WO2004004639A2 - A novel stable formulation - Google Patents
A novel stable formulation Download PDFInfo
- Publication number
- WO2004004639A2 WO2004004639A2 PCT/US2003/020751 US0320751W WO2004004639A2 WO 2004004639 A2 WO2004004639 A2 WO 2004004639A2 US 0320751 W US0320751 W US 0320751W WO 2004004639 A2 WO2004004639 A2 WO 2004004639A2
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- formulation
- antibody
- protein
- dml
- succinic acid
- Prior art date
Links
Classifications
-
- 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
- A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6835—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6849—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a receptor, a cell surface antigen or a cell surface determinant
-
- 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
- A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
- A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
Definitions
- proteins are larger and more complex than traditional organic and inorganic drugs (i.e. possessing multiple functional groups in addition to complex three-dimensional structures), the formulation of such proteins poses special problems.
- a formulation must preserve intact the conformational integrity of at least a core sequence of the protein's amino acids while at the same time protecting the protein's multiple functional groups from degradation.
- Degradation pathways for proteins can involve chemical instability (i.e. any process which involves modification of the protein by bond formation or cleavage resulting in a new chemical entity) or physical instability (i.e. changes in the higher order structure of the protein).
- a stable frozen formulation for monoclonal antibody C242 comprised of the monoclonal antibody protein (concentration range -1-30 mg/mL) in a buffer maintaining the pH in the range of -5.8-6.5 (50 mM succinic acid, pH 6.0), and containing sucrose (-5% w/v).
- a protein "retains its chemical stability" in a pharmaceutical formulation, if the chemical stability at a given time is such that the protein is considered to still retain its biological activity as defined below.
- Chemical stability can be assessed by detecting and quantifying chemically altered forms of the protein.
- Chemical alteration may involve size modification (e.g. clipping) which can be evaluated using size exclusion chromatography, SDS-PAGE and/or matrix-assisted laser desorption ionization/time-of-flight mass spectrometry (MALDI/TOF MS), for example.
- Other types of chemical alteration include charge alteration (e.g. occurring as a result of deamidation) which can be evaluated by ion-exchange chromatography, for example.
- An antibody "retains its biological activity" in a pharmaceutical formulation, if the biological activity of the antibody at a given time is within about 20% (within the errors of the assay) of the biological activity exhibited at the time the pharmaceutical formulation was prepared as determined in an antigen binding assay, for example.
- a surfactant can also be added to the ⁇ «C242-DMl formulation.
- exemplary surfactants include nonionic surfactants such as polysorbates (e.g. polysorbates 20, 80 etc) or poloxamers (e.g. poloxamer 188).
- the amount of surfactant added is such that it reduces aggregation of the formulated immunoconjugate and/or minimizes the formation of particulates in the formulation and/or reduces adsorption.
- the surfactant may be present in the formulation in an amount from about 0.001% to about 0.5%, preferably from about 0.005% to about 0.2% and most preferably from about 0.01% to about 0.1%.
- Pluronic F68 can also be concieved in case where a solution dosage form was desired.
