Drug intelligence / Profile preview

dota-colchicinic acid

Development stage
Preclinical
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
Administration
Intravenous
01

Overview

DOTA-colchicinic acid is a synthetic molecule that consists of colchicinic acid (a derivative of colchicine, a natural alkaloid used for gout and various inflammatory diseases) chemically linked to DOTA, a bifunctional chelator commonly used to enable radiolabeling of molecules for nuclear medicine. The DOTA group allows stable complexation with various metal radioisotopes (such as yttrium-90, lutetium-177, indium-111, and gallium-68), facilitating the development of radiopharmaceuticals for targeted cancer therapy or molecular imaging. The colchicinic acid component retains the microtubule-inhibiting, antimitotic, and cytostatic properties associated with colchicine derivatives—mainly inhibiting polymerization of β-tubulin, disrupting mitosis, and inducing apoptosis in proliferating cells. DOTA-colchicinic acid and its conjugates are primarily researched as payloads for radioimmunoconjugates, peptide drug conjugates, or theranostic agents in preclinical and clinical oncology studies. These conjugates are being developed mainly for the targeted treatment or imaging of malignant tumors.

Other names
dota-colchicinic acidDOTA-conjugated colchicineDOTA–colchicinic acid
02

Targets

TUBB (Tubulin (alpha and beta subunits))

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