JP2014533954A5 - - Google Patents
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- JP2014533954A5 JP2014533954A5 JP2014542584A JP2014542584A JP2014533954A5 JP 2014533954 A5 JP2014533954 A5 JP 2014533954A5 JP 2014542584 A JP2014542584 A JP 2014542584A JP 2014542584 A JP2014542584 A JP 2014542584A JP 2014533954 A5 JP2014533954 A5 JP 2014533954A5
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- JP
- Japan
- Prior art keywords
- composition
- egfr
- linker
- composition according
- cancer
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 102000001301 EGF receptor Human genes 0.000 claims description 45
- 108060006698 EGF receptor Proteins 0.000 claims description 45
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- 108090000623 proteins and genes Proteins 0.000 claims description 16
- 238000002560 therapeutic procedure Methods 0.000 claims description 15
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- -1 2-pyridyldithio Chemical group 0.000 claims description 8
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- 101150040459 RAS gene Proteins 0.000 claims description 8
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- 239000002254 cytotoxic agent Substances 0.000 claims description 8
- 229940121647 egfr inhibitor Drugs 0.000 claims description 8
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- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims description 6
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- JSHOVKSMJRQOGY-UHFFFAOYSA-N (2,5-dioxopyrrolidin-1-yl) 4-(pyridin-2-yldisulfanyl)butanoate Chemical compound O=C1CCC(=O)N1OC(=O)CCCSSC1=CC=CC=N1 JSHOVKSMJRQOGY-UHFFFAOYSA-N 0.000 claims description 4
- GTBCXYYVWHFQRS-UHFFFAOYSA-N (2,5-dioxopyrrolidin-1-yl) 4-(pyridin-2-yldisulfanyl)pentanoate Chemical compound C=1C=CC=NC=1SSC(C)CCC(=O)ON1C(=O)CCC1=O GTBCXYYVWHFQRS-UHFFFAOYSA-N 0.000 claims description 4
- FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims description 4
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- VQNATVDKACXKTF-XELLLNAOSA-N duocarmycin Chemical compound COC1=C(OC)C(OC)=C2NC(C(=O)N3C4=CC(=O)C5=C([C@@]64C[C@@H]6C3)C=C(N5)C(=O)OC)=CC2=C1 VQNATVDKACXKTF-XELLLNAOSA-N 0.000 claims description 4
- 229960001433 erlotinib Drugs 0.000 claims description 4
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims description 4
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- 229960002584 gefitinib Drugs 0.000 claims description 4
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims description 4
- 239000003112 inhibitor Substances 0.000 claims description 4
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- 229960001972 panitumumab Drugs 0.000 claims description 4
- UOWVMDUEMSNCAV-WYENRQIDSA-N rachelmycin Chemical compound C1([C@]23C[C@@H]2CN1C(=O)C=1NC=2C(OC)=C(O)C4=C(C=2C=1)CCN4C(=O)C1=CC=2C=4CCN(C=4C(O)=C(C=2N1)OC)C(N)=O)=CC(=O)C1=C3C(C)=CN1 UOWVMDUEMSNCAV-WYENRQIDSA-N 0.000 claims description 4
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- 101150105382 MET gene Proteins 0.000 claims description 3
