Drug intelligence / Profile preview

pelitinib

Development stage
Phase 2
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Pelitinib is an irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor developed primarily for the treatment of solid tumors such as non-small cell lung cancer. It acts by covalently binding to and inhibiting EGFR tyrosine kinase activity, thereby blocking downstream signaling pathways involved in tumor cell proliferation and survival. Pelitinib has also been shown to inhibit migration and invasion of hepatocellular carcinoma (HCC) cells by inducing degradation of Twist1 through inhibition of MAPK and Akt signaling pathways[6][8]. Additionally, it competitively inhibits drug efflux transporters ABCB1 and ABCG2, enhancing chemosensitivity in cancer stem-like cells[8].

Other names
EKB-569EKB569EKB 569pelitinib
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)ABCB1 (P-glycoprotein)Mpro (3C-like proteinase of SARS-CoV-2)ABCG2 (Breast cancer resistance protein)

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