Identification

Name
Binimetinib
Accession Number
DB11967  (DB05985)
Type
Small Molecule
Groups
Approved, Investigational
Description

Binimetinib, also known as Mektovi, is a potent is a potent and selective oral mitogen-activated protein kinase 1/2 (MEK 1/2) inhibitor which is combined with Encorafenib [4],[8].

On June 27, 2018, the Food and Drug Administration approved the combination of Encorafenib and binimetinib (BRAFTOVI and MEKTOVI, from Array BioPharma Inc.) in combination for patients with unresectable or metastatic melanoma with the BRAF V600E or V600K mutations, as detected by an FDA-approved test [8].

Structure
Thumb
Synonyms
Not Available
External IDs
ARRY-162 / ARRY-438162 / MEK-162 / MEK162 / NVP-MEK162
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
MektoviTablet, film coated15 mg/1OralArray BioPharma Inc.2018-06-30Not applicableUs
Categories
UNII
181R97MR71
CAS number
606143-89-9
Weight
Average: 441.233
Monoisotopic: 440.02956
Chemical Formula
C17H15BrF2N4O3
InChI Key
ACWZRVQXLIRSDF-UHFFFAOYSA-N
InChI
InChI=1S/C17H15BrF2N4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26)
IUPAC Name
5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-1,3-benzodiazole-6-carboxamide
SMILES
CN1C=NC2=C(F)C(NC3=CC=C(Br)C=C3F)=C(C=C12)C(=O)NOCCO

Pharmacology

Indication

On June 27, 2018, the Food and Drug Administration approved encorafenib and binimetinib in combination patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test [8].

Associated Conditions
Pharmacodynamics

Binimetinib is a MEK inhibitor. MEK is an enzyme that regulates the biosynthesis of the inflammatory cytokines TNF, IL-6 and IL-1. MEK inhibitors interfere with these biosynthetic processes [7]. It is a chemotherapeutic agent that has anti-tumor activity [10], [1].

Mechanism of action

Binimetinib, noncompetitive with ATP, binds to and inhibits the activity of MEK1/2. The inhibition of MEK1/2 prevents the activation of MEK1/2-dependent effector proteins and transcription factors. This process can result in the inhibition of growth factor-mediated cell signaling. This may lead to the inhibition of tumor cell proliferation and an inhibition in the production of various inflammatory cytokines including interleukin-1, -6 and tumor necrosis factor. MEK1/2 are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway and are frequently upregulated in a variety of tumor cell types [7].

TargetActionsOrganism
UInterleukin-6Not AvailableHuman
UTumor necrosis factorNot AvailableHuman
UInterleukin-1 betaNot AvailableHuman
AMitogen-activated protein kinase kinase kinase 1
inhibitor
Human
ADual specificity mitogen-activated protein kinase kinase 2
inhibitor
Human
Absorption

Following oral administration in a pharmacokinetic study, at least 50% of the binimetinib dose was absorbed with a median time to maximum concentration (Tmax) of 1.6 hours [Label].

The administration of a single dose of MEKTOVI 45 mg with a high-fat, high-calorie meal (consisting of approximately 150 calories from protein, 350 calories from carbohydrate, and 500 calories from fat) in healthy subjects had no effect on binimetinib exposure [Label].

Volume of distribution

The geometric mean (CV%) of apparent volume of distribution of binimetinib is 92 L (45%) [Label]

Protein binding

Binimetinib is 97% bound to human plasma proteins and the blood-to-plasma ratio is 0.72 [Label]

Metabolism

The primary metabolic pathway is glucuronidation with UGT1A1 contributing up to 61% of the binimetinib metabolism. Other pathways of binimetinib metabolism include N-dealkylation, amide hydrolysis, and loss of ethane-diol from the side chain. The active metabolite M3 produced by CYP1A2 and CYP2C19 represents 8.6% of the binimetinib exposure. Following a single oral dose of 45 mg radiolabeled binimetinib, approximately 60% of the circulating radioactivity AUC in plasma was attributable to binimetinib [Label].

Route of elimination

Following a single oral dose of 45 mg radiolabeled binimetinib in healthy subjects, 62% (32% unchanged) of the administered dose was recovered in the feces while 31% (6.5% unchanged) was recovered in the urine [Label].

Half life

The mean (CV%) terminal half-life (t1/2) of binimetinib is 3.5 hours (28.5%) [Label].

