menu
    • menu

    Find Selumetinib manufacturers, exporters & distributors on PharmaCompass

    Polfa Tarchomin is a leading Polish pharmaceutical company with 200 year tradition in manufacture and sale of pharmaceutical products.

    Virtual Booth

    Contact Supplier

    Aurigene is a global leader in accelerating drug innovation through discovery, development & manufacturing.

    Virtual Booth

    Contact Supplier

    Midas Pharma provides expertise in developing and supplying APIs, finished products, and intermediates.

    Virtual Booth

    Contact Supplier

    ChemWerth works in generic API development & supply, non-infringement patent strategy development and regulatory support.

    Virtual Booth

    Contact Supplier

    Mission CDMO team brings reliability, resourcefulness, & responsiveness in executing your development project.

    Virtual Booth

    Contact Supplier

    xyz-pharma-m-2025-01-06

    Virtual Booth

    Contact Supplier

    ACTIVE PHARMA INGREDIENTS

    DEVELOPMENTS

    FINISHED DOSAGE FORMULATIONS

    DIGITAL CONTENT

    GLOBAL SALES INFORMATION

    MARKET PLACE

    PATENTS & EXCLUSIVITIES

    PharmaCompass

    Synopsis

    Related ProductsRelated Products

    Synopsis

    ACTIVE PHARMA INGREDIENTS

    2

    API Suppliers

    API Suppliers

    0

    USDMF

    US DMFs Filed

    0

    CEP/COS

    CEP/COS Certifications

    0

    JDMF

    JDMFs Filed

    0

    EU WC

    EU WC

    0

    KDMF

    KDMF

    2

    NDC API

    NDC API

    0

    VMF

    NDC API

    2

    Listed Suppliers

    Other Suppliers

    API REF. PRICE (USD/KG)

    $
    $ 17,197

    MARKET PLACE

    2

    API

    0

    FDF

    0INTERMEDIATES

    FINISHED DOSAGE FORMULATIONS

    6

    FDF Dossiers

    FDF Dossiers

    2

    FDA Orange Book

    FDA (Orange Book)

    2

    Europe

    Europe

    0

    Canada

    Canada

    2

    Australia

    Australia

    0

    South Africa

    South Africa

    0

    Listed Dossiers

    Listed Dossiers

    6DRUGS IN DEVELOPMENT

    FDF Dossiers

    DRUG PRODUCT COMPOSITIONS

    REF. STANDARDS OR IMPURITIES

    0

    EDQM

    0

    USP

    0

    JP

    0

    Others

    PATENTS & EXCLUSIVITIES

    10

    US Patents

    4

    US Exclusivities

    0

    Health Canada Patents

    DIGITAL CONTENT

    0

    Data Compilation #PharmaFlow

    0

    Stock Recap #PipelineProspector

    0

    Weekly News Recap #Phispers

    21

    News #PharmaBuzz

    GLOBAL SALES INFORMATION

    US Medicaid

    10,000,943

    Annual Reports

    685

    Finished Drug Prices

    Listed Dossiers

    0RELATED EXCIPIENT COMPANIES

    0EXCIPIENTS BY APPLICATIONS

    Chemistry

    Click the arrow to open the dropdown
    read-moreClick the button for full data set
    read-moreClick the button for full data set
    Also known as: 606143-52-6, Azd6244, Arry-142886, Azd 6244, 5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-n-(2-hydroxyethoxy)-1-methyl-1h-benzimidazole-6-carboxamide, Azd-6244
    Molecular Formula
    C17H15BrClFN4O3
    Molecular Weight
    457.7  g/mol
    InChI Key
    CYOHGALHFOKKQC-UHFFFAOYSA-N
    FDA UNII
    6UH91I579U
    Selumetinib
    Selumetinib is an orally active, small molecule with potential antineoplastic activity. Selumetinib is an ATP-independent inhibitor of mitogen-activated protein kinase kinase (MEK or MAPK/ERK kinase) 1 and 2. MEK 1 and 2 are dual specificity kinases that are essential mediators in the activation of the RAS/RAF/MEK/ERK pathway, are often upregulated in various cancer cells, and are drivers of diverse cellular responses, including proliferation. Inhibition of both MEK1 and 2 by selumetinib prevents the activation of MEK1/2 dependent effector proteins and transcription factors, thereby leading to an inhibition of cellular proliferation in various cancers.
    Selumetinib is a Kinase Inhibitor. The mechanism of action of selumetinib is as a Mitogen-Activated Protein Kinase Kinase 1 Inhibitor, and Mitogen-Activated Protein Kinase Kinase 2 Inhibitor.
    1 2D Structure

