AR092098A1 - ANTICUERPOS ANTI-PCSK9 CON CARACTERISTICAS DE UNION DEPENDIENTES DEL pH - Google Patents
ANTICUERPOS ANTI-PCSK9 CON CARACTERISTICAS DE UNION DEPENDIENTES DEL pHInfo
- Publication number
- AR092098A1 AR092098A1 ARP130102853A ARP130102853A AR092098A1 AR 092098 A1 AR092098 A1 AR 092098A1 AR P130102853 A ARP130102853 A AR P130102853A AR P130102853 A ARP130102853 A AR P130102853A AR 092098 A1 AR092098 A1 AR 092098A1
- Authority
- AR
- Argentina
- Prior art keywords
- antibodies
- exhibit
- binding properties
- dependent binding
- pcsk9
- Prior art date
Links
- 230000001419 dependent effect Effects 0.000 title abstract 5
- 101710180553 Proprotein convertase subtilisin/kexin type 9 Proteins 0.000 abstract 2
- 102100038955 Proprotein convertase subtilisin/kexin type 9 Human genes 0.000 abstract 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 abstract 2
- 108010047041 Complementarity Determining Regions Proteins 0.000 abstract 1
- 230000002378 acidificating effect Effects 0.000 abstract 1
- 150000001413 amino acids Chemical class 0.000 abstract 1
- 239000000427 antigen Substances 0.000 abstract 1
- 102000036639 antigens Human genes 0.000 abstract 1
- 108091007433 antigens Proteins 0.000 abstract 1
- 235000012000 cholesterol Nutrition 0.000 abstract 1
- 208000037765 diseases and disorders Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000012634 fragment Substances 0.000 abstract 1
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 abstract 1
- 125000000487 histidyl group Chemical group [H]N([H])C(C(=O)O*)C([H])([H])C1=C([H])N([H])C([H])=N1 0.000 abstract 1
- 230000007935 neutral effect Effects 0.000 abstract 1
- 238000006467 substitution reaction Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/40—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against enzymes
-
- 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
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/20—Immunoglobulins specific features characterized by taxonomic origin
- C07K2317/21—Immunoglobulins specific features characterized by taxonomic origin from primates, e.g. man
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
- C07K2317/56—Immunoglobulins specific features characterized by immunoglobulin fragments variable (Fv) region, i.e. VH and/or VL
- C07K2317/565—Complementarity determining region [CDR]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/70—Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
- C07K2317/76—Antagonist effect on antigen, e.g. neutralization or inhibition of binding
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/90—Immunoglobulins specific features characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
- C07K2317/92—Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/90—Immunoglobulins specific features characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
- C07K2317/94—Stability, e.g. half-life, pH, temperature or enzyme-resistance
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Immunology (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Obesity (AREA)
- General Chemical & Material Sciences (AREA)
- Peptides Or Proteins (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Abstract
La presente proporciona anticuerpos y fragmentos de unión a antígeno de los mismos que específicamente se unen a proproteína convertasa subtilisina/kexina tipo 9 (PCSK9) con mayor afinidad a pH neutro que a pH ácido. Los anticuerpos de la presente pueden poseer uno o más cambios de aminoácidos en comparación con los anticuerpos que no presentan propiedades de unión dependientes del pH. Por ejemplo, la presente incluye anticuerpos anti-PCSK9 que poseen una o más sustituciones de histidina en una o más regiones determinantes de la complementariedad. Los anticuerpos de la presente, con propiedades de unión dependientes del pH, permanecen en la circulación y exhiben actividad reductora del colesterol en sujetos animales durante períodos de tiempo prolongados en comparación con los anticuerpos anti-PCSK9 que no presentan propiedades de unión dependientes del pH. Por lo tanto, los anticuerpos de la presente son útiles para el tratamiento de enfermedades y trastornos relacionados con concentraciones elevadas de colesterol HDL, por lo que los anticuerpos de la presente se pueden administrar a un paciente en dosis más bajas y/o con menos frecuencia en comparación con los anticuerpos que no exhiben propiedades de unión dependientes del pH.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261682349P | 2012-08-13 | 2012-08-13 | |
| US201261703342P | 2012-09-20 | 2012-09-20 | |
| US201261734398P | 2012-12-07 | 2012-12-07 | |
| US201361761383P | 2013-02-06 | 2013-02-06 | |
| US201361828258P | 2013-05-29 | 2013-05-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR092098A1 true AR092098A1 (es) | 2015-03-25 |
Family
ID=50066319
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130102853A AR092098A1 (es) | 2012-08-13 | 2013-08-12 | ANTICUERPOS ANTI-PCSK9 CON CARACTERISTICAS DE UNION DEPENDIENTES DEL pH |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US9540449B2 (es) |
| EP (1) | EP2882778B1 (es) |
| JP (1) | JP6309521B2 (es) |
| KR (1) | KR20150041662A (es) |
| CN (1) | CN104540852B (es) |
| AR (1) | AR092098A1 (es) |
| AU (1) | AU2013302925B2 (es) |
| CA (1) | CA2881679C (es) |
| EA (1) | EA028244B1 (es) |
| IL (1) | IL236785B (es) |
| MX (1) | MX363213B (es) |
| NZ (1) | NZ704771A (es) |
| TW (1) | TWI596115B (es) |
| UY (1) | UY34975A (es) |
| WO (1) | WO2014028354A1 (es) |
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| CN104540852A (zh) | 2015-04-22 |
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| US20140044730A1 (en) | 2014-02-13 |
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