Clearance

20.2 L/h (24%) [Label]

Toxicity

The most common (≥25%) adverse reactions in patients receiving the combination of this drug with Encorafenib were fatigue, nausea, diarrhea, vomiting, abdominal pain, and arthralgia. Discontinuation of therapy due to adverse reactions occurred in 5% of patients receiving the combination; the most common reasons were hemorrhage and headache [8].

Due to the variety of adverse events associated with this drug, adverse events are categorized by system [12]:

Systemic events: Fatigue (31%) [12]

Musculoskeletal system: Rhabdomyolysis [12]

Ophthalmic events: Retinal hemorrhage, retinal detachment (6%), macular edema, serous retinopathy (20%) [12]

Circulatory system: Hypertension, thromboembolic events such as DVT, resulting in pulmonary embolism (5.6%), peripheral edema or periorbital edema (43.5%), hemorrhage (11.2%)[12]

Pulmonary events: Pneumonitis (1.9%), Pulmonary embolism [12]

Cardiovascular system: QT interval prolongation (3.3%), Left ventricular dysfunction (7%) [12]

Gastrointestinal system: Hepatotoxicity, diarrhea, nausea, vomiting, stomatitis, dry mouth [12]

Dermatologic events: Acneiform dermatitis [9]

Based on findings from animal studies and its mechanism of action, MEKTOVI can cause fetal harm when administered to a pregnant woman [Label].

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of Binimetinib can be decreased when combined with (R)-warfarin.
3-isobutyl-1-methyl-7H-xanthineThe serum concentration of 3-isobutyl-1-methyl-7H-xanthine can be increased when it is combined with Binimetinib.
6-O-benzylguanineThe serum concentration of 6-O-benzylguanine can be increased when it is combined with Binimetinib.
7-DeazaguanineThe serum concentration of 7-Deazaguanine can be increased when it is combined with Binimetinib.
7,9-DimethylguanineThe serum concentration of 7,9-Dimethylguanine can be increased when it is combined with Binimetinib.
8-azaguanineThe serum concentration of 8-azaguanine can be increased when it is combined with Binimetinib.
8-chlorotheophyllineThe serum concentration of 8-chlorotheophylline can be increased when it is combined with Binimetinib.
9-DeazaguanineThe serum concentration of 9-Deazaguanine can be increased when it is combined with Binimetinib.
9-MethylguanineThe serum concentration of 9-Methylguanine can be increased when it is combined with Binimetinib.
AbirateroneThe serum concentration of Binimetinib can be increased when it is combined with Abiraterone.
Food Interactions
Not Available

References

General References
  1. Koelblinger P, Dornbierer J, Dummer R: A review of binimetinib for the treatment of mutant cutaneous melanoma. Future Oncol. 2017 Aug;13(20):1755-1766. doi: 10.2217/fon-2017-0170. Epub 2017 Jun 7. [PubMed:28587477]
  2. Queirolo P, Spagnolo F: Binimetinib for the treatment of NRAS-mutant melanoma. Expert Rev Anticancer Ther. 2017 Nov;17(11):985-990. doi: 10.1080/14737140.2017.1374177. Epub 2017 Sep 8. [PubMed:28851243]
  3. Dummer R, Schadendorf D, Ascierto PA, Arance A, Dutriaux C, Di Giacomo AM, Rutkowski P, Del Vecchio M, Gutzmer R, Mandala M, Thomas L, Demidov L, Garbe C, Hogg D, Liszkay G, Queirolo P, Wasserman E, Ford J, Weill M, Sirulnik LA, Jehl V, Bozon V, Long GV, Flaherty K: Binimetinib versus dacarbazine in patients with advanced NRAS-mutant melanoma (NEMO): a multicentre, open-label, randomised, phase 3 trial. Lancet Oncol. 2017 Apr;18(4):435-445. doi: 10.1016/S1470-2045(17)30180-8. Epub 2017 Mar 9. [PubMed:28284557]
  4. Bendell JC, Javle M, Bekaii-Saab TS, Finn RS, Wainberg ZA, Laheru DA, Weekes CD, Tan BR, Khan GN, Zalupski MM, Infante JR, Jones S, Papadopoulos KP, Tolcher AW, Chavira RE, Christy-Bittel JL, Barrett E, Patnaik A: A phase 1 dose-escalation and expansion study of binimetinib (MEK162), a potent and selective oral MEK1/2 inhibitor. Br J Cancer. 2017 Feb 28;116(5):575-583. doi: 10.1038/bjc.2017.10. Epub 2017 Feb 2. [PubMed:28152546]
  5. Gardner AM, Vaillancourt RR, Lange-Carter CA, Johnson GL: MEK-1 phosphorylation by MEK kinase, Raf, and mitogen-activated protein kinase: analysis of phosphopeptides and regulation of activity. Mol Biol Cell. 1994 Feb;5(2):193-201. [PubMed:8019005]
  6. Wang ZQ, Wu DC, Huang FP, Yang GY: Inhibition of MEK/ERK 1/2 pathway reduces pro-inflammatory cytokine interleukin-1 expression in focal cerebral ischemia. Brain Res. 2004 Jan 16;996(1):55-66. [PubMed:14670631]
  7. Cancer.gov link [Link]
  8. FDA approves encorafenib and binimetinib in combination for unresectable or metastatic melanoma with BRAF mutations [Link]
  9. A phase 1 dose-escalation and expansion study of binimetinib (MEK162), a potent and selective oral MEK1/2 inhibitor [Link]
  10. Binimetinib inhibits MEK and is effective against neuroblastoma tumor cells with low NF1 expression [Link]
  11. Binimetinib [File]
  12. EMA assessment [File]
External Links
PubChem Compound
10288191
PubChem Substance
347828291
ChemSpider
8463660
ChEMBL
CHEMBL3187723
PharmGKB
PA166179867
Wikipedia
Binimetinib