    Selumetinib

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide
    2.1.2 InChI
    InChI=1S/C17H15BrClFN4O3/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)
    2.1.3 InChI Key
    CYOHGALHFOKKQC-UHFFFAOYSA-N
    2.1.4 Canonical SMILES
    CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO
    2.2 Other Identifiers
    2.2.1 UNII
    6UH91I579U
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. Arry 142886

    2. Arry-142886

    3. Arry142886

    4. Azd 6244

    5. Azd-6244

    6. Azd6244

    2.3.2 Depositor-Supplied Synonyms

    1. 606143-52-6

    2. Azd6244

    3. Arry-142886

    4. Azd 6244

    5. 5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-n-(2-hydroxyethoxy)-1-methyl-1h-benzimidazole-6-carboxamide

    6. Azd-6244

    7. Selumetinib (azd6244)

    8. Arry 142886

    9. Arry-886

    10. Azd6244 (selumetinib)

    11. 5-((4-bromo-2-chlorophenyl)amino)-4-fluoro-n-(2-hydroxyethoxy)-1-methyl-1h-benzo[d]imidazole-6-carboxamide

    12. Koselugo

    13. 5-(4-bromo-2-chlorophenylamino)-4-fluoro-n-(2-hydroxyethoxy)-1-methyl-1h-benzo[d]imidazole-6-carboxamide

    14. Chembl1614701

    15. Chebi:90227

    16. 6uh91i579u

    17. Nsc741078

    18. Ncgc00189073-01

    19. Ncgc00189073-02

    20. 6-(4-bromo-2-chloroanilino)-7-fluoro-n-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide

    21. Dsstox_cid_28870

    22. Dsstox_rid_83139

    23. Dsstox_gsid_48944

    24. 1h-benzimidazole-6-carboxamide, 5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-n-(2-hydroxyethoxy)-1-methyl-

    25. 6-[(4-bromo-2-chlorophenyl)amino]-7-fluoro-n-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide

    26. Azd 6244;5-((4-bromo-2-chlorophenyl)amino)-4-fluoro-n-(2-hydroxyethoxy)-1-methyl-1h-benzo[d]imidazole-6-carboxamide;6-(4-bromo-2-chlorophenylamino)-7-fluoro-n-(2-hydroxyethoxy)-3-methyl-3h-benzo[d]imidazole-5-carboxamide

    27. Cas-606143-52-6

    28. Arry142886

    29. Selumetinib [usan:inn]

    30. Selumetinibum

    31. Unii-6uh91i579u

    32. 1h-benzimidazole-6-carboxamide, 5-((4-bromo-2-chlorophenyl)amino)-4-fluoro-n-(2-hydroxyethoxy)-1-methyl-

    33. 3ew

    34. 5-((4-bromo-2-chlorophenyl)amino)-4-fluoro-n-(2-hydroxyethoxy)-1-methyl-1h-benzimidazole-6-carboxamide

    35. Selumetinib [mi]

    36. Selumetinib [inn]

    37. Selumetinib (usan/inn)

    38. Selumetinib [usan]

    39. Azd6244 - Selumetinib

    40. Selumetinib [who-dd]

    41. Schembl155456

    42. Gtpl5665

    43. Selumetinib, Arry-142886

    44. Dtxsid3048944

    45. Ex-a020

    46. Bcpp000367

    47. Hms3244g03

    48. Hms3244g04

    49. Hms3244h03

    50. Hms3265k01

    51. Hms3265k02

    52. Hms3265l01

    53. Hms3265l02

    54. Hms3654o03

    55. Nsc 741o78

    56. Bcp01739

    57. Tox21_113362

    58. Bdbm50355497

    59. Mfcd11977472

    60. Nsc800882

    61. S1008

    62. Zinc31773258

    63. Akos015904255

    64. Tox21_113362_1

    65. Bcp9000354

    66. Ccg-264774

    67. Cs-0059

    68. Db11689

    69. Ex-8621

    70. Nsc-741078

    71. Nsc-800882

    72. Sb14707

    73. Ncgc00189073-07

    74. 6-(4-bromo-2-chloro-anilino)-7-fluoro-n-(2-hydroxyethoxy)-3-methyl-benzimidazole-5-carboxamide

