Design, synthesis and evaluation of anti-CD38 antibody drug conjugate based on Daratumumab and maytansinoid.
Bioorg Med Chem
; 27(3): 479-482, 2019 02 01.
Article
em En
| MEDLINE
| ID: mdl-30594452
ABSTRACT
Daratumumab, an FDA approved antibody drug, displays specific targeting ability to abnormal white blood cells overexpressing CD38 and provides efficacious therapy for multiple myeloma. Here, in order to achieve enhanced remission of multiple myeloma, we designed Dara-DM4, antibody drug conjugates (ADCs) by conjugating Daratumumab and DM4 via a disulfide linker. Dara-DM4 showed significantly higher cellular uptake and inhibitory efficacy on MM1S cells that overexpressing CD38 with an IC50 of 0.88⯵g/mL post 72â¯hr treatment. These results support a promising ADCs strategy for multiple myeloma treatment.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Desenho de Fármacos
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Imunoconjugados
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Maitansina
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Anticorpos Monoclonais
Limite:
Humans
Idioma:
En
Ano de publicação:
2019
Tipo de documento:
Article