Drug intelligence / Profile preview

Myr-K(DOTA)-c(RGDfK)

Development stage
Preclinical
Lead developer
Cancer Institute and Hospital, Chinese Academy of Medical Sciences
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
Administration
Intravenous
01

Overview

Myr-K(DOTA)-c(RGDfK) is a myristic acid-conjugated cyclic RGD peptide (c(RGDfK)) linked to a DOTA chelator, developed by the National Cancer Center of Japan, Osaka Medical and Pharmaceutical University, and Linqmed. It is designed for integrin-targeted peptide receptor radionuclide therapy (PRRT) and molecular imaging of cancers, particularly pancreatic cancer. The cyclic RGDfK peptide moiety selectively targets integrins αvβ3 and αvβ6, which are highly expressed on pancreatic cancer cells and tumor-associated vasculature. The conjugation of myristic acid (a C14 fatty acid) serves as a serum albumin binder, which significantly enhances blood retention and tumor accumulation by slowing renal clearance. The DOTA chelator allows for radiolabeling with various radionuclides, such as indium-111 (111In) for diagnostic imaging, or actinium-225 (225Ac) and lutetium-177 (177Lu) for targeted alpha/beta radionuclide therapy.

Other names
Myr-K(111In-DOTA)-c(RGDfK)Myr-K(177Lu-DOTA)-c(RGDfK)Myr-K(225Ac-DOTA)-c(RGDfK)myristic acid-conjugated RGD peptide
02

Targets

αVβ3 (Integrin αVβ3)αVβ6 (Integrin αVβ6)

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