Ravimig (MTR106) / Meditor, Barkan Pharma, TrioxBio - LARVOL DELTA

Structural insights into the binding of CX-5461 and MTR-106 to G-quadruplex DNA. (PubMed, Nucleic Acids Res) - "Their rigid polyaromatic scaffolds stacked with the 3'-end G-tetrad of G4, while their flexible side chains extended into the groove of QDH to enable spatial recognition. These findings elucidated the molecular basis of G4 recognition by CX-5461 and MTR-106, and provided a structural framework for the rational development of next-generation G4-targeted therapeutics with improved selectivity and efficacy."

Journal • Oncology • Myt1l

In Silico Investigation of the Molecular Mechanism of PARP1 Inhibition for the Treatment of BRCA-Deficient Cancers. (PubMed, Molecules) - "Importantly, vdW interaction was recognized as a decisive factor in the bindings with PARP1 G4 and PARP1. Collectively, these findings demonstrated the ascendancy of MTR-106 over talazoparib at the atomic level and revealed that the dual targeting of PARP1 G4 and PARP1 might be pivotal for PARPi that is capable of overcoming acquired drug resistance, providing valuable information for the design and development of novel drugs."

Journal • Oncology • BRCA

Discovery of MTR-106 as a highly potent G-quadruplex stabilizer for treating BRCA-deficient cancers. (PubMed, Invest New Drugs) - "However, MTR-106 showed modest activity against talazoparib-resistant xenograft models. In rats, the drug rapidly distributes to tissues within 5 min, and its average concentrations were 12-fold higher in the tissues than in the plasma. Overall, we identified MTR-106 as a novel G-quadruplex stabilizer with high tissue distribution, and it may serve as a potential anticancer agent."

Journal • Oncology • BRCA • HRD