RG7713 explained

Width:250px
Routes Of Administration:Intravenous injection
Class:Vasopression VA receptor antagonist
Cas Number:920022-47-5
Pubchem:59657596
Drugbank:DB12721
Chemspiderid:52084863
Unii:LZ0EU1YHCK
Chembl:3416885
Synonyms:RG-7713; RO5028442; RO-5028442; Ro 5028442
Iupac Name:[6-chloro-1-[2-(dimethylamino)ethyl]indol-3-yl]-spiro[1''H''-2-benzofuran-3,4'-piperidine]-1'-ylmethanone
C:25
H:28
Cl:1
N:3
O:2
Smiles:CN(C)CCN1C=C(C2=C1C=C(C=C2)Cl)C(=O)N3CCC4(CC3)C5=CC=CC=C5CO4
Stdinchi: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
Stdinchikey:QZXVLRCMAHJVIP-UHFFFAOYSA-N

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.[1] [2] [3] It is administered by intravenous injection.[4]

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. 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. It reached phase 1 clinical trials. Balovaptan (RG7314) has been described as a follow-up compound of RG7713 and reached later-stage clinical trials but was found to be ineffective.[7]

See also

Notes and References

  1. Web site: RG 7713 . AdisInsight . 28 December 2018 . 27 October 2024.
  2. Chadman KK, Fernandes S, DiLiberto E, Feingold R . Do animal models hold value in Autism spectrum disorder (ASD) drug discovery? . Expert Opinion on Drug Discovery . 14 . 8 . 727–734 . August 2019 . 31132011 . 10.1080/17460441.2019.1621285 .
  3. Hong MP, Erickson CA . Investigational drugs in early-stage clinical trials for autism spectrum disorder . Expert Opinion on Investigational Drugs . 28 . 8 . 709–718 . August 2019 . 31352835 . 10.1080/13543784.2019.1649656 .
  4. László K, Vörös D, Correia P, Fazekas CL, Török B, Plangár I, Zelena D . Vasopressin as Possible Treatment Option in Autism Spectrum Disorder . Biomedicines . 11 . 10 . 2603 . September 2023 . 37892977 . 10603886 . 10.3390/biomedicines11102603 . free .
  5. Lacivita E, Perrone R, Margari L, Leopoldo M . Targets for Drug Therapy for Autism Spectrum Disorder: Challenges and Future Directions . Journal of Medicinal Chemistry . 60 . 22 . 9114–9141 . November 2017 . 29039668 . 10.1021/acs.jmedchem.7b00965 .
  6. Kimi S, Maiti R, Srinivasan A, Mishra BR, Hota D . Efficacy and safety of V1a receptor antagonists in autism spectrum disorder: A meta-analysis . International Journal of Developmental Neuroscience . 84 . 1 . 3–13 . February 2024 . 37641183 . 10.1002/jdn.10297 .
  7. Jacob S, Veenstra-VanderWeele J, Murphy D, McCracken J, Smith J, Sanders K, Meyenberg C, Wiese T, Deol-Bhullar G, Wandel C, Ashford E, Anagnostou E . 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 . March 2022 . 35151410 . 10.1016/S2215-0366(21)00429-6 .

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