Drug intelligence / Profile preview

gemcitabine + irinotecan + thalidomide

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination chemotherapy regimen consisting of three agents—gemcitabine, irinotecan, and thalidomide—used experimentally in the treatment of advanced cancers, particularly non-small cell lung cancer (NSCLC). - **Gemcitabine** is a nucleoside analog that inhibits DNA synthesis by incorporating into DNA during replication, leading to apoptosis in rapidly dividing tumor cells. - **Irinotecan** is a topoisomerase I inhibitor that prevents DNA unwinding and replication by stabilizing the complex between topoisomerase I and DNA, resulting in double-strand breaks and cell death. - **Thalidomide** acts as an immunomodulatory and antiangiogenic agent; it inhibits angiogenesis (formation of new blood vessels) required for tumor growth and modulates immune responses. The combination has been studied in phase II clinical trials for chemonaive patients with advanced NSCLC, showing manageable toxicity profiles with some evidence of disease stabilization[1][6]. The rationale behind this regimen is to combine cytotoxic effects (from gemcitabine and irinotecan) with antiangiogenic activity (from thalidomide), potentially enhancing antitumor efficacy.

02

Targets

RNR (Ribonucleotide reductase)TOP1 (DNA Topoisomerase I)CRBN (Cereblon)

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