Selumetinib
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Also known as ARRY-142886ARRY-886Azd-6244AZD6244AZD-6244 HYD-SULFATEAZD-6244 HYDROGEN SULFATESELUMETINIB SULFATEARRAY142886AZD6244 (SELUMETINIB)AZD 6244SELUMETINIB (AZD6244)AZD-6244/ARRY-886SID144206913SID170466898SID174006431
Summary
Selumetinib (CHEMBL1614701) is an approved small-molecule EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor (ATC L01EE04) targeting MAP2K1; indicated across 52 conditions including neoplasm and non-small cell lung carcinoma; with CIViC clinical evidence for 68 variant-indication associations (e.g. NF1 Mutation in plexiform neurofibroma).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01EE04
- Targets: 1 (MAP2K1)
- Indications: 52 conditions
- Clinical trials: 118
- Precision-oncology evidence (CIViC): 68 variant–indication associations
- Chemistry: 457.7 Da · C17H15BrClFN4O3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1614701 |
| Name | Selumetinib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 10127622 |
| ChEBI | CHEBI:90227 |
| ATC | L01EE04 |
| Molecular formula | C17H15BrClFN4O3 |
| Molecular weight | 457.7 |
| InChIKey | CYOHGALHFOKKQC-UHFFFAOYSA-N |
SMILES: CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO
IUPAC name: 6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide
ChEBI definition: A member of the class of benzimidazoles that is 1-methyl-1H-benzimidazole which is substituted at positions 4, 5, and 6 by fluorine, (4-bromo-2-chlorophenyl)amino, and N-(2-hydroxyethoxy)aminocarbonyl groups, respectively. It is a MEK1 and MEK2 inhibitor.
Pharmacological roles (ChEBI): EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor, antineoplastic agent, anticoronaviral agent.
Also known as: ARRY-142886, ARRY-886, Azd-6244, AZD-6244, AZD6244, Selumetinib, SELUMETINIB, AZD-6244 HYD-SULFATE, AZD-6244 HYDROGEN SULFATE, SELUMETINIB SULFATE, ARRAY142886, AZD6244 (SELUMETINIB)
Parent form; salt/anhydrous children: CHEMBL2105684
Patent coverage: 3,943 distinct patent families (10,221 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 9,196 (90%) 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 | 7.92 | 4.7% | Q02750 |
Broader ChEMBL bioactivity targets: 10 (assay-derived). Sample: Epidermal growth factor receptor, Dual specificity mitogen-activated protein kinase kinase; MEK1/2, Dual specificity mitogen-activated protein kinase kinase 2, Dual specificity mitogen-activated protein kinase kinase 1, AP2-associated protein kinase 1, Casein kinase II subunit alpha’, Structural maintenance of chromosomes protein 1A, Structural maintenance of chromosomes protein 2, Uncharacterized protein FLJ45252, BMP-2-inducible protein kinase.
Bioactivity
ChEMBL activities: 41 potent at pChembl ≥ 5 of 41 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| MAP2K1 | 8.05 | IC50 | 9 | nM | CHEMBL_ACT_18569336 |
| MAP2K1 | 7.85 | IC50 | 14 | nM | CHEMBL_ACT_16423361 |
| MAP2K2 | 7.85 | IC50 | 14 | nM | CHEMBL_ACT_22892123 |
| MAP2K2 | 7.85 | IC50 | 14 | nM | CHEMBL_ACT_24789080 |
| MAP2K1 | 7.85 | IC50 | 14 | nM | CHEMBL_ACT_24953975 |
| MAP2K1 | 7.85 | IC50 | 14 | nM | CHEMBL_ACT_25564480 |
| MAP2K1 | 7.85 | IC50 | 14 | nM | CHEMBL_ACT_29055501 |
