Cobimetinib
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Also known as Gdc 0623Gdc 0973Gdc-0623GDC-0973RG 7420RG-7420RG7420Xl 518Xl518
Summary
Cobimetinib (CHEMBL2146883) is an approved small-molecule EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor (ATC L01EE02) targeting MAP2K1, MAP2K2, and MAP2K7; indicated across 26 conditions including neoplasm and melanoma; with CIViC clinical evidence for 17 variant-indication associations (e.g. BRAF V600 in melanoma).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01EE02
- Targets: 3 (MAP2K1, MAP2K2, MAP2K7)
- Indications: 26 conditions
- Clinical trials: 107
- Precision-oncology evidence (CIViC): 17 variant–indication associations
- Chemistry: 531.3 Da · C21H21F3IN3O2
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL2146883 |
| Name | Cobimetinib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 16222096 |
| ChEBI | CHEBI:90851 |
| ATC | L01EE02 |
| Molecular formula | C21H21F3IN3O2 |
| Molecular weight | 531.3 |
| InChIKey | BSMCAPRUBJMWDF-KRWDZBQOSA-N |
SMILES: C1CCN[C@@H](C1)C2(CN(C2)C(=O)C3=C(C(=C(C=C3)F)F)NC4=C(C=C(C=C4)I)F)O
IUPAC name: [3,4-difluoro-2-(2-fluoro-4-iodoanilino)phenyl]-[3-hydroxy-3-[(2S)-piperidin-2-yl]azetidin-1-yl]methanone
ChEBI definition: A member of the class of N-acylazetidines obtained by selective formal condensation of the carboxy group of 3,4-difluoro-2-(2-fluoro-4-iodoanilino)benzoic acid with the secondary amino group from the azetidine ring of 3-[(2S)-piperidin-2-yl]azetidin-3-ol. An inhibitor of mitogen-activated protein kinase that is used (as its fumarate salt) in combination with vemurafenib for the treatment of patients with unresectable or metastatic melanoma.
Pharmacological roles (ChEBI): EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor, antineoplastic agent.
Also known as: Cobimetinib, Gdc 0623, Gdc 0973, Gdc-0623, GDC-0973, RG 7420, RG-7420, RG7420, Xl 518, Xl518, COBIMETINIB, cobimetinib
Parent form; salt/anhydrous children: CHEMBL2364607, CHEMBL3526209
Patent coverage: 3,767 distinct patent families (9,422 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 9,229 (98%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| MAP2K1 | mitogen-activated protein kinase kinase 1 | Negative | 9.05 | 4.7% | Q02750 |
| MAP2K2 | mitogen-activated protein kinase kinase 2 | Negative | 6.7 | 3.1% | P36507 |
| MAP2K7 | mitogen-activated protein kinase kinase 7 | Negative | 5 | 3.9% | O14733 |
Broader ChEMBL bioactivity targets: 16 (assay-derived). Sample: D(1A) dopamine receptor, Thromboxane A2 receptor, Muscarinic acetylcholine receptor M2, Dual specificity mitogen-activated protein kinase kinase; MEK1/2, Muscarinic acetylcholine receptor M1, Sodium-dependent noradrenaline transporter, Sodium-dependent serotonin transporter, Alpha-1A adrenergic receptor, Mu-type opioid receptor, D(3) dopamine receptor.
