JP2012503602A5 - - Google Patents
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- Publication number
- JP2012503602A5 JP2012503602A5 JP2011527834A JP2011527834A JP2012503602A5 JP 2012503602 A5 JP2012503602 A5 JP 2012503602A5 JP 2011527834 A JP2011527834 A JP 2011527834A JP 2011527834 A JP2011527834 A JP 2011527834A JP 2012503602 A5 JP2012503602 A5 JP 2012503602A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- prodrug
- days
- topoisomerase inhibitor
- administration
- 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.)
- Withdrawn
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- 239000000651 prodrug Substances 0.000 claims description 42
- 229940002612 prodrug Drugs 0.000 claims description 42
- 239000000203 mixture Substances 0.000 claims description 36
- 238000000034 method Methods 0.000 claims description 32
- 239000003534 dna topoisomerase inhibitor Substances 0.000 claims description 29
- 229940044693 topoisomerase inhibitor Drugs 0.000 claims description 29
- 230000036470 plasma concentration Effects 0.000 claims description 19
- 239000002207 metabolite Substances 0.000 claims description 15
- 229960004768 irinotecan Drugs 0.000 claims description 13
- UWKQSNNFCGGAFS-XIFFEERXSA-N irinotecan Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 claims description 13
- 238000001514 detection method Methods 0.000 claims description 12
- 239000008194 pharmaceutical composition Substances 0.000 claims description 12
- 206010028980 Neoplasm Diseases 0.000 claims description 10
- 230000001225 therapeutic effect Effects 0.000 claims description 9
- 230000002459 sustained effect Effects 0.000 claims description 6
- 239000002202 Polyethylene glycol Substances 0.000 claims description 5
- 229920001223 polyethylene glycol Polymers 0.000 claims description 5
- ATHLLZUXVPNPAW-UHFFFAOYSA-N lamellarin d Chemical compound C1=C(O)C(OC)=CC(C2=C3C4=CC(OC)=C(O)C=C4C=CN3C3=C2C=2C=C(OC)C(O)=CC=2OC3=O)=C1 ATHLLZUXVPNPAW-UHFFFAOYSA-N 0.000 claims description 4
- 230000008030 elimination Effects 0.000 claims description 3
- 238000003379 elimination reaction Methods 0.000 claims description 3
- 125000003827 glycol group Chemical group 0.000 claims description 3
- 238000001727 in vivo Methods 0.000 claims description 3
- 230000002035 prolonged effect Effects 0.000 claims description 3
- 206010005003 Bladder 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
- KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 claims description 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 2
- 208000005450 Maxillary Sinus Neoplasms Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 2
- 229940127093 camptothecin Drugs 0.000 claims description 2
- VSJKWCGYPAHWDS-FQEVSTJZSA-N camptothecin Chemical compound C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-FQEVSTJZSA-N 0.000 claims description 2
- 201000010881 cervical cancer Diseases 0.000 claims description 2
- VSJKWCGYPAHWDS-UHFFFAOYSA-N dl-camptothecin Natural products C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)C5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-UHFFFAOYSA-N 0.000 claims description 2
- 238000010255 intramuscular injection Methods 0.000 claims description 2
- 239000007927 intramuscular injection Substances 0.000 claims description 2
- 239000007928 intraperitoneal injection Substances 0.000 claims description 2
- 238000010253 intravenous injection Methods 0.000 claims description 2
- 201000004488 maxillary sinus cancer Diseases 0.000 claims description 2
- 208000019303 maxillary sinus carcinoma Diseases 0.000 claims description 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 2
- 208000000587 small cell lung carcinoma Diseases 0.000 claims description 2
- 238000010254 subcutaneous injection Methods 0.000 claims description 2
- 239000007929 subcutaneous injection Substances 0.000 claims description 2
- 229960000303 topotecan Drugs 0.000 claims description 2
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 claims description 2
- 230000004614 tumor growth Effects 0.000 claims description 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
- JAADFXYIZKIKMN-UHFFFAOYSA-N CCc1c(CN(C2=CC(C34CC3)=C3COC4=O)C3=O)c2nc(cc2)c1cc2OC(N(CC1)CCC1N1CCCCC1)=O Chemical compound CCc1c(CN(C2=CC(C34CC3)=C3COC4=O)C3=O)c2nc(cc2)c1cc2OC(N(CC1)CCC1N1CCCCC1)=O JAADFXYIZKIKMN-UHFFFAOYSA-N 0.000 description 6