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- 229960004891 lapatinib Drugs 0.000 claims description 3
- BCFGMOOMADDAQU-UHFFFAOYSA-N lapatinib Chemical compound O1C(CNCCS(=O)(=O)C)=CC=C1C1=CC=C(N=CN=C2NC=3C=C(Cl)C(OCC=4C=C(F)C=CC=4)=CC=3)C2=C1 BCFGMOOMADDAQU-UHFFFAOYSA-N 0.000 claims description 3
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- 229950010203 nimotuzumab Drugs 0.000 claims description 3
- JKHVDAUOODACDU-UHFFFAOYSA-N (2,5-dioxopyrrolidin-1-yl) 3-(2,5-dioxopyrrol-1-yl)propanoate Chemical compound O=C1CCC(=O)N1OC(=O)CCN1C(=O)C=CC1=O JKHVDAUOODACDU-UHFFFAOYSA-N 0.000 claims description 2
- PVGATNRYUYNBHO-UHFFFAOYSA-N (2,5-dioxopyrrolidin-1-yl) 4-(2,5-dioxopyrrol-1-yl)butanoate Chemical compound O=C1CCC(=O)N1OC(=O)CCCN1C(=O)C=CC1=O PVGATNRYUYNBHO-UHFFFAOYSA-N 0.000 claims description 2
- FUHCFUVCWLZEDQ-UHFFFAOYSA-N 1-(2,5-dioxopyrrolidin-1-yl)oxy-1-oxo-4-(pyridin-2-yldisulfanyl)butane-2-sulfonic acid Chemical compound O=C1CCC(=O)N1OC(=O)C(S(=O)(=O)O)CCSSC1=CC=CC=N1 FUHCFUVCWLZEDQ-UHFFFAOYSA-N 0.000 claims description 2
- SVUOLADPCWQTTE-UHFFFAOYSA-N 1h-1,2-benzodiazepine Chemical compound N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-N 0.000 claims description 2
- OWDQCSBZQVISPN-UHFFFAOYSA-N 2-[(2,5-dioxopyrrolidin-1-yl)amino]-4-(2-iodoacetyl)benzoic acid Chemical compound OC(=O)C1=CC=C(C(=O)CI)C=C1NN1C(=O)CCC1=O OWDQCSBZQVISPN-UHFFFAOYSA-N 0.000 claims description 2
- 239000002146 L01XE16 - Crizotinib Substances 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims description 2
- 239000002253 acid Substances 0.000 claims description 2
- 108010044540 auristatin Proteins 0.000 claims description 2
- 229940049706 benzodiazepine Drugs 0.000 claims description 2
- 229960005061 crizotinib Drugs 0.000 claims description 2
- KTEIFNKAUNYNJU-GFCCVEGCSA-N crizotinib Chemical group O([C@H](C)C=1C(=C(F)C=CC=1Cl)Cl)C(C(=NC=1)N)=CC=1C(=C1)C=NN1C1CCNCC1 KTEIFNKAUNYNJU-GFCCVEGCSA-N 0.000 claims description 2
- KZNICNPSHKQLFF-UHFFFAOYSA-N dihydromaleimide Natural products O=C1CCC(=O)N1 KZNICNPSHKQLFF-UHFFFAOYSA-N 0.000 claims description 2
- 229930188854 dolastatin Natural products 0.000 claims description 2
- 229960004679 doxorubicin Drugs 0.000 claims description 2
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- 229960005501 duocarmycin Drugs 0.000 claims description 2
- 229930184221 duocarmycin Natural products 0.000 claims description 2
- 108010087914 epidermal growth factor receptor VIII Proteins 0.000 claims description 2
- 150000002148 esters Chemical class 0.000 claims description 2
- 201000010536 head and neck cancer Diseases 0.000 claims description 2
- YACHGFWEQXFSBS-RJXCBBHPSA-N leptomycin Chemical class OC(=O)/C=C(C)/C[C@H](C)[C@@H](O)[C@H](C)C(=O)[C@H](C)/C=C(\C)/C=C/C[C@@H](C)\C=C(/CC)\C=C\[C@@H]1OC(=O)C=C[C@@H]1C YACHGFWEQXFSBS-RJXCBBHPSA-N 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- ZNALDVNNEBOGGN-UHFFFAOYSA-N n-(2,5-dioxopyrrol-1-yl)propanamide Chemical compound CCC(=O)NN1C(=O)C=CC1=O ZNALDVNNEBOGGN-UHFFFAOYSA-N 0.000 claims description 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 2
