All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

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

Stem definition	Drug id	CAS RN
MEK (MAPK kinase) tyrosine kinase inhibitors	5388	606143-52-6

Description:

Molecule

Description

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:

Date	Agency	Company	Orphan
April 10, 2020	FDA	ASTRAZENECA LP

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Paronychia	66.65	44.79	12	164	6480	64492076
Blood creatine phosphokinase increased	49.34	44.79	14	162	58544	64440012

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01EE04	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Mitogen-activated protein kinase (MEK) inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000193943	Mitogen-Activated Protein Kinase Kinase 1 Inhibitors
FDA MoA	N0000193944	Mitogen-Activated Protein Kinase Kinase 2 Inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:79091	MEK inhibitor
CHEBI has role	CHEBI:149553	anticoronaviral drug

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Neurofibromatosis type 1	indication	92824003	DOID:0111253

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.84	acidic
pKa2	3.24	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 10MG BASE	KOSELUGO	ASTRAZENECA	N213756	April 10, 2020	RX	CAPSULE	ORAL	9562017	Dec. 12, 2026	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	9562017	Dec. 12, 2026	TREATMENT OF PEDIATRIC PATIENTS 2 YEARS OF AGE AND OLDER WITH NEUROFIBROMATOSIS TYPE 1 (NF1) WHO HAVE SYMPTOMATIC, INOPERABLE PLEXIFORM NEUROFIBROMAS (PN)

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Dual specificity mitogen-activated protein kinase kinase 1	Kinase	Q02750	MP2K1_HUMAN	INHIBITOR	IC50	7.85		SCIENTIFIC LITERATURE	DRUG LABEL
Dual specificity mitogen-activated protein kinase kinase 2	Kinase	P36507	MP2K2_HUMAN	INHIBITOR	IC50	7.85		SCIENTIFIC LITERATURE	DRUG LABEL
BMP-2-inducible protein kinase	Kinase	Q9NSY1	BMP2K_HUMAN		Kd	5.79		CHEMBL
Casein kinase II subunit alpha'	Kinase	P19784	CSK22_HUMAN		Kd	5.55		CHEMBL
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN		Kd	5.66		CHEMBL
Structural maintenance of chromosomes protein 1A	Unclassified	Q14683	SMC1A_HUMAN		Kd	6.44		CHEMBL
Uncharacterized protein FLJ45252	Unclassified	Q6ZSR9	YJ005_HUMAN		Kd	6.09		CHEMBL
Structural maintenance of chromosomes protein 2	Unclassified	O95347	SMC2_HUMAN		Kd	6.68		CHEMBL
AP2-associated protein kinase 1	Kinase	Q2M2I8	AAK1_HUMAN		Kd	5.89		CHEMBL

External reference:

ID	Source
6UH91I579U	UNII
C2980074	UMLSCUI
CHEBI:90227	CHEBI
3EW	PDB_CHEM_ID
CHEMBL1614701	ChEMBL_ID
10127622	PUBCHEM_CID
DB11689	DRUGBANK_ID
CHEMBL2105684	ChEMBL_ID
D10024	KEGG_DRUG
5665	IUPHAR_LIGAND_ID
2289380	RXNORM
332908	MMSL
38304	MMSL
d09410	MMSL
870689004	SNOMEDCT_US
870753001	SNOMEDCT_US
4039314	VANDF
018323	NDDF
018324	NDDF
C517975	MESH_SUPPLEMENTAL_RECORD_UI
9078	INN_ID
943332-08-9	SECONDARY_CAS_RN

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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