    75. Ac-25059

    76. Am808016

    77. Azd6244,selumetinib, Arry-142886

    78. Hy-50706

    79. Selumetinib (arry142886/azd6244)

    80. Azd6244 (selumetinib,arry-142886)

    81. Ft-0674552

    82. Sw202561-3

    83. D09666

    84. 143a526

    85. Q-101405

    86. Q7448840

    87. Brd-k57080016-001-01-9

    88. 1h-benzimidazole-6-carboxamide, 5-((4-bromo-2-chlorophenyl)amino)-4-fluoro-n-(2- Hydroxyethoxy)-1-methyl-

    89. 5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-n-(2-hydroxyethoxy)-1-methyl-1h-1,3-benzodiazole-6-carboxamide

    90. 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3h-benzoimidazole-5-carboxylic Acid (2-hydroxy -ethoxy)-amide

    91. 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3h-benzoimidazole-5-carboxylic Acid (2-hydroxy-ethoxy)-amide

    92. 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3h-benzoimidazole-5-carboxylic Acid(2-hydroxy-ethoxy)-amide

    93. 6-(4-bromo-2-chlorophenylamino)-7-fluoro-3-methyl-3h-benzoimidazole-5-carboxylic Acid (2-hydroxyethoxy)-amide

    94. 6-(4-bromo-2-chlorophenylamino)-7-fluoro-3-methyl-3h-benzoimidazole-5-carboxylic Acid(2-hydroxyethoxy)-amide

    95. 6-(4-bromo-2chloro-phenylamino)-7-fluoro-3-methyl-3h-benzoimidazole-5-carboxylic Acid (2-hydroxy-ethoxy)-amide

    2.4 Create Date
    2006-10-25
    3 Chemical and Physical Properties
    Molecular Weight 457.7 g/mol
    Molecular Formula C17H15BrClFN4O3
    XLogP33.6
    Hydrogen Bond Donor Count3
    Hydrogen Bond Acceptor Count6
    Rotatable Bond Count6
    Exact Mass456.00001 g/mol
    Monoisotopic Mass456.00001 g/mol
    Topological Polar Surface Area88.4 Ų
    Heavy Atom Count27
    Formal Charge0
    Complexity523
    Isotope Atom Count0
    Defined Atom Stereocenter Count0
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Indication

    Although selumetinib has been investigated for the treatment of several types of cancer, it is currently only indicated for the treatment of neurofibromatosis type 1 (NF1) in patients 2 years who have symptomatic, inoperable plexiform neurofibromas (PN).

    FDA Label

    Koselugo as monotherapy is indicated for the treatment of symptomatic, inoperable plexiform neurofibromas (PN) in paediatric patients with neurofibromatosis type 1 (NF1) aged 3 years and above

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    Selumetinib is a non-ATP-competitive mitogen-activated protein kinase kinase 1 and 2 (MEK1 and MEK2) inhibitor. By selectively targeting MEK1 and MEK2, selumetinib is able to inhibit oncogenic downstream effects of the Raf-MEK-ERK signaling pathway, which is often overactive in certain types of cancer. Indeed, a study investigating the effects of selumetinib in children with NF-1 found that treatment with the anti-neoplastic resulted in reduced tumor size. Decreases in tumor-associated pain and improvements in overall function were also subjectively reported. Selumetinib has minimal off-target activity, contributing to its impressive safety profile.

    5.2 FDA Pharmacological Classification
    5.2.1 Active Moiety
    SELUMETINIB
    5.2.2 FDA UNII
    6UH91I579U
    5.2.3 Pharmacological Classes
    Mitogen-Activated Protein Kinase Kinase 1 Inhibitors [MoA]; Mitogen-Activated Protein Kinase Kinase 2 Inhibitors [MoA]; Kinase Inhibitor [EPC]
    5.3 ATC Code

    L - Antineoplastic and immunomodulating agents

    L01 - Antineoplastic agents

    L01E - Protein kinase inhibitors

    L01EE - Mitogen-activated protein kinase (mek) inhibitors

    L01EE04 - Selumetinib

    5.4 Absorption, Distribution and Excretion

    Absorption

    Based on several studies investigating selumetinib at various doses in both pediatric and adult populations, the Tmax generally ranges between 1- 1.5 hours. In healthy adults, the mean absolute oral bioavailability was reported to be 62%. Selumetinib should be administered on an empty stomach since food significantly decreases serum concentrations of the drug.