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentGastrointestinal Stromal Tumors (GISTs)1
1CompletedTreatmentAdvanced Solid Tumors2
1CompletedTreatmentAdvanced or Metastatic Biliary Cancer / Advanced Solid Tumors / Metastatic Colorectal Cancers1
1CompletedTreatmentAdvanced Solid Tumors / Selected Solid Tumors1
1CompletedTreatmentAdvanced and Selected Solid Tumors / Advanced and Selected Solid Tumors, AML, High Risk and Very High Risk MDS / High Risk and Very High Risk MDS / Leukemia Acute Myeloid Leukemia (AML)1
1CompletedTreatmentRecurrent Colon Cancer / Recurrent Rectal Cancer / Stage IVA Colon Cancer / Stage IVA Rectal Cancer / Stage IVB Colon Cancer / Stage IVB Rectal Cancer1
1CompletedTreatmentTumors, Solid / Unspecified Adult Solid Tumor, Protocol Specific1
1RecruitingTreatmentAdvanced KRAS Positive Metastatic Colorectal Cancer1
1RecruitingTreatmentAdvanced Non-Small Cell Lung Cancer / KRAS Gene Mutation / Lung Cancers1
1RecruitingTreatmentCarcinoma of the Lungs / Lungcancer1
1RecruitingTreatmentColorectal Cancers / Tumors, Solid1
1RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC) / Lung Cancers1
1RecruitingTreatmentMetastatic Colorectal Cancers1
1TerminatedTreatmentAdult Acute Minimally Differentiated Myeloid Leukemia (M0) / Adult Acute Monoblastic Leukemia (M5a) / Adult Acute Monocytic Leukemia (M5b) / Adult Acute Myeloblastic Leukemia With Maturation (M2) / Adult Acute Myeloblastic Leukemia Without Maturation (M1) / Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities / Adult Acute Myeloid Leukemia With Del(5q) / Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) / Adult Acute Myeloid Leukemia With T(15;17)(q22;q12) / Adult Acute Myeloid Leukemia With T(16;16)(p13;q22) / Adult Acute Myeloid Leukemia With T(8;21)(q22;q22) / Adult Acute Myelomonocytic Leukemia (M4) / Adult Erythroleukemia (M6a) / Adult Pure Erythroid Leukemia (M6b) / Recurrent Adult Acute Myeloid Leukemia1
1TerminatedTreatmentHepatic Impairment1
1TerminatedTreatmentLeukemias1
1WithdrawnTreatmentRecurrent Non-Small Cell Lung Carcinoma / Stage IV Non-Small Cell Lung Cancer1
1, 2Active Not RecruitingOtherSolid Tumors Harboring a BRAF V600 Mutation1
1, 2Active Not RecruitingTreatmentAdvanced Biliary Tract Carcinoma1
1, 2Active Not RecruitingTreatmentBiliary Tract Cancer1
1, 2Active Not RecruitingTreatmentMSS / RAS-mutant Colorectal Cancer1
1, 2CompletedOtherMetastatic Colorectal Cancers1
1, 2CompletedTreatmentLocally Advanced or Metastatic NRAS Mutant Melanoma1
1, 2RecruitingTreatmentBreast Adenocarcinoma / Estrogen Receptor Negative / HER2/Neu Negative / Progesterone Receptor Negative / Stage III Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer / Triple-Negative Breast Carcinoma1
1, 2RecruitingTreatmentGastrointestinal Stromal Tumors (GISTs)1
1, 2RecruitingTreatmentLow-Grade Gliomas / Malignant Neoplasms, Brain / Soft Tissue Neoplasms1
1, 2RecruitingTreatmentLung Cancers1
1, 2RecruitingTreatmentMalignant Melanoma1
1, 2TerminatedTreatmentUveal Melanoma1
2Active Not RecruitingTreatmentAdenocarcinoma Lung Cancer / Adenocarcinoma Lung Cancer; Squamous Cell Lung Carcinoma1
2Active Not RecruitingTreatmentBRAF or NRAS Mutant Metastatic Melanoma1
