Drug intelligence / Profile preview

larotinib + gemcitabine

Development stage
Unknown
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Larotinib + gemcitabine is a combination therapy consisting of **larotinib**, a first-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, and **gemcitabine**, a nucleoside analog antimetabolite. Larotinib inhibits EGFR tyrosine kinase activity, blocking downstream signaling involved in cell proliferation and survival[6]. Gemcitabine incorporates into DNA and inhibits DNA synthesis, leading to apoptosis and cell cycle arrest. The combination is designed to target malignancies (notably advanced cancers with EGFR overexpression or amplification), aiming for synergistic anti-tumor effects such as increased apoptosis and cell cycle arrest. Preclinical models indicate enhanced apoptosis and G0/G1 arrest in cancer cells when these agents are combined, and larotinib is under investigation for esophageal squamous cell carcinoma; combination with gemcitabine has not reached regulatory approval[3][6].

02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)DNARNR (Ribonucleotide reductase)

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