Binimetinib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2018
- First approval year
- 2018
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Binimetinib
- Molecular weight
- 441.23
- Structure (SMILES)
- Cn1cnc2c(F)c(Nc3ccc(Br)cc3F)c(C(=O)NOCCO)cc21
- mektovi
- Mektovi
- arry 162
- arry 438162
- ARRY 438162
- ARRY-162
- ARRY-438162
- bez235 mek162
- binimetinib
- Binimetinib
- binimetinib [INN]
- BINIMETINIB [JAN]
- BINIMETINIB [MI]
- BINIMETINIB [ORANGE BOOK]
- BINIMETINIB [USAN]
- Binimetinib [WHO-DD]
- Binimetinib 15 MG
- Binimetinib 45 MG
- binimetinib inn
- binimetinib jan
- binimetinib mi
- Binimetinib Oral Tablet
- binimetinib orange book
- binimetinib usan
- binimetinib who dd
- mek 162
- MEK 162
And 6 more, listed on the interactive page.
- CAS registry numbers
- 606143-89-9
- ChEMBL ID
- CHEMBL3187723
- InChIKey
- ACWZRVQXLIRSDF-UHFFFAOYSA-N
- PubChem compound IDs
- 10288191
- RxNorm IDs (RxCUI)
- 2049122
- FDA ingredient codes (UNII)
- 181R97MR71
- L01EE03
- L01XE
Sources for recorded values
- Applicant
- ARRAY BIOPHARMA INC
- Approval date
- 27 Jun 2018
- Application number
- NDA210498
- Status
- Authorised
- Status date
- 20 Sept 2018
- Authorisation date
- 20 Sept 2018
- Approved indications
- MelanomaBinimetinib in combination with encorafenib is indicated for the treatment of adult patients with unresectable or metastatic melanoma with a BRAF V600 mutation.Non-small cell lung cancer (NSCLC)Binimetinib in combination with encorafenib is indicated for the treatment of adult patients with advanced non-small cell lung cancer with a BRAF V600E mutation.
- Product number
- EMEA/H/C/004579
- Authorisation holder
- Pierre Fabre Medicament
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Melanoma
European medicines record
- Patents
- 7
- Designations
- 1
- Earliest recorded loss of exclusivity
- 18 Oct 2033
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Pharmacology name
- binimetinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Mechanism
- Dual specificity mitogen-activated protein kinase kinase 1 inhibitor
- Action type
- Inhibitor
- Target
- Dual specificity mitogen-activated protein kinase kinase 1
- Protein identifier
- Q02750
- Mechanism
- Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
- Action type
- Inhibitor
- Target
- Dual specificity mitogen-activated protein kinase kinase 2
- Protein identifier
- P36507
- Action
- Negative
- Action type
- NEGATIVE
- Target
- mitogen-activated protein kinase kinase 2
- Gene symbol
- MAP2K2
- Protein identifier
- P36507
- Median affinity
- 7.92
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Negative
- Action type
- NEGATIVE
- Target
- mitogen-activated protein kinase kinase 1
- Gene symbol
- MAP2K1
- Protein identifier
- Q02750
- Median affinity
- 7.92
- Affinity units
- pIC50
- Primary target
- Yes
- Mechanism
- Dual specificity mitogen-activated protein kinase kinase 1 inhibitor
- Action type
- Inhibitor
- Target
- Dual specificity mitogen-activated protein kinase kinase 1
- Mechanism
- Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
- Action type
- Inhibitor
- Target
- Dual specificity mitogen-activated protein kinase kinase 2
- Action type
- Inhibitor
- Gene symbol
- MAP2K2
- Protein identifier
- P36507
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- MAP2K1
- Protein identifier
- Q02750
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Breast Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000305
- Subject identifier
- D001943
- Condition
- Melanoma
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000389
- Subject identifier
- D008545
- Condition
- Leukemia
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000565
- Subject identifier
- D007938
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Arthritis, Rheumatoid
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000685
- Subject identifier
- D001172
- Condition
- Melanoma
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000756
- Subject identifier
- D008545
- Condition
- Ovarian Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0001075
- Subject identifier
- D010051
- Condition
- Multiple Myeloma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001378
- Subject identifier
- D009101
- Condition
- Liver Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001421
- Subject identifier
- D008107
- Condition
- Cardiomegaly
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002503
- Subject identifier
- D006332
- Condition
- Melanoma
- Highest recorded phase
- 4
- Condition identifier
- EFO:0002617
- Subject identifier
- D008545
- Condition
- Pancreatic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002618
- Subject identifier
- D010190
- Condition
- Thyroid Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002892
- Subject identifier
- D013964
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Brain Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003833
- Subject identifier
- D001932
- Condition
- Biliary Tract Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003891
- Subject identifier
- D001661
- Condition
- Triple Negative Breast Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005537
- Subject identifier
- D064726
- Condition
- Skin Neoplasms
- Highest recorded phase
- 0.5
- Condition identifier
- EFO:0009259
- Subject identifier
- D012878
- Condition
- Uveal Melanoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:1000616
- Subject identifier
- D000098943
- Condition
- Rectal Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:1000657
- Subject identifier
- D012004
- Condition
- Leukemia, Hairy Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:1000956
- Subject identifier
- D007943
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:1001951
- Subject identifier
- D015179
- Condition
- Klatskin Tumor
- Highest recorded phase
- 2
- Condition identifier
- EFO:1001959
- Subject identifier
- D018285
- Condition
- Peritoneal Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0002087
- Subject identifier
- D010534
- Condition
- Fallopian Tube Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0002158
- Subject identifier
- D005185
And 9 more, listed on the interactive page.
