Avutometinib
Avmapki Fakzynja Co-pack (avutometinib) is a small molecule pharmaceutical. Avutometinib was first approved as Avmapki fakzynja co-pack (copackaged) on 2025-05-08. It is known to target dual specificity mitogen-activated protein kinase kinase 1 and RAF proto-oncogene serine/threonine-protein kinase.
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Commercial
Therapeutic Areas
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Trade Name
FDA
EMA
Combinations
Avmapki fakzynja co-pack
Drug Products
FDA
EMA
Labels
FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| avmapki fakzynja co-pack | New Drug Application | 2025-05-01 |
Indications
FDA
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Agency Specific
FDA
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Patent Expiration
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ATC Codes
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Clinical
Clinical Trials
28 clinical trials
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Indications Phases 4
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Indications Phases 3
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Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Lung neoplasms | D008175 | — | C34.90 | 3 | 3 | — | — | — | 5 |
| Non-small-cell lung carcinoma | D002289 | — | — | 4 | 3 | — | — | — | 5 |
| Neoplasms | D009369 | — | C80 | 4 | 3 | — | — | — | 5 |
| Ovarian neoplasms | D010051 | EFO_0003893 | C56 | 1 | 2 | — | — | — | 3 |
| Pancreatic neoplasms | D010190 | EFO_0003860 | C25 | 2 | 2 | — | — | — | 3 |
| Endometrioid carcinoma | D018269 | — | — | 1 | 1 | — | — | — | 2 |
| Colorectal neoplasms | D015179 | — | — | 1 | 2 | — | — | — | 2 |
| Neoplasm metastasis | D009362 | EFO_0009708 | — | 2 | 2 | — | — | — | 2 |
| Glioblastoma | D005909 | EFO_0000515 | — | 2 | 1 | — | — | — | 2 |
| Brain neoplasms | D001932 | EFO_0003833 | C71 | 2 | 1 | — | — | — | 2 |
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Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Multiple myeloma | D009101 | — | C90.0 | 1 | — | — | — | — | 1 |
| Neuroblastoma | D009447 | EFO_0000621 | — | 1 | — | — | — | — | 1 |
| Glioma | D005910 | EFO_0000520 | — | 1 | — | — | — | — | 1 |
| Central nervous system neoplasms | D016543 | — | — | 1 | — | — | — | — | 1 |
| Plexiform neurofibroma | D018318 | EFO_0000658 | — | 1 | — | — | — | — | 1 |
| Nervous system neoplasms | D009423 | — | — | 1 | — | — | — | — | 1 |
| Optic nerve glioma | D020339 | — | — | 1 | — | — | — | — | 1 |
| Neurofibromatoses | D017253 | — | Q85.00 | 1 | — | — | — | — | 1 |
| Neurofibroma | D009455 | EFO_0000622 | — | 1 | — | — | — | — | 1 |
Indications Without Phase
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Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | Avutometinib |
| INN | avutometinib |
| Description | CH5126766 is a member of the class of coumarins that is 4-methyl-7-[(pyrimidin-2-yl)oxy]coumarin carrying an additional [2-[(methylaminosulfonyl)amino]-3-fluoropyridin-4-yl]methyl substituent at position 3. It has a role as an EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor and an antineoplastic agent. It is an aryloxypyrimidine, a member of coumarins, a member of pyridines, an organofluorine compound and a member of sulfamides. |
| Classification | Small molecule |
| Drug class | tyrosine kinase inhibitors: tyrosine kinase inhibitors; MEK (MAPK kinase) inhibitors |
| Image (chem structure or protein) |  |
| Structure (InChI/SMILES or Protein Sequence) | CNS(=O)(=O)Nc1nccc(Cc2c(C)c3ccc(Oc4ncccn4)cc3oc2=O)c1F |
Identifiers
| PDB | — |
| CAS-ID | 946128-88-7 |
| RxCUI | — |
| ChEMBL ID | CHEMBL3264002 |
| ChEBI ID | 78825 |
| PubChem CID | 16719221 |
| DrugBank | DB15254 |
| UNII ID | D0D4252V97 (ChemIDplus, GSRS) |
Target
Agency Approved
No data
Alternate
MAP2K1
MAP2K1
RAF1
RAF1
Organism
Homo sapiens
Gene name
MAP2K1
Gene synonyms
MEK1, PRKMK1
NCBI Gene ID
Protein name
dual specificity mitogen-activated protein kinase kinase 1
Protein synonyms
ERK activator kinase 1, MAPK/ERK kinase 1, MAPKK 1, MEK 1, protein kinase, mitogen-activated, kinase 1 (MAP kinase kinase 1)
Uniprot ID
Mouse ortholog
Map2k1 (26395)
dual specificity mitogen-activated protein kinase kinase 1 (P31938)
Variants
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Financial
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Trends
PubMed Central
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Safety
Black-box Warning
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Adverse Events
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363 adverse events reported
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