Drug intelligence / Profile preview

LP-261

Development stage
Preclinical
Lead developer
Locus Technologies
Modality
Small Molecules
Administration
Oral
01

Overview

LP-261 is a small molecule tubulin modulator developed by Locus Technologies for the treatment of various cancers. It acts as an antimitotic agent by binding to the colchicine site on tubulin, which inhibits tubulin polymerization and leads to G2/M cell cycle arrest. Preclinical studies have demonstrated that LP-261 possesses potent antitumor and antiangiogenic activity across several models, including non-small-cell lung cancer, colon adenocarcinoma, and prostate cancer. A key advantage of LP-261 is its high oral bioavailability and the fact that it is not a substrate for the ABCB1 (P-glycoprotein) efflux pump, potentially allowing it to bypass common mechanisms of multidrug resistance associated with other tubulin-targeting drugs.

Other names
N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide
02

Targets

TUBB (Tubulin (alpha and beta subunits))

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