Drug intelligence / Profile preview

ec1456

Development stage
Phase 1
Lead developer
Novartis
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Prodrugs/Conditional Activator Small Molecules → Small Molecules, Peptides
Administration
Intravenous
01

Overview

EC1456 is an injectable small molecule drug conjugate (SMDC) designed for targeted cancer therapy. It consists of folic acid (vitamin B9) covalently linked via a bio-releasable linker to the potent microtubule inhibitor and cytotoxic agent tubulysin B hydrazide (TubBH). The drug specifically targets cells expressing the folate receptor alpha (FOLR1), which is overexpressed in many epithelial cancers but has limited expression in normal tissues. Upon binding to FOLR1 on cancer cells, EC1456 is internalized by endocytosis and releases its cytotoxic payload inside the cell, disrupting microtubule polymerization and arresting cell division at metaphase. This mechanism enables selective delivery of a highly potent anti-mitotic agent directly to tumor cells while sparing most normal tissues[1][3][4][5][6].

Other names
folate receptor-targeted tubulysin conjugatefolic acid-tubulysin conjugatefolate-tubulysinfolate-targeted tubulysin - Endocyte
02

Targets

FOLR1 (FRα)TUBB (Tubulin (alpha and beta subunits))

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