CA2797058A1 - Conjugated blood coagulation factor viii - Google Patents
Conjugated blood coagulation factor viii Download PDFInfo
- Publication number
- CA2797058A1 CA2797058A1 CA2797058A CA2797058A CA2797058A1 CA 2797058 A1 CA2797058 A1 CA 2797058A1 CA 2797058 A CA2797058 A CA 2797058A CA 2797058 A CA2797058 A CA 2797058A CA 2797058 A1 CA2797058 A1 CA 2797058A1
- Authority
- CA
- Canada
- Prior art keywords
- fviii
- biocompatible polymer
- pharmaceutical composition
- bond
- group
- 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.)
- Pending
Links
- 102000001690 Factor VIII Human genes 0.000 title 1
- 108010054218 Factor VIII Proteins 0.000 title 1
- 102100026735 Coagulation factor VIII Human genes 0.000 claims abstract 24
- 101000911390 Homo sapiens Coagulation factor VIII Proteins 0.000 claims abstract 24
- 229920000249 biocompatible polymer Polymers 0.000 claims abstract 17
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 13
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims abstract 8
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Chemical group C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 12
- KDCGOANMDULRCW-UHFFFAOYSA-N 7H-purine Chemical group N1=CNC2=NC=NC2=C1 KDCGOANMDULRCW-UHFFFAOYSA-N 0.000 claims 8
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical group C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 8
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 8
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical group C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 8
- 238000000034 method Methods 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 125000002947 alkylene group Chemical group 0.000 claims 5
- MGADZUXDNSDTHW-UHFFFAOYSA-N 2H-pyran Chemical group C1OC=CC=C1 MGADZUXDNSDTHW-UHFFFAOYSA-N 0.000 claims 4
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical group C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 4
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical group C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 4
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical group C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 4
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 4
- 125000005647 linker group Chemical group 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 125000001624 naphthyl group Chemical group 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical group C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims 4
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Chemical group COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 3
- 230000023555 blood coagulation Effects 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 208000014674 injury Diseases 0.000 claims 3
- 229920000642 polymer Polymers 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 230000008733 trauma Effects 0.000 claims 3
- 201000003542 Factor VIII deficiency Diseases 0.000 claims 2
- 238000007259 addition reaction Methods 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 239000003153 chemical reaction reagent Substances 0.000 claims 2
- 150000007944 thiolates Chemical class 0.000 claims 2
- 208000012671 Gastrointestinal haemorrhages Diseases 0.000 claims 1
- 208000032843 Hemorrhage Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 230000021615 conjugation Effects 0.000 claims 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 1
- 235000018417 cysteine Nutrition 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 230000008030 elimination Effects 0.000 claims 1
- 238000003379 elimination reaction Methods 0.000 claims 1
- 239000000839 emulsion Substances 0.000 claims 1
- 208000030304 gastrointestinal bleeding Diseases 0.000 claims 1
- 208000002085 hemarthrosis Diseases 0.000 claims 1
- 230000005847 immunogenicity Effects 0.000 claims 1
- 238000001802 infusion Methods 0.000 claims 1
- 239000007927 intramuscular injection Substances 0.000 claims 1
- 238000010255 intramuscular injection Methods 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 208000007106 menorrhagia Diseases 0.000 claims 1
