Macrocyclic Dimerization Inhibitors of Raf Kinases


Reference #: 01338

The University of South Carolina is offering licensing opportunities for Macrocyclic Dimerization Inhibitors of Raf Kinases.



Despite the clinical success of B-Raf inhibitors like vemurafenib in treating metastatic melanoma, resistance has emerged through “paradoxical MEK/ERK signaling” where rather than blocking cancer growth, tumor formation is stimulated. Tumors with mutant BRAF and also mutant RAS enzymes represent some of the deadliest forms of cancer, such as metastatic melanomas and pancreatic cancers. There is a huge unmet medical need in hundreds of thousands of patients worldwide.


Invention Description:

These dimerization inhibitors block the BRAF enzyme by preventing it from binding to itself, a necessary step for activity and for the signaling process required for tumor growth.


Potential Applications:

These compounds have potential for further development as next generation BRAF inhibitors that avoid paradoxical signaling and successfully target metastatic melanomas and other tumors.


Advantages and Benefits:

Generating next generation BRAF inhibitors will overcome issues currently present with early generation compounds that, rather than blocking cancer growth as intended, actually promote tumor formation in susceptible patients.

These compounds would represent first-in-class drugs that have numerous advantages over currently used compounds and provide treatment for some of the deadliest forms of cancer.



Patent Information:
Title App Type Country Serial No. Patent No. File Date Issued Date Expire Date Patent Status
Peptide Based Inhibitors of Raf Kinase Protein Dimerization and Kinase Activity Utility United States 16/441,054 11,162,083 6/14/2019 11/2/2021   Issued
Design and Optimization of Type IV BRAF Inhibitors for the Treatment of Melanoma Utility United States 17/409,306   8/23/2021     Published
For Information, Contact:
Technology Commercialization
University of South Carolina
Campbell Mcinnes
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