Telotristat etiprate

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MedKoo CAT#: 206122

CAS#: 1137608-69-5 (etiprate)

Description: Telotristat etiprate, its free base also known as LX1606 or LX1032, is an oral serotonin synthesis inhibitor or peripheral tryptophan hydroxylase (TPH) inhibitor . Telotristat etiprate has activity in controlling diarrhea associated with carcinoid syndrome. LX1606 acts by inhibiting the enzyme tryptophan hydoxylase (TPH) and reduces serotonin production both inside and outside the GI tract without affecting brain serotonin levels. TPH is the rate-limiting enzyme involved in serotonin biosynthesis and is present in metastatic carcinoid tumor cells.

Chemical Structure

Telotristat etiprate
CAS# 1137608-69-5 (etiprate)

Theoretical Analysis

MedKoo Cat#: 206122
Name: Telotristat etiprate
CAS#: 1137608-69-5 (etiprate)
Chemical Formula: C36H35ClF3N7O6
Exact Mass:
Molecular Weight: 754.16
Elemental Analysis: C, 57.33; H, 4.68; Cl, 4.70; F, 7.56; N, 13.00; O, 12.73

Price and Availability

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25.0mg USD 150.0 Same day
50.0mg USD 250.0 Same day
100.0mg USD 450.0 Same day
200.0mg USD 750.0 Same day
500.0mg USD 1550.0 Same day
1.0g USD 2550.0 Same day
2.0g USD 4550.0 Same day
5.0g USD 8650.0 Same day
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Related CAS #: 1137608-69-5 (etiprate)   1033805-22-9 (ethyl)   1033805-28-5 (acid)  

Synonym: LX1032 etiprate; LX1032 etiprate; LX 1032 etiprate; LX1606; LX1606 etiprate; LX 1606; LX 1606 Hippurate; Telotristat etiprate;

IUPAC/Chemical Name: (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 2-benzamidoacetate .


InChi Code: InChI=1S/C27H26ClF3N6O3.C9H9NO3/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;11-8(12)6-10-9(13)7-4-2-1-3-5-7/h4-11,13-14,20,24H,3,12,32H2,1-2H3,(H2,33,34,35);1-5H,6H2,(H,10,13)(H,11,12)/t20-,24+;/m0./s1

SMILES Code: O=C(OCC)[C@@H](N)CC1=CC=C(C2=NC(N)=NC(O[C@H](C3=CC=C(Cl)C=C3N4N=C(C)C=C4)C(F)(F)F)=C2)C=C1.O=C(O)CNC(C5=CC=CC=C5)=O

Appearance: white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 754.16 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Pharmacoeconomic Review Report: Telotristat Ethyl (Xermelo): (Ipsen Biopharmaceuticals Canada Inc.): Indication: Refractory carcinoid syndrome diarrhea, in combination with somatostatin analogue (SSA) therapy, in patients inadequately controlled by SSA therapy alone [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2019 Jul. Available from PubMed PMID: 31532601.

2: CADTH Canadian Drug Expert Committee Recommendation: Telotristat Ethyl (Xermelo — Ipsen Biopharmaceuticals Canada Inc): Indication: For the treatment of refractory carcinoid syndrome diarrhea, in combination with somatostatin analogue (SSA) therapy, in patients inadequately controlled by SSA therapy alone [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2019 Jul. No abstract available. Available from PubMed PMID: 31525004.

3: Saavedra C, Barriuso J, McNamara MG, Valle JW, Lamarca A. Spotlight on telotristat ethyl for the treatment of carcinoid syndrome diarrhea: patient selection and reported outcomes. Cancer Manag Res. 2019 Aug 8;11:7537-7556. doi: 10.2147/CMAR.S181439. eCollection 2019. Review. PubMed PMID: 31496810; PubMed Central PMCID: PMC6690650.

4: Telotristat ethyl for carcinoid syndrome diarrhoea. Aust Prescr. 2019 Jun;42(3):112. doi: 10.18773/austprescr.2019.035. Epub 2019 Apr 24. Review. PubMed PMID: 31363315; PubMed Central PMCID: PMC6594843.

5: Strosberg J, Joish VN, Giacalone S, Perez-Olle R, Fish-Steagall A, Kapoor K, Dharba S, Lapuerta P, Benson AB. TELEPRO: Patient-Reported Carcinoid Syndrome Symptom Improvement Following Initiation of Telotristat Ethyl in the Real World. Oncologist. 2019 Nov;24(11):1446-1452. doi: 10.1634/theoncologist.2018-0921. Epub 2019 Jun 12. PubMed PMID: 31189618; PubMed Central PMCID: PMC6853091.

6: Anthony LB, Kulke MH, Caplin ME, Bergsland E, Öberg K, Pavel M, Hörsch D, Warner RRP, O'Dorisio TM, Dillon JS, Lapuerta P, Kassler-Taub K, Jiang W. Long-Term Safety Experience with Telotristat Ethyl Across Five Clinical Studies in Patients with Carcinoid Syndrome. Oncologist. 2019 Aug;24(8):e662-e670. doi: 10.1634/theoncologist.2018-0236. Epub 2019 Jan 16. PubMed PMID: 30651397; PubMed Central PMCID: PMC6693702.

7: Jiang W, Perez-Olle R, Lapuerta P. In Reply: Telotristat Ethyl for Patients With Carcinoid Syndrome Associated With Chest Pain and Hypertension. Pancreas. 2018 Oct;47(9):e57. doi: 10.1097/MPA.0000000000001138. PubMed PMID: 30153219; PubMed Central PMCID: PMC6143199.

