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Mipsagargin, a novel thapsigargin-based PSMA-activated prodrug: results of a first-in-man phase I clinical trial in patients with refractory, advanced or metastatic solid tumours

BACKGROUND: Mipsagargin (G-202; (8-O-(12-aminododecanoyl)-8-O-debutanoyl thapsigargin)-Asp-γ-Glu-γ-Glu-γ-GluGluOH)) is a novel thapsigargin-based targeted prodrug that is activated by PSMA-mediated cleavage of an inert masking peptide. The active moiety is an inhibitor of the sarcoplasmic/endoplasmi...

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Detalles Bibliográficos
Autores principales: Mahalingam, D, Wilding, G, Denmeade, S, Sarantopoulas, J, Cosgrove, D, Cetnar, J, Azad, N, Bruce, J, Kurman, M, Allgood, V E, Carducci, M
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4984914/
https://www.ncbi.nlm.nih.gov/pubmed/27115568
http://dx.doi.org/10.1038/bjc.2016.72