Wikipedia

RG7713

RG7713, or RG-7713, also known as RO5028442, is a small-molecule vasopression V1A receptor antagonist which is or was under development for the treatment of pervasive developmental disorders or autism.[2][3][4] It is administered by intravenous injection.[1][2]

RG7713
Clinical data
Other namesRG-7713; RO5028442; RO-5028442; Ro 5028442
Routes of
administration		Intravenous injection[1][2]
Drug classVasopression VA receptor antagonist
Identifiers
  • [6-chloro-1-[2-(dimethylamino)ethyl]indol-3-yl]-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylmethanone
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC25H28ClN3O2
Molar mass437.97 g·mol−1
3D model (JSmol)
  • CN(C)CCN1C=C(C2=C1C=C(C=C2)Cl)C(=O)N3CCC4(CC3)C5=CC=CC=C5CO4
  • InChI=1S/C25H28ClN3O2/c1-27(2)13-14-29-16-21(20-8-7-19(26)15-23(20)29)24(30)28-11-9-25(10-12-28)22-6-4-3-5-18(22)17-31-25/h3-8,15-16H,9-14,17H2,1-2H3
  • Key:QZXVLRCMAHJVIP-UHFFFAOYSA-N

The drug is centrally penetrant and is devoid of antagonism of the vasopressin V2 and oxytocin receptors.[5] Clinical studies found induction of subtle improvements but also subtle deficits in social communication surrogates with RG7713 in adult men with high-functioning autism.[5][4] A 2024 meta-analysis of vasopressin V1A receptor antagonists including RG7713 for autism found that they may not be effective in the treatment of the core symptoms of autism.[6]

As of December 2018, no recent development has been reported.[2] It reached phase 1 clinical trials.[2] Balovaptan (RG7314) has been described as a follow-up compound of RG7713 and reached later-stage clinical trials but was found to be ineffective.[3][6][7]

See also

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References

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  1. ^ a b László K, Vörös D, Correia P, Fazekas CL, Török B, Plangár I, et al. (September 2023). "Vasopressin as Possible Treatment Option in Autism Spectrum Disorder". Biomedicines. 11 (10): 2603. doi:10.3390/biomedicines11102603. PMC 10603886. PMID 37892977.
  2. ^ a b c d e "RG 7713". AdisInsight. 28 December 2018. Retrieved 27 October 2024.
  3. ^ a b Chadman KK, Fernandes S, DiLiberto E, Feingold R (August 2019). "Do animal models hold value in Autism spectrum disorder (ASD) drug discovery?". Expert Opinion on Drug Discovery. 14 (8): 727–734. doi:10.1080/17460441.2019.1621285. PMID 31132011.
  4. ^ a b Hong MP, Erickson CA (August 2019). "Investigational drugs in early-stage clinical trials for autism spectrum disorder". Expert Opinion on Investigational Drugs. 28 (8): 709–718. doi:10.1080/13543784.2019.1649656. PMID 31352835.
  5. ^ a b Lacivita E, Perrone R, Margari L, Leopoldo M (November 2017). "Targets for Drug Therapy for Autism Spectrum Disorder: Challenges and Future Directions". Journal of Medicinal Chemistry. 60 (22): 9114–9141. doi:10.1021/acs.jmedchem.7b00965. PMID 29039668.
  6. ^ a b Kimi S, Maiti R, Srinivasan A, Mishra BR, Hota D (February 2024). "Efficacy and safety of V1a receptor antagonists in autism spectrum disorder: A meta-analysis". International Journal of Developmental Neuroscience. 84 (1): 3–13. doi:10.1002/jdn.10297. PMID 37641183.
  7. ^ 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.
 

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