XP-102

XP-102 (also known as BI 882370) is a second-generation, potent and selective pan-RAF inhibitor that uniquely binds to the DFG-out conformation of RAF kinases. Unlike marketed BRAF inhibitors that occupy the DFG-in conformation, XP-102 targets both mutant and wild-type RAF isoforms with high selectivity. Preclinical studies have demonstrated superior anti-tumor activity compared to vemurafenib in BRAF V600-mutant colorectal cancer and melanoma models, including efficacy in models resistant to other BRAF inhibitors. The drug is being developed primarily for advanced solid tumors harboring BRAF V600 mutations—including colorectal cancer, malignant melanoma, non-small cell lung cancer (NSCLC), and thyroid cancer—both as monotherapy and in combination with trametinib (a MEK inhibitor). XP-102 was originally discovered by Boehringer Ingelheim and is now being developed by Xynomic Pharmaceuticals[1][3][4][5][6][7].

Other names

BI 882370BI882370BI-882370