| MAP2K1 | 7.51 | IC50 | 31 | nM | CHEMBL_ACT_16423225 |
| MAP2K1 | 7.39 | Kd | 41 | nM | CHEMBL_ACT_17910382 |
| MAP2K2 | 7.28 | Kd | 52 | nM | CHEMBL_ACT_17910562 |
| MAP2K1 | 7.1 | IC50 | 80 | nM | CHEMBL_ACT_13294102 |
| MAP2K1 | 7 | Kd | 99 | nM | CHEMBL_ACT_24954243 |
| MAP2K1 | 7 | Kd | 99 | nM | CHEMBL_ACT_24957538 |
| MAP2K1 | 7 | Kd | 99 | nM | CHEMBL_ACT_7569261 |
| SMC2 | 6.68 | Kd | 209 | nM | CHEMBL_ACT_17939714 |
| SMC1A | 6.44 | Kd | 365 | nM | CHEMBL_ACT_17939561 |
| MAP2K2 | 6.28 | Kd | 530 | nM | CHEMBL_ACT_24954244 |
| MAP2K2 | 6.28 | Kd | 530 | nM | CHEMBL_ACT_24957539 |
| MAP2K2 | 6.28 | Kd | 530 | nM | CHEMBL_ACT_7571046 |
| Q6ZSR9 | 6.09 | Kd | 807 | nM | CHEMBL_ACT_17933787 |
| AAK1 | 5.89 | Kd | 1279 | nM | CHEMBL_ACT_17878246 |
| BMP2K | 5.79 | Kd | 1624 | nM | CHEMBL_ACT_17884833 |
| EGFR | 5.66 | Kd | 2200 | nM | CHEMBL_ACT_7569378 |
| CSNK2A2 | 5.55 | Kd | 2807 | nM | CHEMBL_ACT_17895006 |
| EGFR | 5.52 | Kd | 3000 | nM | CHEMBL_ACT_7569371 |
| MAP2K1 | 5.43 | IC50 | 3700 | nM | CHEMBL_ACT_16423360 |
| EGFR | 5.38 | Kd | 4200 | nM | CHEMBL_ACT_7569369 |
| EGFR | 5.3 | Kd | 5000 | nM | CHEMBL_ACT_7569377 |
| EGFR | 5.28 | Kd | 5200 | nM | CHEMBL_ACT_7569370 |
| EGFR | 5.28 | Kd | 5300 | nM | CHEMBL_ACT_7569372 |
Target pathways
Aggregated over 1 target gene(s): MAP2K1.
Top Reactome pathways
61 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| MAPK3 (ERK1) activation | 1 | MAP2K1 |
| RAF-independent MAPK1/3 activation | 1 | MAP2K1 |
| Developmental Biology | 1 | MAP2K1 |
| Cytokine Signaling in Immune system | 1 | MAP2K1 |
| Signal Transduction | 1 | MAP2K1 |
| Disease | 1 | MAP2K1 |
| Toll Like Receptor 4 (TLR4) Cascade | 1 | MAP2K1 |
| MyD88:MAL(TIRAP) cascade initiated on plasma membrane | 1 | MAP2K1 |
| MyD88-independent TLR4 cascade | 1 | MAP2K1 |
| Signaling by NTRKs | 1 | MAP2K1 |
| Toll Like Receptor 9 (TLR9) Cascade | 1 | MAP2K1 |
| Toll Like Receptor 10 (TLR10) Cascade | 1 | MAP2K1 |
| Toll Like Receptor 3 (TLR3) Cascade | 1 | MAP2K1 |
| Toll Like Receptor 5 (TLR5) Cascade | 1 | MAP2K1 |
| Toll Like Receptor TLR1:TLR2 Cascade | 1 | MAP2K1 |
| Toll Like Receptor 7/8 (TLR7/8) Cascade | 1 | MAP2K1 |
| Toll Like Receptor TLR6:TLR2 Cascade | 1 | MAP2K1 |
| Innate Immune System | 1 | MAP2K1 |
| Immune System | 1 | MAP2K1 |
| Toll-like Receptor Cascades | 1 | MAP2K1 |
| Prolonged ERK activation events | 1 | MAP2K1 |
| Frs2-mediated activation | 1 | MAP2K1 |
| Toll Like Receptor 2 (TLR2) Cascade | 1 | MAP2K1 |
| Signaling by NTRK1 (TRKA) | 1 | MAP2K1 |
| Signalling to ERKs | 1 | MAP2K1 |
| L1CAM interactions | 1 | MAP2K1 |
| Axon guidance | 1 | MAP2K1 |
| Signal transduction by L1 | 1 | MAP2K1 |
| Interleukin-1 family signaling | 1 | MAP2K1 |
| Interleukin-17 signaling | 1 | MAP2K1 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| MAPK cascade | 1 |
| regulation of vascular associated smooth muscle contraction | 1 |
| chemotaxis | 1 |
| response to oxidative stress | 1 |
| signal transduction | 1 |
| heart development | 1 |
| negative regulation of cell population proliferation | 1 |
| positive regulation of autophagy | 1 |
| positive regulation of gene expression | 1 |