- 238000007911 parenteral administration Methods 0.000 claims 1
- 239000000243 solution Substances 0.000 claims 1
- 239000007929 subcutaneous injection Substances 0.000 claims 1
- 238000010254 subcutaneous injection Methods 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/36—Blood coagulation or fibrinolysis factors
- A61K38/37—Factors VIII
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal 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
- A61K47/51—Medicinal 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
- A61K47/56—Medicinal 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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/59—Medicinal 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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
- A61K47/60—Medicinal 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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
- A61K9/0021—Intradermal administration, e.g. through microneedle arrays, needleless injectors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/745—Blood coagulation or fibrinolysis factors
- C07K14/755—Factors VIII, e.g. factor VIII C (AHF), factor VIII Ag (VWF)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Organic Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Zoology (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Biochemistry (AREA)
- Toxicology (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Dermatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1007357.5A GB201007357D0 (en) | 2010-04-30 | 2010-04-30 | Conjugated factor VIII |
| GB1007357.5 | 2010-04-30 | ||
| PCT/GB2011/000662 WO2011135307A1 (en) | 2010-04-30 | 2011-04-28 | Conjugated blood coagulation factor viii |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2797058A1 true CA2797058A1 (en) | 2011-11-03 |
Family
ID=42289987
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2797058A Pending CA2797058A1 (en) | 2010-04-30 | 2011-04-28 | Conjugated blood coagulation factor viii |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US20130150302A1 (enExample) |
| EP (1) | EP2563402A1 (enExample) |
| JP (1) | JP5870088B2 (enExample) |
| KR (1) | KR20130055619A (enExample) |
| CN (1) | CN102939108A (enExample) |
| AP (1) | AP2012006575A0 (enExample) |
| AU (1) | AU2011247147B2 (enExample) |
| BR (1) | BR112012027590A2 (enExample) |
| CA (1) | CA2797058A1 (enExample) |
| CL (1) | CL2012003039A1 (enExample) |
| CO (1) | CO6660443A2 (enExample) |
| CR (1) | CR20120579A (enExample) |
| EA (1) | EA201290938A1 (enExample) |
| EC (1) | ECSP12012314A (enExample) |
| GB (2) | GB201007357D0 (enExample) |
| IL (1) | IL222566A (enExample) |
| MX (1) | MX2012012683A (enExample) |
| MY (1) | MY160922A (enExample) |
| NI (1) | NI201200160A (enExample) |
| NZ (1) | NZ603939A (enExample) |
| PE (1) | PE20130254A1 (enExample) |
| PH (1) | PH12012502150A1 (enExample) |
| RU (1) | RU2012144555A (enExample) |
| SG (1) | SG184906A1 (enExample) |
| WO (1) | WO2011135307A1 (enExample) |
| ZA (1) | ZA201208989B (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11351112B2 (en) | 2012-04-16 | 2022-06-07 | Cantab Biopharmaceuticals Patents Limited | Optimised subcutaneous therapeutic agents |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101557830B (zh) | 2006-12-15 | 2016-06-08 | 巴克斯特国际公司 | 具有延长的体内半衰期的因子VIIa-聚唾液酸结合物 |
| RU2595442C2 (ru) | 2009-07-27 | 2016-08-27 | Баксалта Инкорпорейтед | Конъюгаты белков свертывания крови |
| US8809501B2 (en) | 2009-07-27 | 2014-08-19 | Baxter International Inc. | Nucleophilic catalysts for oxime linkage |
| CA2769244A1 (en) | 2009-07-27 | 2011-02-03 | Lipoxen Technologies Limited | Glycopolysialylation of non-blood coagulation proteins |
| US8642737B2 (en) | 2010-07-26 | 2014-02-04 | Baxter International Inc. | Nucleophilic catalysts for oxime linkage |
| CN104530182A (zh) | 2009-07-27 | 2015-04-22 | 利普森技术有限公司 | 非凝血蛋白的糖基多唾液酸化 |
| BR112013015898A2 (pt) | 2010-12-22 | 2018-06-26 | Baxter International Inc. | derivado de ácido graxo solúvel em água, e, métodos para preparar um derivado de ácido graxo e uma proteína terapêutica conjugada. |
