DOP2011000244A - Sistemas basados en conjugados para entrega farmacologica controlada - Google Patents
Sistemas basados en conjugados para entrega farmacologica controladaInfo
- Publication number
- DOP2011000244A DOP2011000244A DO2011000244A DO2011000244A DOP2011000244A DO P2011000244 A DOP2011000244 A DO P2011000244A DO 2011000244 A DO2011000244 A DO 2011000244A DO 2011000244 A DO2011000244 A DO 2011000244A DO P2011000244 A DOP2011000244 A DO P2011000244A
- Authority
- DO
- Dominican Republic
- Prior art keywords
- certain embodiments
- saccharide
- glucose
- ligands
- conjugates
- Prior art date
Links
Classifications
-
- 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
- C07K14/575—Hormones
- C07K14/62—Insulins
-
- 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
- A61K47/61—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 the organic macromolecular compound being a polysaccharide or a derivative thereof
-
- 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
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
-
- 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
- A61K38/22—Hormones
- A61K38/28—Insulins
-
- 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
- A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- 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
- 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
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- 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
- A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K17/00—Carrier-bound or immobilised peptides; Preparation thereof
- C07K17/02—Peptides being immobilised on, or in, an organic carrier
- C07K17/10—Peptides being immobilised on, or in, an organic carrier the carrier being a carbohydrate
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Endocrinology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Zoology (AREA)
- Gastroenterology & Hepatology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Emergency Medicine (AREA)
- Toxicology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
En un aspecto, la divulgación proporciona procedimientos para la preparación de medicamentos útiles para controlar los perfiles farmacocinéticos (PK) y/o farmacodinán-iicos (PD) de insulina en una forma que es sensible a las concentraciones sistémicas de un sacárido tal como Ia glucosa. Como se discutió en los Ejemplos, se descubrió que cuando Ia insulina fuera conjugada con ligandos sacáridos de alta afinidad, pudo hacerse exhibir perfiles PKJPD que respondieran a cambios de concentración sacárida aún en ausencia de una molécula multivalente y exógena fijadora de sacáridos tal como Con A. Este hallazgo fue inesperado y proporciona una oportunidad sin precedentes para generar sistemas simples de insulina sensibles a sacáridos libres de lectina. En otro aspecto, Ia divulgacíón proporciona conjugados y procedimientos de ejemplo para la fabricación de los mismos. En general, estos conjugados incluyen un fármaco y uno o más Iigandos separados en donde cada uno incluye un sacárido. En ciertas realizaciones, los ligandos son capaces de competir con un sacárido (por ejemplo, glucosa o manosa) para unirse a una molécula fijadora de sacáridos endógenos. En ciertas realizaciones, los ligandos son capaces de competir con la glucosa o manosa por Ia unión a Con A. Como se explica en detalle más adelante, en ciertas realizaciones, los ligandos y el fármaco pueden estar covalente o no covalentemente unidos a una estructura de conjugado. En ciertas realizaciones, la estructura es no polimérica. En ciertas realizaciones, un conjugado puede tener un índice de polidíspersidad de uno y un peso molecular de menos de 20.000 Da aproxìmadamente. En ciertas realizaciones, el conjugado es de larga duración (es decir, presenta un perfil farmacocinético que es más sostenido que la insulina humana recombinante soluble o RHI). Como está discutido en detalle más adelante, se debe entender que los métodos, conjugados y formulaciones que se describen en este documento no están limitados de ninguna manera a solamente la entrega de insulina y se debe entender que pueden ser utilizados para liberar cualquier medicamento. También se debe entender que Ios métodos se pueden utilizar para Iiberar fármacos en respuesta a sacárídos diferentes de la glucosa. En partícular, como se indica en los ejemplos, se ha demostrado que los conjugados de ejemplo responden a sacáridos exógenos como el alfa- metil manosa y L- fucosa. En ciertas realizaciones, esto puede utilizarse para preparar conjugados que pueden ser controlados por la administración de uno de estos sacáridos exógenos (es decir, en lugar de o además de ser controlados por las fluctuaciones en la glucosa endógena).
Applications Claiming Priority (7)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US14787809P | 2009-01-28 | 2009-01-28 | |
US15964309P | 2009-03-12 | 2009-03-12 | |
US16210709P | 2009-03-20 | 2009-03-20 | |
US16308409P | 2009-03-25 | 2009-03-25 | |
US21989709P | 2009-06-24 | 2009-06-24 | |
US22357209P | 2009-07-07 | 2009-07-07 | |
US25285709P | 2009-10-19 | 2009-10-19 |
Publications (1)
Publication Number | Publication Date |
---|---|
DOP2011000244A true DOP2011000244A (es) | 2011-10-15 |
Family
ID=42395986
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DO2011000244A DOP2011000244A (es) | 2009-01-28 | 2011-07-28 | Sistemas basados en conjugados para entrega farmacologica controlada |
Country Status (24)
Country | Link |
---|---|
US (5) | US9050370B2 (es) |
EP (1) | EP2391218B1 (es) |
JP (3) | JP5508438B2 (es) |
KR (2) | KR101635689B1 (es) |
CN (2) | CN102365025A (es) |
AU (2) | AU2015202872B2 (es) |
BR (1) | BRPI1007457A2 (es) |
CA (2) | CA2932926C (es) |
CO (1) | CO6400173A2 (es) |
CR (1) | CR20110408A (es) |
DO (1) | DOP2011000244A (es) |
EA (1) | EA027757B1 (es) |
EC (1) | ECSP11011240A (es) |
ES (1) | ES2791683T3 (es) |
GT (1) | GT201100208A (es) |
IL (1) | IL214099A0 (es) |
MA (1) | MA33064B1 (es) |
MX (1) | MX2011007929A (es) |
NI (1) | NI201100150A (es) |
NZ (1) | NZ594248A (es) |
PE (1) | PE20120583A1 (es) |
SG (3) | SG2014006597A (es) |
TN (1) | TN2011000354A1 (es) |
WO (1) | WO2010088294A1 (es) |
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CA2932926C (en) * | 2009-01-28 | 2018-12-18 | Smartcells, Inc. | Conjugate based systems for controlled drug delivery |
US9095623B2 (en) | 2009-03-20 | 2015-08-04 | Smartcells, Inc. | Terminally-functionalized conjugates and uses thereof |
US8623345B2 (en) | 2009-03-20 | 2014-01-07 | Smartcells | Terminally-functionalized conjugates and uses thereof |
WO2012015691A2 (en) | 2010-07-28 | 2012-02-02 | Smartcells, Inc. | Recombinant lectins, binding-site modified lectins and uses thereof |
US20130131310A1 (en) * | 2010-07-28 | 2013-05-23 | John Kane | Drug-ligand conjugates, synthesis thereof, and intermediates thereto |
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US20130302825A1 (en) * | 2010-10-14 | 2013-11-14 | Merck | Uses of macrophage mannose receptor to screen compounds and uses of these compounds |
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CN108610494B (zh) * | 2018-03-20 | 2020-11-06 | 南京理工大学 | 聚醚砜/功能性含糖聚合物杂化膜的制备方法 |
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