Drug intelligence / Profile preview

everolimus + gemcitabine

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Everolimus + gemcitabine is a combination of two small molecule drugs used primarily in oncology. Everolimus is an oral inhibitor of the mammalian target of rapamycin (mTOR), a serine/threonine kinase involved in cell growth, proliferation, and survival. By binding to FKBP-12 and inhibiting mTORC1 activity, everolimus blocks downstream signaling pathways that promote tumor cell cycle progression from G1 to S phase and angiogenesis[4][5]. Gemcitabine is a nucleoside analog that acts as an antimetabolite; it is phosphorylated intracellularly to active metabolites which are incorporated into DNA during replication. This incorporation leads to masked chain termination and apoptosis by preventing DNA elongation and repair[3]. The combination has shown synergistic or additive anti-tumor effects in various cancers—including pancreatic cancer, cholangiocarcinoma, bladder cancer, non-Hodgkin lymphoma, and malignant meningioma—by inducing cytostatic effects such as cellular senescence or apoptosis[2][6]. Everolimus was developed by Novartis.

02

Targets

mTOR (Mammalian target of rapamycin kinase)RNR (Ribonucleotide reductase)DNA polymerase family

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