Drug intelligence / Profile preview

gefitinib + erlotinib

Development stage
Unknown
Lead developer
Sichuan Provincial People's Hospital
Modality
Small Molecules
Administration
Oral
01

Overview

gefitinib + erlotinib-Sichuan Provincial People's Hospital refers to a treatment regimen evaluated in the Phase III SINDAS trial (NCT02893332) led by Sichuan Provincial People's Hospital. This regimen involves the administration of first-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs), specifically gefitinib or erlotinib, for the treatment of newly diagnosed EGFR-mutated oligometastatic stage IV non-small cell lung cancer (NSCLC). These small molecules function by competitively binding to the adenosine triphosphate (ATP) binding site of the EGFR tyrosine kinase domain, thereby inhibiting the autophosphorylation of the receptor and blocking downstream signaling pathways such as PI3K/Akt, MAPK/ERK, and JAK/STAT that promote tumor cell growth and survival. The SINDAS trial specifically investigated the efficacy of these TKIs when combined with consolidative stereotactic body radiation therapy (SBRT) compared to TKI monotherapy, demonstrating improved progression-free and overall survival in the combination arm.

Brand names
IressaTarceva
Other names
gefitiniberlotinibSINDAS regimen
02

Targets

CYP1A2 (Cytochrome P450 1A2)UGT1A7 (UDP-glucuronosyltransferase 1A7)UGT1A4 (UDP-glucuronosyltransferase 1A4)UGT2B7 (UDP-glucuronosyltransferase 2B7)UGT1A10 (UDP-glucuronosyltransferase family 1 member A10)UGT1A9 (UDP-glucuronosyltransferase 1A9)ABCG2 (Breast cancer resistance protein)CYP3A4 (Cytochrome P450 3A4)EGFR (Epidermal growth factor receptor)IL-1 (IL-1 family)UGT1A1 (UDP-glucuronosyltransferase 1A1)ABCB1 (P-glycoprotein)

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