| negative regulation of gene expression | 1 |
| Schwann cell development | 1 |
| cerebellar cortex formation | 1 |
| central nervous system neuron differentiation | 1 |
| neuron differentiation | 1 |
| keratinocyte differentiation | 1 |
Indications & clinical
Indications
52 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 |
| non-small cell lung carcinoma | 3 | MONDO:0005233 | EFO:0003060 |
| thyroid gland papillary carcinoma | 3 | MONDO:0005075 | EFO:0000641 |
| thyroid gland carcinoma | 3 | MONDO:0015075 | EFO:0002892 |
| uveal melanoma | 3 | MONDO:0006486 | EFO:1000616 |
| plasma cell myeloma | 2 | MONDO:0009693 | EFO:0001378 |
| cutaneous melanoma | 2 | MONDO:0005012 | EFO:0000389 |
| exocrine pancreatic carcinoma | 2 | MONDO:0005192 | EFO:0002618 |
| melanoma | 2 | MONDO:0005105 | EFO:0000756 |
| diffuse large B-cell lymphoma | 2 | MONDO:0018905 | EFO:0000403 |
| adenocarcinoma | 2 | MONDO:0004970 | EFO:0000228 |
| thyroid gland follicular carcinoma | 2 | MONDO:0005034 | EFO:0000501 |
| gastric adenocarcinoma | 2 | MONDO:0005036 | EFO:0000503 |
| squamous cell carcinoma | 2 | MONDO:0005096 | EFO:0000707 |
| squamous cell lung carcinoma | 2 | MONDO:0005097 | EFO:0000708 |
| colorectal neoplasm | 2 | MONDO:0005335 | EFO:0004142 |
| gallbladder neoplasm | 2 | MONDO:0021253 | EFO:0004606 |
| cholangiocarcinoma | 2 | MONDO:0019087 | EFO:0005221 |
| triple-negative breast carcinoma | 2 | MONDO:0005494 | EFO:0005537 |
| gallbladder carcinoma | 2 | MONDO:0003220 | EFO:1001956 |
| metastatic melanoma | 2 | MONDO:0005191 | EFO:0002617 |
| soft tissue sarcoma | 2 | MONDO:0018078 | EFO:1001968 |
| breast neoplasm | 2 | MONDO:0021100 | MONDO:0007254 |
| lung neoplasm | 2 | MONDO:0021117 | MONDO:0008903 |
| plexiform neurofibroma | 2 | MONDO:0003304 | EFO:0000658 |
| malignant peripheral nerve sheath tumor | 2 | MONDO:0017827 | EFO:0000760 |
| neurofibromatosis type 1 | 2 | MONDO:0018975 | MONDO:0018975 |
| sarcoma | 2 | MONDO:0005089 | EFO:0000691 |
| tumor of uterus | 2 | MONDO:0021353 | EFO:0003859 |
| bile duct carcinoma | 2 | MONDO:0005496 | EFO:0005540 |
| Kaposi’s sarcoma | 1 | MONDO:0005055 | EFO:0000558 |
| rectal cancer | 1 | MONDO:0006519 | EFO:1000657 |
| chronic myeloid leukemia | 1 | MONDO:0011996 | EFO:0000339 |
| colon carcinoma | 1 | MONDO:0002032 | EFO:1001950 |
| acute lymphoblastic leukemia | 1 | MONDO:0004967 | EFO:0000220 |
| optic nerve glioma | 1 | MONDO:0003235 | EFO:0009254 |
| astrocytoma (excluding glioblastoma) | 1 | MONDO:0019781 | MONDO:0016691 |
| colonic neoplasm | 1 | MONDO:0005401 | MONDO:0021063 |
| heart failure | 1 | MONDO:0005252 | EFO:0003144 |
| glioma | 1 | MONDO:0021042 | MONDO:0021637 |
12 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 118.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 60 |
| PHASE1 | 37 |
| PHASE1/PHASE2 | 12 |
| PHASE3 | 7 |
| Not specified | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT01933932 | PHASE3 | ACTIVE_NOT_RECRUITING | Assess Efficacy & Safety of Selumetinib in Combination With Docetaxel in Patients Receiving 2nd Line Treatment for v-Ki-ras2 Kirsten Rat Sarcoma Viral Oncogene Homolog (KRAS) Positive NSCLC |
