Novel matrix metalloproteinases (MMPs) Inhibitor and MMP-targeted imaging tracers

• Upregulation of MMPs is associated with a wide range of diseases including cancers, inflammation and cardiovascular diseases.
• Measurement of MMP expression and activation in vivo could enable physicians to accurately diagnose and treat MMP-associated diseases.
• Currently there are no tracers available in the clinic for imaging MMP activity.
• A new type of a MMP inhibitor (1) has been developed, which also serves as a versatile scaffold (3) for developing MMP-targeted imaging agents.
• Additionally, a novel precursor was also designed as a parent building block for making different type of hydrophilic MMP imaging tracers.
• These novel scaffolds display improved pharmacokinetics and water solubility as compared to previously reported MMP SEPCT probes (i.e.RP805)
• Lead Innovator: Mehran Sadeghi, PhD
• IP status: PCT/US2017/026610

Ex-vivo photography (A) and autoradiography (B) of aortae and carotid arteries from apoE-/- mice with CaCl2-induced carotid aneurysm injected with 99mTc-RYM1 without (left) and with the pre-injection of an excess of MMP inhibitor, RYM (right).