2Active Not RecruitingTreatmentMelanoma1
2Active Not RecruitingTreatmentSolid Tumor and Hematologic Malignancies1
2Not Yet RecruitingTreatmentBRAF V600E-mutant Metastatic Colorectal Cancer1
2Not Yet RecruitingTreatmentColorectal Cancers / Metastatic Cancers1
2RecruitingTreatmentAdvanced Malignant Neoplasm / Advanced Malignant Solid Neoplasm / Bladder Carcinoma / Carcinoma, Breast / Carcinoma, Colorectal / Carcinoma, Pancreatic / Cervical Carcinoma / Colon Carcinoma / Endometrial Carcinoma / Gastric Carcinoma / Gliomas / Head and Neck Carcinoma / Liver and Intrahepatic Bile Duct Carcinoma / Lung, Carcinoma / Malignant Lymphomas / Malignant Uterine Neoplasm / Melanoma / Oesophageal Carcinoma / Ovarian Carcinoma / Plasma Cell Myeloma / Prostate Cancer / Rectal Carcinoma / Recurrent Bladder Carcinoma / Recurrent Breast Carcinoma / Recurrent Cervical Carcinoma / Recurrent Colon Carcinoma / Recurrent Colorectal Carcinoma / Recurrent Esophageal Carcinoma / Recurrent Gastric Carcinoma / Recurrent Gliomas / Recurrent Head and Neck Carcinoma / Recurrent Liver Carcinoma / Recurrent Lung Carcinoma / Recurrent Lymphoma / Recurrent Malignant Solid Neoplasm / Recurrent Melanoma / Recurrent Ovarian Carcinoma / Recurrent Pancreatic Carcinoma / Recurrent Plasma Cell Myeloma / Recurrent Prostate Carcinoma / Recurrent Rectal Carcinoma / Recurrent Skin Carcinoma / Recurrent Solid Neoplasm / Recurrent Thyroid Gland Carcinoma / Recurrent Uterine Corpus Carcinoma / Refractory Lymphomas / Refractory Malignant Neoplasm / Refractory Malignant Solid Neoplasm / Refractory Plasma Cell Myeloma / Renal Carcinoma / Skin Carcinoma / Solid Neoplasms / Thyroid Gland Carcinoma / Uterine Corpus Cancer1
2RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC) / Malignancies / Malignant Neoplasm of Pancreas1
2RecruitingTreatmentMetastatic Melanoma1
2RecruitingTreatmentNeurofibromatosis Type 1 / Plexiform Neurofibroma1
2RecruitingTreatmentPatients With BRAFV600 E or BRAFV600K Mutation / Relapsed Or Refractory Multiple Myeloma1
2RecruitingTreatmentStage IV Melanoma / Unresectable Stage III Melanoma1
2TerminatedTreatmentBRAF Mutated Melanoma / KRAS Mutated Colorectal Adenocarcinoma / Pancreatic Adenocarcinoma Metastatic1
2WithdrawnTreatmentCardiomegaly1
2WithdrawnTreatmentRecurrent Melanoma / Stage IV Melanoma1
3Active Not RecruitingTreatmentLow-grade Serous Fallopian Tube Cancer / Low-grade Serous Ovarian Cancer / Low-grade Serous Peritoneal Cancer1
3Active Not RecruitingTreatmentMelanoma1
3Active Not RecruitingTreatmentMetastatic or Unresectable Cutaneous Melanoma1
3RecruitingTreatmentBRAF V600E-mutant Metastatic Colorectal Cancer1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Tablet, film coatedOral15 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US9314464No2016-04-192031-07-04Us
US9850229No2017-12-262030-08-27Us
US10005761No2010-08-272030-08-27Us
US9593100No2017-03-142030-08-27Us
US9980944No2018-05-292033-10-18Us
US9598376No2017-03-212033-10-18Us
US8193229No2012-06-052023-03-13Us
US8513293No2013-08-202023-03-13Us
US7777050No2010-08-172023-03-13Us
US8178693No2012-05-152023-03-13Us
US9562016No2017-02-072033-10-18Us

