Telotristat ethyl
Xermelo (telotristat ethyl) is a small molecule pharmaceutical. Telotristat ethyl was first approved as Xermelo on 2017-09-17. It is used to treat diarrhea and malignant carcinoid syndrome in the USA. It has been approved in Europe to treat carcinoid tumor and neuroendocrine tumors. It is known to target tryptophan 5-hydroxylase 1.
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Trade Name
FDA
EMA
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Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
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Labels
FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| xermelo | New Drug Application | 2022-10-25 |
Indications
FDA
EMA
Indication | Ontology | MeSH | ICD-10 |
|---|---|---|---|
| diarrhea | HP_0002014 | D003967 | R19.7 |
| malignant carcinoid syndrome | — | D008303 | E34.0 |
Agency Specific
FDA
EMA
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Patent Expiration
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ATC Codes
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HCPCS
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Clinical
Clinical Trials
27 clinical trials
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Indications Phases 4
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Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Carcinoid heart disease | D002275 | EFO_1001769 | — | — | 1 | — | — | 1 |
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Neuroendocrine tumors | D018358 | EFO_1001901 | D3A.8 | — | 3 | — | — | 1 | 4 |
| Pancreatic neoplasms | D010190 | EFO_0003860 | C25 | — | 1 | — | — | 1 | 2 |
| Diarrhea | D003967 | HP_0002014 | R19.7 | — | 1 | — | — | — | 1 |
| Biliary tract neoplasms | D001661 | C24.9 | — | 1 | — | — | — | 1 | |
| Ulcerative colitis | D003093 | EFO_0000729 | K51 | — | 1 | — | — | — | 1 |
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Drug interactions | D004347 | 4 | — | — | — | — | 4 | ||
| Hepatic insufficiency | D048550 | 2 | — | — | — | — | 2 | ||
| Renal insufficiency | D051437 | HP_0000083 | N19 | 1 | — | — | — | — | 1 |
| Healthy volunteers/patients | — | 1 | — | — | — | — | 1 |
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | TELOTRISTAT ETHYL |
| INN | — |
| Description | Telotristat ethyl (USAN, brand name Xermelo) is a prodrug of telotristat, which is an inhibitor of tryptophan hydroxylase. It is formulated as telotristat etiprate — a hippurate salt of telotristat ethyl.
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| Classification | Small molecule |
| Drug class | enzyme inhibitors: tryptophan hydroxylase inhibitors |
| Image (chem structure or protein) | |
| Structure (InChI/SMILES or Protein Sequence) | CCOC(=O)[C@@H](N)Cc1ccc(-c2cc(O[C@H](c3ccc(Cl)cc3-n3ccc(C)n3)C(F)(F)F)nc(N)n2)cc1 |
Identifiers
| PDB | — |
| CAS-ID | 1033805-22-9 |
| RxCUI | 1872441 |
| ChEMBL ID | CHEMBL2105695 |
| ChEBI ID | — |
| PubChem CID | 25181577 |
| DrugBank | DB12095 |
| UNII ID | — |
Target
Agency Approved
No data
Alternate
TPH1
TPH1
Organism
Homo sapiens
Gene name
TPH1
Gene synonyms
TPH, TPRH, TRPH
NCBI Gene ID
Protein name
tryptophan 5-hydroxylase 1
Protein synonyms
indoleacetic acid-5-hydroxylase, L-tryptophan hydroxylase, Tryptophan 5-monooxygenase 1, tryptophan hydroxylase (tryptophan 5-monooxygenase)
Uniprot ID
Mouse ortholog
Tph1 (21990)
tryptophan 5-hydroxylase 1 (P17532)
Variants
Clinical Variant
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Financial
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Trends
PubMed Central
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Additional graphs summarizing 200 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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12,978 adverse events reported
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