| NCT03871257 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of the Drugs Selumetinib Versus Carboplatin/Vincristine in Patients With Neurofibromatosis and Low-Grade Glioma |
| NCT04166409 | PHASE3 | RECRUITING | A Study of the Drugs Selumetinib vs. Carboplatin and Vincristine in Patients With Low-Grade Glioma |
| NCT04576117 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study to Compare Treatment With the Drug Selumetinib Alone Versus Selumetinib and Vinblastine in Patients With Recurrent or Progressive Low-Grade Glioma |
| NCT04924608 | PHASE3 | ACTIVE_NOT_RECRUITING | Efficacy and Safety of Selumetinib in Adults With NF1 Who Have Symptomatic, Inoperable Plexiform Neurofibromas |
| NCT01843062 | PHASE3 | TERMINATED | Comparing Complete Remission After Treatment With Selumetinib/Placebo in Patient With Differentiated Thyroid Cancer |
| NCT01974752 | PHASE3 | COMPLETED | Selumetinib (AZD6244: ARRY-142886) (Hyd-Sulfate) in Metastatic Uveal Melanoma (SUMIT) |
| NCT01089101 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | Selumetinib in Treating Young Patients With Recurrent or Refractory Low Grade Glioma |
| NCT01362803 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | AZD6244 Hydrogen Sulfate for Children With Nervous System Tumors |
| NCT02151084 | PHASE2 | ACTIVE_NOT_RECRUITING | A Study of Different Dosing Schedules of Selumetinib With Cisplatin/Gemcitabine (CIS/GEM) Versus CIS/GEM Alone in Biliary Cancer |
| NCT02299999 | PHASE2 | ACTIVE_NOT_RECRUITING | SAFIR02_Breast - Efficacy of Genome Analysis as a Therapeutic Decision Tool for Patients With Metastatic Breast Cancer |
| NCT02407405 | PHASE2 | ACTIVE_NOT_RECRUITING | MEK 1/2 Inhibitor Selumetinib (AZD6244 Hydrogen Sulfate) in Adults With Neurofibromatosis Type 1 (NF1) and Inoperable Plexiform Neurofibromas |
| NCT02813135 | PHASE1/PHASE2 | RECRUITING | European Proof-of-Concept Therapeutic Stratification Trial of Molecular Anomalies in Relapsed or Refractory Tumors |
| NCT03155620 | PHASE2 | ACTIVE_NOT_RECRUITING | Targeted Therapy Directed by Genetic Testing in Treating Pediatric Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphomas, or Histiocytic Disorders (The Pediatric MATCH Screening Trial) |
| NCT03392246 | PHASE2 | ACTIVE_NOT_RECRUITING | A Phase 2 Study of Osimertinib in Combination With Selumetinib in EGFR Inhibitor naïve Advanced EGFR Mutant Lung Cancer |
| NCT03944772 | PHASE2 | ACTIVE_NOT_RECRUITING | Phase 2 Platform Study in Patients With Advanced Non-Small Lung Cancer Who Progressed on First-Line Osimertinib Therapy (ORCHARD) |
| NCT05253131 | PHASE2 | NOT_YET_RECRUITING | Trial of Selumetinib and Bromodomain Inhibitor With Durvalumab for Sarcomas |
| NCT05554328 | PHASE2 | RECRUITING | Testing the Use of the Combination of Selumetinib and Olaparib or Selumetinib Alone Targeted Treatment for RAS Pathway Mutant Recurrent or Persistent Ovarian and Endometrial Cancers, A ComboMATCH Treatment Trial |
| NCT05564377 | PHASE2 | RECRUITING | Targeted Therapy Directed by Genetic Testing in Treating Patients With Locally Advanced or Advanced Solid Tumors, The ComboMATCH Screening Trial |
| NCT06188741 | PHASE2 | RECRUITING | Selumetinib for the Prevention of Plexiform Neurofibroma Growth in NF Type 1 |