- Condition identifier
- EFO_0000305
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000565
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000658
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000685
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000756
- Condition identifier
- EFO_0001421
- Highest recorded phase
- 1
- Condition identifier
- EFO_0002503
- Highest recorded phase
- 2
- Condition identifier
- EFO_0002617
- Condition identifier
- EFO_0002618
- Highest recorded phase
- 2
- Condition identifier
- EFO_0002892
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003060
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003833
- Condition identifier
- EFO_1000069
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000616
- Condition identifier
- EFO_1000956
- Highest recorded phase
- 2
- Condition identifier
- EFO_1001480
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0002087
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0002108
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002158
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0002158
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0003059
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0003060
- Condition identifier
- MONDO_0003060
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004992
- Highest recorded phase
- 2
And 39 more, listed on the interactive page.
- Event
- acute kidney injury
- Reports
- 41
- Reporting signal score
- 28.8717
- Event
- blood creatine phosphokinase increased
- Reports
- 20
- Reporting signal score
- 21.5512
- Event
- chorioretinopathy
- Reports
- 5
- Reporting signal score
- 12.027
- Event
- colitis
- Reports
- 20
- Reporting signal score
- 25.9132
- Event
- death
- Reports
- 6
- Reporting signal score
- 18.5692
- Event
- diarrhoea
- Reports
- 73
- Reporting signal score
- 19.9011
- Event
- disease progression
- Reports
- 46
- Reporting signal score
- 54.7809
- Event
- hepatic function abnormal
- Reports
- 15
- Reporting signal score
- 13.7934
- Event
- hospice care
- Reports
- 16
- Reporting signal score
- 44.6428
- Event
- keratosis follicular
- Reports
- 4
- Reporting signal score
- 22.0103
- Event
- large intestinal ulcer
- Reports
- 8
- Reporting signal score
- 22.644
- Event
- nausea
- Reports
- 85
- Reporting signal score
- 21.0493
- Event
- neoplasm progression
- Reports
- 37
- Reporting signal score
- 80.4828
- Event
- ocular toxicity
- Reports
- 5
- Reporting signal score
- 16.8102
- Event
- pneumonitis
- Reports
- 16
- Reporting signal score
- 21.2095
- Event
- pyrexia
- Reports
- 88
- Reporting signal score
- 62.3659
- Event
- retinal detachment
- Reports
- 11
- Reporting signal score
- 22.4547
- Event
- serous retinal detachment
- Reports
- 46
- Reporting signal score
- 277.59
- Event
- serous retinopathy
- Reports
- 11
- Reporting signal score
- 76.6569
- Event
- transient acantholytic dermatosis
- Reports
- 5
- Reporting signal score
- 23.5141
- Event
- uveitis
- Reports
- 10
- Reporting signal score
- 15.7378
- Event
- vision blurred
- Reports
- 29
- Reporting signal score
- 23.5226
- Event
- visual impairment
- Reports
- 25
- Reporting signal score
- 24.8813
- Event
- vitreous floaters
- Reports
- 9
- Reporting signal score
- 19.0656
- Event
- vomiting
- Reports
- 56
- Reporting signal score
- 13.8879
- NCT00650767
- NCT01320085
- NCT02631447
- NCT02910700
- NCT03864042
- NCT05103891
- NCT05304546
- NCT05810740
- NCT01337765
- NCT01363232
- NCT01469130
- NCT01543698
- NCT01885195
- NCT03839342
- NCT04800822
- NCT05203172
- NCT01556568
- NCT01649336
- NCT01849874
- NCT01763164
- NCT05767879
- NCT01781572
- NCT01909453
- NCT02159066
- NCT02263898
And 54 more, listed on the interactive page.