Abstract
Description
Claims
Priority Applications (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US10/519,033 US20060246060A1 (en) | 2002-07-02 | 2003-07-02 | Novel stable formulation |
EP03763089A EP1539239A4 (en) | 2002-07-02 | 2003-07-02 | A novel stable formulation |
NZ537610A NZ537610A (en) | 2002-07-02 | 2003-07-02 | Stable formulations of the C242 antibody |
AU2003247686A AU2003247686A1 (en) | 2002-07-02 | 2003-07-02 | A novel stable formulation |
JP2004519737A JP2005532395A (en) | 2002-07-02 | 2003-07-02 | New stable formulation |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US39318902P | 2002-07-02 | 2002-07-02 | |
US60/393,189 | 2002-07-02 |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2004004639A2 true WO2004004639A2 (en) | 2004-01-15 |
WO2004004639A3 WO2004004639A3 (en) | 2004-04-01 |
Family
ID=30115555
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/US2003/020751 WO2004004639A2 (en) | 2002-07-02 | 2003-07-02 | A novel stable formulation |
Country Status (6)
Country | Link |
---|---|
US (1) | US20060246060A1 (en) |
EP (1) | EP1539239A4 (en) |
JP (1) | JP2005532395A (en) |
AU (1) | AU2003247686A1 (en) |
NZ (1) | NZ537610A (en) |
WO (1) | WO2004004639A2 (en) |
Cited By (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1917030A2 (en) * | 2005-08-03 | 2008-05-07 | Immunogen, Inc. | Immunoconjugate formulations |
EP2069379A2 (en) * | 2006-10-31 | 2009-06-17 | Immunogen, Inc. | Methods for improving antibody production |
US7705132B2 (en) | 2006-10-20 | 2010-04-27 | Amgen Inc. | Stable polypeptide formulations |
EP2371388A2 (en) | 2004-10-20 | 2011-10-05 | Genentech, Inc. | Antibody formulations |
AU2011201150B2 (en) * | 2003-05-14 | 2013-10-10 | Immunogen, Inc. | Drug conjugate composition |
US8858935B2 (en) | 2005-05-19 | 2014-10-14 | Amgen Inc. | Compositions and methods for increasing the stability of antibodies |
WO2015075201A1 (en) | 2013-11-21 | 2015-05-28 | Genmab A/S | Antibody-drug conjugate lyophilised formulation |
WO2017121867A1 (en) | 2016-01-13 | 2017-07-20 | Genmab A/S | Formulation for antibody and drug conjugate thereof |
WO2018158716A1 (en) | 2017-03-02 | 2018-09-07 | Cadila Healthcare Limited | Novel protein drug conjugate formulation |
WO2019039483A1 (en) | 2017-08-23 | 2019-02-28 | 第一三共株式会社 | Antibody-drug conjugate preparation and lyophilization for same |
US10647779B2 (en) | 2009-04-29 | 2020-05-12 | Bayer Intellectual Property Gmbh | Anti-mesothelin immunoconjugates and uses therefor |
WO2020234114A1 (en) | 2019-05-21 | 2020-11-26 | Bayer Aktiengesellschaft | A novel stable high concentration formulation for anetumab ravtansine |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2853551B1 (en) * | 2003-04-09 | 2006-08-04 | Lab Francais Du Fractionnement | STABILIZING FORMULATION FOR IMMUNOGLOBULIN G COMPOSITIONS IN LIQUID FORM AND LYOPHILIZED FORM |
WO2009131553A2 (en) | 2006-12-29 | 2009-10-29 | Osteogenex Inc. | Methods of altering bone growth by administration of sost or wise antagonist or agonist |
MX2021009851A (en) | 2019-02-18 | 2021-09-10 | Lilly Co Eli | Therapeutic antibody formulation. |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SE9102074D0 (en) * | 1991-07-03 | 1991-07-03 | Kabi Pharmacia Ab | TOMOUR ANTIGEN SPECIFIC ANTIBODY |
CA2226575C (en) * | 1995-07-27 | 2011-10-18 | Genentech, Inc. | Stabile isotonic lyophilized protein formulation |
US6171586B1 (en) * | 1997-06-13 | 2001-01-09 | Genentech, Inc. | Antibody formulation |
EP2266607A3 (en) * | 1999-10-01 | 2011-04-20 | Immunogen, Inc. | Immunoconjugates for treating cancer |
-
2003
- 2003-07-02 EP EP03763089A patent/EP1539239A4/en not_active Withdrawn