| NCT06620354 | PHASE2 | NOT_YET_RECRUITING | Clinical Study on the Treatment of Type I Neurofibromatosis With Smeitinib Hydrosulfate Capsule |
| NCT06621082 | PHASE2 | NOT_YET_RECRUITING | The Clinical Study of the Treatment of Patients With Type I Neurofibromatosis With Smetinib Hydrosulfate Capsule |
| NCT06735820 | PHASE1/PHASE2 | NOT_YET_RECRUITING | Early Phase Study Evaluating MEK and MDM2 Inhibition in Patients With NF1 and MPNST |
| NCT06763315 | PHASE2 | NOT_YET_RECRUITING | Low-dose Selumetinib for the Treatment of Plexiform Neurofibromas in Chinese Children |
| NCT00338130 | PHASE2 | COMPLETED | Randomised Study to Compare the Efficacy of AZD6244 vs TMZ |
| NCT00372788 | PHASE2 | COMPLETED | AZD6244 Versus Pemetrexed (Alimta®) in Patients With Non-small Cell Lung Cancer, Who Have Failed One or Two Prior Chemotherapy Regimen |
| NCT00372944 | PHASE2 | COMPLETED | AZD6244 vs. Capecitabine (Xeloda®) in Patients With Advanced or Metastatic Pancreatic Cancer, Who Have Failed First Line Gemcitabine Therapy |
| NCT00514761 | PHASE2 | COMPLETED | Phase II Efficacy Study of AZD6244 in Colorectal Cancer |
| NCT00551070 | PHASE2 | COMPLETED | Selumetinib Sulfate in Treating Woman With Recurrent Low-Grade Ovarian Cancer or Peritoneum Cancer |
| NCT00553332 | PHASE2 | COMPLETED | Selumetinib in Treating Patients With Biliary Cancer That Cannot Be Removed By Surgery |
| NCT00559949 | PHASE2 | COMPLETED | Selumetinib in Treating Patients With Papillary Thyroid Cancer That Did Not Respond to Radioactive Iodine |
| NCT00588809 | PHASE2 | COMPLETED | Selumetinib in Treating Patients With Recurrent or Refractory Acute Myeloid Leukemia |
| NCT00604721 | PHASE2 | COMPLETED | Selumetinib in Treating Patients With Locally Advanced or Metastatic Liver Cancer |
| NCT00780676 | PHASE2 | TERMINATED | Personalized Treatment Selection for Metastatic Breast Cancer |
| NCT00866177 | PHASE2 | COMPLETED | MEK Inhibitor AZD6244 in Treating Patients With Stage III or Stage IV Melanoma |
| NCT00888134 | PHASE2 | COMPLETED | Selumetinib in Cancers With BRAF Mutations |
| NCT00890825 | PHASE2 | COMPLETED | AZD6244 in Combination With Docetaxel Versus Docetaxel Alone in KRAS Mutation Positive NSCLC Patients |
| NCT00936221 | PHASE2 | COMPLETED | Comparison of AZD6244 in Combination With Dacarbazine Versus (vs) Dacarbazine Alone in BRAF Mutation Positive Melanoma Patients |
| NCT01011933 | PHASE2 | COMPLETED | Selumetinib in Treating Patients With Recurrent or Persistent Endometrial Cancer |
| NCT01029418 | PHASE1/PHASE2 | TERMINATED | AZD6244 and Sorafenib in Advanced Hepatocellular Carcinoma |
Clinical evidence (CIViC)
Variant × indication × effect (68 predictive associations from 73 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| NF1 Mutation | Plexiform Neurofibroma | Sensitivity/Response | Selumetinib | CIViC A | EID11176 +2 |
| KRAS Mutation | Lung Non-small Cell Carcinoma | Resistance | Selumetinib + Docetaxel | CIViC A | EID2998 |
| BRAF V600E | High Grade Glioma | Sensitivity/Response | Selumetinib | CIViC B | EID2145 +1 |
| KIAA1549::BRAF Fusion | Childhood Pilocytic Astrocytoma | Sensitivity/Response | Selumetinib | CIViC B | EID7486 +1 |
