今日,根据中国国家药监局药品审评中心(CDE)官网公示,Bicycle Therapeutics的BT8009在中国申报临床。BT8009是一款靶向Nectin-4的多肽偶联药物(PDC),属于第二代双环肽偶联毒素。 关于BT8009 BT8009由靶向Nectin-4的双环肽、可裂解连接子和MMAE毒素偶联而成。临床前毒性研究中,BT8009通常与MMAE细胞毒素有效载荷相关的一部...
今日,根据中国国家药监局药品审评中心(CDE)官网公示,Bicycle Therapeutics的BT8009在中国申报临床。BT8009是一款靶向Nectin-4的多肽偶联药物(PDC),属于第二代双环肽偶联毒素。 关于BT8009 BT8009由靶向Nectin-4的双环肽、可裂解连接子和MMAE毒素偶联而成。临床前毒性研究中,BT8009通常与MMAE细胞毒素有效载荷相关的一部...
在这里,作者描述BT8009的发现,这是一种靶向Nectin-4的多肽偶联药物,目前正处于临床评估。Nectin-4在多种肿瘤类型中过表达,并且是经临床验证的选择性递送细胞毒素有效载荷的靶标。靶向Nectin-4的双环肽通过噬菌体展示方式鉴定,显示出对Nectin-4的高选择性结合,但血浆稳定性低,理化性质差。多种化学优化如引入非天然...
BT8009;Nectin-4为靶点的毒素偶联物;Nectin-4特异性双环肽;BT8009是以Nectin-4为靶点的毒素偶联物,其对人Nectin-4细胞外结构域(ECD)的Kd值为2.5 nmol/L。该化合物由Nectin-4特异性双环肽、可裂解的连接子以及monomethylauristatin E (MMAE)构成,主要用于晚期及转移性尿路上皮癌研究。 楚肽生物提供 NOTA-N188 ...
BT8009是一款BTC(bicycle peptide toxin conjugate,多肽偶联药物[PDC]的一种新形式,理论上优于ADC),靶向Nectin-4(在肺癌、乳腺癌、膀胱癌和胰腺癌等多类癌症中过表达,大约97%的尿路上皮癌患者存在Nectin-4的过表达)。 此前,FDA曾批准同靶点的抗体-药物偶联物(ADC)Enfortumab Vedotin-ejfv(Padcev)用于治疗经...
2022 AACR会议上,Bicycle Therapeutics 公布了其基于双环肽在研疗法BT8009的最新临床试验结果。Bicycle Therapeutics 公司基于Bicycle技术开发了2款靶向Nectin-4的疗法。一种Bicycle Toxin Conjugate(BTC)—BT8009;另一种是双特异性双环肽—BT7480。图片上传中...BT8
BT8009: A bicyclic peptide toxin conjugate targeting Nectin-4 (PVRL4) displays efficacy in preclinical tumour models Mike Rigby AACR Annual Meeting 2019 Atlanta 4479 Bicycles®: a new therapeutic modality • Bicycles® are bicyclic peptides : • Highly constrained: sub-nM binding affinities ...
TPS4619#Background:BT8009 is a Bicycle toxin conjugate (BTC), comprising a highly selective bicyclic peptide targeting nectin-4 linked to the cytotoxin monomethyl auristatin E (MMAE) via a cleavable linker. Nectin-4 is an adhesion molecule commonly expressed in many tumor types, including ...
BT8009, a Bicycle® Toxin Conjugate targeting Nectin-4, shows target selectivity, and ABSTRACT# efficacy in preclinical large and small tumor models. Michael Rigby, 1 Gavin Bennett, 1 Liuhong Chen, 1 Gemma Mudd, 1 Paul Beswick, 1 Helen Harrison, 1 Sophie Watcham, 1 Heather Allen, 1 ...
A phase 2/3 study of Bicycle toxin conjugate BT8009 targeting nectin-4 in patients with locally advanced or metastatic urothelial cancer (la/mUC): Duravelo-2. TPS4619#Background:BT8009 is a Bicycle toxin conjugate (BTC), comprising a highly selective bicyclic peptide targeting nectin-4 linked...