS. The primary route of elimination for [14C]-orforglipron-related radioactivity was via the feces (87% ± 2.8%) with minimal urinary excretion (0.2% ± 0.02%). Total recovery of administered radioactivity was 88% over 384 hours after the dose. Metabolite profiling from study B showed that orforglipron underwent extensive oxidative metabolism, followed by microbial metabolism of the oxadiazolone ring. Orforglipron was the most abundant plasma component (93.3%) with minor oxidative metabolites M7 (3.3%) and M23 (1.6%).</p>","PeriodicalId":10495,"journal":{"name":"Clinical Pharmacology in Drug Development","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144945461","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Food Effect of Bexicaserin in Healthy Participants: A First-in-Human Randomized, Double-Blind, Placebo-Controlled Single Ascending Dose Escalation Phase 1 Study.","authors":"Rosa Chan, Chad Orevillo, Gale O'Connell, Dewey McLin, Shikha Polega, Nuggehally R Srinivas, Randall Kaye","doi":"10.1002/cpdd.1600","DOIUrl":"https://doi.org/10.1002/cpdd.1600","url":null,"abstract":"<p><p>Bexicaserin (LP352) is a selective 5-hydroxytryptamine 2C (5-HT_2C) superagonist in development for the treatment of seizures in developmental and epileptic encephalopathies (DEEs). This double-blind, placebo-controlled, single ascending dose (SAD) Phase 1 study aimed to assess the safety, tolerability, and pharmacokinetic (PK) and pharmacodynamic (PD) profiles of single oral doses of bexicaserin and determine any relevant food effects. Forty healthy adult females were randomized to six treatment groups (1, 3, 6, 12, and 24 mg fasted; 6 mg fed) or placebo. Bexicaserin was generally safe and well tolerated: treatment-related adverse events were mild to moderate. Bexicaserin was rapidly absorbed into circulation (median T_max 1.02-1.54 h), with a mean terminal elimination half-life ranging from 4.67-6.66 h. Mean C_max and AUC_last of bexicaserin increased by at least >55-fold for a 24-fold dose increase. Three pharmacologically inactive circulatory metabolites (M9, M12, and M20) were further characterized. M20 was the major metabolite, with levels ranging from 3.47 to 10.8 times higher than bexicaserin. In comparison, M12 ranged from 0.35 to 0.98 times, and M9 from 0.037 to 0.53 times, relative to bexicaserin. Metabolism was the major route of clearance, as <5% of parent bexicaserin was eliminated in the urine. A high-fat meal did not alter the exposure of bexicaserin, supporting administration without regard to food. Increases in prolactin concentrations, a potential PD marker, were dose-dependent, suggesting central 5-HT_2C receptor engagement. In summary, this Phase 1 SAD study demonstrated safety, tolerability, and adequate characterization of PK/PD of bexicaserin, which is currently in Phase 3 clinical development.</p>","PeriodicalId":10495,"journal":{"name":"Clinical Pharmacology in Drug Development","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-08-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144945577","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Multiple Ascending Doses and Dose Titration of Bexicaserin in Healthy Participants in a Randomized, Double-Blind, Placebo-Controlled Study.","authors":"Jonathan Williams, Rosa Chan, Chad Orevillo, Gale O'Connell, Dewey McLin, Shikha Polega, Nuggehally R Srinivas, Randall Kaye","doi":"10.1002/cpdd.1602","DOIUrl":"https://doi.org/10.1002/cpdd.1602","url":null,"abstract":"<p><p>Bexicaserin (LP352) is a selective superagonist of the 5-hydroxytryptamine 2C (5-HT_2C) receptor currently in development for the treatment of seizures that arise from developmental and epileptic encephalopathies. This phase 1, double-blind, placebo-controlled multiple ascending dose (MAD) study assessed the safety, tolerability, and pharmacokinetic profile of bexicaserin in healthy participants. Doses ranging from 3 to 24 mg three times daily (TID) were administered for up to 14 days. Serial blood and urine samples were collected to assess pharmacokinetics, and prolactin was assessed as a pharmacodynamic biomarker. Bexicaserin was generally safe and well-tolerated, rapidly absorbed, metabolized to three circulatory pharmacologically inactive metabolites, and had a median T_max of about 1-2 h. C_max accumulation ranged from 1.5 to 5.1-fold for all analytes after multiple doses. M20 was the major metabolite, with exposures ranging from 9 to 33-fold versus bexicaserin. Overall clearance of bexicaserin ranged from 45.9 to 125 L/h, with renal clearance between 5.04 to 6.58 L/h, suggesting that hepatic metabolism and/or excretion is the main elimination pathway. There was a weak dose-dependent positive correlation between bexicaserin C_max and prolactin mean percentage change from baseline, suggesting successful engagement of central 5-HT_2C receptors. Overall, this Phase 1 MAD study demonstrated bexicaserin to be safe and well-tolerated, with rapid absorption, presence of one major metabolite, accumulation upon multiple dosing TID, and a greater than dose-proportional increase in exposures. These findings support the continued development of bexicaserin, which is currently in Phase 3 clinical trials.</p>","PeriodicalId":10495,"journal":{"name":"Clinical Pharmacology in Drug Development","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-08-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144945443","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Comparative Bioequivalence Study of 2 Clevidipine Formulations in Healthy Chinese participants: A Single-Dose, 2-Period Crossover Trial.","authors":"Zhuo Chen, Fengshan Li, Qin Yu, Shiyin Feng, Linrui Cai, Feng Hu, Chunfeng Du, Xiaohong Liu","doi":"10.1002/cpdd.1591","DOIUrl":"https://doi.org/10.1002/cpdd.1591","url":null,"abstract":"<p><p>Clevidipine emulsion is an intravenous antihypertensive agent indicated for acute blood pressure control when oral therapies are contraindicated or ineffective. To address this gap in availability, a randomized, 2-period, 2-sequence crossover trial was conducted to evaluate the bioequivalence and safety of a generic clevidipine emulsion versus the reference product in 32 healthy Chinese adults. Participants received a 30-minute intravenous infusion of 3 mg of clevidipine (test or reference formulation) in each study period, with serial blood samples collected from the contralateral arm relative to the infusion site for pharmacokinetic analysis. Treatment-emergent adverse events (TEAEs) were monitored throughout the study. All participants completed both treatment phases. The generic formulation satisfied bioequivalence criteria for all primary pharmacokinetic parameters, with geometric mean ratios (90% confidence intervals) of C_max, AUC_0-t, and AUC_0-∞ fully contained within the 80%-125% equivalence range. Three participants (9.4%) experienced mild TEAEs assessed as treatment-related, including transient sinus tachycardia (n = 2) and asymptomatic alanine aminotransferase elevation (n = 1). The generic formulation met bioequivalence criteria and exhibited comparable safety profiles to the reference product.</p>","PeriodicalId":10495,"journal":{"name":"Clinical Pharmacology in Drug Development","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144945481","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}