| BRAF V600E | Childhood Pilocytic Astrocytoma | Sensitivity/Response | Selumetinib | CIViC B | EID7485 |
| BRAF V600E OR KIAA1549::BRAF Fusion | Pilocytic Astrocytoma | Sensitivity/Response | Selumetinib | CIViC B | EID11316 |
| BRAF V600E OR NRAS Mutation OR HRAS Mutation OR KRAS Mutation OR NF1 Inactivating Mutation | Cancer | Sensitivity/Response | Selumetinib | CIViC B | EID11696 |
| BRAF V600E OR NRAS Mutation OR HRAS Mutation OR KRAS Mutation OR NF1 Mutation | Cancer | Sensitivity/Response | Selumetinib | CIViC B | EID11681 |
| GNA11 Q209 | Uveal Melanoma | Sensitivity/Response | Selumetinib | CIViC B | EID1212 |
| GNAQ Q209 | Uveal Melanoma | Sensitivity/Response | Selumetinib | CIViC B | EID1213 |
| KIT RS3733542 | Acute Myeloid Leukemia | Sensitivity/Response | Selumetinib | CIViC B | EID1136 |
| KRAS Exon 2 Mutation | Colorectal Cancer | Sensitivity/Response | Selumetinib + Irinotecan | CIViC B | EID1326 |
| KRAS G12C | Lung Non-small Cell Carcinoma | Sensitivity/Response | Docetaxel + Selumetinib | CIViC B | EID1142 |
| KRAS G12V | Lung Non-small Cell Carcinoma | Sensitivity/Response | Selumetinib + Docetaxel | CIViC B | EID1143 |
| KRAS Mutation | Colorectal Cancer | Sensitivity/Response | Cetuximab + Selumetinib | CIViC B | EID4866 |
| KRAS Mutation | Lung Non-small Cell Carcinoma | Sensitivity/Response | Selumetinib + Erlotinib | CIViC B | EID4868 |
| KRAS Mutation | Lung Non-small Cell Carcinoma | Sensitivity/Response | Selumetinib + Docetaxel | CIViC B | EID999 |
| NF1 Mutation | Childhood Low-grade Glioma | Sensitivity/Response | Selumetinib | CIViC B | EID7487 |
| FLT3 ITD | Acute Myeloid Leukemia | Resistance | Selumetinib | CIViC B | EID1137 |
| MAP2K1 Q56_V60del | Ovarian Serous Carcinoma | Sensitivity/Response | Selumetinib | CIViC C | EID1661 |
| NF1 D1644H AND NF1 Q1189* | Diffuse Astrocytoma | Sensitivity/Response | Selumetinib | CIViC C | EID12342 |
| NF1 Mutation AND Methylation signature PA-NF1 | Malignant Astrocytoma | Sensitivity/Response | Selumetinib | CIViC C | EID12270 |
| NF1 Splice Site (c.205-1G>C) AND NF1 G629R | Pilocytic Astrocytoma | Sensitivity/Response | Vincristine + Carboplatin + Trametinib + Selumetinib | CIViC C | EID12271 |
| NRAS Q61 | Skin Melanoma | Sensitivity/Response | Selumetinib | CIViC C | EID1473 |
| MAP2K1 K57N | Melanoma | Resistance | Selumetinib | CIViC C | EID7709 |
| BRAF V600E | Melanoma | Sensitivity/Response | Selumetinib | CIViC D | EID2129 +1 |
| ATM F858L | Lung Cancer | Sensitivity/Response | Selumetinib | CIViC D | EID5127 |
| BRAF V600E | Melanoma | Sensitivity/Response | Dactolisib + Selumetinib | CIViC D | EID1005 |
| ERBB3 Overexpression | Cancer | Sensitivity/Response | Selumetinib + Afatinib | CIViC D | EID1152 |
| FLT3 ITD OR FLT3 TKD MUTATION OR NRAS EXON 2-3 MUTATION OR PTPN11 Mutation OR KRAS Exon 2-3 Mutation | Acute Lymphoblastic Leukemia | Sensitivity/Response | Selumetinib | CIViC D | EID12553 |
+38 more predictive associations (showing top 30 by level).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 12 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
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.
