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Balovaptan

From Wikipedia, the free encyclopedia
Chemical compound

Pharmaceutical compound
Balovaptan
Clinical data
Other namesRG7314
ATC code
  • None
Identifiers
  • 8-Chloro-5-methyl-1-(4-pyridin-2-yloxycyclohexyl)-4,6-dihydro-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
CAS Number
PubChemCID
DrugBank
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC22H24ClN5O
Molar mass409.92 g·mol−1
3D model (JSmol)
  • CN1CC2=NN=C([C@H]3CC[C@@H](CC3)OC3=CC=CC=N3)N2C2=C(C1)C=C(Cl)C=C2
  • InChI=1S/C22H24ClN5O/c1-27-13-16-12-17(23)7-10-19(16)28-20(14-27)25-26-22(28)15-5-8-18(9-6-15)29-21-4-2-3-11-24-21/h2-4,7,10-12,15,18H,5-6,8-9,13-14H2,1H3/t15-,18-
  • Key:GMPZPHGHNDMRKL-RZDIXWSQSA-N

Balovaptan (INNTooltip International Nonproprietary Name; developmental code nameRG7314), is aselectivesmall moleculeantagonist of thevasopressin V1A receptor which is under development byRoche for the treatment ofpost-traumatic stress disorder (PTSD).[1]

Research

[edit]

Post-traumatic stress disorder

[edit]

It was in aphase III clinical trial for adults and a phase II clinical trial for children for post-traumatic stress disorder.[2]

Autism

[edit]

In January 2018, Roche announced that the USFood and Drug Administration (FDA) had grantedbreakthrough therapy designation for balovaptan in people with autism spectrum disorder (ASD).[3] The FDA granted this based on the results of the adult phase II clinical trial called VANILLA (Vasopressin ANtagonist to Improve sociaL communication in Autism) study.[4]

The phase III study concluded that balovaptan did not improve social communication in autistic adults.[5]

Stroke

[edit]

It was also in phase II studies for the treatment ofstroke. However, it has since been discontinued for both of those indications.[6]

References

[edit]
  1. ^"Roche - Pipeline". 2023. Retrieved5 April 2023.
  2. ^Clinical trial numberNCT01793441 for "Study of RG7314 to Investigate Efficacy and Safety in Individuals With Autism Spectrum Disorders" atClinicalTrials.gov
  3. ^"FDA grants Breakthrough Therapy Designation for Roche's balovaptan in autism spectrum disorder" (Press release). 29 January 2018. Retrieved6 February 2018.
  4. ^Bolognani F, Del Valle Rubido M, Squassante L, Wandel C, Derks M, Murtagh L, et al. (May 2019)."A phase 2 clinical trial of a vasopressin V1a receptor antagonist shows improved adaptive behaviors in men with autism spectrum disorder".Science Translational Medicine.11 (491).doi:10.1126/scitranslmed.aat7838.PMID 31043521.
  5. ^Jacob S, Veenstra-VanderWeele J, Murphy D, McCracken J, Smith J, Sanders K, et al. (March 2022). "Efficacy and safety of balovaptan for socialisation and communication difficulties in autistic adults in North America and Europe: a phase 3, randomised, placebo-controlled trial".The Lancet. Psychiatry.9 (3):199–210.doi:10.1016/s2215-0366(21)00429-6.PMID 35151410.
  6. ^"Balovaptan".Adis Insight. Springer Nature Switzerland AG. Retrieved5 April 2023.
Oxytocin
Vasopressin
V1A
V1B
V2
Unsorted
Others
1,4-Benzodiazepines
1,5-Benzodiazepines
2,3-Benzodiazepines*
Triazolobenzodiazepines
Imidazobenzodiazepines
Oxazolobenzodiazepines
Thienodiazepines
Thienotriazolodiazepines
Thienobenzodiazepines*
Pyridodiazepines
Pyridotriazolodiazepines
Pyrazolodiazepines
Pyrrolodiazepines
Tetrahydroisoquinobenzodiazepines
Pyrrolobenzodiazepines*
Benzodiazepine prodrugs
* atypical activity profile (notGABAA receptor ligands)
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