1. Signaling Pathways
  2. Antibody-drug Conjugate/ADC Related
  3. Antibody-Drug Conjugates (ADCs)

Antibody-Drug Conjugates (ADCs) (抗体偶联药物)

Antibody-Drug Conjugates

The antibody-drug conjugate (ADC), a humanized or human monoclonal antibody conjugated with highly cytotoxic small molecules (payloads) through chemical linkers, is a novel therapeutic format and has great potential to make a paradigm shift in cancer chemotherapy. This antibody-based molecular platform enables selective delivery of a potent cytotoxic payload to target cancer cells, resulting in improved efficacy, reduced systemic toxicity, and preferable pharmacokinetics (PK)/pharmacodynamics (PD) and biodistribution compared to traditional chemotherapy.

All three component parts of an ADC, the antibody, the cytotoxic agent, and the linker that joins them, are critical elements in its design. The antibody moiety should be specific for a cell surface target molecule that is selectively expressed on cancer cells, or overexpressed on cancer cells relative to normal cells. The payload of an ADC must be highly cytotoxic so that it can kill tumor cells at the intracellular concentrations achievable following distribution of the ADC into solid tumor tissue, and because only a limited number of payloads can be linked to an antibody molecule (typically an average of 3-4 payloads per antibody) without severely compromising its biophysical and pharmacokinetic properties. The cytotoxic compounds include derivatives of calicheamicin, a class of highly cytotoxic enediyne antibiotics which kill cells by causing DNA double-strand breaks, and derivatives of the potent antimitotic microtubule-disrupting agents, dolastatin 10 (auristatins) and maytansine.

The third vital component of an ADC is the linker that forms a chemical connection between the payload and the antibody. The linker should be sufficiently stable in circulation to allow the payload to remain attached to the antibody while in circulation as it distributes into tissues (including solid tumor tissue), yet should allow efficient release of an active cell-killing agent once the ADC is taken up into the cancer cells. Linkers can be characterized as either cleavable, or as non-cleavable.

Antibody-Drug Conjugates (ADCs) 相关产品 (39):

目录号 产品名 作用方式 纯度
  • HY-138298A
    Trastuzumab deruxtecan ≥99.0%
    Trastuzumab deruxtecan (DS-8201a) 是一种抗人表皮生长因子受体 2 (HER2) 抗体-药物偶联物 (ADC)。Trastuzumab deruxtecan 由人源化抗 HER2 抗体,酶促裂解的肽接头和拓扑异构酶 I 抑制剂组成。Trastuzumab deruxtecan 可用于 HER2 阳性乳腺癌和胃癌的研究。
  • HY-138298
    Trastuzumab deruxtecan (solution) 99.40%
    Trastuzumab deruxtecan (DS-8201a) (solution) 是一种抗人表皮生长因子受体 2 (HER2) 抗体-药物偶联物 (ADC)。Trastuzumab deruxtecan (solution) 由人源化抗 HER2 抗体,酶促裂解的肽接头和拓扑异构酶 I 抑制剂组成。Trastuzumab deruxtecan (solution) 可用于 HER2 阳性乳腺癌和胃癌的研究。
  • HY-P9921
    Trastuzumab emtansine


    Trastuzumab emtansine (Ado-Trastuzumab emtansine) 是一种抗体偶联药物 (ADC),其结合了 HER2 靶向的曲妥珠单抗的抗肿瘤特性以及微管抑制剂 DM1 的细胞毒活性。Trastuzumab emtansine 可用于晚期乳腺癌的研究。
  • HY-P9985
    Disitamab vedotin
    Disitamab vedotin (RC48) 是一种抗体-药物偶联物 (ADC),包含抗人表皮生长因子受体2 (HER2) 的单克隆抗体,该单克隆抗体通过可降解连接子结合到细胞毒性剂 MMAE。Disitamab vedotin 增强抗肿瘤免疫。
  • HY-132254
    Sacituzumab govitecan 98.00%
    Sacituzumab govitecan (IMMU-132) 是一种抗体-药物偶联物 (ADC),靶向 Trop-2 传递 SN-38。Sacituzumab govitecan 具有抗癌活性。
  • HY-P99349
    Loncastuximab tesirine
    Loncastuximab tesirine 是一种人簇分化 19 (CD19) 靶向的抗体-药物偶联物 (ADC)。一旦与细胞膜上的 CD19 结合,Loncastuximab tesirine 被迅速内化,引发细胞死亡。Loncastuximab tesirin 诱导细胞凋亡,可用于弥漫型 B 细胞淋巴瘤的研究。
  • HY-P99612
    Farletuzumab ecteribulin
    Farletuzumab ecteribulin (MORAb-202) 是一种抗体-药物偶联物 (ADC),由人源化抗人叶酸受体 α (FRA) 抗体 Farletuzumab (HY-P99153) 通过还原的链间二硫键与 Mal-PEG2-Val-Cit-PAB-eribulin 偶联而成。Farletuzumab ecteribulin 的药物抗体比为 4.0。Farletuzumab ecteribulin 在体外对 FRA 阳性细胞具有高度细胞毒性。Farletuzumab ecteribulin 具有有效的抗肿瘤活性。
  • HY-P99492
    Cantuzumab mertansine


