telotristat: a tryptophan hydroxylase inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 25025298 |
| CHEMBL ID | 2103855 |
| CHEBI ID | 177736 |
| SCHEMBL ID | 612353 |
| MeSH ID | M000599125 |
| Synonym |
|---|
| (2s)-2-amino-3-[4-[2-amino-6-[(1r)-1-[4-chloro-2-(3-methylpyrazol-1-yl)phenyl]-2,2,2-triluoroethoxy]pyrimidin-4-yl]phenyl]propanoic acid |
| 1033805-28-5 |
| telotristat |
| CHEBI:177736 |
| D09973 |
| telotristat (usan/inn) |
| (s)-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)propanoic acid |
| lp-778902 |
| 381v4fcv2z , |
| telotristat [usan:inn] |
| unii-381v4fcv2z |
| lp 778902 |
| CHEMBL2103855 |
| telotristat [mi] |
| telotristat [usan] |
| l-phenylalanine, 4-(2-amino-6-((1r)-1-(4-chloro-2-(3-methyl-1h-pyrazol-1-yl)phenyl)- 2,2,2-trifluoroethoxy)-4-pryrimidinyl)- |
| 2s)-2-amino-3-(4-(2-amino-6-(((1r)-1-(4-chloro-2-(3-methyl-1h-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethyl)oxy)pyrimidin-4-yl)phenyl)propanoic acid |
| 4-(2-amino-6-((1r)-1-(4-chloro-2-(3-methyl-1h-pyrazol-1-yl)phenyl)-2,2,2- trifluoroethoxy)pryrimidin-4-yl)-l-phenylalanine |
| telotristat [who-dd] |
| telotristat [inn] |
| HY-13055B |
| SCHEMBL612353 |
| DTXSID60145805 , |
| bdbm50145648 |
| AKOS027338710 |
| mfcd20528907 |
| NCGC00485953-01 |
| telotristat, lp778902 |
| EX-A1620 |
| DB14218 |
| (2s)-2-amino-3-(4-{2-amino-6-[(1r)-1-[4-chloro-2-(3-methyl-1h-pyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]pyrimidin-4-yl}phenyl)propanoic acid |
| Q27256725 |
| MS-30026 |
| (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]propanoic acid |
| F86418 |
| l-phenylalanine, 4-(2-amino-6-((1r)-1-(4-chloro-2-(3-methyl-1h-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)-4-pryrimidinyl)- |
| 4-(2-amino-6-((1r)-1-(4-chloro-2-(3-methyl-1h-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pryrimidin-4-yl)-l-phenylalanine |
| dtxcid4068296 |
| a16ax15 |
| telotristatum |
| AC-35764 |
Telotristat is an inhibitor of tryptophan hydroxylase (TPH), preventing the production of serotonin. It has demonstrated in the phase III TELESTAR clinical trial a significant improvement in the control of bowel movements in patients with NETs.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Telotristat is an inhibitor of tryptophan hydroxylase (TPH), preventing the production of serotonin." | ( The journey from gene knockout to clinical medicine: telotristat and sotagliflozin. Rendell, MS, 2019) | 1.48 |
| "Telotristat etiprate is a potent inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the synthesis of serotonin, that has demonstrated in the phase III TELESTAR clinical trial a significant improvement in the control of bowel movements in patients with NETs who have carcinoid syndrome and who have progressed to an SSA." | ( Inhibition of Peripheral Synthesis of Serotonin as a New Target in Neuroendocrine Tumors. Alonso-Gordoa, T; Grande, E; Martínez-Sáez, O; Molina-Cerrillo, J, 2016) | 1.16 |
| "Telotristat ethyl is a tryptophan hydroxylase inhibitor, developed for the treatment of carcinoid syndrome." | ( Telotristat ethyl: a new option for the management of carcinoid syndrome. Barriuso, J; Hubner, RA; Lamarca, A; McNamara, MG; Valle, JW, 2016) | 2.6 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
| Class | Description |
|---|---|
| phenylalanine derivative | An amino acid derivative resulting from reaction of alanine at the amino group or the carboxy group, or from the replacement of any hydrogen of phenylalanine by a heteroatom. The definition normally excludes peptides containing phenylalanine residues. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Tryptophan 5-hydroxylase 1 | Homo sapiens (human) | IC50 (µMol) | 0.2673 | 0.0160 | 0.3462 | 0.7700 | AID1278166; AID1298868; AID1885931 |
| Tryptophan 5-hydroxylase 2 | Homo sapiens (human) | IC50 (µMol) | 0.7100 | 0.7100 | 0.7100 | 0.7100 | AID1885932 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| iron ion binding | Tryptophan 5-hydroxylase 1 | Homo sapiens (human) |
| protein binding | Tryptophan 5-hydroxylase 1 | Homo sapiens (human) |
| tryptophan 5-monooxygenase activity | Tryptophan 5-hydroxylase 1 | Homo sapiens (human) |
| tryptophan 5-monooxygenase activity | Tryptophan 5-hydroxylase 2 | Homo sapiens (human) |
| iron ion binding | Tryptophan 5-hydroxylase 2 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| cytosol | Tryptophan 5-hydroxylase 1 | Homo sapiens (human) |
| neuron projection | Tryptophan 5-hydroxylase 1 | Homo sapiens (human) |
| cytosol | Tryptophan 5-hydroxylase 2 | Homo sapiens (human) |
| neuron projection | Tryptophan 5-hydroxylase 2 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347163 | 384 well plate NINDS AMC confirmatory qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347169 | Tertiary RLuc qRT-PCR qHTS assay for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347157 | Confirmatory screen GU Rhodamine qHTS for Zika virus inhibitors qHTS | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347161 | Confirmatory screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347164 | 384 well plate NINDS Rhodamine confirmatory qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347172 | Secondary qRT-PCR qHTS assay for selected Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347170 | Vero cells viability counterscreen for qRT-PCR qHTS assay of selected Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1885931 | Inhibition of N-terminal MBP-tagged full length human TPH1 assessed as reduction in 5-HTP formation incubated for 5 to 10 mins by fluorescence microplate reader analysis | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16 | Structure-Based Design of Xanthine-Benzimidazole Derivatives as Novel and Potent Tryptophan Hydroxylase Inhibitors. |
| AID1298868 | Inhibition of TPH1 (unknown origin) | 2016 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12 | Discovery of acyl guanidine tryptophan hydroxylase-1 inhibitors. |
| AID1885932 | Inhibition of N-terminal MBP-tagged full length human TPH2 assessed as reduction in 5-HTP formation incubated for 5 to 10 mins by fluorescence microplate reader analysis | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16 | Structure-Based Design of Xanthine-Benzimidazole Derivatives as Novel and Potent Tryptophan Hydroxylase Inhibitors. |
| AID1278166 | Inhibition of TPH1 (unknown origin) | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Discovery of spirocyclic proline tryptophan hydroxylase-1 inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 13 (72.22) | 24.3611 |
| 2020's | 5 (27.78) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (53.23) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 3 (16.67%) | 5.53% |
| Reviews | 5 (27.78%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 10 (55.56%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||