Drug intelligence / Profile preview

EKB-569 + capecitabine

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

EKB-569 + capecitabine is a combination therapy under investigation for the treatment of advanced solid tumors, particularly colorectal cancer. EKB-569 (also known as pelitinib) is an oral, selective, irreversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. Capecitabine is an oral prodrug that is enzymatically converted to 5-fluorouracil (5-FU), a cytotoxic antimetabolite that inhibits DNA synthesis in rapidly dividing cells. The rationale for combining these agents lies in their complementary mechanisms—targeted inhibition of EGFR signaling by EKB-569 and direct cytotoxicity from 5-FU generated by capecitabine. Clinical studies have shown this combination can be safely administered and may increase plasma levels of 5-FU compared to capecitabine alone[1][2][3].

Other names
pelitinib + capecitabine
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)TS (Thymidylate synthase)

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