Drug intelligence / Profile preview

lauroyl-gemcitabine

Development stage
Preclinical
Lead developer
UCLouvain
Modality
Small Molecules
Administration
Intratumoral, Implant
01

Overview

Lauroyl-gemcitabine (Gem-C12) is a lipophilic prodrug of the antimetabolite gemcitabine, synthesized by conjugating a lauroyl (dodecanoyl) fatty acid chain to the 4-N position of gemcitabine. This modification increases the lipophilicity of the drug, enhancing its membrane permeability, protecting it from enzymatic deamination by cytidine deaminase (CDA), and allowing its incorporation into lipid-based nanocarriers such as lipid nanocapsules (LNCs) or hydrogels. In preclinical studies, lauroyl-gemcitabine lipid nanocapsules (GemC12-LNC) formulated as an injectable hydrogel have been investigated for the local treatment of glioblastoma (GBM) to bypass the blood-brain barrier and delay tumor recurrence post-resection.

Other names
4-(N)-lauroyl gemcitabine4-(N)-lauroyl-gemcitabinelauroyl gemcitabine
02

Targets

DNARRM1

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