- 2003-07-02 AU AU2003247686A patent/AU2003247686A1/en not_active Abandoned
- 2003-07-02 WO PCT/US2003/020751 patent/WO2004004639A2/en active Application Filing
- 2003-07-02 NZ NZ537610A patent/NZ537610A/en unknown
- 2003-07-02 US US10/519,033 patent/US20060246060A1/en not_active Abandoned
- 2003-07-02 JP JP2004519737A patent/JP2005532395A/en active Pending
Non-Patent Citations (2)
Title |
---|
DATABASE IMS R&D FOCUS (FILE 445) [Online] 'Cantuzumab mertansine ImmunoGen, SmithKline Beecham US FDA accepts IND', XP002973485 Retrieved from DIALOG Database accession no. 00031958 & R & D FOCUS DRUG NEWS 04 October 1999, * |
See also references of EP1539239A2 * |
Cited By (24)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU2016216585B2 (en) * | 2003-05-14 | 2017-11-23 | Immunogen, Inc. | Drug conjugate composition |
AU2014200091B2 (en) * | 2003-05-14 | 2016-05-26 | Immunogen, Inc. | Drug conjugate composition |
AU2011201150B2 (en) * | 2003-05-14 | 2013-10-10 | Immunogen, Inc. | Drug conjugate composition |
EP3498294A1 (en) | 2004-10-20 | 2019-06-19 | Genentech, Inc. | Antibody formulations |
EP2371388A2 (en) | 2004-10-20 | 2011-10-05 | Genentech, Inc. | Antibody formulations |
US8372396B2 (en) | 2004-10-20 | 2013-02-12 | Genetech, Inc. | Antibody formulations |
US9017671B2 (en) | 2004-10-20 | 2015-04-28 | Genentech, Inc. | Method of treating cancer with a pharmaceutical formulation comprising a HER2 antibody |
US8858935B2 (en) | 2005-05-19 | 2014-10-14 | Amgen Inc. | Compositions and methods for increasing the stability of antibodies |
US9114179B2 (en) | 2005-08-03 | 2015-08-25 | Immunogen, Inc. | Immunoconjugate formulations |
EP1917030A4 (en) * | 2005-08-03 | 2011-03-09 | Immunogen Inc | Immunoconjugate formulations |
EP1917030A2 (en) * | 2005-08-03 | 2008-05-07 | Immunogen, Inc. | Immunoconjugate formulations |
KR101566393B1 (en) | 2005-08-03 | 2015-11-05 | 이뮤노젠 아이엔씨 | Immunoconjugate formulations |
US8241632B2 (en) | 2006-10-20 | 2012-08-14 | Amgen Inc. | Stable polypeptide formulations |
US7705132B2 (en) | 2006-10-20 | 2010-04-27 | Amgen Inc. | Stable polypeptide formulations |
EP2069379A4 (en) * | 2006-10-31 | 2011-02-16 | Immunogen Inc | Methods for improving antibody production |
EP2069379A2 (en) * | 2006-10-31 | 2009-06-17 | Immunogen, Inc. | Methods for improving antibody production |
US10647779B2 (en) | 2009-04-29 | 2020-05-12 | Bayer Intellectual Property Gmbh | Anti-mesothelin immunoconjugates and uses therefor |
US10781263B2 (en) | 2009-04-29 | 2020-09-22 | Bayer Intellectual Property Gmbh | Anti-mesothelin immunoconjugates and uses therefor |
WO2015075201A1 (en) | 2013-11-21 | 2015-05-28 | Genmab A/S | Antibody-drug conjugate lyophilised formulation |
WO2017121867A1 (en) | 2016-01-13 | 2017-07-20 | Genmab A/S | Formulation for antibody and drug conjugate thereof |
WO2018158716A1 (en) | 2017-03-02 | 2018-09-07 | Cadila Healthcare Limited | Novel protein drug conjugate formulation |
WO2019039483A1 (en) | 2017-08-23 | 2019-02-28 | 第一三共株式会社 | Antibody-drug conjugate preparation and lyophilization for same |
KR20200044044A (en) | 2017-08-23 | 2020-04-28 | 다이이찌 산쿄 가부시키가이샤 | Antibody-drug conjugate preparation and freeze-drying method thereof |
WO2020234114A1 (en) | 2019-05-21 | 2020-11-26 | Bayer Aktiengesellschaft | A novel stable high concentration formulation for anetumab ravtansine |
Also Published As
Publication number | Publication date |
---|---|
US20060246060A1 (en) | 2006-11-02 |
NZ537610A (en) | 2006-07-28 |
EP1539239A2 (en) | 2005-06-15 |
WO2004004639A3 (en) | 2004-04-01 |
EP1539239A4 (en) | 2005-09-14 |
AU2003247686A1 (en) | 2004-01-23 |
JP2005532395A (en) | 2005-10-27 |
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