| GB201417589D0 (en) | 2014-10-06 | 2014-11-19 | Cantab Biopharmaceuticals Patents Ltd | Pharmaceutical Formulations |
| GB201518170D0 (en) | 2015-10-14 | 2015-11-25 | Cantab Biopharmaceuticals Patents Ltd | Colloidal particles for subcutaneous administration with intravenous administration of therapeutic agent |
| GB201518171D0 (en) | 2015-10-14 | 2015-11-25 | Cantab Biopharmaceuticals Patents Ltd | Colloidal particles for topical administration with therapeutic agent |
| GB201518172D0 (en) | 2015-10-14 | 2015-11-25 | Cantab Biopharmaceuticals Patents Ltd | Colloidal particles for use in medicine |
| KR20190086269A (ko) * | 2018-01-12 | 2019-07-22 | 재단법인 목암생명과학연구소 | 체내 지속형 재조합 당단백질 및 이의 제조방법 |
| EP3816181A4 (en) | 2018-05-18 | 2022-04-20 | Zhengzhou Gensciences Inc. | Improved fviii fusion protein and use thereof |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004075923A2 (en) * | 2003-02-26 | 2004-09-10 | Nektar Therapeutics Al, Corporation | Polymer-factor viii moiety conjugates |
| GB0316294D0 (en) | 2003-07-11 | 2003-08-13 | Polytherics Ltd | Conjugated biological molecules and their preparation |
| ES2633916T3 (es) * | 2004-11-12 | 2017-09-26 | Bayer Healthcare Llc | Modificación de FVIII dirigida al sitio |
| DK1835938T3 (da) * | 2004-12-27 | 2013-11-04 | Baxter Int | Polymer-von Willebrand-faktor-konjugater |
| JP2009532351A (ja) * | 2006-03-31 | 2009-09-10 | バクスター・インターナショナル・インコーポレイテッド | ペグ化第ｖｉｉｉ因子 |
| EP2209494B1 (en) | 2007-10-09 | 2016-07-20 | Polytherics Limited | Novel conjugated proteins and peptides |
| WO2009130602A2 (en) * | 2008-04-24 | 2009-10-29 | Celtic Pharma Peg Ltd. | Factor ix conjugates with extended half-lives |
| US8969626B2 (en) * | 2008-07-21 | 2015-03-03 | Polytherics Limited | Reagents and method for conjugating biological molecules |
| GB0912485D0 (en) * | 2009-07-17 | 2009-08-26 | Polytherics Ltd | Improved conjugation method |
-
2010
- 2010-04-30 GB GBGB1007357.5A patent/GB201007357D0/en not_active Ceased
-
2011
- 2011-04-28 BR BR112012027590A patent/BR112012027590A2/pt not_active IP Right Cessation
- 2011-04-28 AU AU2011247147A patent/AU2011247147B2/en not_active Ceased
- 2011-04-28 PE PE2012002104A patent/PE20130254A1/es not_active Application Discontinuation
- 2011-04-28 NZ NZ603939A patent/NZ603939A/xx not_active IP Right Cessation
- 2011-04-28 CN CN2011800218881A patent/CN102939108A/zh active Pending
- 2011-04-28 WO PCT/GB2011/000662 patent/WO2011135307A1/en not_active Ceased
- 2011-04-28 SG SG2012077087A patent/SG184906A1/en unknown
- 2011-04-28 MY MYPI2012004710A patent/MY160922A/en unknown
- 2011-04-28 JP JP2013506735A patent/JP5870088B2/ja not_active Expired - Fee Related
- 2011-04-28 AP AP2012006575A patent/AP2012006575A0/xx unknown
- 2011-04-28 RU RU2012144555/15A patent/RU2012144555A/ru not_active Application Discontinuation
- 2011-04-28 KR KR1020127031386A patent/KR20130055619A/ko not_active Ceased
- 2011-04-28 US US13/643,287 patent/US20130150302A1/en not_active Abandoned
- 2011-04-28 EP EP11719040A patent/EP2563402A1/en not_active Withdrawn
- 2011-04-28 PH PH1/2012/502150A patent/PH12012502150A1/en unknown
- 2011-04-28 CA CA2797058A patent/CA2797058A1/en active Pending
- 2011-04-28 GB GB201220667A patent/GB2492935B8/en not_active Expired - Fee Related
- 2011-04-28 EA EA201290938A patent/EA201290938A1/ru unknown
- 2011-04-28 MX MX2012012683A patent/MX2012012683A/es not_active Application Discontinuation
-
2012
- 2012-10-21 IL IL222566A patent/IL222566A/en not_active IP Right Cessation
- 2012-10-29 CL CL2012003039A patent/CL2012003039A1/es unknown
- 2012-10-29 NI NI201200160A patent/NI201200160A/es unknown
- 2012-11-14 CR CR20120579A patent/CR20120579A/es unknown
- 2012-11-28 ZA ZA2012/08989A patent/ZA201208989B/en unknown
- 2012-11-28 EC ECSP12012314 patent/ECSP12012314A/es unknown
- 2012-11-29 CO CO12216949A patent/CO6660443A2/es unknown
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11351112B2 (en) | 2012-04-16 | 2022-06-07 | Cantab Biopharmaceuticals Patents Limited | Optimised subcutaneous therapeutic agents |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20160215 |