Bioactivity
ChEMBL activities: 21 potent at pChembl ≥ 5 of 28 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| MAP2K2 | 9.7 | IC50 | 0.2 | nM | CHEMBL_ACT_12041238 |
| MAP2K1 | 9.7 | IC50 | 0.2 | nM | CHEMBL_ACT_29186985 |
| MAP2K1 | 9.05 | IC50 | 0.9 | nM | CHEMBL_ACT_12041220 |
| MAP2K1 | 9.05 | IC50 | 0.9 | nM | CHEMBL_ACT_26186113 |
| MAP2K1 | 9.05 | IC50 | 0.9 | nM | CHEMBL_ACT_29186981 |
| BRAF | 8.74 | IC50 | 1.8 | nM | CHEMBL_ACT_15461647 |
| MAP2K1 | 8.38 | IC50 | 4.2 | nM | CHEMBL_ACT_15461649 |
| MAP2K1 | 8.38 | IC50 | 4.2 | nM | CHEMBL_ACT_24954265 |
| MAP2K1 | 8.38 | IC50 | 4.2 | nM | CHEMBL_ACT_25564478 |
| MAP2K1 | 8.38 | IC50 | 4.2 | nM | CHEMBL_ACT_26276968 |
| MAP2K1 | 8.18 | IC50 | 6.6 | nM | CHEMBL_ACT_29065673 |
| MAP2K2 | 7.66 | Kd | 22 | nM | CHEMBL_ACT_17910662 |
| MAP2K2 | 7.64 | IC50 | 23 | nM | CHEMBL_ACT_24957049 |
| MAP2K1 | 7.51 | IC50 | 31 | nM | CHEMBL_ACT_24957048 |
| ACTR3 | 7.44 | Kd | 36 | nM | CHEMBL_ACT_17880444 |
| ACTR3 | 7.28 | IC50 | 53 | nM | CHEMBL_ACT_24957047 |
| OPRM1 | 6.57 | AC50 | 271.4 | nM | CHEMBL_ACT_25158356 |
| MAP2K1 | 6.51 | Kd | 309 | nM | CHEMBL_ACT_17910460 |
| KCNH2 | 5.89 | AC50 | 1300 | nM | CHEMBL_ACT_25117961 |
| SLC6A3 | 5.14 | AC50 | 7295 | nM | CHEMBL_ACT_25125140 |
| SLC6A4 | 5.11 | AC50 | 7824 | nM | CHEMBL_ACT_25151508 |
Target pathways
Aggregated over 3 target gene(s): MAP2K1, MAP2K2, MAP2K7.
Top Reactome pathways
69 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Disease | 3 | MAP2K1, MAP2K2, MAP2K7 |
| Uptake and function of anthrax toxins | 3 | MAP2K1, MAP2K2, MAP2K7 |
| Uptake and actions of bacterial toxins | 3 | MAP2K1, MAP2K2, MAP2K7 |
| Infectious disease | 3 | MAP2K1, MAP2K2, MAP2K7 |
| Bacterial Infection Pathways | 3 | MAP2K1, MAP2K2, MAP2K7 |
| RAF-independent MAPK1/3 activation | 2 | MAP2K1, MAP2K2 |
| Developmental Biology | 2 | MAP2K1, MAP2K2 |
| Cytokine Signaling in Immune system | 2 | MAP2K1, MAP2K7 |
| Signal Transduction | 2 | MAP2K1, MAP2K2 |
| Toll Like Receptor 4 (TLR4) Cascade | 2 | MAP2K1, MAP2K7 |
| MyD88:MAL(TIRAP) cascade initiated on plasma membrane | 2 | MAP2K1, MAP2K7 |
| MyD88-independent TLR4 cascade | 2 | MAP2K1, MAP2K7 |
| Signaling by NTRKs | 2 | MAP2K1, MAP2K2 |
| Toll Like Receptor 9 (TLR9) Cascade | 2 | MAP2K1, MAP2K7 |
| Toll Like Receptor 10 (TLR10) Cascade | 2 | MAP2K1, MAP2K7 |
| Toll Like Receptor 3 (TLR3) Cascade | 2 | MAP2K1, MAP2K7 |
| Toll Like Receptor 5 (TLR5) Cascade | 2 | MAP2K1, MAP2K7 |
| Toll Like Receptor TLR1:TLR2 Cascade | 2 | MAP2K1, MAP2K7 |
| Toll Like Receptor 7/8 (TLR7/8) Cascade | 2 | MAP2K1, MAP2K7 |
| Toll Like Receptor TLR6:TLR2 Cascade | 2 | MAP2K1, MAP2K7 |
| Innate Immune System | 2 | MAP2K1, MAP2K7 |
| Immune System | 2 | MAP2K1, MAP2K7 |
| Toll-like Receptor Cascades | 2 | MAP2K1, MAP2K7 |
| Prolonged ERK activation events | 2 | MAP2K1, MAP2K2 |
| Frs2-mediated activation | 2 | MAP2K1, MAP2K2 |
| Toll Like Receptor 2 (TLR2) Cascade | 2 | MAP2K1, MAP2K7 |
| Signaling by NTRK1 (TRKA) | 2 | MAP2K1, MAP2K2 |
| Signalling to ERKs | 2 | MAP2K1, MAP2K2 |
| L1CAM interactions | 2 | MAP2K1, MAP2K2 |
