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    Chemistry

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    Also known as: 1033805-22-9, Lx1606, Lx 1606, Xermelo, (s)-ethyl 2-amino-3-(4-(2-amino-6-((r)-1-(4-chloro-2-(3-methyl-1h-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate, Lx-1606
    Molecular Formula
    C27H26ClF3N6O3
    Molecular Weight
    575.0  g/mol
    InChI Key
    MDSQOJYHHZBZKA-GBXCKJPGSA-N
    FDA UNII
    8G388563M7
    Telotristat Ethyl
    Telotristat Ethyl is the ethyl ester form of telotristat, a tryptophan hydroxylase (TPH) inhibitor, with potential anti-serotonergic activity. Upon administration, telotristat binds to and inhibits the activity of TPH. This may result in a reduction in peripheral serotonin (5-HT) production and improvement of serotonin-mediated gastrointestinal effects such as severe diarrhea. TPH, the rate-limiting enzyme in serotonin biosynthesis, is overexpressed in carcinoid tumor cells.
    1 2D Structure

    Telotristat Ethyl

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    ethyl (2S)-2-amino-3-[4-[2-amino-6-[(1R)-1-[4-chloro-2-(3-methylpyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]pyrimidin-4-yl]phenyl]propanoate
    2.1.2 InChI
    InChI=1S/C27H26ClF3N6O3/c1-3-39-25(38)20(32)12-16-4-6-17(7-5-16)21-14-23(35-26(33)34-21)40-24(27(29,30)31)19-9-8-18(28)13-22(19)37-11-10-15(2)36-37/h4-11,13-14,20,24H,3,12,32H2,1-2H3,(H2,33,34,35)/t20-,24+/m0/s1
    2.1.3 InChI Key
    MDSQOJYHHZBZKA-GBXCKJPGSA-N
    2.1.4 Canonical SMILES
    CCOC(=O)C(CC1=CC=C(C=C1)C2=CC(=NC(=N2)N)OC(C3=C(C=C(C=C3)Cl)N4C=CC(=N4)C)C(F)(F)F)N
    2.1.5 Isomeric SMILES
    CCOC(=O)[C@H](CC1=CC=C(C=C1)C2=CC(=NC(=N2)N)O[C@H](C3=C(C=C(C=C3)Cl)N4C=CC(=N4)C)C(F)(F)F)N
    2.2 Other Identifiers
    2.2.1 UNII
    8G388563M7
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. Lx1032

    2. Xermelo

    2.3.2 Depositor-Supplied Synonyms

    1. 1033805-22-9

    2. Lx1606

    3. Lx 1606

    4. Xermelo

    5. (s)-ethyl 2-amino-3-(4-(2-amino-6-((r)-1-(4-chloro-2-(3-methyl-1h-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate

    6. Lx-1606

    7. Telotristat Ethyl [usan]

    8. Lx 1032

    9. Lx1032

    10. Lx-1032

    11. Ethyl (2s)-2-amino-3-[4-[2-amino-6-[(1r)-1-[4-chloro-2-(3-methylpyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]pyrimidin-4-yl]phenyl]propanoate

    12. 8g388563m7

    13. Telotristat Ethyl (usan)

    14. Lx-1606 Hippurate

    15. Telotristat Etiprate (lx 1606 Hippurate)

    16. Telotristat-ethyl

    17. Unii-8g388563m7

    18. Xermelo (tn)

    19. Schembl610588

    20. Telotristat Ethyl [mi]

    21. Gtpl9490

    22. Chembl2105695

    23. Ex-a322

    24. Bdbm445704

    25. Dtxsid001102271

    26. Telotristat Ethyl [who-dd]

    27. Amy38688

    28. Hy-13055a

    29. Lx1606lx1606

    30. Mfcd18251583

    31. Zinc43205655

    32. Bcp9000866

    33. Db12095

    34. Us10683309, Example Lx1606

    35. Ncgc00390241-01

    36. Ncgc00390241-07

    37. As-35061

    38. D09974

    39. J-524318

    40. Q27270371

    41. Ethyl 4-(2-amino-6-((1r)-1-(4-chloro-2-(3-methyl-1h-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pryrimidin-4-yl)-l-phenylalaninate

