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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.
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