biostudies-literatureUnknown15Han M<h4>Background</h4>Mefunidone is a novel synthetic compound and is better when compared to pirfenidone for the anti-fibrotic treatment of renal fibrosis in end-stage renal disease. We conducted this first-in-human, phase I clinical trial to determine the safety, tolerability, and pharmacokinetic (PK) (including food effect) profiles of mefunidone administered orally as single and multiple ascending doses in healthy subjects.<h4>Methods</h4>Part A assessed single ascending doses of mefunidone from 25 mg to 800 mg or placebo once daily in the fasting state. Part A also assessed the effect of food on tolerability and PK in the 100 mg cohort. Part B consisted of three treatment groups who received 100 mg, 200 mg, or 400 mg of mefunidone or placebo twice daily (BID, <i>bis in die</i>) on days 1Frontiers in pharmacology1414066https://www.ebi.ac.uk/biostudies/studies/S-EPMC11199538biostudies-literatureA phase I, randomized study to evaluate the safety, tolerability, and pharmacokinetics of mefunidone in healthy subjects.PMC11199538Li JLu XHan MHuo BWu BZhang SWang JMi NHu GZhang XCui GBian ZWu WJin JXiao CfalseA phase I, randomized study to evaluate the safety, tolerability, and pharmacokinetics of mefunidone in healthy subjects.<h4>Background</h4>Mefunidone is a novel synthetic compound and is better when compared to pirfenidone for the anti-fibrotic treatment of renal fibrosis in end-stage renal disease. We conducted this first-in-human, phase I clinical trial to determine the safety, tolerability, and pharmacokinetic (PK) (including food effect) profiles of mefunidone administered orally as single and multiple ascending doses in healthy subjects.<h4>Methods</h4>Part A assessed single ascending doses of mefunidone from 25 mg to 800 mg or placebo once daily in the fasting state. Part A also assessed the effect of food on tolerability and PK in the 100 mg cohort. Part B consisted of three treatment groups who received 100 mg, 200 mg, or 400 mg of mefunidone or placebo twice daily (BID, <i>bis in die</i>) on days 12024-01-01T00:00:00Z20242025-04-26T22:35:32.062Z2025-04-06T17:18:15.42ZS-EPMC111995383893366910.3389/fphar.2024.1414066