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0499 mg/mLALOGPS
logP3ALOGPS
logP3.81ChemAxon
logS-4ALOGPS
pKa (Strongest Acidic)10.26ChemAxon
pKa (Strongest Basic)5.3ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area88.41 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity98.02 m3·mol-1ChemAxon
Polarizability38.55 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as 3-halobenzoic acids and derivatives. These are benzoic acids or derivatives carrying a halogen atom at the 3-position of the benzene ring.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Benzoic acids and derivatives
Direct Parent
3-halobenzoic acids and derivatives
Alternative Parents
Benzimidazoles / Aniline and substituted anilines / Fluorobenzenes / Bromobenzenes / Primary aromatic amines / Aryl bromides / Aryl fluorides / N-substituted imidazoles / Vinylogous amides / Heteroaromatic compounds
show 8 more
Substituents
3-halobenzoic acid or derivatives / Benzimidazole / Aniline or substituted anilines / Bromobenzene / Fluorobenzene / Halobenzene / Aryl bromide / Aryl fluoride / Aryl halide / N-substituted imidazole
show 23 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Interleukin-6 receptor binding
Specific Function
Cytokine with a wide variety of biological functions. It is a potent inducer of the acute phase response. Plays an essential role in the final differentiation of B-cells into Ig-secreting cells Inv...
Gene Name
IL6
Uniprot ID
P05231
Uniprot Name
Interleukin-6
Molecular Weight
23717.965 Da
References
  1. Cancer.gov link [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Tumor necrosis factor receptor binding
Specific Function
Cytokine that binds to TNFRSF1A/TNFR1 and TNFRSF1B/TNFBR. It is mainly secreted by macrophages and can induce cell death of certain tumor cell lines. It is potent pyrogen causing fever by direct ac...
Gene Name
TNF
Uniprot ID
P01375
Uniprot Name
Tumor necrosis factor
Molecular Weight
25644.15 Da
References
  1. Cancer.gov link [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Protein domain specific binding
Specific Function
Potent proinflammatory cytokine. Initially discovered as the major endogenous pyrogen, induces prostaglandin synthesis, neutrophil influx and activation, T-cell activation and cytokine production, ...
Gene Name
IL1B
Uniprot ID
P01584
Uniprot Name
Interleukin-1 beta
Molecular Weight
30747.7 Da
References
  1. Cancer.gov link [Link]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Zinc ion binding
Specific Function
Component of a protein kinase signal transduction cascade. Activates the ERK and JNK kinase pathways by phosphorylation of MAP2K1 and MAP2K4. Activates CHUK and IKBKB, the central protein kinases o...
Gene Name
MAP3K1
Uniprot ID
Q13233
Uniprot Name
Mitogen-activated protein kinase kinase kinase 1
Molecular Weight
164468.265 Da
References
  1. Koelblinger P, Dornbierer J, Dummer R: A review of binimetinib for the treatment of mutant cutaneous melanoma. Future Oncol. 2017 Aug;13(20):1755-1766. doi: 10.2217/fon-2017-0170. Epub 2017 Jun 7. [PubMed:28587477]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Scaffold protein binding
Specific Function
Catalyzes the concomitant phosphorylation of a threonine and a tyrosine residue in a Thr-Glu-Tyr sequence located in MAP kinases. Activates the ERK1 and ERK2 MAP kinases (By similarity).
Gene Name
MAP2K2
Uniprot ID
P36507
Uniprot Name
Dual specificity mitogen-activated protein kinase kinase 2
Molecular Weight
44423.735 Da
References
  1. Koelblinger P, Dornbierer J, Dummer R: A review of binimetinib for the treatment of mutant cutaneous melanoma. Future Oncol. 2017 Aug;13(20):1755-1766. doi: 10.2217/fon-2017-0170. Epub 2017 Jun 7. [PubMed:28587477]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
Gene Name
UGT1A1
Uniprot ID
P22309
Uniprot Name
UDP-glucuronosyltransferase 1-1
Molecular Weight
59590.91 Da
References
  1. FDA label [File]
  2. EMA assessment report [File]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. EMA assessment report [File]
  2. FDA label, Binimetinib [File]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da

Drug created on October 20, 2016 15:06 / Updated on November 02, 2018 07:18