| Axon guidance | 2 | MAP2K1, MAP2K2 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| positive regulation of DNA-templated transcription | 3 |
| protein phosphorylation | 3 |
| MAPK cascade | 2 |
| signal transduction | 2 |
| heart development | 2 |
| positive regulation of gene expression | 2 |
| Schwann cell development | 2 |
| thyroid gland development | 2 |
| regulation of stress-activated MAPK cascade | 2 |
| ERBB2-ERBB3 signaling pathway | 2 |
| myelination | 2 |
| insulin-like growth factor receptor signaling pathway | 2 |
| thymus development | 2 |
| regulation of axon regeneration | 2 |
| positive regulation of axonogenesis | 2 |
Indications & clinical
Indications
26 indications (2 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| neoplasm | 4 | MONDO:0005070 | EFO:0000616 |
| melanoma | 3 | MONDO:0005105 | EFO:0000756 |
| cutaneous melanoma | 3 | MONDO:0005012 | EFO:0000389 |
| metastatic melanoma | 3 | MONDO:0005191 | EFO:0002617 |
| colorectal carcinoma | 3 | MONDO:0024331 | EFO:1001951 |
| colorectal neoplasm | 3 | MONDO:0005335 | MONDO:0005575 |
| non-small cell lung carcinoma | 2 | MONDO:0005233 | EFO:0003060 |
| craniopharyngioma | 2 | MONDO:0018907 | EFO:1000209 |
| breast neoplasm | 2 | MONDO:0021100 | MONDO:0007254 |
| breast carcinoma | 2 | MONDO:0004989 | EFO:0000305 |
| chronic myelomonocytic leukemia | 2 | MONDO:0020311 | EFO:1001779 |
| thyroid gland carcinoma | 2 | MONDO:0015075 | EFO:0002892 |
| gallbladder carcinoma | 2 | MONDO:0003220 | EFO:1001956 |
| arteriovenous malformations of the brain | 2 | MONDO:0007154 | Orphanet:46724 |
| lymphoid neoplasm | 2 | MONDO:0005157 | EFO:0001642 |
| acute myeloid leukemia | 1 | MONDO:0018874 | EFO:0000222 |
| gastric adenocarcinoma | 1 | MONDO:0005036 | EFO:0000503 |
| plasma cell myeloma | 1 | MONDO:0009693 | EFO:0001378 |
| sarcoma | 1 | MONDO:0005089 | EFO:0000691 |
| carcinoma of esophagus | 1 | MONDO:0019086 | EFO:0002916 |
| ovarian cancer | 1 | MONDO:0008170 | MONDO:0008170 |
| skin neoplasm | 1 | MONDO:0002531 | MONDO:0002898 |
| adenocarcinoma | 1 | MONDO:0004970 | MONDO:0003219 |
| exocrine pancreatic carcinoma | 0 | MONDO:0005192 | EFO:0002618 |
| pancreatic ductal adenocarcinoma | 0 | MONDO:0005184 | MONDO:0005184 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 107.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 47 |
| PHASE1 | 31 |
| PHASE1/PHASE2 | 14 |
| PHASE3 | 7 |
| Not specified | 4 |
| PHASE2/PHASE3 | 2 |
| EARLY_PHASE1 | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT03178552 | PHASE2/PHASE3 | ACTIVE_NOT_RECRUITING | A Study to Evaluate the Efficacy and Safety of Multiple Targeted Therapies as Treatments for Participants With Non-Small Cell Lung Cancer (NSCLC) |
| NCT03768063 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study in Patients Previously Enrolled in a Genentech and/or F. Hoffmann-La Roche Ltd Sponsored Atezolizumab Study |
| NCT05768178 | PHASE2/PHASE3 | RECRUITING | DETERMINE Trial Treatment Arm 05: Vemurafenib in Combination With Cobimetinib in Adult Patients With BRAF Positive Cancers. |
| NCT01689519 | PHASE3 | COMPLETED | A Study Comparing Vemurafenib Versus Vemurafenib Plus Cobimetinib in Participants With Metastatic Melanoma |
