FDA-approved and investigational MAP3K, MAP2K, and MAPK inhibitors
| Drug | Status | Indication | |
| MAP3Ks | |||
| BRAF | Vemurafenib | Approved | Melanoma, Erdheim-Chester disease |
| Dabrafenib | Approved | Monotherapy: melanoma In combination with trametinib: melanoma, NSCLC, anaplastic thyroid cancer | |
| Encorafenib | Approved | In combination with: - Binimetinib: melanoma - Cetuximab: colorectal cancer | |
| PLX8394 | I/II | Unresectable solid tumors | |
| BRAF/CRAF | LHX254 | II | Melanoma and NSCLC, in combination with LTT462, trametinib or ribociclib |
| pan-RAF | TAK580 | I | Gliomas and other tumors |
| Lifirafenib | I/II | Advanced or refractory solid tumors, in combination with mirdametinib | |
| DAY101 | II | Relapsed or progressive low-grade glioma | |
| dualRAF/MEK | VERSUS-6766 | II | Low-grade serous ovarian cancer, NSCLC: monotherapy and in combination with defactinib |
| RO5126766 | I | RAS-RAF-MEK pathway mutant solid tumors: in combination with everolimus Advanced solid tumors: in combination with FAK inhibitor VERSUS-6063 | |
| MAP2Ks | |||
| MEK1/2 | Trametinib | Approved | Monotherapy: melanoma In combination with dabrafenib: melanoma, NSCLC, anaplastic thyroid cancer |
| Cobimetinib | Approved | In combination with vemurafenib: melanoma | |
| Selumetinib | Approved | Pediatric neurofibromatosis type 1 | |
| Binimetinib | Approved | In combination with encorafenib: melanoma | |
| Pimasertib | I/II | Cancer with brain metastases | |
| Mirdametinib | I/II | Advanced or refractory solid tumors, in combination with lifirafenib | |
| E6201 | I | Metastatic melanoma central nervous system metastases | |
| RO5126766 | I | Solid tumors, NSCLC, multiple myeloma: monotherapy or in combination with everolimus | |
| HL-085 | I/II | Melanoma, solid tumors, NSCLC: monotherapy or in combination with vemurafenib | |
| SHR7390 | II | Metastatic castration-resistant prostate cancer | |
| CS-3006 | I | Advanced or metastatic solid tumors | |
| FCN-159 | I | Melanoma | |
| MAPKs | |||
| ERK1/2 | Ulixertinib | I/II | Several active studies in solid tumors and melanoma, in monotherapies or in combination |
| MK-8353 | I | Colorectal cancer, in combination with pembrolizumab | |
| LTT462 | I/II | Melanoma and NSCLC, in combination with LXH254 Myelofibrosis, in combination with JAK inhibitor ruxolitinib | |
| LY3214996 | I/II | Several active studies in solid tumors and AML, in monotherapies or in combination | |
| HH2710 | I/II | Advanced tumors | |
| JSI-1187 | I | Monotherapy and in combination with dabrafenib: solid tumors with MAPK pathway mutations | |
| p38α | Neflamapimod | II | Dementia and Alzheimer |
| p38α/β | Losmapimod (GW856553X) | III | SARS-CoV-2 |
AML, Acute myelogenous leukemia; JAK, Janus Kinase; SARS-CoV, severe acute respiratory syndrome coronavirus.