From Wikipedia, the free encyclopedia
Danavorexton
Clinical data
Other namesTAK-925
Routes of
administration
Intravenous [1] [2]
Drug class Orexin receptor agonist
Identifiers
  • methyl (2R,3S)-3-(methanesulfonamido)-2-[(cis-4-phenylcyclohexyl)oxymethyl]piperidine-1-carboxylate
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
PDB ligand
CompTox Dashboard ( EPA)
Chemical and physical data
FormulaC21H32N2O5S
Molar mass424.56 g·mol−1
3D model ( JSmol)
  • COC(=O)N1CCC[C@H](NS(C)(=O)=O)[C@@H]1CO[C@H]1CC[C@H](CC1)C1=CC=CC=C1
  • 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]

See also

References

  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.

External links



From Wikipedia, the free encyclopedia
Danavorexton
Clinical data
Other namesTAK-925
Routes of
administration
Intravenous [1] [2]
Drug class Orexin receptor agonist
Identifiers
  • methyl (2R,3S)-3-(methanesulfonamido)-2-[(cis-4-phenylcyclohexyl)oxymethyl]piperidine-1-carboxylate
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
PDB ligand
CompTox Dashboard ( EPA)
Chemical and physical data
FormulaC21H32N2O5S
Molar mass424.56 g·mol−1
3D model ( JSmol)
  • COC(=O)N1CCC[C@H](NS(C)(=O)=O)[C@@H]1CO[C@H]1CC[C@H](CC1)C1=CC=CC=C1
  • 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]

See also

References

  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.

External links




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