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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

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:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	0.15 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

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Date	Agency	Company
April 10, 2020	FDA	ASTRAZENECA LP
June 17, 2021	EMA	ASTRAZENECA AB
Sept. 26, 2022	PMDA	ALEXION PHARMA GK

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FDA Adverse Event Reporting System (Female)

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FDA Adverse Event Reporting System (Male)

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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
Blood creatine phosphokinase increased	75.56	57.58	21	156	44836	34911918
Paronychia	66.98	57.58	12	165	3393	34953361

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FDA Adverse Event Reporting System (Geriatric)

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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
Blood creatine phosphokinase increased	107.90	38.66	29	300	66061	79677998
Paronychia	102.81	38.66	19	310	7789	79736270
Dermatitis acneiform	50.68	38.66	11	318	9982	79734077

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01EE04	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Mitogen-activated protein kinase (MEK) inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:79091	MEK inhibitor
CHEBI has role	CHEBI:149553	anticoronaviral drug
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

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

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Disease	Relation	SNOMED_ID	DOID
Neurofibromatosis type 1	indication	92824003	DOID:0111253
Plexiform neurofibroma	indication	403818001	DOID:5151

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🐶 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)

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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)

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Orange Book exclusivity data (new drug applications)

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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 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, 2025	NEW CHEMICAL ENTITY
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)

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	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

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External reference:

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ID	Source
018323	NDDF
018324	NDDF
10127622	PUBCHEM_CID
1217205000	SNOMEDCT_US
2289380	RXNORM
332908	MMSL
38304	MMSL
3EW	PDB_CHEM_ID
4039314	VANDF
5665	IUPHAR_LIGAND_ID

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Pharmaceutical products:

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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

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