    Route of Elimination

    Approximately 59% of selumetinib is eliminated in the feces, while 33% is eliminated in the urine.

    Volume of Distribution

    The mean apparent volume of distribution of selumetinib at steady state in pediatric patients ranged from 78 L to 171 L. A study in healthy adult males found a mean apparent volume of distribution of 146 L. Another study observing the pharmacokinetic effects of various selumetinib doses and regimens in select Japanese patients found that the apparent volume of distribution values at steady-state ranged from 73.2 - 148.1 L.

    Clearance

    The clearance of selumetinib in pediatric patients is 8.8 L/hr. A study in healthy adult males found a clearance value of 15.7 L/hr. Another study observing the pharmacokinetic effects of various selumetinib doses and regimens in select Japanese patients found clearance values that ranged from 9.2 - 15.9 L/hr.

    5.5 Metabolism/Metabolites

    Selumetinib is heavily metabolized in the liver and the proposed metabolic pathway is as follows: Hydrolysis of selumetinibs amide functional group produces M15 (AZ13326637), which contains a carboxylic acid. Elimination of the ethanediol moiety from the parent compound results in the formation of the primary amide M14 (AZ12791138) metabolite. Amide hydrolysis transforms M14 into M15, glucuronidation and further oxidation of M14 leads to M2, M6 and M1, and N-demethylation of M14 produces M12. The amide glucuronide (M2) is thought to be the major circulating metabolite. Demethylation of selumetinib produces the pharmacologically active M8 (AZ12442942), and further oxidation of M8 leads to M11. Glucuronidation of M8 produces M3 or M5, and elimination of the ethanediol moiety from M8 results in a primary amide, producing M12. Although the N-demethylated metabolite (M8) accounts for <10% of the circulating metabolites, it is responsible for approximately 21-35% of any observed pharmacological activity. Ribose conjugation transforms M12 into M9, while oxidation of M12 leads to M10 and M13 metabolites. Glucuronidation of M10 produces M1. Direct glucuronidation of selumetinib produces M4 or M7, which can both eventually transform into M3 and M5 metabolites.

    5.6 Biological Half-Life

    Selumetinib is characterized by a short half-life. The elimination half-life associated with a dose of 25 mg/m2 in pediatric patients is 6.2 hours. In a study observing the pharmacokinetic effects of various selumetinib regimens in select Japanese patients, the half-life ranged from 9.2- 10.6 hours. In other studies where selumetinib 75 mg is administered twice daily, the half-life is reported to be approximately 13 hours.

    5.7 Mechanism of Action

    The Ras-Raf-MEK-ERK signaling cascade is known to be activated in several types of cancer, and regulates the transcription of proteins involved in apoptosis. In addition, studies have shown that mutations of the Raf component of the pathway can contribute to chemotherapy drug resistance. Ras as well as several kinases and phosphatases are responsible for regulating the Raf-MEK-ERK pathway. Often in cancers, Ras (a G-protein coupled receptor) is deregulated, allowing downstream signalling to proceed unchecked. Through several complex steps, Raf phosphorylates and activates MEK, which then phosphorylates and activates ERK. ERK is then able to exert its effects on several downstream targets. As such, therapies inhibiting upstream components of this pathway have become attractive targets for cancer treatment. Selumetinib exerts its effects by selectively inhibiting MEK1 and MEK2 which can effectively blunt the pleiotropic effects of the Ras-Raf-MEK-ERK cascade. By inhibiting this oncogenic pathway, selumetinib reduces cell proliferation, and promotes pro-apoptotic signal transduction.

    Digital Content read-more

    Create Content with PharmaCompass, ask us

    NEWS #PharmaBuzz

    read-more
    read-more

    Global Sales Information

    Do you need Business Intel? Ask us

    Market Place

    Do you need sourcing support? Ask us

    Patents & EXCLUSIVITIES

    Check the patents & exclusivity for this product

    ABOUT THIS PAGE

    Selumetinib Manufacturers

    A Selumetinib manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of Selumetinib, including repackagers and relabelers. The FDA regulates Selumetinib manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. Selumetinib API Manufacturers are required to adhere to Good Manufacturing Practices (GMP) to ensure that their products are consistently manufactured to meet established quality criteria.

    click here to find a list of Selumetinib manufacturers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PhamaCompass.

