Drug intelligence / Profile preview

afatinib + loperamide

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

Overview

Afatinib + loperamide is a non-fixed combination therapy used in the management of non-small cell lung cancer (NSCLC) where afatinib, an irreversible ErbB family blocker and epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, is administered as an anticancer agent. Loperamide, a peripherally acting μ-opioid receptor agonist, is co-administered to manage or prevent diarrhea—a common and sometimes severe adverse effect of afatinib therapy. Afatinib inhibits EGFR signaling pathways involved in tumor proliferation and survival. Loperamide acts on intestinal opioid receptors to reduce gut motility and fluid secretion without central nervous system effects at recommended doses. This combination does not represent a single pharmaceutical product but rather a clinical practice approach for supportive care during cancer treatment[1][4][5][6].

Brand names
Gilotrif (afatinib)Imodium (loperamide)
Other names
afatinib and loperamide combinationafatinib plus loperamide
02

Targets

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

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