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    Pralsetinib

    ACTIVE PHARMA INGREDIENTS

    DEVELOPMENTS

    INTERMEDIATES

    FINISHED DOSAGE FORMULATIONS

    DIGITAL CONTENT

    GLOBAL SALES INFORMATION

    PATENTS & EXCLUSIVITIES

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    2D Structure
    Also known as: Blu-667, 2097132-94-8, Pralsetinib free base, Gavreto, Cis-pralsetinib, Blu667
    Molecular Formula
    C27H32FN9O2
    Molecular Weight
    533.6  g/mol
    InChI Key
    GBLBJPZSROAGMF-SIYOEGHHSA-N
    FDA UNII
    1WPE73O1WV
    Pralsetinib is an orally bioavailable selective inhibitor of mutant forms of and fusion products involving the proto-oncogene receptor tyrosine kinase RET, with potential antineoplastic activity. Upon administration, pralsetinib binds to and targets various RET mutants and RET-containing fusion product. RET gene mutations and translocations result in the upregulation and/or activation of RET tyrosine kinase activity in various cancer cell types; dysregulation of RET activity plays a key role in the development and regression of these cancers.
    Pralsetinib is a Kinase Inhibitor. The mechanism of action of pralsetinib is as a Rearranged during Transfection (RET) Inhibitor.
    1 2D Structure

    2D Structure

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    N-[(1S)-1-[6-(4-fluoropyrazol-1-yl)pyridin-3-yl]ethyl]-1-methoxy-4-[4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]cyclohexane-1-carboxamide
    2.1.2 InChI
    InChI=1S/C27H32FN9O2/c1-16-11-22(33-23-12-17(2)35-36-23)34-25(31-16)19-7-9-27(39-4,10-8-19)26(38)32-18(3)20-5-6-24(29-13-20)37-15-21(28)14-30-37/h5-6,11-15,18-19H,7-10H2,1-4H3,(H,32,38)(H2,31,33,34,35,36)/t18-,19?,27?/m0/s1
    2.1.3 InChI Key
    GBLBJPZSROAGMF-SIYOEGHHSA-N
    2.1.4 Canonical SMILES
    CC1=CC(=NN1)NC2=NC(=NC(=C2)C)C3CCC(CC3)(C(=O)NC(C)C4=CN=C(C=C4)N5C=C(C=N5)F)OC
    2.1.5 Isomeric SMILES
    CC1=CC(=NN1)NC2=NC(=NC(=C2)C)C3CCC(CC3)(C(=O)N[C@@H](C)C4=CN=C(C=C4)N5C=C(C=N5)F)OC
    2.2 Other Identifiers
    2.2.1 UNII
    1WPE73O1WV
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. Blu-667

    2. Cyclohexanecarboxamide, N-((1s)-1-(6-(4-fluoro-1h-pyrazol-1-yl)-3-pyridinyl)ethyl)-1-methoxy-4-(4-methyl-6-((5-methyl-1h-pyrazol-3-yl)amino)-2-pyrimidinyl)-, Trans-

    3. Gavreto

    4. Trans-n-((1s)-1-(6-(4-fluoro-1h-pyrazol-1-yl)-3-pyridinyl)ethyl)-1-methoxy-4-(4-methyl-6-((5-methyl-1h-pyrazol-3-yl)amino)-2-pyrimidinyl)cyclohexanecarboxamide

    2.3.2 Depositor-Supplied Synonyms

    1. Blu-667

    2. 2097132-94-8

    3. Pralsetinib Free Base

    4. Gavreto

    5. Cis-pralsetinib

    6. Blu667

    7. Trans-pralsetinib

    8. Pralsetinib [inn]

    9. Pralsetinib [usan]

    10. Blu123244

    11. 1wpe73o1wv

    12. 2097132-93-7

    13. X581238

    14. 2097132-94-8 (free Base)

    15. Blu-123244

    16. N-[(1s)-1-[6-(4-fluoropyrazol-1-yl)pyridin-3-yl]ethyl]-1-methoxy-4-[4-methyl-6-[(5-methyl-1h-pyrazol-3-yl)amino]pyrimidin-2-yl]cyclohexane-1-carboxamide

    17. X-581238

    18. (cis)-n-((s)-1-(6-(4-fluoro-1h-pyrazol-1-yl)pyridin-3-yl)ethyl)-1-methoxy-4-(4-methyl-6-(5-methyl-1h-pyrazol-3-ylamino)pyrimidin-2-yl)cyclohexanecarboxamide

