(10,19-Diethyl-7-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaen-19-yl) carbonochloridate

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 喜树碱
• 英文名称: (10,19-Diethyl-7-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaen-19-yl) carbonochloridate
• 英文别名: (10,19-diethyl-7-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaen-19-yl) carbonochloridate
• 化学式: C₂₃H₁₉ClN₂O₆
• 分子量: 454.9
• InChiKey: FPVJLJVDMXHBCS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  32
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  106
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• Dosages of Immunoconjugates of Antibodies and SN-38 for Improved Efficacy and Decreased Toxicity
  申请人：IMMUNOMEDICS, INC.

  公开号：US20150196661A1

  公开（公告）日：2015-07-16

  The present invention relates to therapeutic immunoconjugates comprising SN-38 attached to an antibody or antigen-binding antibody fragment. The antibody may bind to EGP-1 (TROP-2), CEACAM5, CEACAM6, CD74, CD19, CD20, CD22, CSAp, HLA-DR, AFP or MUC5ac and the immunoconjugate may be administered at a dosage of between 4 mg/kg and 24 mg/kg, preferably 4, 6, 8, 9, 10, 12, 16 or 18 mg/kg. When administered at specified dosages and schedules, the immunoconjugate can reduce solid tumors in size, reduce or eliminate metastases and is effective to treat cancers resistant to standard therapies, such as radiation therapy, chemotherapy or immunotherapy.

  本发明涉及治疗免疫偶联物，其包括将SN-38连接到抗体或抗原结合抗体片段上。该抗体可以结合到EGP-1（TROP-2）、CEACAM5、CEACAM6、CD74、CD19、CD20、CD22、CSAp、HLA-DR、AFP或MUC5ac，并且该免疫偶联物可以以每公斤4毫克至24毫克的剂量给予，优选为每公斤4、6、8、9、10、12、16或18毫克。当以特定的剂量和计划给予该免疫偶联物时，它可以减小实体瘤的大小，减少或消除转移，并且对于对标准治疗（如放疗、化疗或免疫疗法）有抗药性的癌症是有效的。
• Immunoconjugates with an Intracellularly-Cleavable Linkage
  申请人：Immunomedics, Inc.

  公开号：US20170028081A1

  公开（公告）日：2017-02-02

  The present invention relates to therapeutic conjugates with improved ability to target various diseased cells containing a targeting moiety (such as an antibody or antibody fragment), a linker and a therapeutic moiety, and further relates to processes for making and using the conjugates.
• US8741300B2
  申请人：——

  公开号：US8741300B2

  公开（公告）日：2014-06-03
• US9475884B2
  申请人：——

  公开号：US9475884B2

  公开（公告）日：2016-10-25
• US9493573B2
  申请人：——

  公开号：US9493573B2

  公开（公告）日：2016-11-15