    Selumetinib Suppliers

    A Selumetinib supplier is an individual or a company that provides Selumetinib active pharmaceutical ingredient (API) or Selumetinib finished formulations upon request. The Selumetinib suppliers may include Selumetinib API manufacturers, exporters, distributors and traders.

    click here to find a list of Selumetinib suppliers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PharmaCompass.

    Selumetinib NDC

    National Drug Code is a comprehensive database maintained by the FDA that contains information on all drugs marketed in the US. This directory includes information about finished drug products, unfinished drug products, and compounded drug products, including those containing Selumetinib as an active pharmaceutical ingredient (API).

    Finished drug products

    The FDA updates the NDC directory daily. The NDC numbers for Selumetinib API and other APIs are published in this directory by the FDA.

    Unfinished drugs

    The NDC unfinished drugs database includes product listing information submitted for all unfinished drugs, such as active pharmaceutical ingredients (APIs), drugs intended for further processing and bulk drug substances for compounding.

    Pharmaceutical companies that manufacture Selumetinib as an active pharmaceutical ingredient (API) must furnish the FDA with an updated record of all drugs that they produce, prepare, propagate, compound, or process for commercial distribution in the US at their facilities.

    Compounded drug products

    The NDC directory also contains data on finished compounded human drug products that contain Selumetinib and are produced by outsourcing facilities. While these outsourcing facilities are not mandated to assign a Selumetinib NDC to their finished compounded human drug products, they may choose to do so.

    click here to find a list of Selumetinib suppliers with NDC on PharmaCompass.

    Selumetinib GMP

    Selumetinib Active pharmaceutical ingredient (API) is produced in GMP-certified manufacturing facility.

    GMP stands for Good Manufacturing Practices, which is a system used in the pharmaceutical industry to make sure that goods are regularly produced and monitored in accordance with quality standards. The FDA’s current Good Manufacturing Practices requirements are referred to as cGMP or current GMP which indicates that the company follows the most recent GMP specifications. The World Health Organization (WHO) has its own set of GMP guidelines, called the WHO GMP. Different countries can also set their own guidelines for GMP like China (Chinese GMP) or the EU (EU GMP).

    PharmaCompass offers a list of Selumetinib GMP manufacturers, exporters & distributors, which can be sorted by USDMF, JDMF, KDMF, CEP (COS), WC, API price, and more, enabling you to easily find the right Selumetinib GMP manufacturer or Selumetinib GMP API supplier for your needs.

    Selumetinib CoA

    A Selumetinib CoA (Certificate of Analysis) is a formal document that attests to Selumetinib's compliance with Selumetinib specifications and serves as a tool for batch-level quality control.

    Selumetinib CoA mostly includes findings from lab analyses of a specific batch. For each Selumetinib CoA document that a company creates, the USFDA specifies specific requirements, such as supplier information, material identification, transportation data, evidence of conformity and signature data.

    Selumetinib may be tested according to a variety of international standards, such as European Pharmacopoeia (Selumetinib EP), Selumetinib JP (Japanese Pharmacopeia) and the US Pharmacopoeia (Selumetinib USP).

    Inform the supplier about your product requirements, specifying if you need a product with particular monograph like EP (Ph. Eur.), USP, JP, BP, or any other quality. In addition, clarify whether you need hydrochloride (HCl), anhydricum, base, micronisatum or a specific level of purity. To find reputable suppliers, utilize the filters and select those certified by GMP, FDA, or any other certification as per your requirement.
    For your convenience, we have listed synonyms and CAS numbers to help you find the best supplier. The use of synonyms and CAS numbers can be helpful in identifying potential suppliers, but it is crucial to note that they might not always indicate the exact same product. It is important to confirm the product details with the supplier before making a purchase to ensure that it meets your requirements.
    Ask Us for Pharmaceutical Supplier and Partner
    Ask Us, Find A Supplier / Partner
    No Commissions, No Strings Attached, Get Connected for FREE

    What are you looking for?

    How can we help you?

    The request can't be empty

    Please read our Privacy Policy carefully

    You must agree to the privacy policy

    The name can't be empty
    The company can't be empty.
    The email can't be empty Please enter a valid email.
    The mobile can't be empty

    Market Place

    Market Place

    PharmaCompass

    Home

    Market Place

    Menu

    Post Enquiry

    Post Enquiry

    Market Place

    Market Place

    Search