JP2012506448A5 - - Google Patents
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- JP2012506448A5 JP2012506448A5 JP2011533309A JP2011533309A JP2012506448A5 JP 2012506448 A5 JP2012506448 A5 JP 2012506448A5 JP 2011533309 A JP2011533309 A JP 2011533309A JP 2011533309 A JP2011533309 A JP 2011533309A JP 2012506448 A5 JP2012506448 A5 JP 2012506448A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- patient
- combination
- activated prodrug
- composition
- 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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- 239000002246 antineoplastic agent Substances 0.000 claims description 31
- 206010021143 Hypoxia Diseases 0.000 claims description 30
- 229940002612 prodrug Drugs 0.000 claims description 30
- 239000000651 prodrug Substances 0.000 claims description 30
- 230000007954 hypoxia Effects 0.000 claims description 27
- 206010028980 Neoplasm Diseases 0.000 claims description 25
- 201000011510 cancer Diseases 0.000 claims description 25
- 229940041181 antineoplastic drug Drugs 0.000 claims description 24
- 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 16
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims description 10
- 229960005277 gemcitabine Drugs 0.000 claims description 10
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 8
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims description 8
- 229960003668 docetaxel Drugs 0.000 claims description 8
- 229960004679 doxorubicin Drugs 0.000 claims description 8
- 229960005079 pemetrexed Drugs 0.000 claims description 8
- QOFFJEBXNKRSPX-ZDUSSCGKSA-N pemetrexed Chemical compound C1=N[C]2NC(N)=NC(=O)C2=C1CCC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 QOFFJEBXNKRSPX-ZDUSSCGKSA-N 0.000 claims description 8
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims description 6
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 6
- 206010039491 Sarcoma Diseases 0.000 claims description 6
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims description 6
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims description 6
- 229960004316 cisplatin Drugs 0.000 claims description 6
- 229960002949 fluorouracil Drugs 0.000 claims description 6
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 6
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 6
- 201000002528 pancreatic cancer Diseases 0.000 claims description 6
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 201000002120 neuroendocrine carcinoma Diseases 0.000 claims description 5
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 4
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 4
- 206010060862 Prostate cancer Diseases 0.000 claims description 4
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 4
- -1 TH-281 Chemical compound 0.000 claims description 4
- 229960004562 carboplatin Drugs 0.000 claims description 4
- 190000008236 carboplatin Chemical compound 0.000 claims description 4
- 229940079593 drug Drugs 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 201000004101 esophageal cancer Diseases 0.000 claims description 4
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 4
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 4
- BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Chemical compound [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 claims description 4
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 4
- 229920000053 polysorbate 80 Polymers 0.000 claims description 4
- 230000001146 hypoxic effect Effects 0.000 claims description 3
- 230000003442 weekly effect Effects 0.000 claims description 3
- ZORQXIQZAOLNGE-UHFFFAOYSA-N 1,1-difluorocyclohexane Chemical group FC1(F)CCCCC1 ZORQXIQZAOLNGE-UHFFFAOYSA-N 0.000 claims description 2
- YZBAXVICWUUHGG-UHFFFAOYSA-N 2-[[4-[2-[dimethyl(oxido)azaniumyl]ethylamino]-5,8-dihydroxy-9,10-dioxoanthracen-1-yl]amino]-n,n-dimethylethanamine oxide Chemical compound O=C1C2=C(O)C=CC(O)=C2C(=O)C2=C1C(NCC[N+](C)(C)[O-])=CC=C2NCC[N+](C)([O-])C YZBAXVICWUUHGG-UHFFFAOYSA-N 0.000 claims description 2
