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Momelotinib
Momelotinib is a small molecule pharmaceutical. It is currently being investigated in clinical studies. The pharmaceutical is active against tyrosine-protein kinase JAK1 and tyrosine-protein kinase JAK2. In addition, it is known to target tyrosine-protein kinase JAK3 and serine/threonine-protein kinase ULK3.
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Commercial
Therapeutic Areas
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Trade Name
FDA
EMA
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Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
No data
Labels
FDA
EMA
No data
Indications
FDA
EMA
No data
Agency Specific
FDA
EMA
No data
Patent Expiration
No data
ATC Codes
No data
HCPCS
No data
Clinical
Clinical Trials
13 clinical trials
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Indications Phases 4
No data
Indications Phases 3
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Primary myelofibrosisD055728D47.4243—18
Pancreatic ductal carcinomaD021441——1——1
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Essential thrombocythemiaD013920D47.3—2———2
Polycythemia veraD011087D45—2———2
Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Pancreatic neoplasmsD010190EFO_0003860C251————1
Non-small-cell lung carcinomaD0022891————1
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameMOMELOTINIB
INNmomelotinib
Description
Momelotinib is a benzamide obtained by formal condensation of the carboxy group of 4-{2-[4-(morpholin-4-yl)anilino]pyrimidin-4-yl}benzoic acid with the primary amino group of aminoacetonitrile. It is an ATP-competitive JAK1/JAK2 inhibitor with IC50 of 11 nM and 18 nM, respectively. Used for the treatment of patients with intermediate- or high-risk myelofibrosis. It has a role as an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor, an antineoplastic agent, an anti-anaemic agent and an apoptosis inducer. It is an aminopyrimidine, a member of morpholines, a secondary amino compound, a tertiary amino compound, a member of benzamides and a nitrile.
Classification
Small molecule
Drug classtyrosine kinase inhibitors
Image (chem structure or protein)
Structure (InChI/SMILES or Protein Sequence)
N#CCNC(=O)c1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1
Identifiers
PDB6FDZ
CAS-ID1056634-68-4
RxCUI—
ChEMBL IDCHEMBL1078178
ChEBI ID—
PubChem CID25062766
DrugBankDB11763
UNII ID6O01GMS00P (ChemIDplus, GSRS)
Target
Agency Approved
JAK1
JAK1
JAK2
JAK2
Organism
Homo sapiens
Gene name
JAK1
Gene synonyms
JAK1A, JAK1B
NCBI Gene ID
3716
Protein name
tyrosine-protein kinase JAK1
Protein synonyms
JAK-1, Janus kinase 1
Uniprot ID
Q9UD26
Mouse ortholog
Jak1 (16451)
tyrosine-protein kinase JAK1 (P52332)
Alternate
JAK3
JAK3
ULK3
ULK3
Organism
Homo sapiens
Gene name
JAK3
Gene synonyms
NCBI Gene ID
3718
Protein name
tyrosine-protein kinase JAK3
Protein synonyms
JAK-3, Janus kinase 3, Janus kinase 3 (a protein tyrosine kinase, leukocyte), L-JAK, Leukocyte janus kinase
Uniprot ID
Q9Y6S2
Mouse ortholog
Jak3 (16453)
tyrosine-protein kinase JAK3 (Q62137)
Variants
Clinical Variant
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 572 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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11 adverse events reported
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