    42. L-phenylalanine, 4-(2-amino-6-((1r)-1-(4-chloro-2-(3-methyl-1h-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)-4-pryrimidinyl)-, Ethyl Ester

    2.4 Create Date
    2009-03-16
    3 Chemical and Physical Properties
    Molecular Weight 575.0 g/mol
    Molecular Formula C27H26ClF3N6O3
    XLogP35.1
    Hydrogen Bond Donor Count2
    Hydrogen Bond Acceptor Count11
    Rotatable Bond Count10
    Exact Mass574.1707009 g/mol
    Monoisotopic Mass574.1707009 g/mol
    Topological Polar Surface Area131 Ų
    Heavy Atom Count40
    Formal Charge0
    Complexity821
    Isotope Atom Count0
    Defined Atom Stereocenter Count2
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Information
    1 of 1  
    Drug NameXERMELO
    Active IngredientTELOTRISTAT ETIPRATE
    CompanyLEXICON PHARMS INC (Application Number: N208794. Patents: 7553840, 7709493, 7968559, 8193204, 8653094)

    4.2 Drug Indication

    As a serotonin synthesis inhibitor, telotristat etiprate, has the potential to reduce serotonin levels and address the key elements of carcinoid syndrome.

    Xermelo is indicated for the treatment of carcinoid syndrome diarrhoea in combination with somatostatin analogue (SSA) therapy in adults inadequately controlled by SSA therapy.

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    Activity is mainly in the gastrointestinal tract, with minimal effects reported on the brain and cardiovascular system, accompanied by an excellent safety profile. In normal mice, telotristat etiprate (administered once daily for 4 days at doses of 15300 mg/kg/day) was found to reduce serotonin levels throughout the gastrointestinal tract. These reductions occurred in a dose dependent fashion with maximal effects observed with doses of telotristat etiprate 150 mg/kg. No significant change in brain serotonin or 5-hydroxyindoleacetic acid (5-HIAA, a serotonin metabolite) was observed. Similar findings were seen in Sprague-Dawley rats. Gastrointestinal motility studies were conducted in rats using the charcoal meal test. There was a significant dose-related delay in both gastrointestinal transit and gastric emptying, associated with a reduction in blood serotonin levels and proximal colon serotonin. A quantitative whole-body autoradiography study was conducted to assess the absorption, distribution and excretion of radioactivity in rats following a single oral dose of telotristat etiprate labeled with carbon 14. Rats were administered either 30 mg/kg or 100 mg/kg of the compound. The distribution of radioactivity was limited to tissues of the hepatic and renal system and the contents of the GI tract. There was no measurable radioactivity in the brain at any dose tested.

    5.2 FDA Pharmacological Classification
    5.2.1 Pharmacological Classes
    Tryptophan Hydroxylase Inhibitors [MoA]; Tryptophan Hydroxylase Inhibitor [EPC]
    5.3 ATC Code

    A16A

    5.4 Absorption, Distribution and Excretion

    Absorption

    Low systemic absorption. Tmax of 24 h, supporting the 8-hourly administration

    Route of Elimination

    Telotristat ethyl is mainly excreted in feces.

    Clearance

    Not available

    5.5 Metabolism/Metabolites

    Metabolized by the liver.

    5.6 Biological Half-Life

    412 h

    5.7 Mechanism of Action

    Telotristat etiprate is an ethyl ester prodrug which is hydrolyzed to its active moiety LP-778902 both in vivo and in vitro. Systemic exposure of telotristat etiprate is relatively low, as the hydrolysis to the active moiety is rapid. LP-778902 is a potent inhibitor of TPH with an in vivo IC50 of 0.028 M. While existing treatments for carcinoid syndrome work to reduce the release of serotonin outside tumor cells, telotristat etiprate works at the source to reduce serotonin production within the tumor cells. By specifically inhibiting serotonin production, telotristat etiprate seeks to control this important driver of carcinoid syndrome and, in turn, provide patients with more control over their disease.

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