WO2004069159A3 - Vitamin receptor binding drug delivery conjugates - Google Patents

Vitamin receptor binding drug delivery conjugates Download PDF

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Publication number
WO2004069159A3
WO2004069159A3 PCT/US2004/002070 US2004002070W WO2004069159A3 WO 2004069159 A3 WO2004069159 A3 WO 2004069159A3 US 2004002070 W US2004002070 W US 2004002070W WO 2004069159 A3 WO2004069159 A3 WO 2004069159A3
Authority
WO
WIPO (PCT)
Prior art keywords
receptor binding
vitamin receptor
drug delivery
drug
vitamin
Prior art date
Application number
PCT/US2004/002070
Other languages
French (fr)
Other versions
WO2004069159A2 (en
Inventor
Iontcho Radoslavov Vlahov
Christopher Paul Leamon
Matthew A Parker
Stephen J Howard
Hari Krishna Santhapuram
Apparao Satyam
Joseph Anand Reddy
Original Assignee
Endocyte Inc
Iontcho Radoslavov Vlahov
Christopher Paul Leamon
Matthew A Parker
Stephen J Howard
Hari Krishna Santhapuram
Apparao Satyam
Joseph Anand Reddy
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Priority to DK04705573.6T priority Critical patent/DK1592457T3/en
Priority to ES04705573T priority patent/ES2395082T3/en
Priority to EP04705573A priority patent/EP1592457B1/en
Priority to NZ541846A priority patent/NZ541846A/en
Priority to CA2512867A priority patent/CA2512867C/en
Priority to AU2004210136A priority patent/AU2004210136C1/en
Application filed by Endocyte Inc, Iontcho Radoslavov Vlahov, Christopher Paul Leamon, Matthew A Parker, Stephen J Howard, Hari Krishna Santhapuram, Apparao Satyam, Joseph Anand Reddy filed Critical Endocyte Inc
Priority to SI200431940T priority patent/SI1592457T1/en
Priority to JP2005518938A priority patent/JP5576007B2/en
Publication of WO2004069159A2 publication Critical patent/WO2004069159A2/en
Publication of WO2004069159A3 publication Critical patent/WO2004069159A3/en
Priority to IL169469A priority patent/IL169469A/en
Priority to IL238935A priority patent/IL238935A0/en

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    • 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
    • A61K47/54—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 compound
    • A61K47/55—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 compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • 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
    • A61K47/54—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 compound
    • A61K47/55—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 compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • A61K47/551—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 compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic acid
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    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
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    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
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    • 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
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    • 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
    • A61K47/6851—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 determinant of a tumour cell
    • A—HUMAN NECESSITIES
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    • 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
    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/30—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
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    • C07K2317/55—Fab or Fab'

Abstract

The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety is a vitamin, or a vitamin receptor binding analog or a derivative thereof, and the drug includes analogs or derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) comprises one or more spacer linkers, releasable linkers, and heteroatom linkers. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.
PCT/US2004/002070 2003-01-27 2004-01-27 Vitamin receptor binding drug delivery conjugates WO2004069159A2 (en)

Priority Applications (10)

Application Number Priority Date Filing Date Title
ES04705573T ES2395082T3 (en) 2003-01-27 2004-01-27 Folate-Vinblastine Conjugate As Medicine
EP04705573A EP1592457B1 (en) 2003-01-27 2004-01-27 Folate-vinblastine conjugate as medicament
NZ541846A NZ541846A (en) 2003-01-27 2004-01-27 Vitamin receptor binding drug delivery conjugates
CA2512867A CA2512867C (en) 2003-01-27 2004-01-27 Vitamin receptor binding drug delivery conjugates
AU2004210136A AU2004210136C1 (en) 2003-01-27 2004-01-27 Vitamin receptor binding drug delivery conjugates
DK04705573.6T DK1592457T3 (en) 2003-01-27 2004-01-27 FOLATE-VINBLASTIN CONJUGATE AS MEDICINAL
SI200431940T SI1592457T1 (en) 2003-01-27 2004-01-27 Folate-vinblastine conjugate as medicament
JP2005518938A JP5576007B2 (en) 2003-01-27 2004-01-27 Vitamin receptor binding drug delivery conjugates
IL169469A IL169469A (en) 2003-01-27 2005-06-30 Folic acid derivatives containing disulfide linkers, pharmaceutical compositions comprising them and uses thereof
IL238935A IL238935A0 (en) 2003-01-27 2015-05-21 Vitamin receptor binding drug delivery conjugates

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US44284503P 2003-01-27 2003-01-27
US60/442,845 2003-01-27
US49211903P 2003-08-01 2003-08-01
US60/492,119 2003-08-01
US51618803P 2003-10-31 2003-10-31
US60/516,188 2003-10-31

Publications (2)

Publication Number Publication Date
WO2004069159A2 WO2004069159A2 (en) 2004-08-19
WO2004069159A3 true WO2004069159A3 (en) 2005-06-16

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2004/002070 WO2004069159A2 (en) 2003-01-27 2004-01-27 Vitamin receptor binding drug delivery conjugates

Country Status (14)

Country Link
US (6) US7601332B2 (en)
EP (4) EP2529758A3 (en)
JP (4) JP5576007B2 (en)
AR (1) AR042942A1 (en)
AU (1) AU2004210136C1 (en)
CA (1) CA2512867C (en)
CY (1) CY1113258T1 (en)
DK (1) DK1592457T3 (en)
ES (1) ES2395082T3 (en)
IL (2) IL169469A (en)
NZ (1) NZ541846A (en)
PT (1) PT1592457E (en)
TW (3) TWI492750B (en)
WO (1) WO2004069159A2 (en)

Cited By (12)

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US8795633B2 (en) 2005-09-23 2014-08-05 Purdue Research Foundation Multiphoton in vivo flow cytometry method and device
US8858914B2 (en) 2002-02-07 2014-10-14 Endocyte, Inc. Folate targeted enhanced tumor and folate receptor positive tissue optical imaging technology
US8907058B2 (en) 2007-08-17 2014-12-09 Purdue Research Foundation PSMA binding ligand-linker conjugates and methods for using
US8916167B2 (en) 2001-05-02 2014-12-23 Purdue Research Foundation Treatment and diagnosis of macrophage mediated disease
US8961926B2 (en) 2007-05-25 2015-02-24 Purdue Research Foundation Method of imaging localized infections
US9138484B2 (en) 2007-06-25 2015-09-22 Endocyte, Inc. Conjugates containing hydrophilic spacer linkers
US9180215B2 (en) 2007-02-07 2015-11-10 Purdue Research Foundation Positron emission tomography imaging method
US9187521B2 (en) 2007-10-25 2015-11-17 Endocyte, Inc. Tubulysins and processes for preparing
US9505747B2 (en) 2012-03-29 2016-11-29 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
US9550734B2 (en) 2004-07-23 2017-01-24 Endocyte, Inc. Bivalent linkers and conjugates thereof
US9555139B2 (en) 2007-03-14 2017-01-31 Endocyte, Inc. Binding ligand linked drug delivery conjugates of tubulysins
US9572886B2 (en) 2005-12-22 2017-02-21 Nitto Denko Corporation Agent for treating myelofibrosis

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Publication number Priority date Publication date Assignee Title
CN1441676B (en) 2000-03-31 2012-08-22 普渡研究基金会 Method of treatment using ligand-immunogen conjugates
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