Nonclinical Development of Next-generation Site-specific HER2-targeting Antibody-drug Conjugate (ARX788) for Breast Cancer Treatment.
Animals
Antibodies, Monoclonal
/ administration & dosage
Antineoplastic Agents
/ administration & dosage
Azides
/ chemistry
Breast Neoplasms
/ drug therapy
Cell Line, Tumor
Dose-Response Relationship, Drug
Drug Stability
Female
Ferrichrome
/ chemistry
Haplorhini
Humans
Male
Mice
Oligopeptides
/ administration & dosage
Rats
Receptor, ErbB-2
/ metabolism
Treatment Outcome
Xenograft Model Antitumor Assays
Journal
Molecular cancer therapeutics
ISSN: 1538-8514
Titre abrégé: Mol Cancer Ther
Pays: United States
ID NLM: 101132535
Informations de publication
Date de publication:
09 2020
09 2020
Historique:
received:
12
07
2019
revised:
01
12
2019
accepted:
02
06
2020
pubmed:
6
6
2020
medline:
29
6
2021
entrez:
6
6
2020
Statut:
ppublish
Résumé
Conventional antibody-drug conjugates (ADC) utilize native surface-exposed lysines or cysteines on the antibody of interest to conjugate cytotoxic payload. The nonspecific conjugation results in a mixture with variable drug-to-antibody ratios (DAR), conjugation sites, and ADCs that are often unstable in systemic circulation. ARX788 is an ADC consisting of a HER2-targeting antibody site-specifically conjugated with a potent antitubulin cytotoxic drug-linker, AS269. The site-specific conjugation is achieved by first incorporating the nonnatural amino acid,
Identifiants
pubmed: 32499302
pii: 1535-7163.MCT-19-0692
doi: 10.1158/1535-7163.MCT-19-0692
doi:
Substances chimiques
ARX788
0
Antibodies, Monoclonal
0
Antineoplastic Agents
0
Azides
0
Oligopeptides
0
p-azidobenzoyloxyferricrocin
0
Ferrichrome
15630-64-5
ERBB2 protein, human
EC 2.7.10.1
Receptor, ErbB-2
EC 2.7.10.1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
1822-1832Informations de copyright
©2020 American Association for Cancer Research.