IBI351,a synthetic compound,exerts its anti-tumor effects by specifically,covalently,and irreversibly modifying the 12th cysteine residue of KRAS G12C.However,the pharmacokinetic profile of IBI351 in humans has not ye...IBI351,a synthetic compound,exerts its anti-tumor effects by specifically,covalently,and irreversibly modifying the 12th cysteine residue of KRAS G12C.However,the pharmacokinetic profile of IBI351 in humans has not yet been reported.The current study aimed to investigate the pharmacokinetics and safety of IBI351 in healthy Chinese male subjects.A single oral dose of 600 mg combined with 150μCi[^(14)C]IBI351 was administered to six healthy male volunteers.Blood,urine,and fecal samples were collected at multiple time points to quantify the parent drug and its metabolites.IBI351 showed favorable pharmacokinetic characteristics and was well tolerated by all participants.Seventeen major metabolites were identified in plasma,urine,and feces.The main metabolic pathways included oxidation,hydrogenation,sulfonate conjugation,glucuronide conjugation,and cysteine conjugation.Excretion of IBI351 and its metabolites occurred mainly through feces.Collectively,this first-in-human study provides essential data on the metabolism and safety of IBI351 in Chinese subjects and lays the foundation for its further clinical development as a novel anti-tumor drug.展开更多
2025年4月29日,IBIS Worldwide在英国伦敦宣布,2025年IBIS全球峰会(IBIS Global Summit 2025)的日程已正式发布,这标志着这场事故车维修行业最具影响力的全球会议进入筹备新阶段。2025年6月24日-26日,来自全球事故车维修领域的高层领导...2025年4月29日,IBIS Worldwide在英国伦敦宣布,2025年IBIS全球峰会(IBIS Global Summit 2025)的日程已正式发布,这标志着这场事故车维修行业最具影响力的全球会议进入筹备新阶段。2025年6月24日-26日,来自全球事故车维修领域的高层领导与决策者将齐聚伊斯坦布尔的博斯普鲁斯瑞士酒店,展开为期2天的高端洞察分享、结构化讨论与战略性人脉拓展。展开更多
基金supported by funding from the 13th Five-Year Plan New Drug Creation Program—Isotope Tracer Technology Platform for Clinical Evaluation of Innovative Drugs(Grant No.2017ZX09304032 with project leaders Jun Zhao and Chen Zhou).
文摘IBI351,a synthetic compound,exerts its anti-tumor effects by specifically,covalently,and irreversibly modifying the 12th cysteine residue of KRAS G12C.However,the pharmacokinetic profile of IBI351 in humans has not yet been reported.The current study aimed to investigate the pharmacokinetics and safety of IBI351 in healthy Chinese male subjects.A single oral dose of 600 mg combined with 150μCi[^(14)C]IBI351 was administered to six healthy male volunteers.Blood,urine,and fecal samples were collected at multiple time points to quantify the parent drug and its metabolites.IBI351 showed favorable pharmacokinetic characteristics and was well tolerated by all participants.Seventeen major metabolites were identified in plasma,urine,and feces.The main metabolic pathways included oxidation,hydrogenation,sulfonate conjugation,glucuronide conjugation,and cysteine conjugation.Excretion of IBI351 and its metabolites occurred mainly through feces.Collectively,this first-in-human study provides essential data on the metabolism and safety of IBI351 in Chinese subjects and lays the foundation for its further clinical development as a novel anti-tumor drug.
文摘2025年4月29日,IBIS Worldwide在英国伦敦宣布,2025年IBIS全球峰会(IBIS Global Summit 2025)的日程已正式发布,这标志着这场事故车维修行业最具影响力的全球会议进入筹备新阶段。2025年6月24日-26日,来自全球事故车维修领域的高层领导与决策者将齐聚伊斯坦布尔的博斯普鲁斯瑞士酒店,展开为期2天的高端洞察分享、结构化讨论与战略性人脉拓展。