    Cantuzumab mertansine (SB-408075; huC242-DM1) 是一种 ADC,是强效美登素衍生物 (DM1; HY-19792) 和针对 CanAg 的人源化单克隆抗体 (huC242) 的免疫偶联物。Cantuzumab mertansine 对结肠癌细胞具有细胞毒性,并且对一系列 CanAg 阳性人肿瘤异种移植物具有广泛的抗肿瘤活性。
  • HY-109539
    Gemtuzumab ozogamicin 98.0%
    Gemtuzumab ozogamicin 是一种抗体偶联药物,由一种针对 CD33 的单克隆抗体组成,该单克隆抗体与 Calicheamicin 的细胞毒性衍生物相连。Gemtuzumab ozogamicin 可用于急性髓系白血病的研究。
  • HY-P99107
    Brentuximab vedotin

    维布妥昔单抗; 本妥昔单抗

    Brentuximab vedotin (cAC10-vcMMAE) 是一种抗体-药物偶联物 (ADC),由抗 CD30 抗体和 Monomethyl auristatin E (MMAE) 组成。Brentuximab vedotin 抑制 CD30 阳性细胞,其 IC50 值为 2.5 ng/mL。Brentuximab vedotin 可用于复发难治性霍奇金淋巴瘤的研究。
  • HY-P99016A
    Enfortumab vedotin-ejfv 98.0%
    Enfortumab vedotin-ejfv 是一种 anti-Nectin-4 antibody-drug conjugate,用于尿路上皮癌的研究。
  • HY-P99774
    Pivekimab sunirine
    Pivekimab sunirine (IMGN 632) 是一种靶向 CD123抗体-药物偶联物 (ADC)。Pivekimab sunirine 包含高亲和力的 CD123 抗体、可裂解连接子和 indolinobenzodiazepine pseudodimer (IGN)。Pivekimab sunirine 可用于血液恶性肿瘤的研究。
  • HY-132253
    Polatuzumab vedotin
    Polatuzumab vedotin 是一种靶向 CD79b 的抗体药物偶联物。它由一种人源化抗 CD79b IgG1 单克隆抗体与一种有效的微管抑制剂单甲基 auristatin E (MMAE) 相连,是一种有效的微管抑制剂。Polatuzumab vedotin 具有研究大 B 细胞淋巴瘤 (LBCL) 的潜力。
  • HY-P99334
    Vorsetuzumab mafodotin
    Vorsetuzumab mafodotin (SGN-75) 是一种基于 Auristatin 的抗 CD70 抗体药物偶联物 (ADC) Vorsetuzumab mafodotin 由人源化单克隆抗体 Vorsetuzumab 和 ADC 细胞毒素 MMAF 组成,具有抗肿瘤活性。
  • HY-P3239
    Belantamab mafodotin
    Belantamab mafodotin (GSK2857916) 是由人源化、聚焦化的抗 B 细胞成熟抗原 (BCMA) 单克隆抗体和 McMMAF 组成,具有抗骨髓瘤活性。
  • HY-P99789
    Praluzatamab ravtansine
    Praluzatamab ravtansine (CX-2009) 是一种抗 CD166 抗体药物偶联物 (ADC),Kd 值为 25.15 nM。Praluzatamab ravtansine 显示出肿瘤靶向性和抗癌性。
  • HY-P99956
    Zilovertamab vedotin
    Zilovertamab vedotin (VLS-101) 是一种新型抗体-药物偶联物 (ADC),包含人源化单克隆抗体 zilovertamab 和抗微管细胞毒素单甲基 vedotin。Zilovertamab vedotin 与肿瘤细胞 ROR1 结合导致快速内化、转运至溶酶体、抗体-药物偶联物裂解和单甲基 vedotin 释放。Zilovertamab vedotin 诱导细胞凋亡。Zilovertamab vedotin 可用于癌症研究。
  • HY-P99255
    Moxetumomab pasudotox
    Moxetumomab pasudotox (CAT 8015) 是一种抗 CD22 免疫毒素,含有抗 CD22 FvPseudomonas exotoxin。CD22 是在多种恶性 B 细胞上表达的细胞表面受体。Moxetumomab pasudotox 可用于毛细胞白血病 (HCL) 的研究。
  • HY-P99894
    Serclutamab talirine
    Serclutamab talirine (ABBV-321) 是一种 EGFR 靶向抗体药物偶联物 (ADC)。Serclutamab talirine 由针对激活 EGFR 的抗体 (AM-1-ABT-806) 和吡咯苯二氮卓 (PBD) 二聚体组成。Serclutamab talirine 显示出较强的抗肿瘤活性。
  • HY-P99681
    Labetuzumab govitecan
    Labetuzumab govitecan (IMMU 130) 是一种抗 CEACAM5/SN-38抗体-药物偶联物 (ADC)。Labetuzumab govitecan 由抗体 Labetuzumab、SN-38 和 pH 敏感连接子组成。Labetuzumab govitecan 可用于癌症研究,如结直肠癌