Drug intelligence / Profile preview

EC1169

Development stage
Phase 1
Lead developer
Novartis
Modality
Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

EC1169 is an investigational, injectable, water-soluble small molecule drug conjugate (SMDC) designed for targeted cancer therapy. It consists of a ligand specific for prostate-specific membrane antigen (PSMA), which is highly expressed on most prostate cancer cells but not in most normal tissues. This ligand is conjugated via a stable, enzyme-cleavable linker to the cytotoxic agent tubulysin B hydrazide (TubBH). Upon binding to PSMA-expressing tumor cells and subsequent endocytosis, EC1169 releases tubulysin B hydrazide inside the cell, where it acts as a potent antimitotic by inhibiting tubulin polymerization. Preclinical studies have shown complete remissions and cures in mouse models with PSMA-positive tumors. EC1169 has been evaluated in phase 1 clinical trials for metastatic castration-resistant prostate cancer (mCRPC), both in taxane-naïve and taxane-exposed patients[1][2][4][6][8].

02

Targets

PSMA (Prostate-specific membrane antigen)TUBB (Tubulin (alpha and beta subunits))

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