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1. WO2010096838 - PROPROTEINS AND METHODS OF USE THEREOF

Publication Number WO/2010/096838
Publication Date 26.08.2010
International Application No. PCT/US2010/025121
International Filing Date 23.02.2010
IPC
A01N 37/18 2006.01
AHUMAN NECESSITIES
01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
37Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
18containing the group -CO-N, e.g. carboxylic acid amides or imides; Thio-analogues thereof
A61K 38/10 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
10Peptides having 12 to 20 amino acids
CPC
A61K 38/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
A61K 47/64
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
62the modifying agent being a protein, peptide or polyamino acid
64Drug-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
A61K 47/65
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
62the modifying agent being a protein, peptide or polyamino acid
65Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
A61P 1/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 31/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
14for RNA viruses
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
Applicants
  • CYTOMX THERAPEUTICS, INC. (AllExceptUS)
  • STAGLIANO, Nancy, E. [US]/[US] (UsOnly)
  • WEST, James, W. [US]/[US] (UsOnly)
  • KAMATH, Kathryn [US]/[US] (UsOnly)
  • BESSETTE, Paul, H. [US]/[US] (UsOnly)
  • SAGERT, Jason [US]/[US] (UsOnly)
Inventors
  • STAGLIANO, Nancy, E.
  • WEST, James, W.
  • KAMATH, Kathryn
  • BESSETTE, Paul, H.
  • SAGERT, Jason
Agents
  • ELRIFI, Ivor
Priority Data
61/154,73023.02.2009US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PROPROTEINS AND METHODS OF USE THEREOF
(FR) PROPROTÉINES ET LEURS PROCÉDÉS D'UTILISATION
Abstract
(EN)
The present disclosure provides for proprotein and activatable proprotein compositions. A proprotein contains a functional protein (i.e. a full length protein or functional fragment thereof) which is coupled to a peptide mask that inhibits the binding of the functional protein to its target or binding partner. An activatable proprotein contains a functional protein coupled to a peptide mask, and further coupled to an activatable linker, wherein in an non-activated state, the peptide mask inhibits binding of the functional protein to its target or binding partner and in an activated state the peptide mask does not inhibit binding of the functional protein to its target or binding partner. Proproteins can provide for reduced toxicity and adverse side effects that could otherwise result from binding of a functional protein at non-treatment sites if it were not inhibited from binding its binding partner. Proproteins can further provide improved biodistribution characteristics. Proproteins containing a peptide mask can display a longer in vivo or serum half-life than the corresponding functional protein not containing a peptide mask. The disclosure further provides methods of screening for, making, and using these proproteins.
(FR)
La présente invention concerne une proprotéine et des compositions de proprotéine activable. Une proprotéine contient une protéine fonctionnelle (à savoir, une protéine pleine longueur ou un fragment fonctionnel de celle-ci) qui est reliée à un masque peptidique qui inhibe la liaison de la protéine fonctionnelle à sa cible ou à son partenaire de liaison. Une proprotéine activable contient une protéine fonctionnelle reliée à un masque peptidique et reliée en outre à un lieur activable. Dans un état non activé, le masque peptidique inhibe la liaison de la protéine fonctionnelle à sa cible ou à son partenaire de liaison, ce qui ne se produit pas lorsque le masque peptidique est dans un état activé. Les proprotéines permettent de réduire la toxicité et les effets secondaires indésirables qui pourraient autrement résulter de la liaison d'une protéine fonctionnelle à des sites non destinés au traitement si on ne l'empêchait pas de se lier à son partenaire de liaison. Les proprotéines peuvent en outre améliorer les caractéristiques de biodistribution. Les proprotéines contenant un masque peptidique peuvent afficher une demi-vie in vivo ou dans du sérum plus longue que la protéine fonctionnelle correspondante ne contenant pas de masque peptidique. L'invention concerne en outre des procédés de criblage, de fabrication et d'utilisation de ces proprotéines.
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