- 229920001223 polyethylene glycol Polymers 0.000 claims description 2
- 229940002612 prodrug Drugs 0.000 claims description 2
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- 125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims description 2
- 206010041823 squamous cell carcinoma Diseases 0.000 claims description 2
- 229960002317 succinimide Drugs 0.000 claims description 2
- 230000005945 translocation Effects 0.000 claims description 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 42
- 230000004663 cell proliferation Effects 0.000 claims 2
- 229960000513 necitumumab Drugs 0.000 claims 2
- UQVNRKBFAXNOGA-LWTNMJDUSA-N (E)-tomaymycin Chemical class CO[C@H]1NC2=CC(O)=C(OC)C=C2C(=O)N2C\C(=C\C)C[C@@H]12 UQVNRKBFAXNOGA-LWTNMJDUSA-N 0.000 claims 1
- 108091008794 FGF receptors Proteins 0.000 claims 1
- 231100000433 cytotoxic Toxicity 0.000 claims 1
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- 102000052178 fibroblast growth factor receptor activity proteins Human genes 0.000 claims 1
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- 208000037841 lung tumor Diseases 0.000 claims 1
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- 230000004565 tumor cell growth Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 41
- 229940034982 antineoplastic agent Drugs 0.000 description 3
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- ANZJBCHSOXCCRQ-FKUXLPTCSA-N mertansine Chemical compound CO[C@@H]([C@@]1(O)C[C@H](OC(=O)N1)[C@@H](C)[C@@H]1O[C@@]1(C)[C@@H](OC(=O)[C@H](C)N(C)C(=O)CCS)CC(=O)N1C)\C=C\C=C(C)\CC2=CC(OC)=C(Cl)C1=C2 ANZJBCHSOXCCRQ-FKUXLPTCSA-N 0.000 description 2
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- 101000984753 Homo sapiens Serine/threonine-protein kinase B-raf Proteins 0.000 description 1
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- 239000002525 vasculotropin inhibitor Substances 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161562157P | 2011-11-21 | 2011-11-21 | |
| US61/562,157 | 2011-11-21 | ||
| US201261639452P | 2012-04-27 | 2012-04-27 | |
| US61/639,452 | 2012-04-27 | ||
| PCT/US2012/066205 WO2013078271A1 (en) | 2011-11-21 | 2012-11-21 | Method of treatment of tumors that are resistant to egfr therapies by egfr antibody cytotoxic agent conjugate |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014533954A JP2014533954A (ja) | 2014-12-18 |
| JP2014533954A5 true JP2014533954A5 (cg-RX-API-DMAC7.html) | 2016-01-21 |
Family
ID=48470279
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014542584A Pending JP2014533954A (ja) | 2011-11-21 | 2012-11-21 | Ｅｇｆｒ抗体細胞傷害性薬物複合体による、ｅｇｆｒ療法に耐性である腫瘍の治療方法 |
Country Status (16)
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103298489A (zh) | 2010-10-29 | 2013-09-11 | 伊缪诺金公司 | 新型egfr结合分子及其免疫偶联物 |
| JP5828902B2 (ja) | 2010-10-29 | 2015-12-09 | イミュノジェン， インコーポレイテッド | 非拮抗性ｅｇｆｒ結合分子およびその免疫複合体 |
| PT2668209T (pt) | 2011-01-24 | 2021-04-07 | Gilead Sciences Inc | Anticorpos seletivos para células que apresentam egfr em alta densidade |