- Dose
- 45 mg
- Route
- Oral
- How often
- Twice daily
Conditions of use
- Take with or without food
- Hydrogen bond acceptors
- 6
- Hydrogen bond donors
- 3
- Polar surface area
- 88.41
- Calculated partition coefficient (ALogP)
- 3.01
- Calculated partition coefficient (XLogP)
- 3.1
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 6
- Heavy atoms
- 27
- Molecular formula
- C17H15BrF2N4O3
- Monoisotopic mass
- 440.02956
- Natural product
- No
- 70255-010
- Recorded assays
- 948
- Active assays
- 120
- Confirmatory
- Other
- Screening
Related records
Trials (129)
- (Neo)Adjuvant BRAF/MEK Inhibition in pN1c Melanoma
- A Clinical Trial of Three Study Medicines (Encorafenib, Binimetinib, and Pembrolizumab) in Patients With Advanced or Metastatic Melanoma
- A FIH Study of PF-07284890 in Participants With BRAF V600 Mutant Solid Tumors With and Without Brain Involvement
- A Phase I Study of Oral MEK162 in Japanese Patients With Advanced Solid Tumors
- A Phase I/Ib Study of MEK162, a MEK Inhibitor, in Combination With Carboplatin and Pemetrexed in Patients With Non-squamous Carcinoma of the Lung
- A Phase I/IB Trial of MEK162 in Combination With Erlotinib in NSCLC Harboring KRAS or EGFR Mutation
- A Phase Ib Study of MEK162 Plus BYL719 in Adult Patients With Selected Advanced Solid Tumors
- A Phase Ib/II Study of AEB071 and MEK162 in Adult Patients With Metastatic Uveal Melanoma
- A Phase Ib/II Study of LEE011 in Combination With MEK162 in Patients With NRAS Mutant Melanoma
- A Phase Ib/II Study of LGX818 in Combination With MEK162 in Adult Patients With BRAF Dependent Advanced Solid Tumors
- A Phase II Study of Single Agent MEK162 in Patients With Advanced Melanoma
- A Phase II, Open Label, Multiple Arm Study of AUY922, BYL719, INC280, LDK378 and MEK162 in Chinese Patients With Advanced Non-small Cell Lung Cancer
- A Study Comparing 3 Study Medicines (Encorafenib, Binimetinib, Pembrolizumab) to 2 Study Medicines (Ipilimumab and Nivolumab) in Patients With Advanced Melanoma
- A Study of ARRY-438162 (MEK162) in Patients With Advanced Cancer
- A Study of ARRY-438162 in Patients With Rheumatoid Arthritis
- A Study of Avelumab, Binimetinib and Talazoparib in Patients With Locally Advanced or Metastatic RAS-mutant Solid Tumors
- A Study of Binimetinib and Encorafenib in Advanced BRAF Mutant Cancers
- A Study of MEK162 (Binimetinib) in Combination With Pexidartinib in Patients With Advanced Gastrointestinal Stromal Tumor (GIST)
- A Study of MEK162 and AMG 479 in Patients With Selected Solid Tumors
- A Study of MEK162 and Paclitaxel in Patients With Epithelial Ovarian, Fallopian Tube or Peritoneal Cancer
Approved for (5)
- Cancer
- Cutaneous melanoma
- Melanoma
- Metastatic melanoma
- Neoplasm
In development for (28)
- Biliary tract cancer Phase 3
- Biliary tract neoplasm Phase 3
- Brain neoplasm Phase 1
- Breast cancer Phase 2
- Breast carcinoma Phase 2
- Colorectal cancer Phase 2
- Colorectal carcinoma Phase 2
- Exocrine pancreatic carcinoma Phase 2
- Fallopian tube cancer Phase 3
- Gastrointestinal stromal tumor Phase 1
- Hairy cell leukemia Phase 2
- Hilar cholangiocarcinoma Phase 2
- Leukemia Phase 1
- Liver disorder Phase 1
- Low grade glioma Phase 1
- Lung cancer Phase 1
- Malignant colon neoplasm Phase 1
- Non-small cell lung carcinoma Phase 2
- Ovarian cancer Phase 3
- Ovarian carcinoma Phase 3