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Koselugo(selumetinib)
Koselugo (selumetinib) is a small molecule pharmaceutical. Selumetinib was first approved as Koselugo on 2020-04-10. It is used to treat neurofibromatosis 1 in the USA. It has been approved in Europe to treat neurofibromatosis 1. The pharmaceutical is active against dual specificity mitogen-activated protein kinase kinase 1. In addition, it is known to target serine/threonine-protein kinase B-raf.
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FDA Novel Drug Approvals 2020
Commercial
Therapeutic Areas
Therapeutic Area
MeSH
neoplasmsD009369
nervous system diseasesD009422
hereditary congenital and neonatal diseases and abnormalitiesD009358
Trade Name
FDA
EMA
Koselugo
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Selumetinib sulfate
Tradename
Company
Number
Date
Products
KOSELUGOAstraZenecaN-213756 RX2020-04-10
2 products, RLD, RS
Labels
FDA
EMA
Brand Name
Status
Last Update
koselugoNew Drug Application2020-05-12
Indications
FDA
EMA
Indication
Ontology
MeSH
ICD-10
neurofibromatosis 1—D009456Q85.01
Agency Specific
FDA
EMA
Expiration
Code
SELUMETINIB SULFATE, KOSELUGO, ASTRAZENECA
2027-04-10ODE-288
2025-04-10NCE
Patent Expiration
Patent
Expires
Flag
FDA Information
Selumetinib Sulfate, Koselugo, Astrazeneca
91567952026-12-12DS, DP
95620172026-12-12DPU-2800
74256372024-03-13DP
81786932023-03-13DS, DP
ATC Codes
L: Antineoplastic and immunomodulating agents
— L01: Antineoplastic agents
— L01E: Protein kinase inhibitors, antineoplastic and immunomodulating agents
— L01EE: Mitogen-activated protein kinase (mek) inhibitors
— L01EE04: Selumetinib
HCPCS
No data
Clinical
Clinical Trials
121 clinical trials
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Mock data
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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
Neurofibromatosis 1D009456Q85.01782——13
Plexiform neurofibromaD018318EFO_0000658331——5
Thyroid neoplasmsD013964EFO_0003841—21—14
Small cell lung carcinomaD055752—21——3
GliomaD005910EFO_0000520—21——3
AstrocytomaD001254EFO_0000271112——3
Uveal neoplasmsD014604EFO_1001230111——3
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Non-small-cell lung carcinomaD002289914———20
NeoplasmsD009369C80101———11
MelanomaD00854546———10
Breast neoplasmsD001943EFO_0003869C5034———7
Pancreatic neoplasmsD010190EFO_0003860C2526———7
Colorectal neoplasmsD01517934———6
Lung neoplasmsD008175C34.9033———5
Biliary tract neoplasmsD001661C24.931———4
AdenocarcinomaD000230—3———3
Triple negative breast neoplasmsD06472613———3
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Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Healthy volunteers/patients—4————4
Colonic neoplasmsD003110C183————3
Rectal neoplasmsD0120042————2
Primary myelofibrosisD055728D47.41————1
Bcr-abl positive chronic myelogenous leukemiaD015464EFO_00003401————1
Head and neck neoplasmsD0062581————1
Urinary bladder neoplasmsD001749C671————1
Kidney neoplasmsD007680EFO_0003865C641————1
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameSELUMETINIB
INNselumetinib
Description
Selumetinib is 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. It has a role as an EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor, an antineoplastic agent and an anticoronaviral agent. It is a member of benzimidazoles, a hydroxamic acid ester, a member of monochlorobenzenes, a member of bromobenzenes, an organofluorine compound and a secondary amino compound.
Classification
Small molecule
Drug classtyrosine kinase inhibitors: tyrosine kinase inhibitors; MEK (MAPK kinase) inhibitors
Image (chem structure or protein)
Structure (InChI/SMILES or Protein Sequence)
Cn1cnc2c(F)c(Nc3ccc(Br)cc3Cl)c(C(=O)NOCCO)cc21
Identifiers
PDB7M0T
CAS-ID606143-52-6
RxCUI—
ChEMBL IDCHEMBL1614701
ChEBI ID90227
PubChem CID10127622
DrugBankDB11689
UNII ID6UH91I579U (ChemIDplus, GSRS)
Target
Agency Approved
MAP2K1
MAP2K1
Organism
Homo sapiens
Gene name
MAP2K1
Gene synonyms
MEK1, PRKMK1
NCBI Gene ID
5604
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
Q02750
Mouse ortholog
Map2k1 (26395)
dual specificity mitogen-activated protein kinase kinase 1 (P31938)
Alternate
BRAF
BRAF
Organism
Homo sapiens
Gene name
BRAF
Gene synonyms
BRAF1, RAFB1
NCBI Gene ID
673
Protein name
serine/threonine-protein kinase B-raf
Protein synonyms
94 kDa B-raf protein, B-Raf proto-oncogene serine/threonine-protein kinase (p94), B-Raf serine/threonine-protein, murine sarcoma viral (v-raf) oncogene homolog B1, p94, Proto-oncogene B-Raf, v-raf murine sarcoma viral oncogene homolog B, v-Raf murine sarcoma viral oncogene homolog B1
Uniprot ID
Q9Y6T3
Mouse ortholog
Braf (109880)
serine/threonine-protein kinase B-raf (P28028)
Variants
Clinical Variant
No data
Financial
Koselugo - AstraZeneca
$
€
£
₣
Mock data
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Tabular view
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 4,997 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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204 adverse events reported
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