Drug intelligence / Profile preview

BRG399

Development stage
Preclinical
Lead developer
Berg
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

BRG399 is a novel, orally available small molecule drug developed by BPGbio for the treatment of both solid and liquid tumors. It acts as a microtubule-binding agent that disrupts cell division, leading to anti-cancer activity in vitro and in vivo. Notably, it is brain permeant and not a substrate for P-glycoprotein (Pgp), which may enhance its effectiveness against brain tumors such as glioblastoma. Preclinical studies have shown that BRG399 induces tumor regression and immune memory responses in glioblastoma models, suggesting potential to prevent tumor recurrence. Additionally, it exhibits immune-modulatory properties by altering the tumor microenvironment and reducing T cell exhaustion markers, potentially reinvigorating anti-tumor immunity. Mechanistically, it also modulates UBE2K (ubiquitin conjugating enzyme E2 K), implicating effects on protein degradation pathways relevant to cancer progression[1][2][3][4][7].

Other names
BRG-399BRG399BRG 399
02

Targets

TUBB (Tubulin (alpha and beta subunits))UBE2K (Ubiquitin-conjugating enzyme E2 K)

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