General Information of Drug (ID: DM1P6FR)

Drug Name
Arry-162 Drug Info
Synonyms
606143-89-9; Binimetinib; MEK162; MEK-162; ARRY-438162; 5-[(4-Bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide; ARRY 162; UNII-181R97MR71; Binimetinib (MEK162, ARRY-162, ARRY-438162); 181R97MR71; MEK162 (ARRY-162, ARRY-438162); 6-(4-bromo-2-fluorophenylamino)-7-fluoro-N-(2-hydroxyethoxy)-3-methyl-3H-benzo[d]imidazole-5-carboxamide; Binimetinib [USAN:INN]; MEK 162; ARRY 438162; MEK162(Binimetinib); Binimetinib (JAN/USAN); D0C4LF; NVP-ME
Indication
Disease Entry ICD 11 Status REF
Melanoma 2C30 Approved [1]
Cross-matching ID
PubChem CID
10288191
ChEBI ID
CHEBI:145371
CAS Number
CAS 606143-89-9
TTD Drug ID
DM1P6FR
VARIDT Drug ID
DR01336
INTEDE Drug ID
DR0214
ACDINA Drug ID
D00883

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Drug(s) Metabolized By Cytochrome P450 1A2 (CYP1A2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fluorouracil DMUM7HZ Solid tumour/cancer 2A00-2F9Z Approved [6]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [7]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [8]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [9]
Acetaminophen DMUIE76 Pain MG30-MG3Z Approved [10]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [11]
Etoposide DMNH3PG Solid tumour/cancer 2A00-2F9Z Approved [12]
Oxaliplatin DMQNWRD Colorectal cancer 2B91.Z Approved [13]
Verapamil DMA7PEW Hypertension BA00-BA04 Approved [14]
Diclofenac DMPIHLS Osteoarthritis FA00-FA05 Approved [15]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [16]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [17]
Acetaminophen DMUIE76 Pain MG30-MG3Z Approved [18]
Etoposide DMNH3PG Solid tumour/cancer 2A00-2F9Z Approved [19]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [20]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [21]
Mycophenolate mofetil DMPQAGE Organ transplant rejection NE84 Approved [22]
Metronidazole DMTIVEN Amoebiasis 1A36 Approved [23]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [24]
Ethanol DMDRQZU Chronic pain MG30 Approved [25]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Bacterial infection 1A00-1C4Z Approved [26]
Doxorubicin DMVP5YE Solid tumour/cancer 2A00-2F9Z Approved [27]
Methotrexate DM2TEOL leukaemia 2A60-2B33 Approved [28]
Folic acid DMEMBJC Folate-deficiency anemia 3A02.Y Approved [29]
Fluorouracil DMUM7HZ Solid tumour/cancer 2A00-2F9Z Approved [28]
Cisplatin DMRHGI9 Solid tumour/cancer 2A00-2F9Z Approved [28]
Progesterone DMUY35B Premature labour JB00 Approved [30]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [28]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [31]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [32]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Solid tumour/cancer 2A00-2F9Z Approved [33]
Methotrexate DM2TEOL leukaemia 2A60-2B33 Approved [34]
Folic acid DMEMBJC Folate-deficiency anemia 3A02.Y Approved [35]
Fluorouracil DMUM7HZ Solid tumour/cancer 2A00-2F9Z Approved [36]
Cisplatin DMRHGI9 Solid tumour/cancer 2A00-2F9Z Approved [37]
Progesterone DMUY35B Premature labour JB00 Approved [38]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [39]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [38]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [40]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [41]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Trametinib DM2JGQ3 Melanoma 2C30 Approved [42]
Bay 86-9766 DMPW5SB Solid tumour/cancer 2A00-2F9Z Phase 3 [43]
Selumetinib DMC7W6R Melanoma 2C30 Phase 3 [44]
MSC1936369B DMH1DYU Colorectal cancer 2B91.Z Phase 2 [45]
RO-5126766 DM3U9BY Non-small cell lung cancer 2C25 Phase 2 [46]
E6201 DMOSL9P Psoriasis vulgaris EA90 Phase 2 [47]
PD-0325901 DM27D4J Breast cancer 2C60-2C65 Phase 2 [2]
WX-554 DMRABOS Solid tumour/cancer 2A00-2F9Z Phase 1/2 [2]
RG7304 DMGFAVQ Solid tumour/cancer 2A00-2F9Z Phase 1 [48]
BI-847325 DMY4B6J Solid tumour/cancer 2A00-2F9Z Phase 1 [49]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting ERK activator kinase (MEK)
Drug Name Drug ID Indication ICD 11 Highest Status REF
HL-085 DMJDVCW Melanoma 2C30 Phase 1/2 [50]
RG7304 DMGFAVQ Solid tumour/cancer 2A00-2F9Z Phase 1 [48]
GDC-0623 DMDY08K Solid tumour/cancer 2A00-2F9Z Phase 1 [51]
BI 3011441 DMFJGUL Solid tumour/cancer 2A00-2F9Z Phase 1 [52]
Pyridinone compound 1 DM2GR5Q N. A. N. A. Patented [53]
Quinazolines and azaquinazoline derivative 1 DME24BI N. A. N. A. Patented [53]
PMID28594589-Compound-TABLE3C2 DMVYG0U N. A. N. A. Patented [53]
Benzoheterocyclic compound 1 DM3K25J N. A. N. A. Patented [53]
Benzoimidazole derivative 1 DMUJFCK N. A. N. A. Patented [53]
PMID28594589-Compound-TABLE3C12 DMPK7IU N. A. N. A. Patented [53]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
ERK activator kinase (MEK) TTZCRP3 NOUNIPROTAC Inhibitor [1]
MAPK/ERK kinase kinase (MAP3K) TTROQ37 NOUNIPROTAC Modulator [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [3]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
UDP-glucuronosyltransferase 1A1 (UGT1A1) Main DME DEYGVN4 UD11_HUMAN Substrate [4]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Substrate [5]

