Drug intelligence / Profile preview

afatinib + celecoxib

Development stage
Preclinical
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

Afatinib + celecoxib is an investigational combination of two small molecule drugs, afatinib and celecoxib. Afatinib is a second-generation, irreversible tyrosine kinase inhibitor (TKI) that targets the ErbB family of receptors, including EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4). It covalently binds to these receptors' kinase domains, blocking autophosphorylation and downstream signaling involved in cell proliferation—primarily used in non-small cell lung cancer (NSCLC) with EGFR mutations[1][2]. Celecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor that reduces pain and inflammation by inhibiting prostaglandin synthesis; it is approved for conditions such as osteoarthritis, rheumatoid arthritis, acute pain, ankylosing spondylitis, and primary dysmenorrhea[4]. Preclinical studies suggest that combining afatinib with celecoxib may synergistically enhance radiosensitivity in NSCLC cells by promoting apoptosis and modulating cell cycle arrest mechanisms[2].

02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)

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