This review will mainly discuss BRAF inhibitors (vemurafenib, dabrafenib, and encorafenib) and MEK 1/2 inhibitors (trametinib, cobimetinib, and binimetinib), their indications across various types of cancers, combinations with immunotherapy, associated toxicities, resistance mechanisms, as well as novel drugs and future perspectives. The gene discussed is BRAF; the disease is cancer.