References

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4 Binimetinib - European Medicines Agency - European Union
5 FDA Label of Binimetinib. The 2020 official website of the U.S. Food and Drug Administration.
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12 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
13 The influence of metabolic gene polymorphisms on urinary 1-hydroxypyrene concentrations in Chinese coke oven workers. Sci Total Environ. 2007 Aug 1;381(1-3):38-46.
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20 Interindividual variability in pharmacokinetics of generic nucleoside reverse transcriptase inhibitors in TB/HIV-coinfected Ghanaian patients: UGT2B7*1c is associated with faster zidovudine clearance and glucuronidation. J Clin Pharmacol. 2009 Sep;49(9):1079-90.
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22 Characterization of rat intestinal microsomal UDP-glucuronosyltransferase activity toward mycophenolic acid. Drug Metab Dispos. 2006 Sep;34(9):1632-9.
23 Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8.
24 Substrate-dependent modulation of UDP-glucuronosyltransferase 1A1 (UGT1A1) by propofol in recombinant human UGT1A1 and human liver microsomes. Basic Clin Pharmacol Toxicol. 2007 Sep;101(3):211-4.
25 Identification and preliminary characterization of UDP-glucuronosyltransferases catalyzing formation of ethyl glucuronide. Anal Bioanal Chem. 2014 Apr;406(9-10):2325-32.
26 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
27 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
28 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
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32 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
33 Doxorubicin transport by RALBP1 and ABCG2 in lung and breast cancer. Int J Oncol. 2007 Mar;30(3):717-25.
34 Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Res. 2003 Sep 1;63(17):5538-43.
35 The effect of low pH on breast cancer resistance protein (ABCG2)-mediated transport of methotrexate, 7-hydroxymethotrexate, methotrexate diglutamate, folic acid, mitoxantrone, topotecan, and resveratrol in in vitro drug transport models. Mol Pharmacol. 2007 Jan;71(1):240-9.
36 Role of BCRP as a biomarker for predicting resistance to 5-fluorouracil in breast cancer. Cancer Chemother Pharmacol. 2009 May;63(6):1103-10.
37 Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478. Biochem Pharmacol. 2009 Mar 1;77(5):781-93.
38 Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51.
39 The phytoestrogen genistein enhances multidrug resistance in breast cancer cell lines by translational regulation of ABC transporters. Cancer Lett. 2016 Jun 28;376(1):165-72.
40 Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
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44 Intrinsic resistance to selumetinib, a selective inhibitor of MEK1/2, by cAMP-dependent protein kinase A activation in human lung and colorectal cancer cells.Br J Cancer.2012 May 8;106(10):1648-59.
45 Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells. Int J Cancer. 2013 Nov;133(9):2089-101.
46 The dual RAF/MEK inhibitor CH5126766/RO5126766 may be a potential therapy for RAS-mutated tumor cells.PLoS One.2014 Nov 25;9(11):e113217.
47 E6201, a novel kinase inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase-1 and mitogen-activated protein kinase/extracellular signal-regulated kinase kinase kinase-1: in vivo effects on cutaneous inflammatory responses by topical administration. J Pharmacol Exp Ther. 2010 Oct;335(1):23-31.
48 Clinical pipeline report, company report or official report of Roche.
49 doi: 10.1158/1535-7163.TARG-13-B281
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