| NCT02427893 | PHASE3 | WITHDRAWN | Trial of Vemurafenib and Cobimetinib in Patients With Advanced BRAFV600 Mutant Melanoma |
| NCT02788279 | PHASE3 | COMPLETED | A Study to Investigate Efficacy and Safety of Cobimetinib Plus Atezolizumab and Atezolizumab Monotherapy Versus Regorafenib in Participants With Metastatic Colorectal Adenocarcinoma (COTEZO IMblaze370) |
| NCT02908672 | PHASE3 | COMPLETED | A Study of Atezolizumab Plus Cobimetinib and Vemurafenib Versus Placebo Plus Cobimetinib and Vemurafenib in Previously Untreated BRAFv600 Mutation-Positive Patients With Metastatic or Unresectable Locally Advanced Melanoma |
| NCT03273153 | PHASE3 | TERMINATED | A Study of Cobimetinib Plus Atezolizumab Versus Pembrolizumab in Participants With Previously Untreated Advanced BRAFv600 Wild-Type Melanoma |
| NCT04007848 | PHASE3 | COMPLETED | Cobimetinib for BRAF-wild-type or Mutated Histiocytoses |
| NCT02693535 | PHASE2 | RECRUITING | TAPUR: Testing the Use of Food and Drug Administration (FDA) Approved Drugs That Target a Specific Abnormality in a Tumor Gene in People With Advanced Stage Cancer |
| NCT03175432 | PHASE2 | ACTIVE_NOT_RECRUITING | Bevacizumab and Atezolizumab With or Without Cobimetinib in Treating Patients With Untreated Melanoma Brain Metastases |
| NCT03181100 | PHASE2 | ACTIVE_NOT_RECRUITING | Atezolizumab With Chemotherapy in Treating Patients With Anaplastic or Poorly Differentiated Thyroid Cancer |
| NCT03202316 | PHASE2 | ACTIVE_NOT_RECRUITING | Atezolizumab, Cobimetinib, and Eribulin in Treating Patients With Chemotherapy Resistant Metastatic Inflammatory Breast Cancer |
| NCT03202940 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | A Phase IB/II Study of Alectinib Combined With Cobimetinib in Advanced ALK-Rearranged (ALK+) NSCLC |
| NCT03224767 | PHASE2 | ACTIVE_NOT_RECRUITING | Vemurafenib and Cobimetinib in Treating Patients With BRAF V600E Mutation Positive Craniopharyngioma |
| NCT03600701 | PHASE2 | ACTIVE_NOT_RECRUITING | Atezolizumab and Cobimetinib in Treating Patients With Metastatic, Recurrent, or Refractory Non-small Cell Lung Cancer |
| NCT04079179 | PHASE2 | RECRUITING | Cobimetinib in Refractory Langerhans Cell Histiocytosis (LCH), and Other Histiocytic Disorders |
| NCT04185831 | PHASE2 | ACTIVE_NOT_RECRUITING | A MolEcularly Guided Anti-Cancer Drug Off-Label Trial |
| NCT04302025 | PHASE2 | RECRUITING | A Study of Multiple Therapies in Biomarker-selected Participants With Resectable Stages IB-III Non-small Cell Lung Cancer (NSCLC) |
| NCT04409639 | PHASE2 | ACTIVE_NOT_RECRUITING | Cobimetinib in Newly Diagnosed or HMA-treated CMML Patients With RAS Pathway Mutations |
| NCT04931342 | PHASE2 | ACTIVE_NOT_RECRUITING | A Study Evaluating the Efficacy and Safety of Biomarker-Driven Therapies in Patients With Persistent or Recurrent Rare Epithelial Ovarian Tumors |
| NCT04941287 | PHASE2 | ACTIVE_NOT_RECRUITING | Testing A New Combination of Anti-cancer Immune Therapies, Atezolizumab and CDX-1127 (Varlilumab) With or Without the Addition of a Third Anti-cancer Drug, Cobimetinib, for Advanced-Stage Biliary Tract Cancer |
