CN110392580A - 用靶向trop-2的拓扑异构酶-i抑制性抗体-药物缀合物(adc)治疗小细胞肺癌(sclc) - Google Patents

用靶向trop-2的拓扑异构酶-i抑制性抗体-药物缀合物(adc)治疗小细胞肺癌(sclc) Download PDF

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Publication number
CN110392580A
CN110392580A CN201880017528.6A CN201880017528A CN110392580A CN 110392580 A CN110392580 A CN 110392580A CN 201880017528 A CN201880017528 A CN 201880017528A CN 110392580 A CN110392580 A CN 110392580A
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antibody
cancer
adc
patients
antibodies
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CN201880017528.6A
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Chinese (zh)
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D.M.戈登伯格
S.V.戈文丹
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Immunomedical Co
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Immunomedical Co
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Priority claimed from US15/820,708 external-priority patent/US10413539B2/en
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/30Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/135Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/137Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/255Esters, e.g. nitroglycerine, selenocyanates of sulfoxy acids or sulfur analogues thereof
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • AHUMAN NECESSITIES
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • AHUMAN NECESSITIES
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    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • AHUMAN NECESSITIES
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    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/68037Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a camptothecin [CPT] or derivatives
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    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
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  • Oncology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
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CN201880017528.6A 2017-02-24 2018-02-21 用靶向trop-2的拓扑异构酶-i抑制性抗体-药物缀合物(adc)治疗小细胞肺癌(sclc) Pending CN110392580A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201762463316P 2017-02-24 2017-02-24
US62/463316 2017-02-24
US15/820708 2017-11-22
US15/820,708 US10413539B2 (en) 2012-12-13 2017-11-22 Therapy for metastatic urothelial cancer with the antibody-drug conjugate, sacituzumab govitecan (IMMU-132)
PCT/US2018/019025 WO2018156634A1 (en) 2017-02-24 2018-02-21 Therapy of small-cell lung cancer (sclc) with a topoisomerase-i inhibiting antibody-drug conjugate (adc) targeting trop-2

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Publication Number Publication Date
CN110392580A true CN110392580A (zh) 2019-10-29

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CN201880017528.6A Pending CN110392580A (zh) 2017-02-24 2018-02-21 用靶向trop-2的拓扑异构酶-i抑制性抗体-药物缀合物(adc)治疗小细胞肺癌(sclc)

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EP (1) EP3585442B1 (https=)
JP (1) JP7188837B2 (https=)
CN (1) CN110392580A (https=)
CA (1) CA3043766A1 (https=)
ES (1) ES2966466T3 (https=)
PL (1) PL3585442T3 (https=)
RU (1) RU2019124477A (https=)
WO (1) WO2018156634A1 (https=)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021143741A1 (zh) * 2020-01-15 2021-07-22 北京海步医药科技有限公司 靶向多肽-药物缀合物及其用途
CN114288265A (zh) * 2021-11-24 2022-04-08 宁波市第一医院 一种包含顺铂-亚油酸和sn38-亚油酸的纳米颗粒、制备方法及应用
CN117180447A (zh) * 2023-04-23 2023-12-08 中山大学肿瘤防治中心(中山大学附属肿瘤医院、中山大学肿瘤研究所) Immu-132在制备用于治疗结直肠癌药物中的应用

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JP7673255B2 (ja) * 2021-06-11 2025-05-08 ギリアード サイエンシーズ, インコーポレイテッド Mcl-1阻害剤と抗体薬物コンジュゲートとの組み合わせ
WO2023208341A1 (en) 2022-04-27 2023-11-02 ITM Isotope Technologies Munich SE Combination treatment of small-cell lung cancer
CA3221834A1 (en) * 2023-06-30 2025-06-17 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Combination therapies for the treatment of non-small cell lung cancer
WO2025199464A1 (en) * 2024-03-22 2025-09-25 Eisai R&D Management Co., Ltd. Anti-trop2 antibody-drug conjugates and methods of use

Citations (3)

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US20140377287A1 (en) * 2002-03-01 2014-12-25 Immunomedics, Inc. Anti-trop-2 antibody-drug conjugates and uses thereof
US20160193357A1 (en) * 2012-12-13 2016-07-07 Immunomedics, Inc. Dosages of Immunoconjugates of Antibodies and SN-38 for Improved Efficacy and Decreased Toxicity
WO2016172427A1 (en) * 2015-04-22 2016-10-27 Immunomedics, Inc. Isolation, detection, diagnosis and/or characterization of circulating trop-2-positive cancer cells

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US20130029909A1 (en) * 2009-09-15 2013-01-31 John Ryan Treatment of cancer
US9492566B2 (en) * 2012-12-13 2016-11-15 Immunomedics, Inc. Antibody-drug conjugates and uses thereof
EP4257134A3 (en) 2015-06-25 2024-01-24 Immunomedics, Inc. Combining anti-hla-dr or anti-trop-2 antibodies with microtubule inhibitors, parp inhibitors, bruton kinase inhibitors or phosphoinositide 3-kinase inhibitors significantly improves therapeutic outcome in cancer

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140377287A1 (en) * 2002-03-01 2014-12-25 Immunomedics, Inc. Anti-trop-2 antibody-drug conjugates and uses thereof
US20160193357A1 (en) * 2012-12-13 2016-07-07 Immunomedics, Inc. Dosages of Immunoconjugates of Antibodies and SN-38 for Improved Efficacy and Decreased Toxicity
WO2016172427A1 (en) * 2015-04-22 2016-10-27 Immunomedics, Inc. Isolation, detection, diagnosis and/or characterization of circulating trop-2-positive cancer cells

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021143741A1 (zh) * 2020-01-15 2021-07-22 北京海步医药科技有限公司 靶向多肽-药物缀合物及其用途
CN114288265A (zh) * 2021-11-24 2022-04-08 宁波市第一医院 一种包含顺铂-亚油酸和sn38-亚油酸的纳米颗粒、制备方法及应用
CN117180447A (zh) * 2023-04-23 2023-12-08 中山大学肿瘤防治中心(中山大学附属肿瘤医院、中山大学肿瘤研究所) Immu-132在制备用于治疗结直肠癌药物中的应用

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EP3585442C0 (en) 2023-10-11
RU2019124477A3 (https=) 2021-03-30
WO2018156634A1 (en) 2018-08-30
EP3585442A4 (en) 2020-09-09
ES2966466T3 (es) 2024-04-22
PL3585442T3 (pl) 2024-03-11
EP3585442A1 (en) 2020-01-01
EP3585442B1 (en) 2023-10-11
CA3043766A1 (en) 2018-08-30
JP7188837B2 (ja) 2022-12-13
RU2019124477A (ru) 2021-03-24

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