- 206010061424 Anal cancer Diseases 0.000 claims description 2
- 208000007860 Anus Neoplasms Diseases 0.000 claims description 2
- 206010004593 Bile duct cancer Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- FXHOOIRPVKKKFG-UHFFFAOYSA-N N,N-Dimethylacetamide Chemical compound CN(C)C(C)=O FXHOOIRPVKKKFG-UHFFFAOYSA-N 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 229930012538 Paclitaxel Natural products 0.000 claims description 2
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 208000006265 Renal cell carcinoma Diseases 0.000 claims description 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims description 2
- 229940123237 Taxane Drugs 0.000 claims description 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 2
- 206010046431 Urethral cancer Diseases 0.000 claims description 2
- 206010046458 Urethral neoplasms Diseases 0.000 claims description 2
- 239000004480 active ingredient Substances 0.000 claims description 2
- 201000011165 anus cancer Diseases 0.000 claims description 2
- 208000026900 bile duct neoplasm Diseases 0.000 claims description 2
- 208000006990 cholangiocarcinoma Diseases 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 201000010893 malignant breast melanoma Diseases 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- 210000004877 mucosa Anatomy 0.000 claims description 2
- 239000002736 nonionic surfactant Substances 0.000 claims description 2
- 229960001592 paclitaxel Drugs 0.000 claims description 2
- 201000001219 parotid gland cancer Diseases 0.000 claims description 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 2
- 229910052697 platinum Inorganic materials 0.000 claims description 2
- 229920000136 polysorbate Polymers 0.000 claims description 2
- 229950008882 polysorbate Drugs 0.000 claims description 2
- 208000000587 small cell lung carcinoma Diseases 0.000 claims description 2
- 235000011069 sorbitan monooleate Nutrition 0.000 claims description 2
- 239000001593 sorbitan monooleate Substances 0.000 claims description 2
- 229940035049 sorbitan monooleate Drugs 0.000 claims description 2
- 239000003381 stabilizer Substances 0.000 claims description 2
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims description 2
- 201000002510 thyroid cancer Diseases 0.000 claims description 2
- 239000003860 topical agent Substances 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 14
- 239000003560 cancer drug Substances 0.000 claims 1
- 230000000955 neuroendocrine Effects 0.000 claims 1
- 210000003462 vein Anatomy 0.000 claims 1
- 238000000034 method Methods 0.000 description 22
- 208000023915 Ureteral Neoplasms Diseases 0.000 description 1
- 206010046392 Ureteric cancer Diseases 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 0.000 description 1
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10725308P | 2008-10-21 | 2008-10-21 | |
| US61/107,253 | 2008-10-21 | ||
| US11836808P | 2008-11-26 | 2008-11-26 | |
| US61/118,368 | 2008-11-26 | ||
| US15070009P | 2009-02-06 | 2009-02-06 | |
| US61/150,700 | 2009-02-06 | ||
| US15116309P | 2009-02-09 | 2009-02-09 | |
| US61/151,163 | 2009-02-09 | ||
| US24417209P | 2009-09-21 | 2009-09-21 | |
| US61/244,172 | 2009-09-21 | ||
| PCT/US2009/061541 WO2010048330A1 (en) | 2008-10-21 | 2009-10-21 | Treatment of cancer using hypoxia activated prodrugs |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012506448A JP2012506448A (ja) | 2012-03-15 |
| JP2012506448A5 true JP2012506448A5 (2) | 2012-12-13 |
| JP5765634B2 JP5765634B2 (ja) | 2015-08-19 |
Family
ID=42119663
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011533309A Active JP5765634B2 (ja) | 2008-10-21 | 2009-10-21 | 低酸素活性化型プロドラッグを用いるがんの処置 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US8946275B2 (2) |
| EP (1) | EP2350664B1 (2) |