49 molecules share ≥1 primary target. Top 49 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| BINIMETINIB | ChEMBL + PubChem | Phase 4 (approved) | MAP2K1 |
| TRAMETINIB | ChEMBL + PubChem | Phase 4 (approved) | MAP2K1 |
| AXITINIB | ChEMBL | Phase 4 (approved) | MAP2K1 |
| BOSUTINIB | ChEMBL | Phase 4 (approved) | MAP2K1 |
| COBIMETINIB | ChEMBL | Phase 4 (approved) | MAP2K1 |
| DASATINIB | ChEMBL | Phase 4 (approved) | MAP2K1 |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | MAP2K1 |
| GILTERITINIB | ChEMBL | Phase 4 (approved) | MAP2K1 |
| NERATINIB | ChEMBL | Phase 4 (approved) | MAP2K1 |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | MAP2K1 |
| RUXOLITINIB | ChEMBL | Phase 4 (approved) | MAP2K1 |
| SORAFENIB | ChEMBL | Phase 4 (approved) | MAP2K1 |
| SUNITINIB | ChEMBL | Phase 4 (approved) | MAP2K1 |
| TOFACITINIB | ChEMBL | Phase 4 (approved) | MAP2K1 |
| VANDETANIB | ChEMBL | Phase 4 (approved) | MAP2K1 |
| VEMURAFENIB | ChEMBL | Phase 4 (approved) | MAP2K1 |
| AVUTOMETINIB | ChEMBL | Phase 3 | MAP2K1 |
| CANERTINIB | ChEMBL | Phase 3 | MAP2K1 |
| DOVITINIB | ChEMBL | Phase 3 | MAP2K1 |
| LESTAURTINIB | ChEMBL | Phase 3 | MAP2K1 |
| LINSITINIB | ChEMBL | Phase 3 | MAP2K1 |
| ORANTINIB | ChEMBL | Phase 3 | MAP2K1 |
| SARACATINIB | ChEMBL | Phase 3 | MAP2K1 |
| CENISERTIB | ChEMBL | Phase 2 | MAP2K1 |
| CEP-32496 | ChEMBL | Phase 2 | MAP2K1 |
| CI-1040 | ChEMBL | Phase 2 | MAP2K1 |
| DEFOSBARASERTIB | ChEMBL | Phase 2 | MAP2K1 |
| E-6201 | ChEMBL | Phase 2 | MAP2K1 |
| FORETINIB | ChEMBL | Phase 2 | MAP2K1 |
| ILORASERTIB | ChEMBL | Phase 2 | MAP2K1 |
| MIRDAMETINIB | ChEMBL | Phase 2 | MAP2K1 |
| PELITINIB | ChEMBL | Phase 2 | MAP2K1 |
| PIMASERTIB | ChEMBL | Phase 2 | MAP2K1 |
| R-406 | ChEMBL | Phase 2 | MAP2K1 |
| REFAMETINIB | ChEMBL | Phase 2 | MAP2K1 |
| SOTRASTAURIN | ChEMBL | Phase 2 | MAP2K1 |
| SU-014813 | ChEMBL | Phase 2 | MAP2K1 |
| TAK-733 | ChEMBL | Phase 2 | MAP2K1 |
| TOLONIUM CHLORIDE | ChEMBL | Phase 2 | MAP2K1 |
| TOZASERTIB | ChEMBL | Phase 2 | MAP2K1 |
| ZAPNOMETINIB | ChEMBL | Phase 2 | MAP2K1 |
| Afatinib | PubChem | Approved | MAP2K1 |
| Crizotinib | PubChem | Approved | MAP2K1 |
| dacomitinib | PubChem | Approved | MAP2K1 |
| Fostamatinib | PubChem | Approved | MAP2K1 |
| Gefitinib | PubChem | Approved | MAP2K1 |
| Idelalisib | PubChem | Approved | MAP2K1 |
| Pazopanib | PubChem | Approved | MAP2K1 |
| regorafenib | PubChem | Approved | MAP2K1 |
Related Atlas pages
- Genes: MAP2K1
- Diseases: neoplasm, non-small cell lung carcinoma, thyroid gland papillary carcinoma, thyroid gland carcinoma, uveal melanoma, plexiform neurofibroma, malignant glioma, childhood pilocytic astrocytoma, pilocytic astrocytoma, cancer, acute myeloid leukemia by FAB classification, colorectal carcinoma, childhood low-grade glioma, ovarian serous adenocarcinoma, diffuse astrocytoma, anaplastic astrocytoma, cutaneous melanoma, melanoma, lung carcinoma, acute lymphoblastic leukemia
- Drugs: Binimetinib, Trametinib, Axitinib, Bosutinib, Cobimetinib, Dasatinib, Fedratinib, Gilteritinib, Neratinib, Nintedanib, Ruxolitinib, Sorafenib, Sunitinib, Tofacitinib, Vandetanib, Vemurafenib, Avutometinib, Canertinib, Dovitinib, Lestaurtinib, Linsitinib, Orantinib, Saracatinib, Afatinib, Crizotinib, dacomitinib, Fostamatinib, Gefitinib, Idelalisib, Pazopanib, regorafenib
- Biomarker genes: BRAF, FLT3, GNA11, GNAQ, HRAS, KIT, KRAS, NF1, NF2, NRAS