Balovaptan

Balovaptan (INN; developmental code name RG7314), is a selective small molecule antagonist of the vasopressin V1A receptor which is under development by Roche for the treatment of autism.[1] As of August 2019, it is in a phase III clinical trial for adults and a phase II clinical trial for children for this indication.[2] On 29 January 2018, Roche announced that the US Food and Drug Administration (FDA) had granted Breakthrough Therapy Designation for balovaptan in individuals 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 currently-recruiting (Until March 2020) phase III adult study is called V1aduct and the currently-closed (August 2019) phase II child study is called Av1ation.

Balovaptan
Clinical data
Other namesRG7314
Legal status
Legal status
Identifiers
IUPAC name
  • 8-Chloro-5-methyl-1-(4-pyridin-2-yloxycyclohexyl)-4,6-dihydro-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC22H24ClN5O
Molar mass409.92 g·mol−1
3D model (JSmol)
SMILES
  • CN1CC2=NN=C([C@H]3CC[C@@H](CC3)OC3=CC=CC=N3)N2C2=C(C1)C=C(Cl)C=C2
InChI
  • 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

See also

References
  1. "Roche - Pipeline". 2014. Retrieved 1 August 2014.
  2. Clinical trial number NCT01793441 for "Study of RG7314 to Investigate Efficacy and Safety in Individuals With Autism Spectrum Disorders" at ClinicalTrials.gov
  3. "FDA grants Breakthrough Therapy Designation for Roche's balovaptan in autism spectrum disorder" (Press release). 29 January 2018. Retrieved 6 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.
  • "Balovaptan". Drug Information Portal. U.S. National Library of Medicine.


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