| NCT05159245 | PHASE2 | RECRUITING | The Finnish National Study to Facilitate Patient Access to Targeted Anti-cancer Drugs |
| NCT06440850 | PHASE2 | RECRUITING | Vemurafenib and Cobimetinib for the Treatment of Patients With High Risk Differentiated Thyroid Carcinoma With BRAFV600E Mutation |
| NCT06813079 | PHASE2 | NOT_YET_RECRUITING | Using Tumor Models to Determine Treatments |
| NCT07449754 | PHASE2 | RECRUITING | Belvarafenib in Combination With Cobimetinib in Patients With Locally Advanced or Metastatic NRAS-Mutant Melanoma |
| NCT01495988 | PHASE2 | TERMINATED | Trial of Vemurafenib/Cobimetinib With or Without Bevacizumab in Patients With Stage IV BRAFV600 Mutant Melanoma |
| NCT01813214 | PHASE2 | TERMINATED | The Effects of Vemurafenib + Cobimetinib on Immunity in Patients With Melanoma |
| NCT01928394 | PHASE1/PHASE2 | COMPLETED | A Study of Nivolumab by Itself or Nivolumab Combined With Ipilimumab in Patients With Advanced or Metastatic Solid Tumors |
| NCT01959633 | PHASE1/PHASE2 | COMPLETED | Vemurafenib Plus Cobimetinib Plus PEG-interferon in Advanced Melanoma Patients Harboring the V600BRAF Mutation |
| NCT02036086 | PHASE2 | UNKNOWN | Study of Neo-adjuvant Use of Vemurafenib Plus Cobimetinib for BRAF Mutant Melanoma With Palpable Lymph Node Metastases |
| NCT02060188 | PHASE2 | COMPLETED | A Study of Nivolumab Alone or Nivolumab Combination Therapy in Colon Cancer That Has Come Back or Has Spread |
| NCT02091141 | PHASE2 | COMPLETED | My Pathway: A Study Evaluating Herceptin/Perjeta, Tarceva, Zelboraf/Cotellic, Erivedge, Alecensa, and Tecentriq Treatment Targeted Against Certain Molecular Alterations in Participants With Advanced Solid Tumors |
| NCT02230306 | PHASE2 | TERMINATED | Phase II Study of Cobimetinib in Combination With Vemurafenib in Active Melanoma Brain Metastases |
| NCT02291289 | PHASE2 | COMPLETED | A Study of Biomarker-Driven Therapy in Metastatic Colorectal Cancer (mCRC) |
| NCT02303951 | PHASE2 | TERMINATED | Neoadjuvant Vemurafenib + Cobimetinib + Atezolizumab in Melanoma: NEO-VC |
| NCT02322814 | PHASE2 | TERMINATED | A Study of Cobimetinib Plus Paclitaxel, Cobimetinib Plus Atezolizumab Plus Paclitaxel, or Cobimetinib Plus Atezolizumab Plus Nab-Paclitaxel as Initial Treatment for Participants With Triple-Negative Breast Cancer That Has Spread |
| NCT02537600 | PHASE2 | COMPLETED | Vemurafenib and Cobimetinib Combination in BRAF Mutated Melanoma With Brain Metastasis |
| NCT02583516 | PHASE2 | COMPLETED | Clinical Trial to Evaluate the Efficacy of Vemurafenib in Combination With Cobimetinib (Continuous and Intermittent) in BRAFV600-mutation Positive Patients With Unresectable Locally Advanced or Metastatic Melanoma |
| NCT02639546 | PHASE1/PHASE2 | COMPLETED | Safety and Pharmacokinetics of Cobimetinib in Pediatric and Young Adult Participants With Previously Treated Solid Tumors |
Clinical evidence (CIViC)
Variant × indication × effect (17 predictive associations from 18 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| BRAF V600 | Melanoma | Sensitivity/Response | Cobimetinib + Vemurafenib | CIViC A | EID6044 +1 |