- 150000001875 compounds Chemical class 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US9951608P | 2008-09-23 | 2008-09-23 | |
| US61/099,516 | 2008-09-23 | ||
| US10693108P | 2008-10-20 | 2008-10-20 | |
| US61/106,931 | 2008-10-20 | ||
| US17343309P | 2009-04-28 | 2009-04-28 | |
| US61/173,433 | 2009-04-28 | ||
| PCT/US2009/005284 WO2010036335A1 (en) | 2008-09-23 | 2009-09-23 | Compositions and methods for achieving sustained therapeutic drug concentrations in a subject |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014232556A Division JP6076317B2 (ja) | 2008-09-23 | 2014-11-17 | 対象において持続的治療薬濃度を実現するための組成物及び方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012503602A JP2012503602A (ja) | 2012-02-09 |
| JP2012503602A5 true JP2012503602A5 (cg-RX-API-DMAC7.html) | 2012-08-23 |
Family
ID=41268391
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011527834A Withdrawn JP2012503602A (ja) | 2008-09-23 | 2009-09-23 | 対象において持続的治療薬濃度を実現するための組成物及び方法 |
| JP2014232556A Active JP6076317B2 (ja) | 2008-09-23 | 2014-11-17 | 対象において持続的治療薬濃度を実現するための組成物及び方法 |
| JP2016186670A Withdrawn JP2016216510A (ja) | 2008-09-23 | 2016-09-26 | 対象において持続的治療薬濃度を実現するための組成物及び方法 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014232556A Active JP6076317B2 (ja) | 2008-09-23 | 2014-11-17 | 対象において持続的治療薬濃度を実現するための組成物及び方法 |
| JP2016186670A Withdrawn JP2016216510A (ja) | 2008-09-23 | 2016-09-26 | 対象において持続的治療薬濃度を実現するための組成物及び方法 |
Country Status (21)
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2349346B1 (en) | 2008-09-23 | 2019-08-28 | Nektar Therapeutics | Method of metronomic dosing with camptothecin prodrugs (e.g. peg-irinotecan) |
| ES2779225T3 (es) * | 2011-04-08 | 2020-08-14 | Sphaera Pharma Pte Ltd | Reactivos de merilformilo sustituido y procedimiento de uso de los mismos para modificar propiedades fisicoquímicas y/o farmacocinéticas de compuestos |
| JP6284541B2 (ja) * | 2012-11-28 | 2018-02-28 | ネクター セラピューティクス | 長時間作用型トポイソメラーゼi阻害薬による乳癌治療の有効性を評価及び予測する方法 |
| CA2976912A1 (en) * | 2015-02-17 | 2016-08-25 | Mallinckrodt Llc | Modified docetaxel liposome formulations and uses thereof |
| CA3026144A1 (en) | 2016-06-02 | 2017-12-07 | Innopharmax, Inc. | Metronomic oral gemcitabine for cancer therapy |
| CN106539557A (zh) * | 2016-10-08 | 2017-03-29 | 西安交通大学 | 一种基于恒速静脉输入的药代动力学参数的测定方法 |
| AU2019344783B2 (en) | 2018-09-17 | 2025-10-23 | The Children's Hospital Of Philadelphia | Polymer-based macromolecular prodrugs |
| US20240156808A1 (en) * | 2021-02-23 | 2024-05-16 | Edison Oncology | Compositions and methods to improve the therapeutic benefit of suboptimally chemical compounds and biological therapies including substituted camptothecins such as irinotecan and topotecan for the treatment of benign and neoplastic hyperproliferative disease conditions, infections, inflammatory and immunological diseases |
| CN115317486B (zh) * | 2022-08-17 | 2024-04-19 | 南昌大学 | 一种共载紫杉醇和伊立替康前药纳米制剂及其制备方法 |
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| US5614549A (en) | 1992-08-21 | 1997-03-25 | Enzon, Inc. | High molecular weight polymer-based prodrugs |
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| US5965566A (en) | 1993-10-20 | 1999-10-12 | Enzon, Inc. | High molecular weight polymer-based prodrugs |
| US5919455A (en) | 1993-10-27 | 1999-07-06 | Enzon, Inc. | Non-antigenic branched polymer conjugates |
| US5605976A (en) | 1995-05-15 | 1997-02-25 | Enzon, Inc. | Method of preparing polyalkylene oxide carboxylic acids |
| TW438775B (en) | 1995-04-07 | 2001-06-07 | Pharmacia & Upjohn Co Llc | Novel intermediates and process for the manufacture of camptothecin derivatives (CPT-11) and related compounds |
| US5726181A (en) | 1995-06-05 | 1998-03-10 | Bionumerik Pharmaceuticals, Inc. | Formulations and compositions of poorly water soluble camptothecin derivatives |
| SG50747A1 (en) | 1995-08-02 | 1998-07-20 | Tanabe Seiyaku Co | Comptothecin derivatives |
| ATE314843T1 (de) | 1996-03-12 | 2006-02-15 | Pg Txl Co Lp | Wasserlösliche paclitaxel-prodrogen |
| US6011042A (en) | 1997-10-10 | 2000-01-04 | Enzon, Inc. | Acyl polymeric derivatives of aromatic hydroxyl-containing compounds |
| US6111107A (en) | 1997-11-20 | 2000-08-29 | Enzon, Inc. | High yield method for stereoselective acylation of tertiary alcohols |
| US6153655A (en) | 1998-04-17 | 2000-11-28 | Enzon, Inc. | Terminally-branched polymeric linkers and polymeric conjugates containing the same |