| EP2794010A4 (en) | 2011-11-21 | 2015-10-21 | Immunogen Inc | METHOD OF TREATING TUMORS RESISTANT TO EGFR THERAPIES BY A CYTOTOXIC EGFR-AGENT ANTIBODY CONJUGATE |
| AU2014286872B2 (en) * | 2013-07-05 | 2020-01-23 | Formation Biologics Inc. | EGFR antibody conjugates |
| WO2015035410A1 (en) * | 2013-09-09 | 2015-03-12 | Triact Therapeutic, Inc. | Cancer therapy |
| WO2015073721A1 (en) | 2013-11-13 | 2015-05-21 | Zymeworks Inc. | Monovalent antigen binding constructs targeting egfr and/or her2 and uses thereof |
| CN113425727A (zh) | 2014-02-04 | 2021-09-24 | 安斯泰来制药株式会社 | 以二氨基杂环甲酰胺化合物为有效成分的医药组合物 |
| CN110841074B (zh) * | 2014-03-21 | 2023-07-18 | 艾伯维公司 | 抗-egfr抗体及抗体药物偶联物 |
| CN109147874A (zh) | 2014-09-02 | 2019-01-04 | 伊缪诺金公司 | 用于配制抗体药物缀合物组合物的方法 |
| MA40968A (fr) * | 2014-10-31 | 2017-10-04 | Formation Biologics Inc | Polythérapie à base d'anticorps anti-egfr |
| KR101692044B1 (ko) * | 2014-12-05 | 2017-01-04 | 사회복지법인 삼성생명공익재단 | 교모세포종에서 표피 성장인자 수용체 억제제의 치료 효과를 예측하는 방법 |
| US20180117053A1 (en) * | 2015-05-27 | 2018-05-03 | Metastat, Inc. | The Method of Use for Inhibitors of Epidermal Growth Factor Receptor Variants II, III and VI |
| US10426842B2 (en) | 2015-07-15 | 2019-10-01 | The Curators Of The University Of Missouri | Targeted nanoparticle conjugate and method for co-delivery of siRNA and drug |
| RU2019134769A (ru) * | 2017-03-31 | 2021-04-30 | Дзе Кьюрейторз Оф Дзе Юниверсити Оф Миссури | Композиции для лечения резистентных к лекарственным средствам опухолей и способы их применения |
| CN107496933B (zh) * | 2017-08-21 | 2019-12-24 | 山东新华制药股份有限公司 | 一种用于治疗胰腺癌的抗体药物偶联物及其制备方法 |
| KR20230106506A (ko) * | 2022-01-03 | 2023-07-13 | 한국생명공학연구원 | Cda 억제제를 포함하는 alk 저해제 내성 비소세포폐암 치료용 조성물 |
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-
2012
- 2012-11-21 EP EP12850911.4A patent/EP2794010A4/en not_active Withdrawn
- 2012-11-21 US US13/682,948 patent/US9233171B2/en not_active Expired - Fee Related
- 2012-11-21 WO PCT/US2012/066205 patent/WO2013078271A1/en not_active Ceased
- 2012-11-21 SG SG11201402343SA patent/SG11201402343SA/en unknown
- 2012-11-21 JP JP2014542584A patent/JP2014533954A/ja active Pending
- 2012-11-21 AU AU2012340686A patent/AU2012340686A1/en not_active Abandoned
- 2012-11-21 CA CA2856411A patent/CA2856411A1/en not_active Abandoned
- 2012-11-21 HK HK15102403.0A patent/HK1201772A1/xx unknown
- 2012-11-21 KR KR1020147016745A patent/KR20140105765A/ko not_active Withdrawn
- 2012-11-21 CN CN201280056769.4A patent/CN104066481A/zh active Pending
- 2012-11-21 RU RU2014121820/15A patent/RU2014121820A/ru not_active Application Discontinuation
- 2012-11-21 MX MX2014006087A patent/MX2014006087A/es not_active Application Discontinuation
- 2012-11-21 BR BR112014012155A patent/BR112014012155A2/pt not_active IP Right Cessation
-
2014
- 2014-05-15 CL CL2014001282A patent/CL2014001282A1/es unknown
- 2014-05-18 IL IL232666A patent/IL232666A0/en unknown
- 2014-05-19 PH PH12014501119A patent/PH12014501119A1/en unknown
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