Drug intelligence / Profile preview

erlotinib + tosedostat

Development stage
Discontinued
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

Erlotinib + tosedostat is an experimental combination therapy consisting of two small molecule drugs with distinct mechanisms of action. Erlotinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that blocks EGFR-mediated signaling pathways involved in cell proliferation and survival. Tosedostat is a first-in-class oral aminopeptidase inhibitor that disrupts protein turnover and amino acid supply in tumor cells by inhibiting the M1 family of aminopeptidases, leading to amino acid deprivation and apoptosis. The combination was investigated for potential synergistic antitumor effects in solid tumors such as non-small cell lung cancer (NSCLC), but clinical development was limited due to poor recruitment and lack of significant efficacy signals[2][4]. Both agents have been studied individually for various cancers.

02

Targets

ANPEP (Aminopeptidase N)LTA4H (Leukotriene A4 hydrolase)PSA (Puromycin-sensitive aminopeptidase)EGFR (Epidermal growth factor receptor)

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