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 (35):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-138298A
    Trastuzumab deruxtecan 99.16%
    Trastuzumab deruxtecan (T-DXd; DS-8201a) 是一种抗人表皮生长因子受体 2 (HER2) 抗体-活性分子偶联物 (ADC)。Trastuzumab deruxtecan 由人源化抗 HER2 抗体、酶促裂解的肽接头、拓扑异构酶 I 抑制剂 (毒素成分 Dxd) 组成。Trastuzumab deruxtecan 可用于 HER2 阳性乳腺癌和胃癌的研究。
    Trastuzumab deruxtecan
  • HY-P9921
    Trastuzumab emtansine

    曲妥珠单抗-美坦新偶联物

    99.74%
    Trastuzumab emtansine (Ado-Trastuzumab emtansine) 是一种抗体偶联活性分子 (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。
    Trastuzumab emtansine
  • HY-138298
    Trastuzumab deruxtecan (solution) 98.75%
    Trastuzumab deruxtecan (T-DXd; DS-8201a) (solution) 是一种抗人表皮生长因子受体 2 (HER2) 抗体-活性分子偶联物 (ADC)。Trastuzumab deruxtecan 由人源化抗 HER2 抗体、酶促裂解的肽接头、拓扑异构酶 I 抑制剂 (毒素成分 Dxd) 组成。Trastuzumab deruxtecan 可用于 HER2 阳性乳腺癌和胃癌的研究。
    Trastuzumab deruxtecan (solution)
  • HY-132254
    Sacituzumab govitecan 98.00%
    Sacituzumab govitecan (IMMU-132) 是一种抗体-活性分子偶联物 (ADC),靶向 Trop-2 传递 SN-38。Sacituzumab govitecan 具有抗癌活性。
    Sacituzumab govitecan
  • HY-P9985
    Disitamab vedotin ≥99.0%
    Disitamab vedotin (RC48) 是一种抗体-活性分子偶联物 (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。
    Disitamab vedotin
  • HY-132258A
    Mirvetuximab soravtansine (solution)
    Mirvetuximab soravtansine (solution) (IMGN853 (solution)) 是一种抗体药物偶联物 (ADC)。
    Mirvetuximab soravtansine (solution)
  • HY-P99016B
    Enfortumab vedotin-ejfv (solution) 99.74%
    Enfortumab vedotin-ejfv (solution) 是一种全人 IgG1-kappa 抗体,通过蛋白酶可切割的马来酰亚胺己酰缬氨酸-瓜氨酸接头 (SGD-1006) 与微管破坏剂 monomethyl auristatin E (MMAE) 缀合。
    Enfortumab vedotin-ejfv (solution)
  • HY-P99107A
    Brentuximab vedotin (solution) 99.23%
    Brentuximab vedotin 溶液是 Brentuximab vedotin (HY-P99107) 的溶液形式。Brentuximab vedotin (cAC10-vcMMAE) 是一种抗体-药物偶联物 (ADC),包含抗 CD30 抗体和细胞毒性剂单甲基 auristatin E (MMAE)。
    Brentuximab vedotin (solution)
  • HY-P99107
    Brentuximab vedotin

    维布妥昔单抗; 本妥昔单抗

    98.00%
    Brentuximab vedotin (cAC10-vcMMAE) 是一种抗体-活性分子偶联物 (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。
    Brentuximab vedotin
  • HY-P99016A
    Enfortumab vedotin-ejfv
    Enfortumab vedotin-ejfv 是一种 anti-Nectin-4 antibody-drug conjugate,用于尿路上皮癌的研究。
    Enfortumab vedotin-ejfv
  • HY-109539
    Gemtuzumab ozogamicin 98.00%
    Gemtuzumab ozogamicin 是一种抗体-药物偶联物 (ADC),由 Calicheamicin 的细胞毒性衍生物和靶向 CD33 抗原的单克隆抗体组成,CD33 抗原主要存在于急性髓性白血病的白血病成髓细胞上 (AML)。Calicheamicin 是一种细胞毒性抗生素。 Gemtuzumab ozogamicin 可用于急性髓性白血病的研究。
    Gemtuzumab ozogamicin
  • HY-141598
    Datopotamab deruxtecan 99.54%
    Datopotamab deruxtecan (DS-1062; Dato-DXd) 是一种滋养层细胞表面抗原 2 (TROP2) 导向的抗体活性分子偶联物 (ADC)。Datopotamab deruxtecan 具有强大的抗肿瘤活性。
    Datopotamab deruxtecan
  • HY-132258
    Mirvetuximab soravtansine 99.90%
    Mirvetuximab soravtansine (IMGN853) 是一种抗体药物偶联物 (ADC),由细胞毒性 maytansoid DM4 组成,共价连接到人源化单克隆抗体 M9346A。Mirvetuximab soravtansine 选择性结合叶酸受体1 (FOLR1)。Mirvetuximab soravtansine 具有抑制生长和增强 DNA 损伤的抗增殖作用。
    Mirvetuximab soravtansine
  • HY-P99813
    Patritumab deruxtecan
    Patritumab deruxtecan (HER3-DXd) 是一种抗体-活性分子偶联物 (ADC),由全人抗 HER3 IgG1 单克隆抗体 Patritumab (HY-P99275) 通过基于四肽的可裂解接头连接到拓扑异构酶 I 抑制剂有效载荷组成 [1]
    Patritumab deruxtecan
  • HY-P3239
    Belantamab mafodotin 98.45%
    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。
    Belantamab mafodotin
  • HY-141601
    Telisotuzumab vedotin 99.81%
    Telisotuzumab vedotin (ABBV-399) 是一种靶向 c-Met 的抗体-药物偶联物 (ADCs)。Telisotuzumab vedotin 由 Monomethyl Auristatin E (MMAE)、Telisotuzumab 抗体和可裂解的 mc-val-cit-PABC 型 linker 偶联而成。 Telisotuzumab vedotin 可用于癌症的研究。
    Telisotuzumab vedotin
  • HY-P99542
    Tusamitamab ravtansine 99.42%
    Tusamitamab ravtansine (SAR408701) 是一种针对表达 CEACAM5 的肿瘤细胞的靶向 ADC,由人源化抗 CEACAM5 单克隆抗体组成,通过可裂解接头与强效细胞毒性剂美登木素生物碱 DM4 (HY-12454) 共价连接。Tusamitamab ravtansine 的平均药物抗体比 (DAR) 为 3.8。
    Tusamitamab ravtansine
  • HY-P99349
    Loncastuximab tesirine 99.37%
    Loncastuximab tesirine 是一种人簇分化 19 (CD19) 靶向的抗体-活性分子偶联物 (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。
    Loncastuximab tesirine
  • HY-P99681
    Labetuzumab govitecan 98.33%
    Labetuzumab govitecan (IMMU 130) 是一种抗 CEACAM5/SN-38抗体-活性分子偶联物 (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。
    Labetuzumab govitecan
  • HY-132253
    Polatuzumab vedotin
    Polatuzumab vedotin 是一种靶向 CD79b 的抗体活性分子偶联物。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。
    Polatuzumab vedotin