JDQ443 + trametinib

JDQ443 + trametinib is a combination therapy of two small molecule inhibitors under clinical investigation for the treatment of advanced solid tumors harboring the KRAS G12C mutation. **JDQ443** (also known as Opnurasib) is an oral, covalent, selective inhibitor of mutant KRAS G12C protein, locking it in its inactive GDP-bound state and preventing downstream oncogenic signaling. **Trametinib** (also known as Mekinist or TMT212) is an oral allosteric inhibitor of MEK1 and MEK2, key kinases within the RAS–RAF–MEK–ERK signaling pathway. The combination aims to suppress tumor growth more effectively than KRAS G12C inhibition alone by overcoming adaptive resistance mechanisms associated with RAS pathway reactivation. Early preclinical data and clinical trials have demonstrated enhanced antitumor activity for the combination compared to monotherapy, especially in non-small cell lung cancer (NSCLC) and colorectal cancer with KRAS G12C mutations[1][3][4][5].

Brand names

Mekinist

Other names

OpnurasibTMT212TMT-212TMT 212