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

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

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5290	606143-89-9

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: binimetinib mektovi MEK162 ARRY-162 ARRY-438162

Binimetinib is a reversible inhibitor of mitogen-activated extracellular signal regulated kinase 1 (MEK1) and MEK2 activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway. In vitro, binimetinib inhibited extracellular signal-related kinase (ERK) phosphorylation in cellfree assays as well as viability and MEK-dependent phosphorylation of BRAF-mutant human melanoma cell lines. Binimetinib also inhibited in vivo ERK phosphorylation and tumor growth in BRAF-mutant murine xenograft models. Molecular weight: 441.23 Formula: C17H15BrF2N4O3 CLOGP: 3.16 LIPINSKI: 0 HAC: 7 HDO: 3 TPSA: 88.41 ALOGS: -3.95 ROTB: 6 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

Dose	Unit	Route
90	mg	O

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Sept. 20, 2018	EMA	Pierre Fabre Medicament
June 27, 2018	FDA	ARRAY BIOPHARMA INC
Jan. 8, 2019	PMDA	ONO PHARMACEUTICAL CO., LTD.

FDA Adverse Event Reporting System (Female)

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
Serous retinal detachment	361.22	35.18	46	1382	191	50603505
Neoplasm progression	93.74	35.18	34	1394	29123	50574573
Serous retinopathy	76.11	35.18	9	1419	16	50603680
Off label use	47.27	35.18	62	1366	474364	50129332
Retinal detachment	45.67	35.18	13	1415	5116	50598580
Macular detachment	40.96	35.18	6	1422	79	50603617
Pyrexia	39.81	35.18	51	1377	380152	50223544
Hepatic function abnormal	36.51	35.18	18	1410	32663	50571033

FDA Adverse Event Reporting System (Male)

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
Serous retinal detachment	372.16	35.29	55	1614	365	29572493
Serous retinopathy	95.63	35.29	14	1655	85	29572773
Neoplasm progression	92.66	35.29	36	1633	18576	29554282

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
Serous retinal detachment	684.97	31.74	98	3022	600	64495012
Neoplasm progression	178.67	31.74	69	3051	40895	64454717
Serous retinopathy	166.70	31.74	23	3097	102	64495510
Death	63.93	31.74	96	3024	482609	64013003
Retinal detachment	63.39	31.74	21	3099	7955	64487657
Off label use	61.04	31.74	109	3011	632697	63862915
Pyrexia	56.09	31.74	98	3022	558546	63937066
Blood creatine phosphokinase increased	55.99	31.74	35	3085	58523	64437089
Vision blurred	48.75	31.74	38	3082	90278	64405334
Hepatic function abnormal	48.19	31.74	33	3087	64280	64431332
Nausea	39.40	31.74	104	3016	785696	63709916
Macular detachment	39.39	31.74	7	3113	185	64495427
Disease progression	39.38	31.74	41	3079	141639	64353973
Hospice care	37.31	31.74	14	3106	7611	64488001
Second primary malignancy	33.99	31.74	15	3105	12322	64483290
Uveitis	33.57	31.74	15	3105	12693	64482919
Colitis	32.31	31.74	25	3095	58649	64436963

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01EE03	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:68495	Type I cell-death inducers
CHEBI has role	CHEBI:79091	MEK inhibitor

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

Disease	Relation	SNOMED_ID	DOID
Metastatic malignant melanoma	indication	443493003
Unresectable malignant melanoma with BRAF gene mutation	indication	830150003
BRAF mutation-positive colorectal cancer	indication

🐶 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	4.05	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
15MG	MEKTOVI	ARRAY BIOPHARMA INC	N210498	June 27, 2018	RX	TABLET	ORAL	8193229	March 13, 2023	METHOD OF TREATING MELANOMA
15MG	MEKTOVI	ARRAY BIOPHARMA INC	N210498	June 27, 2018	RX	TABLET	ORAL	8513293	March 13, 2023	INDICATED IN COMBINATION WITH ENCORAFENIB FOR THE TREATMENT OF MELANOMA
15MG	MEKTOVI	ARRAY BIOPHARMA INC	N210498	June 27, 2018	RX	TABLET	ORAL	10005761	Aug. 27, 2030	INDICATED IN COMBINATION WITH ENCORAFENIB FOR THE TREATMENT OF MELANOMA
15MG	MEKTOVI	ARRAY BIOPHARMA INC	N210498	June 27, 2018	RX	TABLET	ORAL	9850229	Aug. 27, 2030	INDICATED IN COMBINATION WITH ENCORAFENIB FOR THE TREATMENT OF MELANOMA WITH A BRAF MUTATION
15MG	MEKTOVI	ARRAY BIOPHARMA INC	N210498	June 27, 2018	RX	TABLET	ORAL	9314464	July 4, 2031	INDICATED IN COMBINATION WITH ENCORAFENIB FOR THE TREATMENT OF MELANOMA MEDIATED BY A B-RAF PROTEIN KINASE
15MG	MEKTOVI	ARRAY BIOPHARMA INC	N210498	June 27, 2018	RX	TABLET	ORAL	9598376	Oct. 18, 2033	METHOD OF TREATING MELANOMA
15MG	MEKTOVI	ARRAY BIOPHARMA INC	N210498	June 27, 2018	RX	TABLET	ORAL	9980944	Oct. 18, 2033	TREATMENT OF MELANOMA WITH A BRAF MUTATION

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
15MG	MEKTOVI	ARRAY BIOPHARMA INC	N210498	June 27, 2018	RX	TABLET	ORAL	June 27, 2023	NEW CHEMICAL ENTITY
15MG	MEKTOVI	ARRAY BIOPHARMA INC	N210498	June 27, 2018	RX	TABLET	ORAL	June 27, 2025	ENCORAFENIB IS INDICATED IN COMBINATION WITH BINIMETINIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH A BRAF V600E OR V600K MUTATION, AS DETECTED BY AN FDA-APPROVED TEST

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	7.90		IUPHAR	DRUG LABEL
Dual specificity mitogen-activated protein kinase kinase 2	Kinase	P36507	MP2K2_HUMAN	INHIBITOR	IC50	7.90		IUPHAR	DRUG LABEL
Ribosyldihydronicotinamide dehydrogenase [quinone]	Enzyme	P16083	NQO2_HUMAN		Kd	4.83		CHEMBL

External reference:

ID	Source
181R97MR71	UNII
C3899947	UMLSCUI
CHEBI:145371	CHEBI
QO7	PDB_CHEM_ID
CHEMBL3187723	ChEMBL_ID
10288191	PUBCHEM_CID
DB11967	DRUGBANK_ID
D10604	KEGG_DRUG
7921	IUPHAR_LIGAND_ID
2049122	RXNORM
283903	MMSL
34461	MMSL
d08818	MMSL
772095008	SNOMEDCT_US
772195005	SNOMEDCT_US
4037645	VANDF
017616	NDDF
C581313	MESH_SUPPLEMENTAL_RECORD_UI
9764	INN_ID

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
MEKTOVI	HUMAN PRESCRIPTION DRUG LABEL	1	70255-010	TABLET, FILM COATED	15 mg	ORAL	NDA	29 sections
MEKTOVI	HUMAN PRESCRIPTION DRUG LABEL	1	70255-010	TABLET, FILM COATED	15 mg	ORAL	NDA	29 sections