selumetinib Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
MEK (MAPK kinase) tyrosine kinase inhibitors 5388 606143-52-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • selumetinib
  • selumetinib sulfate
  • koselugo
  • AZD6244
  • ARRY-142886
Selumetinib is an inhibitor of mitogen-activated protein kinase kinases 1 and 2 (MEK1/2). MEK1/2 proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway. Both MEK and ERK are critical components of the RAS-regulated RAF-MEK-ERK pathway, which is often activated in different types of cancers
  • Molecular weight: 457.68
  • Formula: C17H15BrClFN4O3
  • CLOGP: 3.73
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 3
  • TPSA: 88.41
  • ALOGS: -4.34
  • ROTB: 6

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
April 10, 2020 FDA ASTRAZENECA LP

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EE04 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Mitogen-activated protein kinase (MEK) inhibitors
CHEBI has role CHEBI:35610 cytostatic
CHEBI has role CHEBI:79091 mitogen-activated protein kinase inhibitors
CHEBI has role CHEBI:149553 anti-coronaviral agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Neurofibromatosis type 1 indication 92824003 DOID:0111253

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.84 acidic
pKa2 3.24 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 10MG BASE KOSELUGO ASTRAZENECA N213756 April 10, 2020 RX CAPSULE ORAL April 10, 2025 NEW CHEMICAL ENTITY
EQ 25MG BASE KOSELUGO ASTRAZENECA N213756 April 10, 2020 RX CAPSULE ORAL April 10, 2025 NEW CHEMICAL ENTITY
EQ 10MG BASE KOSELUGO ASTRAZENECA N213756 April 10, 2020 RX CAPSULE ORAL April 10, 2027 INDICATED FOR THE TREATMENT OF PEDIATRIC PATIENTS 2 YEARS OF AGE AND OLDER WITH NEUROFIBROMATOSIS TYPE 1 (NF1) WHO HAVE SYMPTOMATIC, INOPERABLE PLEXIFORM NEUROFIBROMAS (PN)
EQ 25MG BASE KOSELUGO ASTRAZENECA N213756 April 10, 2020 RX CAPSULE ORAL April 10, 2027 INDICATED FOR THE TREATMENT OF PEDIATRIC PATIENTS 2 YEARS OF AGE AND OLDER WITH NEUROFIBROMATOSIS TYPE 1 (NF1) WHO HAVE SYMPTOMATIC, INOPERABLE PLEXIFORM NEUROFIBROMAS (PN)

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Dual specificity mitogen-activated protein kinase kinase 1 Kinase INHIBITOR IC50 7.85 SCIENTIFIC LITERATURE DRUG LABEL
Dual specificity mitogen-activated protein kinase kinase 2 Kinase INHIBITOR IC50 7.85 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
943332-08-9 SECONDARY_CAS_RN
4039314 VANDF
C1541456 UMLSCUI
CHEBI:90227 CHEBI
3EW PDB_CHEM_ID
CHEMBL1614701 ChEMBL_ID
CHEMBL2105684 ChEMBL_ID
10127622 PUBCHEM_CID
D10024 KEGG_DRUG
5665 IUPHAR_LIGAND_ID
C517975 MESH_SUPPLEMENTAL_RECORD_UI
9078 INN_ID
DB11689 DRUGBANK_ID
6UH91I579U UNII
2289380 RXNORM
332908 MMSL
38304 MMSL
d09410 MMSL
018323 NDDF
018324 NDDF
870689004 SNOMEDCT_US
870753001 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
KOSELUGO HUMAN PRESCRIPTION DRUG LABEL 1 0310-0610 CAPSULE 10 mg ORAL NDA 28 sections
KOSELUGO HUMAN PRESCRIPTION DRUG LABEL 1 0310-0625 CAPSULE 25 mg ORAL NDA 28 sections