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 (8):

目录号 产品名 作用方式 纯度
  • 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

    曲妥珠单抗-美坦新偶联物

    ≥99.40%
    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-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-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-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-P3239
    Belantamab mafodotin
    Belantamab mafodotin (GSK2857916) 是一种人源化、聚焦化的抗 B 细胞成熟抗原 (BCMA) 单克隆抗体偶联药物,通过马来酰咪多烯丙基连接物 (McMMAF, HY-15578) 与 MMAF (HY-15579) 结合。Belantamab mafodotin 具有抗骨髓瘤活性。
  • 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。