    19. Cis-n-{(1s)-1-[6-(4-fluoro-1h-pyrazol-1-yl)pyridin-3-yl]ethyl}-1-methoxy-4-{4-methyl-6-[(5-methyl-1h-pyrazol-3-yl)amino]pyrimidin-2-yl}cyclohexane-1-carboxamide

    20. Cyclohexanecarboxamide, N-((1s)-1-(6-(4-fluoro-1h-pyrazol-1-yl)-3-pyridinyl)ethyl)-1-methoxy-4-(4-methyl-6-((5-methyl-1h-pyrazol-3-yl)amino)-2-pyrimidinyl)-, Cis-

    21. Cyclohexanecarboxamide, N-[(1s)-1-[6-(4-fluoro-1h-pyrazol-1-yl)-3-pyridinyl]ethyl]-1-methoxy-4-[4-methyl-6-[(5-methyl-1h-pyrazol-3-yl)amino]-2-pyrimidinyl]-, Cis-

    22. Q4j

    23. Blu667blu667

    24. Cis-blu-667

    25. Pralsetinib (usan/inn)

    26. Blu-667 (pralsetinib)

    27. Unii-1wpe73o1wv

    28. Pralsetinib [who-dd]

    29. Chembl4582651

    30. Schembl18789228

    31. Schembl18789229

    32. Schembl18806610

    33. Gtpl10033

    34. Bdbm435009

    35. Bdbm435010

    36. Dtxsid901336540

    37. Amy16875

    38. Ex-a1944

    39. Ex-a3347

    40. Nsc811429

    41. S8716

    42. Us10584114, Compound 129

    43. Us10584114, Compound 130

    44. Who 11004

    45. Akos037648884

    46. Hy-112301a

    47. Nsc-811429

    48. Ac-35657

    49. Bs-15942

    50. Hy-112301

    51. Cs-0043448

    52. Cs-0044766

    53. D11712

    54. Blu-667; Trans-n-{(1s)-1-[6-(4-fluoro-1h-pyrazol-1-yl)pyridin-3-yl]ethyl}-1-methoxy-4-{4-methyl-6-[(5-methyl-1h-pyrazol-3-yl)amino]pyrimidin-2-yl}cyclohexane-1-carboxamide

    55. Trans-n-{(1s)-1-[6-(4-fluoro-1h-pyrazol-1-yl)pyridin-3-yl]ethyl}-1-methoxy-4-{4-methyl-6-[(5-methyl-1h-pyrazol-3-yl)amino]pyrimidin-2-yl}cyclohexane-1-carboxamide

    2.4 Create Date
    2017-08-04
    3 Chemical and Physical Properties
    Molecular Weight 533.6 g/mol
    Molecular Formula C27H32FN9O2
    XLogP33.1
    Hydrogen Bond Donor Count3
    Hydrogen Bond Acceptor Count9
    Rotatable Bond Count8
    Exact Mass533.26629946 g/mol
    Monoisotopic Mass533.26629946 g/mol
    Topological Polar Surface Area136 Ų
    Heavy Atom Count39
    Formal Charge0
    Complexity816
    Isotope Atom Count0
    Defined Atom Stereocenter Count1
    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

    Treatment of lung cancer (small cell and non-small cell lung cancer )

    Gavreto is indicated as monotherapy for the treatment of adult patients with rearranged during transfection (RET) fusion-positive advanced non-small cell lung cancer (NSCLC) not previously treated with a RET inhibitor.

    Treatment of thyroid cancer

    5 Pharmacology and Biochemistry
    5.1 MeSH Pharmacological Classification

    Antineoplastic Agents

    Substances that inhibit or prevent the proliferation of NEOPLASMS. (See all compounds classified as Antineoplastic Agents.)

    5.2 FDA Pharmacological Classification
    5.2.1 Active Moiety
    PRALSETINIB
    5.2.2 FDA UNII
    1WPE73O1WV
    5.2.3 Pharmacological Classes
    Rearranged during Transfection (RET) Inhibitors [MoA]; Kinase Inhibitor [EPC]
    5.3 ATC Code

    L01XE

    L - Antineoplastic and immunomodulating agents

    L01 - Antineoplastic agents

    L01E - Protein kinase inhibitors

    L01EX - Other protein kinase inhibitors

    L01EX23 - Pralsetinib