| JP (1) | JP5765634B2 (2) |
| ES (1) | ES2884674T3 (2) |
| WO (1) | WO2010048330A1 (2) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102746336B (zh) | 2005-06-29 | 2015-08-19 | 施瑞修德制药公司 | 氨基磷酸酯烷化剂前体药物 |
| WO2012009288A2 (en) | 2010-07-12 | 2012-01-19 | Threshold Pharmaceuticals, Inc. | Administration of hypoxia activated prodrugs and antiangiogenic agents for the treatment of cancer |
| JP2014509658A (ja) | 2011-04-01 | 2014-04-21 | スレッショルド ファーマシューティカルズ、インク． | ガン処置方法 |
| KR20140045931A (ko) * | 2011-04-15 | 2014-04-17 | 쓰레솔드 파마슈티컬스, 인코포레이티드 | 경구 투여를 위한 단위투여량 형태 |
| WO2013096687A1 (en) | 2011-12-22 | 2013-06-27 | Threshold Pharmaceuticals, Inc. | Administration of hypoxia activated prodrugs in combination with chk1 inhibitors for treating cancer |
| EP2793899A4 (en) * | 2011-12-22 | 2015-06-17 | Threshold Pharmaceuticals Inc | HYPOXIA-ACTIVATED PRODRUGS AND MTOR INHIBITORS FOR CANCER TREATMENT |
| US20160045522A1 (en) * | 2012-02-21 | 2016-02-18 | Threshold Pharmaceuticals, Inc. | Treatment of Cancer |
| JP2014001204A (ja) * | 2012-05-23 | 2014-01-09 | Kumamoto Univ | 腫瘍細胞選択的抗がん剤 |
| WO2014062856A1 (en) | 2012-10-16 | 2014-04-24 | Halozyme, Inc. | Hypoxia and hyaluronan and markers thereof for diagnosis and monitoring of diseases and conditions and related methods |
| US10037382B2 (en) | 2012-10-29 | 2018-07-31 | Kyocera Corporation | Surface acoustic wave sensor |
| WO2014169035A1 (en) * | 2013-04-10 | 2014-10-16 | Threshold Pharmaceuticals, Inc. | Predictive and response biomarker for th-302 anti-cancer therapy |
| US20160158253A1 (en) | 2013-07-26 | 2016-06-09 | Threshold Pharmaceuticals, Inc. | Treatment of pancreatic cancer with a combination of a hypoxia-activated prodrug and a taxane |
| US10071109B2 (en) | 2013-11-06 | 2018-09-11 | Molecular Templates, Inc. | Predictive biomarker for hypoxia-activated prodrug therapy |
| CN104628772A (zh) * | 2013-11-07 | 2015-05-20 | 四川恒康发展有限责任公司 | 一种抗肿瘤前药及其激活剂、组合物和应用 |
| KR102359214B1 (ko) | 2014-04-04 | 2022-02-07 | 델 마 파마슈티컬스 | 폐의 비소세포 암종 및 난소암을 치료하기 위한 디안하이드로갈락티톨 및 이의 유사체 또는 유도체 |
| WO2016011195A1 (en) * | 2014-07-17 | 2016-01-21 | Threshold Pharmaceuticals, Inc. | Th-302 solid forms and methods related thereto |
| BR112017019287B1 (pt) | 2015-03-10 | 2024-01-02 | Obi Pharma, Inc | Composto, e composição farmaceuticamente aceitável |
| US10829437B2 (en) | 2015-04-02 | 2020-11-10 | Obi Pharma, Inc. | Nitrobenzyl derivatives of anti-cancer agents |
| WO2016210175A1 (en) | 2015-06-24 | 2016-12-29 | Threshold Pharmaceuticals, Inc. | Aziridine containing dna alkylating agents |
| CN108348463A (zh) * | 2016-05-13 | 2018-07-31 | 泰克利森有限公司 | 用于治疗肝脏组织的方法 |
| US20210369746A1 (en) * | 2016-08-01 | 2021-12-02 | Molecular Templates, Inc. | Administration of hypoxia activated prodrugs in combination with immune modulatory agents for treating cancer |
| PT3565806T (pt) | 2017-01-06 | 2022-05-19 | Rivus Pharmaceuticals Inc | Novos derivados de fenilo |
| JP2019094284A (ja) * | 2017-11-21 | 2019-06-20 | 日本化薬株式会社 | ペメトレキセドを含有する注射用溶液製剤 |
| CN109999183B (zh) * | 2019-04-15 | 2021-03-09 | 中国科学技术大学 | 一种含有乏氧激活前药的纳米簇化酶及其制备方法和应用 |
| WO2023025312A1 (zh) | 2021-08-27 | 2023-03-02 | 深圳艾欣达伟医药科技有限公司 | 使用th-302治疗parp抑制剂耐药的患者 |
| JP2024531479A (ja) | 2021-08-27 | 2024-08-29 | アセンタウィッツ ファーマシューティカルズ リミテッド | 凍結乾燥製剤溶液および凍結乾燥製剤、ならびにそれらの方法および使用 |
| US20250186468A1 (en) | 2022-03-15 | 2025-06-12 | Ascentawits Pharmaceuticals, Ltd. | Method for treating patient with brca-mutated cancer |
| US20250295677A1 (en) | 2022-04-15 | 2025-09-25 | Ascentawits Pharmaceuticals, Ltd. | Method for treating cancer by using th-302 alone or in combination with parp inhibitor |
| CN119233822A (zh) | 2022-05-23 | 2024-12-31 | 深圳艾欣达伟医药科技有限公司 | 烷化剂前药与细胞周期抑制剂联用治疗癌症的方法 |
| WO2024061346A1 (zh) | 2022-09-22 | 2024-03-28 | 深圳艾欣达伟医药科技有限公司 | 乏氧激活的化合物在制备治疗癌症患者的药物中的用途 |
| TW202434258A (zh) | 2023-02-27 | 2024-09-01 | 大陸商深圳艾欣達偉醫藥科技有限公司 | 溶液、凍乾製劑、凍乾製劑單位包裝、注射液及注射液配製方法 |
