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1. WO2017136769 - PEPTIDE DRUG CONJUGATES

Publication Number WO/2017/136769
Publication Date 10.08.2017
International Application No. PCT/US2017/016575
International Filing Date 03.02.2017
IPC
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
A61K 47/6415
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
6415Toxins or lectins, e.g. clostridial toxins or Pseudomonas exotoxins
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
Applicants
  • EISAI R&D MANAGEMENT CO., LTD. [JP]/[JP]
Inventors
  • MCGONIGLE, Sharon
  • MAJUMDER, Utpal
  • CUSTAR, Daniel W.
  • WU, Jiayi
  • POSTEMA, Maarten H.D.
Agents
  • WALTERS, Todd R.
  • STEWART, Duane A., III
  • MARKOWSKI, Mythili
Priority Data
62/291,27004.02.2016US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PEPTIDE DRUG CONJUGATES
(FR) CONJUGUÉS PEPTIDES-MÉDICAMENTS
Abstract
(EN)
Embodiments provide protein-drug conjugates for treatment of cancer. Protein-drug conjugates may include protein-drug conjugates of Formula I: Ctx-L-Cp (I) or a pharmaceutically acceptable salt or solvate thereof, wherein: Ctx is chlorotoxin or a chlorotoxin analog; Cp is a cryptophycin amide, and L is a linker wherein the linker is bound to Ctx at an X2 moiety of the linker and at one of a lysine residue and the N-terminus of the chlorotoxin or chlorotoxin analog.
(FR)
Selon certains modes de réalisation, la présente invention concerne des conjugués protéines-médicaments pour le traitement du cancer. Des conjugués protéines-médicaments peuvent comprendre des conjugués protéines-médicaments de Formule I: Ctx-L-Cp (I) ou un sel ou solvate pharmaceutiquement acceptable de celui-ci, dans laquelle: Ctx est la chlorotoxine ou un analogue de chlorotoxine; Cp est un amide de cryptophycine, et L est un lieur, le lieur étant lié à Ctx au niveau d'une fraction X2 du lieur et au niveau d'un résidu lysine et de l'extrémité N-terminale de la chlorotoxine ou de l'analogue de chlorotoxine.
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