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Danavorexton information


Danavorexton
Clinical data
Other namesTAK-925
Routes of
administration
Intravenous[1][2]
Drug classOrexin receptor agonist
Identifiers
IUPAC name
  • methyl (2R,3S)-3-(methanesulfonamido)-2-[(cis-4-phenylcyclohexyl)oxymethyl]piperidine-1-carboxylate
CAS Number
  • 2114324-48-8
PubChem CID
  • 130310079
ChemSpider
  • 68011464
UNII
  • 1QMD83K4YN
ChEMBL
  • ChEMBL4650341
PDB ligand
  • A6F (PDBe, RCSB PDB)
CompTox Dashboard (EPA)
  • DTXSID401336757 Edit this at Wikidata
Chemical and physical data
FormulaC21H32N2O5S
Molar mass424.56 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • COC(=O)N1CCC[C@H](NS(C)(=O)=O)[C@@H]1CO[C@H]1CC[C@H](CC1)C1=CC=CC=C1
InChI
  • InChI=1S/C21H32N2O5S/c1-27-21(24)23-14-6-9-19(22-29(2,25)26)20(23)15-28-18-12-10-17(11-13-18)16-7-4-3-5-8-16/h3-5,7-8,17-20,22H,6,9-15H2,1-2H3/t17-,18+,19-,20-/m0/s1
  • Key:UXZAJSZFFARTEI-YRPNKDGESA-N

Danavorexton (developmental code name TAK-925) is a selective orexin 2 receptor agonist.[1] It is a small-molecule compound and is administered intravenously.[1][2] The compound was found to dose-dependently produce wakefulness to a similar degree as modafinil in a phase 1 clinical trial.[1][3] As of March 2021, danavorexton is under development for the treatment of narcolepsy, idiopathic hypersomnia, and sleep apnea.[2][1][4] It is related to another orexin receptor agonist, firazorexton (TAK-994), the development of which was discontinued for safety reasons in October 2021.[1][5]

  1. ^ a b c d e f Jacobson LH, Hoyer D, de Lecea L (January 2022). "Hypocretins (orexins): The ultimate translational neuropeptides". J Intern Med. 291 (5): 533–556. doi:10.1111/joim.13406. PMID 35043499. S2CID 248119793.
  2. ^ a b c "Danavorexton - Takeda". Adis Insight. Springer Nature Switzerland AG. Retrieved 7 March 2021.
  3. ^ Evans, R., Hazel, J., Faessel, H., Wu, J., Hang, Y., Alexander, R., ... & Hartman, D. (2019). Results of a phase 1, 4-period crossover, placebo-controlled, randomized, single dose study to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of TAK-925, a novel orexin 2 receptor agonist, in sleep-deprived healthy adults, utilizing modafinil as an active comparator. Sleep Medicine, 64, S106. https://scholar.google.com/scholar?cluster=10933819770107034612
  4. ^ Evans R, Tanaka S, Tanaka S, Touno S, Shimizu K, Sakui S, et al. (December 2019). "A Phase 1 single ascending dose study of a novel orexin 2 receptor agonist, TAK-925, in healthy volunteers (HV) and subjects with narcolepsy type 1 (NT1) to assess safety, tolerability, pharmacokinetics, and pharmacodynamic outcomes". Sleep Medicine. 64: S105–S106. doi:10.1016/j.sleep.2019.11.290. S2CID 213696542.
  5. ^ Tong A (6 October 2021). "Takeda flashes red light on 'breakthrough' narcolepsy drug after PhII trials turned up mysterious safety signal". Endpoints News.

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Danavorexton

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Danavorexton (developmental code name TAK-925) is a selective orexin 2 receptor agonist. It is a small-molecule compound and is administered intravenously...

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orexin receptor agonists (two are currently under development by Takeda, danavorexton and TAK-994) CE-123 is under patent by Red Bull. Milgram, Norton W.;...

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Narcolepsy

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treatments methods such as future drugs like hypocretin agonists (such as danavorexton) or hypocretin replacement, in the form of hypocretin 1 given intravenous...

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Suvorexant

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In animals and humans, orexin receptor agonists such as orexin-A and danavorexton dose-dependently produce wakefulness and locomotor activity while orexin...

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Lemborexant

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Suvorexant TCS-1102 Vornorexant (ORN-0829, TS-142) YZJ-1139 OX2 Agonists: Danavorexton (TAK-925) Firazorexton Orexin (A, B) SB-668875 Suntinorexton TAK-861...

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List of investigational sleep drugs

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(IMB-115, IT-1315, S-117957, V-117957) – nociceptin receptor agonist [7][8] Danavorexton (TAK-925) – OX2 receptor-selective agonist via IV infusion[9] TAK-994 –...

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Orexin antagonist

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Suvorexant TCS-1102 Vornorexant (ORN-0829, TS-142) YZJ-1139 OX2 Agonists: Danavorexton (TAK-925) Firazorexton Orexin (A, B) SB-668875 Suntinorexton TAK-861...

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Firazorexton

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selectivity over the orexin receptor 1 (OX1). Firazorexton is related to danavorexton (TAK-925). The compound reached phase 2 clinical trials for narcolepsy...

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Orexin

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Suvorexant TCS-1102 Vornorexant (ORN-0829, TS-142) YZJ-1139 OX2 Agonists: Danavorexton (TAK-925) Firazorexton Orexin (A, B) SB-668875 Suntinorexton TAK-861...

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Daridorexant

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Suvorexant TCS-1102 Vornorexant (ORN-0829, TS-142) YZJ-1139 OX2 Agonists: Danavorexton (TAK-925) Firazorexton Orexin (A, B) SB-668875 Suntinorexton TAK-861...

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Suntinorexton

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Suvorexant TCS-1102 Vornorexant (ORN-0829, TS-142) YZJ-1139 OX2 Agonists: Danavorexton (TAK-925) Firazorexton Orexin (A, B) SB-668875 Suntinorexton TAK-861...

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Seltorexant

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Suvorexant TCS-1102 Vornorexant (ORN-0829, TS-142) YZJ-1139 OX2 Agonists: Danavorexton (TAK-925) Firazorexton Orexin (A, B) SB-668875 Suntinorexton TAK-861...

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Orexin receptor

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5- to 10-fold selectivity for the OX2 receptor over the OX1 receptor Danavorexton (TAK-925) – selective OX2 receptor agonist Firazorexton – selective OX2...

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Almorexant

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Suvorexant TCS-1102 Vornorexant (ORN-0829, TS-142) YZJ-1139 OX2 Agonists: Danavorexton (TAK-925) Firazorexton Orexin (A, B) SB-668875 Suntinorexton TAK-861...

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Filorexant

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Suvorexant TCS-1102 Vornorexant (ORN-0829, TS-142) YZJ-1139 OX2 Agonists: Danavorexton (TAK-925) Firazorexton Orexin (A, B) SB-668875 Suntinorexton TAK-861...

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Vornorexant

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Suvorexant TCS-1102 Vornorexant (ORN-0829, TS-142) YZJ-1139 OX2 Agonists: Danavorexton (TAK-925) Firazorexton Orexin (A, B) SB-668875 Suntinorexton TAK-861...

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