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双抗ADC技术平台


抗体偶联药物(Antibody-drug conjugates, ADC)兼具抗体精确靶向和小分子高效杀伤的双重优势,已成为抗体药物研发的热点之一。经几十年的发展,包括偶联、linker/payload等ADC技术得到了较大突破,但目前获批的ADC药物靶点很有限,安全和有效的创新性靶点仍然是ADC药物研发的关键。
      双抗将产生单抗或联用所不具备的新的药物机制。同样,靶向双肿瘤相关抗原(tumor-associated antigen,TAA)的双抗ADC具有多种潜在抗肿瘤优势:1. 同时靶向双肿瘤驱动信号通路,克服耐药性;2. 高效结合并杀伤双TAA共表达的肿瘤细胞,增加靶向肿瘤特异性,降低脱靶引起的毒性;3. 新的双靶点结合和内吞动力学机制,将产生更高效的肿瘤杀伤协同作用。



基于RenLite的双抗ADC技术平台优势


1. 利用RenLite小鼠产生的全人抗体具有共同的轻链,从而可以有效解决双抗开发过程中的重链和轻链错配的问题,提高组装正确率。

2. RenLite小鼠能够产生表位丰富且亲和力强的抗体。结合KIH(knobs-into-holes)技术连接两个母本单抗的重链,可组装成结构稳定具有单抗结构的双抗分子,保障了后续ADC药物偶联的方便性和成功率。

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图1. 基于RenLite平台高通量地产出双抗ADC


3. 依托于百奥赛图“千鼠万抗”计划,以及整合的抗体发现、偶联技术、药理药效平台,我们将对数百个TAA靶点进行高通量抗体发现和筛选,随之对所有潜在双抗ADC组合进行体内外药效筛选,并在自主的大动物转化医学平台进一步验证,获得更具价值的转化数据,提高临床成功率。

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图2. 百奥赛图双抗ADC药物开发全流程


百奥赛图双抗ADC研发平台可实现高通量筛选和开发双抗ADC组合,源源不断产生具备高度差异化和创新性的双抗ADC分子。


双抗ADC产品开发


资料下载

AACR 2022:YH012, a Novel Bispecific Anti-HER2 and TROP2 Antibody-Drug Conjugate, Exhibits Potent Antitumor Efficacy  点击下载

World ADC San Diego2022:YH013, a fully-human EGFR x MET bispecific ADC exhibits outstanding specificity and anti-tumor efficacy 点击下载

PEGS EUROPE 2022:YH013, a fully-human EGFR x c-MET bispecific ADC exhibits outstanding specificity and anti-tumor efficacy 点击下载


AACR 2023: A First-In-Class Anti-HER2/TROP2 Bispecific Antibody-Drug Conjugate (YH012) Exhibits Potent Anti-Tumor Efficacy 点击下载

AACR 2023: YH013, a Novel Bispecific EGFR x MET Antibody-Drug Conjugate, Exhibits Potent Anti-Tumor Efficacy 点击下载

AACR 2023: A Novel EGFR x MUC1 Bispecific Antibody-Drug Conjugate, BSA01, Targets MUC1 Transmembrane Cleavage Products and Improves Tumor Selectivity 点击下载

AACR 2023: BCG022: A Novel Bispecific Antibody-Drug Conjugate Targeting HER3 and MET 点击下载

AACR2023:Discovery of BCG033, A Novel Anti-PTK7xTROP2 Bispecific Antibody-Drug Conjugate with Promising Efficacy Against Triple-Negative Breast Cancer 点击下载

AACR 2023: A First-In-Class Anti-TROP2/EGFR Bispecific Antibody-Drug Conjugate, DM001, Exhibits Potent Anti-Tumor Efficacy 点击下载

AACR 2023: A First-In-Class Bispecific Antibody-Drug Conjugate (DM002) Targeting HER3 and the Juxtamembrane Domain of MUC1 点击下载

AACR 2023: Identification of DM004, A First-In-Class Anti-5T4/MET Bispecific Antibody-Drug Conjugate 点击下载