8: Kasi PM. Telotristat ethyl for the treatment of carcinoid syndrome diarrhea not controlled by somatostatin analogues. Drugs Today (Barc). 2018 Jul;54(7):423-432. doi: 10.1358/dot.2018.54.7.2834460. Review. PubMed PMID: 30090879.

9: Lyseng-Williamson KA. Telotristat Ethyl: A Review in Carcinoid Syndrome Diarrhoea. Drugs. 2018 Jun;78(9):941-950. doi: 10.1007/s40265-018-0935-1. Review. PubMed PMID: 29931594.

10: Weickert MO, Kaltsas G, Hörsch D, Lapuerta P, Pavel M, Valle JW, Caplin ME, Bergsland E, Kunz PL, Anthony LB, Grande E, Öberg K, Welin S, Lombard-Bohas C, Ramage JK, Kittur A, Yang QM, Kulke MH. Changes in Weight Associated With Telotristat Ethyl in the Treatment of Carcinoid Syndrome. Clin Ther. 2018 Jun;40(6):952-962.e2. doi: 10.1016/j.clinthera.2018.04.006. Epub 2018 May 1. PubMed PMID: 29724499.

11: Dillon JS, Chandrasekharan C. Telotristat ethyl: a novel agent for the therapy of carcinoid syndrome diarrhea. Future Oncol. 2018 May;14(12):1155-1164. doi: 10.2217/fon-2017-0340. Epub 2018 Jan 19. PubMed PMID: 29350062; PubMed Central PMCID: PMC6734517.

12: Pavel M, Gross DJ, Benavent M, Perros P, Srirajaskanthan R, Warner RRP, Kulke MH, Anthony LB, Kunz PL, Hörsch D, Weickert MO, Lapuerta P, Jiang W, Kassler-Taub K, Wason S, Fleming R, Fleming D, Garcia-Carbonero R. Telotristat ethyl in carcinoid syndrome: safety and efficacy in the TELECAST phase 3 trial. Endocr Relat Cancer. 2018 Mar;25(3):309-322. doi: 10.1530/ERC-17-0455. Epub 2018 Jan 12. PubMed PMID: 29330194; PubMed Central PMCID: PMC5811631.

13: Kasi PM. Telotristat Ethyl for Patients With Carcinoid Syndrome Associated With Chest Pain and Hypertension. Pancreas. 2018 Jan;47(1):e2. doi: 10.1097/MPA.0000000000000971. PubMed PMID: 29232344.

14: Joish VN, Frech F, Lapuerta P. Budgetary Impact of Telotristat Ethyl, a Novel Treatment for Patients with Carcinoid Syndrome Diarrhea: A US Health Plan Perspective. Clin Ther. 2017 Dec;39(12):2338-2344. doi: 10.1016/j.clinthera.2017.10.019. Epub 2017 Nov 23. PubMed PMID: 29175096.

15: Anthony L, Ervin C, Lapuerta P, Kulke MH, Kunz P, Bergsland E, Hörsch D, Metz DC, Pasieka J, Pavlakis N, Pavel M, Caplin M, Öberg K, Ramage J, Evans E, Yang QM, Jackson S, Arnold K, Law L, DiBenedetti DB. Understanding the Patient Experience with Carcinoid Syndrome: Exit Interviews from a Randomized, Placebo-controlled Study of Telotristat Ethyl. Clin Ther. 2017 Nov;39(11):2158-2168. doi: 10.1016/j.clinthera.2017.09.013. Epub 2017 Oct 23. PubMed PMID: 29074312.

16: Masab M, Saif MW. Telotristat ethyl: proof of principle and the first oral agent in the management of well-differentiated metastatic neuroendocrine tumor and carcinoid syndrome diarrhea. Cancer Chemother Pharmacol. 2017 Dec;80(6):1055-1062. doi: 10.1007/s00280-017-3462-y. Epub 2017 Oct 19. Review. PubMed PMID: 29051994.

17: Joish VN, Frech F, Lapuerta P. Cost-effectiveness analysis of telotristat ethyl for treatment of carcinoid syndrome diarrhea inadequately controlled with somatostatin analogs. J Med Econ. 2018 Feb;21(2):182-188. doi: 10.1080/13696998.2017.1387120. Epub 2017 Oct 9. PubMed PMID: 28959913.

18: Telotristat ethyl (Xermelo) for carcinoid syndrome diarrhea. Med Lett Drugs Ther. 2017 Jul 17;59(1525):119-120. PubMed PMID: 28699933.

19: Markham A. Telotristat Ethyl: First Global Approval. Drugs. 2017 May;77(7):793-798. doi: 10.1007/s40265-017-0737-x. PubMed PMID: 28382568.

20: Kulke MH, Hörsch D, Caplin ME, Anthony LB, Bergsland E, Öberg K, Welin S, Warner RR, Lombard-Bohas C, Kunz PL, Grande E, Valle JW, Fleming D, Lapuerta P, Banks P, Jackson S, Zambrowicz B, Sands AT, Pavel M. Telotristat Ethyl, a Tryptophan Hydroxylase Inhibitor for the Treatment of Carcinoid Syndrome. J Clin Oncol. 2017 Jan;35(1):14-23. Epub 2016 Oct 28. PubMed PMID: 27918724.

Additional Information

Related CAS#
CAS#1033805-22-9 (Telotristat ethyl)
CAS#1033805-28-5 (Telotristat)
CAS#1137608-69-5 (Telotristat etiprate)