WO2001017568A3 - Bioconjugation in vivo to pulmonary or blood components - Google Patents

Bioconjugation in vivo to pulmonary or blood components Download PDF

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Publication number
WO2001017568A3
WO2001017568A3 PCT/IB2000/001429 IB0001429W WO0117568A3 WO 2001017568 A3 WO2001017568 A3 WO 2001017568A3 IB 0001429 W IB0001429 W IB 0001429W WO 0117568 A3 WO0117568 A3 WO 0117568A3
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WO
WIPO (PCT)
Prior art keywords
drug
vivo
therapeutic agents
bioconjugation
acid
Prior art date
Application number
PCT/IB2000/001429
Other languages
French (fr)
Other versions
WO2001017568A2 (en
Inventor
Alan M Ezrin
Angelica Fleser
Martin Robitaille
Peter G Milner
Dominique P Bridon
Original Assignee
Conjuchem Inc
Alan M Ezrin
Angelica Fleser
Martin Robitaille
Peter G Milner
Dominique P Bridon
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
Application filed by Conjuchem Inc, Alan M Ezrin, Angelica Fleser, Martin Robitaille, Peter G Milner, Dominique P Bridon filed Critical Conjuchem Inc
Priority to JP2001521356A priority Critical patent/JP2003508501A/en
Priority to EP00962766A priority patent/EP1235618A2/en
Priority to AU74406/00A priority patent/AU781380B2/en
Priority to CA002383798A priority patent/CA2383798A1/en
Publication of WO2001017568A2 publication Critical patent/WO2001017568A2/en
Publication of WO2001017568A3 publication Critical patent/WO2001017568A3/en
Priority to AU2005203768A priority patent/AU2005203768A1/en

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    • 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
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • 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
    • A61K47/62—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
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A61K47/643—Albumins, e.g. HSA, BSA, ovalbumin or a Keyhole Limpet Hemocyanin [KHL]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
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    • A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A61P5/16—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

Abstract

In order to meet these needs, the present invention is directed to therapeutic and diagnostic agents capable of forming covalent bonds to blood and pulmonary fluid proteins or other components ex vivo or in vivo. The therapeutic agents of this invention have a long duration of action for the management of disease. The invention relates to ex vivo and in vivo bioconjugation of therapeutic agents to protein (e.g. albumin), as well as an intrapulmonary in vivo bioconjugation of therapeutic agents to endogenous pulmonary fluid proteins or other components to dramatically increase the half life of the therapeutic agents and avoid the need for parenteral administration. This invention is further directed to the use of reactive chemistries including: N-hydroxy sulfosuccinimide, maleimide-benzoyl-succinimide, gamma-maleimido-butyryloxy succinimide ester, maleimidopropionic acid, isocyanate, thiolester, thionocarboxylic acid ester, imino ester, and carbodiimide anhydride. Maleimidopropionic acid is the preferred reactive chemistry, but the invention also contemplates the selection of the above and like reactive chemistries as an electrophilic moeity for bioconjugations with albumin or other proteins. Modified therapeutic agents mentioned are the anti-histamine drug loratidine or cetirizine, a hypothyroid drug, the anti-angina drug tirofiban, the anti-hypertensive drug enalapril, the anti-arrhytmic drug capobenic acid, the antidepressant drug fluoxetine, the bronchodilation drug the obromineacetamine, the antiinflammatory drug loxoprofen, the anti-thyroid deficiency drug thyroxin, and 4-anilino-1-(2-phenethyl)piperidine.
PCT/IB2000/001429 1999-09-07 2000-09-07 Bioconjugation in vivo to pulmonary or blood components WO2001017568A2 (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
JP2001521356A JP2003508501A (en) 1999-09-07 2000-09-07 Pulmonary delivery for biological binding
EP00962766A EP1235618A2 (en) 1999-09-07 2000-09-07 Bioconjugation in vivo to pulmonary or blood components
AU74406/00A AU781380B2 (en) 1999-09-07 2000-09-07 Pulmonary delivery for bioconjugation
CA002383798A CA2383798A1 (en) 1999-09-07 2000-09-07 Pulmonary delivery for bioconjugation
AU2005203768A AU2005203768A1 (en) 1999-09-07 2005-08-22 Pulmonary delivery for bioconjugation

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US15268199P 1999-09-07 1999-09-07
US60/152,681 1999-09-07

Publications (2)

Publication Number Publication Date
WO2001017568A2 WO2001017568A2 (en) 2001-03-15
WO2001017568A3 true WO2001017568A3 (en) 2002-07-11

Family

ID=22543945

Family Applications (2)

Application Number Title Priority Date Filing Date
PCT/IB2000/001427 WO2001017614A2 (en) 1999-09-07 2000-09-07 Methods and compositions containing succinimide or maleimide derivatives of antineoplastic agents
PCT/IB2000/001429 WO2001017568A2 (en) 1999-09-07 2000-09-07 Bioconjugation in vivo to pulmonary or blood components

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PCT/IB2000/001427 WO2001017614A2 (en) 1999-09-07 2000-09-07 Methods and compositions containing succinimide or maleimide derivatives of antineoplastic agents

Country Status (5)

Country Link
EP (2) EP1235618A2 (en)
JP (2) JP2003508502A (en)
AU (3) AU7440400A (en)
CA (2) CA2383798A1 (en)
WO (2) WO2001017614A2 (en)

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JP5503837B2 (en) * 2003-03-26 2014-05-28 ポール，サッドヒル Covalent binding of ligands to nucleophilic proteins induced by non-covalent bonds
DE10356346A1 (en) * 2003-11-28 2005-06-23 TransMIT Gesellschaft für Technologietransfer mbH Invention relating to the prophylaxis and therapy of diseases caused by or caused by thrombus formation
WO2005053615A2 (en) * 2003-12-01 2005-06-16 Medi-Physics, Inc. Novel differential imaging method
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JP5475992B2 (en) * 2005-08-19 2014-04-16 エンドサイト，インコーポレイテッド Multidrug ligand conjugate
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Cited By (7)

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US9440034B2 (en) 2001-05-24 2016-09-13 Alexza Pharmaceuticals, Inc. Drug condensation aerosols and kits
US8955512B2 (en) 2001-06-05 2015-02-17 Alexza Pharmaceuticals, Inc. Method of forming an aerosol for inhalation delivery
US9308208B2 (en) 2001-06-05 2016-04-12 Alexza Pharmaceuticals, Inc. Aerosol generating method and device
US9439907B2 (en) 2001-06-05 2016-09-13 Alexza Pharmaceutical, Inc. Method of forming an aerosol for inhalation delivery
US8991387B2 (en) 2003-05-21 2015-03-31 Alexza Pharmaceuticals, Inc. Self-contained heating unit and drug-supply unit employing same
US9370629B2 (en) 2003-05-21 2016-06-21 Alexza Pharmaceuticals, Inc. Self-contained heating unit and drug-supply unit employing same

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WO2001017614A3 (en) 2002-02-28
CA2383798A1 (en) 2001-03-15
WO2001017568A2 (en) 2001-03-15
AU781380B2 (en) 2005-05-19
JP2003508502A (en) 2003-03-04
AU7440400A (en) 2001-04-10
AU7440600A (en) 2001-04-10
CA2383794A1 (en) 2001-03-15
AU2005203768A1 (en) 2005-09-15
EP1212120A2 (en) 2002-06-12
JP2003508501A (en) 2003-03-04
EP1235618A2 (en) 2002-09-04

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