| JP2002542304A (ja) | 1999-04-28 | 2002-12-10 | ベクトレイムド インコーポレイテッド | 酵素的に活性化された重合薬物接合体 |
| WO2000066125A1 (en) | 1999-04-29 | 2000-11-09 | Aventis Pharma S.A. | Method for treating cancer using camptothecin derivatives and 5-fluorouracil |
| JP4861586B2 (ja) | 1999-12-22 | 2012-01-25 | ネクター セラピューティックス | 水溶性ポリマーの立体的に妨害される誘導体 |
| WO2001062299A2 (en) | 2000-02-28 | 2001-08-30 | Shearwater Corporation | Water-soluble polymer conjugates of artelinic acid |
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| TWI246524B (en) | 2001-01-19 | 2006-01-01 | Shearwater Corp | Multi-arm block copolymers as drug delivery vehicles |
| US7401013B2 (en) | 2001-10-15 | 2008-07-15 | Lockheed Martin Corporation | Method to optimize test data |
| EP1441772A2 (en) | 2001-10-29 | 2004-08-04 | Nektar Therapeutics Al, Corporation | Polymer conjugates of protein kinase c inhibitors |
| CA2464346A1 (en) | 2001-10-30 | 2003-05-08 | Nektar Therapeutics Al, Corporation | Water-soluble polymer conjugates of retinoic acid |
| AU2002346686A1 (en) * | 2001-12-07 | 2003-06-23 | Intermune, Inc. | Compositions and method for treating hepatitis virus infection |
| US6608076B1 (en) | 2002-05-16 | 2003-08-19 | Enzon, Inc. | Camptothecin derivatives and polymeric conjugates thereof |
| BR0312685A (pt) | 2002-06-06 | 2005-09-06 | Univ Washington | Métodos de utilização de compostos do tipo artemisinina para prevenir ou retardar o aparecimento de cancêr |
| US7122189B2 (en) | 2002-08-13 | 2006-10-17 | Enzon, Inc. | Releasable polymeric conjugates based on aliphatic biodegradable linkers |
| EP1534340B1 (en) | 2002-09-06 | 2011-11-16 | Cerulean Pharma Inc. | Cyclodextrin-based polymers for delivering the therapeutic agents covalently bound thereto |
| US8394365B2 (en) | 2003-09-17 | 2013-03-12 | Nektar Therapeutics | Multi-arm polymer prodrugs |
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| US7462627B2 (en) * | 2006-02-09 | 2008-12-09 | Enzon Pharmaceuticals, Inc. | Multi-arm polymeric conjugates of 7-ethyl-10-hydroxycamptothecin for treatment of breast, colorectal, pancreatic, ovarian and lung cancers |
| CN101421282B (zh) * | 2006-02-17 | 2013-08-14 | 俄勒冈州由俄勒冈州立大学代表高等教育委员会行使 | 用长春花生物碱n-氧化物和类似物治疗过度增殖性疾病 |
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| EP2349346B1 (en) | 2008-09-23 | 2019-08-28 | Nektar Therapeutics | Method of metronomic dosing with camptothecin prodrugs (e.g. peg-irinotecan) |
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2009
- 2009-09-23 EP EP09789364.8A patent/EP2349346B1/en active Active
- 2009-09-23 JP JP2011527834A patent/JP2012503602A/ja not_active Withdrawn
- 2009-09-23 AU AU2009297091A patent/AU2009297091B2/en active Active
- 2009-09-23 PL PL09789364T patent/PL2349346T3/pl unknown
- 2009-09-23 CN CN2009801371326A patent/CN102164617A/zh active Pending
- 2009-09-23 US US13/120,551 patent/US8906353B2/en active Active
- 2009-09-23 KR KR1020117005982A patent/KR20110063457A/ko not_active Ceased
- 2009-09-23 HR HRP20192120TT patent/HRP20192120T1/hr unknown
- 2009-09-23 WO PCT/US2009/005284 patent/WO2010036335A1/en not_active Ceased
- 2009-09-23 ES ES09789364T patent/ES2744975T3/es active Active
- 2009-09-23 SM SM20190609T patent/SMT201900609T1/it unknown
- 2009-09-23 LT LTEP09789364.8T patent/LT2349346T/lt unknown
- 2009-09-23 PT PT97893648T patent/PT2349346T/pt unknown
- 2009-09-23 MX MX2011003063A patent/MX2011003063A/es active IP Right Grant
- 2009-09-23 DK DK09789364.8T patent/DK2349346T3/da active
- 2009-09-23 SI SI200932010T patent/SI2349346T1/sl unknown
- 2009-09-23 HU HUE09789364A patent/HUE047352T2/hu unknown
- 2009-09-23 RS RS20191501A patent/RS59607B1/sr unknown
- 2009-09-23 CA CA2736939A patent/CA2736939C/en active Active
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2011
- 2011-03-23 IL IL211888A patent/IL211888A/en active IP Right Grant
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2014
- 2014-11-17 JP JP2014232556A patent/JP6076317B2/ja active Active
- 2014-11-26 US US14/555,440 patent/US9801873B2/en active Active
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2016
- 2016-09-26 JP JP2016186670A patent/JP2016216510A/ja not_active Withdrawn
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2017
- 2017-10-03 US US15/723,981 patent/US10525051B2/en active Active
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2019
- 2019-09-17 CY CY20191100970T patent/CY1122208T1/el unknown