| BRAF V600 | Melanoma | Sensitivity/Response | Atezolizumab + Vemurafenib + Cobimetinib | CIViC A | EID11238 |
| ARAF Mutation | Langerhans-cell Histiocytosis | Sensitivity/Response | Cobimetinib | CIViC B | EID11297 |
| ARAF Mutation AND ARAF S225V AND ARAF P216A | Erdheim-Chester Disease | Sensitivity/Response | Cobimetinib | CIViC B | EID11296 |
| BRAF Non-V600 | Erdheim-Chester Disease | Sensitivity/Response | Cobimetinib | CIViC B | EID11298 |
| BRAF Non-V600 | Langerhans-cell Histiocytosis | Sensitivity/Response | Cobimetinib | CIViC B | EID11299 |
| BRAF V600 | Melanoma | Sensitivity/Response | Vemurafenib + Cobimetinib | CIViC B | EID1422 |
| BRAF V600E | Melanoma | Sensitivity/Response | Cobimetinib + Vemurafenib | CIViC B | EID1421 |
| BRAF V600E OR BRAF K601E | Colorectal Cancer | Sensitivity/Response | Cobimetinib + Vemurafenib | CIViC B | EID11670 |
| NRAS Mutation OR KRAS Mutation OR RAF1 Mutation OR MAP2K1 Mutation OR MAP2K2 Mutation | Erdheim-Chester Disease | Sensitivity/Response | Cobimetinib | CIViC B | EID11328 |
| NRAS Mutation OR KRAS Mutation OR RAF1 Mutation OR MAP2K1 Mutation OR MAP2K2 Mutation | Langerhans-cell Histiocytosis | Sensitivity/Response | Cobimetinib | CIViC B | EID11329 |
| BRAF V600E | Ganglioglioma | Sensitivity/Response | Vemurafenib + Cobimetinib | CIViC C | EID11310 |
| BRAF V600E AND CDKN2A Deletion AND CDKN2B Deletion AND TET2 E796K AND BAX L76R AND AXIN2 P455K | Ganglioglioma | Sensitivity/Response | Cobimetinib + Vemurafenib | CIViC C | EID11314 |
| GOLGA4::RAF1 Fusion | Melanoma | Sensitivity/Response | Trametinib + Cobimetinib | CIViC C | EID8374 |
| KRAS G12R | Histiocytosis-Lymphadenopathy Plus Syndrome | Sensitivity/Response | Cobimetinib | CIViC C | EID7310 |
| KRAS G12R AND GATA3 Mutation AND GNAS Mutation | Histiocytosis-Lymphadenopathy Plus Syndrome | Sensitivity/Response | Cobimetinib | CIViC C | EID11330 |
| BRAF V600E | Cancer | Sensitivity/Response | Cobimetinib | CIViC D | EID1141 |
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
77 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| AXITINIB | ChEMBL + PubChem | Phase 4 (approved) | MAP2K1, MAP2K2, MAP2K7 |
| BOSUTINIB | ChEMBL + PubChem | Phase 4 (approved) | MAP2K1, MAP2K2, MAP2K7 |
| FEDRATINIB | ChEMBL + PubChem | Phase 4 (approved) | MAP2K1, MAP2K2, MAP2K7 |
| RUXOLITINIB | ChEMBL + PubChem | Phase 4 (approved) | MAP2K1, MAP2K2, MAP2K7 |
| SELUMETINIB | ChEMBL + PubChem | Phase 4 (approved) | MAP2K1, MAP2K2, MAP2K7 |
| SORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | MAP2K1, MAP2K2, MAP2K7 |
| SUNITINIB | ChEMBL + PubChem | Phase 4 (approved) | MAP2K1, MAP2K2, MAP2K7 |
| VANDETANIB | ChEMBL + PubChem | Phase 4 (approved) | MAP2K1, MAP2K2, MAP2K7 |
| VEMURAFENIB | ChEMBL + PubChem | Phase 4 (approved) | MAP2K1, MAP2K2, MAP2K7 |
| NERATINIB | ChEMBL | Phase 4 (approved) | MAP2K1, MAP2K2, MAP2K7 |
| CANERTINIB | ChEMBL | Phase 3 | MAP2K1, MAP2K2, MAP2K7 |
| LESTAURTINIB | ChEMBL | Phase 3 | MAP2K1, MAP2K2, MAP2K7 |
| Afatinib | PubChem | Approved | MAP2K1, MAP2K2, MAP2K7 |
| Crizotinib | PubChem | Approved | MAP2K1, MAP2K2, MAP2K7 |
| Gefitinib | PubChem | Approved | MAP2K1, MAP2K2, MAP2K7 |