| AU2024317010A1 (en) | 2023-07-28 | 2026-02-26 | Ascentawits Pharmaceuticals, Ltd. | Treatment of p53 gene mutation or defect negative cancer and tumor patients |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4636195A (en) | 1982-04-02 | 1987-01-13 | Harvey Wolinsky | Method and apparatus for removing arterial constriction |
| EP0383492A3 (en) | 1989-02-14 | 1991-08-07 | Thoro System Products Inc. | Dispersion system for rapid curing cement compositions |
| US5049132A (en) | 1990-01-08 | 1991-09-17 | Cordis Corporation | Balloon catheter for delivering therapeutic agents |
| EP0533816B1 (en) | 1990-06-15 | 1995-06-14 | Cortrak Medical, Inc. | Drug delivery apparatus |
| US6017948A (en) | 1998-10-30 | 2000-01-25 | Supergen, Inc. | Water-miscible pharmaceutical compositions |
| US6060083A (en) | 1999-04-01 | 2000-05-09 | Topical Technologies, Inc. | Topical DMSO treatment for palmar-plantar erythrodysethesia |
| GB9909612D0 (en) | 1999-04-26 | 1999-06-23 | Cancer Res Campaign Tech | N-protected amines and their use as prodrugs |
| AU5331300A (en) | 1999-06-11 | 2001-01-02 | Henceforth Hibernia, Inc. | Prophylactic, therapeutic and industrial antioxidant compositions enhanced with stabilized atomic hydrogen/free electrons and methods to prepare and use such compositions |
| JP2005508838A (ja) * | 2001-03-23 | 2005-04-07 | アフトン コーポレーション | 膵癌の組合せ治療 |
| NZ521851A (en) | 2002-10-08 | 2005-02-25 | Auckland Uniservices Ltd | Nitroaniline-based unsymmetrical mustard alkylating agents for gene dependent enzyme prodrug therapy |
| ZA200507752B (en) | 2003-03-28 | 2007-01-31 | Threshold Pharmaceuticals Inc | Compositions and methods for treating cancer |
| US7629332B2 (en) | 2003-10-31 | 2009-12-08 | Auckland Uniservices Limited | Nitrophenyl mustard and nitrophenylaziridine alcohols and their corresponding phosphates and their use as targeted cytotoxic agents |
| WO2005086951A2 (en) | 2004-03-10 | 2005-09-22 | Threshold Pharmaceuticals, Inc. | Hypoxia-activated anti-cancer agents |
| SE0400642D0 (sv) | 2004-03-15 | 2004-03-15 | Electrolux Ab | Floor cleaning implement |
| MX2007006102A (es) | 2004-11-22 | 2007-07-11 | Threshold Pharmaceuticals Inc | Agentes anti-cancer de union a tubulina y profarmacos de los mismos. |
| US20070117784A1 (en) * | 2005-03-04 | 2007-05-24 | Novacea, Inc. | Treatment of hyperproliferative diseases with anthraquinones |
| KR101332869B1 (ko) | 2005-04-15 | 2013-11-25 | 알버트 아인슈타인 컬리지 오브 메디신 오브 예쉬바 유니버시티 | 항-ｅｇｆｒ 치료법에 속발된 피부 발진의 예방 및 치료를위한 비타민 ｋ |
| CN102746336B (zh) * | 2005-06-29 | 2015-08-19 | 施瑞修德制药公司 | 氨基磷酸酯烷化剂前体药物 |
| EP1931769A2 (en) | 2005-10-03 | 2008-06-18 | Genetix Pharmaceuticals Inc. | Method for selectively depleting hypoxic cells |
| EP1989212B1 (en) | 2006-02-17 | 2013-06-19 | Cascade Prodrug Inc. | Treatment of hyperproliferative diseases with vinca alkaloid n-oxide and analogs |
| EP2114157B1 (en) * | 2006-12-26 | 2021-05-26 | ImmunoGenesis, Inc. | Phosphoramidate alkylator prodrug for the treatment of cancer |
| WO2008151253A1 (en) | 2007-06-04 | 2008-12-11 | Threshold Pharmaceuticals, Inc. | Hypoxia activated prodrugs of antineoplastic agents |
| WO2009018163A1 (en) | 2007-07-27 | 2009-02-05 | Threshold Pharmaceuticals, Inc. | Hypoxia activated prodrugs of anthracyclines |
| WO2009033165A1 (en) | 2007-09-06 | 2009-03-12 | Threshold Pharmaceuticals, Inc. | Hypoxia activated prodrugs of bis-alkylating agents |
-
2009
- 2009-10-21 JP JP2011533309A patent/JP5765634B2/ja active Active
- 2009-10-21 EP EP09822657.4A patent/EP2350664B1/en active Active
- 2009-10-21 US US13/125,303 patent/US8946275B2/en active Active
- 2009-10-21 WO PCT/US2009/061541 patent/WO2010048330A1/en not_active Ceased
- 2009-10-21 ES ES09822657T patent/ES2884674T3/es active Active
-
2014
- 2014-12-17 US US14/574,082 patent/US20150258125A1/en not_active Abandoned
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