| Idelalisib | PubChem | Approved | MAP2K1, MAP2K2, MAP2K7 |
| Pazopanib | PubChem | Approved | MAP2K1, MAP2K2, MAP2K7 |
| BINIMETINIB | ChEMBL + PubChem | Phase 4 (approved) | MAP2K1, MAP2K2 |
| Lapatinib | ChEMBL + PubChem | Phase 4 (approved) | MAP2K2, MAP2K7 |
| TRAMETINIB | ChEMBL + PubChem | Phase 4 (approved) | MAP2K1, MAP2K2 |
| DASATINIB | ChEMBL | Phase 4 (approved) | MAP2K1, MAP2K2 |
| GILTERITINIB | ChEMBL | Phase 4 (approved) | MAP2K1, MAP2K2 |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | MAP2K1, MAP2K2 |
| AVUTOMETINIB | ChEMBL | Phase 3 | MAP2K1, MAP2K2 |
| DOVITINIB | ChEMBL | Phase 3 | MAP2K1, MAP2K2 |
| LINSITINIB | ChEMBL | Phase 3 | MAP2K1, MAP2K2 |
| ORANTINIB | ChEMBL | Phase 3 | MAP2K1, MAP2K2 |
| SARACATINIB | ChEMBL | Phase 3 | MAP2K1, MAP2K2 |
| CENISERTIB | ChEMBL | Phase 2 | MAP2K1, MAP2K2 |
| CEP-32496 | ChEMBL | Phase 2 | MAP2K1, MAP2K2 |
| CI-1040 | ChEMBL | Phase 2 | MAP2K1, MAP2K2 |
| DEFOSBARASERTIB | ChEMBL | Phase 2 | MAP2K1, MAP2K2 |
| FORETINIB | ChEMBL | Phase 2 | MAP2K1, MAP2K2 |
| ILORASERTIB | ChEMBL | Phase 2 | MAP2K1, MAP2K2 |
| MIRDAMETINIB | ChEMBL | Phase 2 | MAP2K1, MAP2K2 |
| PELITINIB | ChEMBL | Phase 2 | MAP2K1, MAP2K2 |
| PIMASERTIB | ChEMBL | Phase 2 | MAP2K1, MAP2K2 |
| R-406 | ChEMBL | Phase 2 | MAP2K1, MAP2K2 |
| REFAMETINIB | ChEMBL | Phase 2 | MAP2K1, MAP2K2 |
| SU-014813 | ChEMBL | Phase 2 | MAP2K1, MAP2K2 |
| TAK-733 | ChEMBL | Phase 2 | MAP2K1, MAP2K2 |
| TOZASERTIB | ChEMBL | Phase 2 | MAP2K1, MAP2K2 |
| dacomitinib | PubChem | Approved | MAP2K1, MAP2K2 |
| Erlotinib | PubChem | Approved | MAP2K2, MAP2K7 |
| Fostamatinib | PubChem | Approved | MAP2K1, MAP2K2 |
| Ibrutinib | PubChem | Approved | MAP2K2, MAP2K7 |
| Imatinib | PubChem | Approved | MAP2K2, MAP2K7 |
| Quizartinib | PubChem | Approved | MAP2K2, MAP2K7 |
| regorafenib | PubChem | Approved | MAP2K1, MAP2K2 |
| TOFACITINIB | ChEMBL | Phase 4 (approved) | MAP2K1 |
| CEDIRANIB | ChEMBL | Phase 3 | MAP2K2 |
| LINIFANIB | ChEMBL | Phase 3 | MAP2K2 |
| BIIB-091 | ChEMBL | Phase 2 | MAP2K2 |
| E-6201 | ChEMBL | Phase 2 | MAP2K1 |
| SCH-900776 | ChEMBL | Phase 2 | MAP2K2 |
| SOTRASTAURIN | ChEMBL | Phase 2 | MAP2K1 |
| TOLONIUM CHLORIDE | ChEMBL | Phase 2 | MAP2K1 |
| ZAPNOMETINIB | ChEMBL | Phase 2 | MAP2K1 |
| Baricitinib | PubChem | Approved | MAP2K2 |
| Cabozantinib | PubChem | Approved | MAP2K2 |
Related Atlas pages
- Genes: MAP2K1, MAP2K2, MAP2K7
- Diseases: neoplasm, melanoma, cutaneous melanoma, metastatic melanoma, colorectal carcinoma, colorectal neoplasm, Langerhans cell histiocytosis specific to childhood, Erdheim-Chester disease, ganglioglioma, cancer
- Drugs: Axitinib, Bosutinib, Fedratinib, Ruxolitinib, Selumetinib, Sorafenib, Sunitinib, Vandetanib, Vemurafenib, Neratinib, Canertinib, Lestaurtinib, Afatinib, Crizotinib, Gefitinib, Idelalisib, Pazopanib, Binimetinib, Lapatinib, Trametinib, Dasatinib, Gilteritinib, Nintedanib, Avutometinib, Dovitinib, Linsitinib, Orantinib, Saracatinib, dacomitinib, Erlotinib, Fostamatinib, Ibrutinib, Imatinib, Quizartinib, regorafenib, Tofacitinib, Cediranib, Linifanib, Baricitinib, Cabozantinib