Chemistry:RG7713

From HandWiki

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][1]

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][3] 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.[1] It reached phase 1 clinical trials.[1] Balovaptan (RG7314) has been described as a follow-up compound of RG7713 and reached later-stage clinical trials but was found to be ineffective.[2][6][7]

See also

References

  1. 1.0 1.1 1.2 1.3 "RG 7713". 28 December 2018. https://adisinsight.springer.com/drugs/800043668. 
  2. 2.0 2.1 "Do animal models hold value in Autism spectrum disorder (ASD) drug discovery?". Expert Opinion on Drug Discovery 14 (8): 727–734. August 2019. doi:10.1080/17460441.2019.1621285. PMID 31132011. 
  3. 3.0 3.1 "Investigational drugs in early-stage clinical trials for autism spectrum disorder". Expert Opinion on Investigational Drugs 28 (8): 709–718. August 2019. doi:10.1080/13543784.2019.1649656. PMID 31352835. 
  4. "Vasopressin as Possible Treatment Option in Autism Spectrum Disorder". Biomedicines 11 (10): 2603. September 2023. doi:10.3390/biomedicines11102603. PMID 37892977. 
  5. 5.0 5.1 "Targets for Drug Therapy for Autism Spectrum Disorder: Challenges and Future Directions". Journal of Medicinal Chemistry 60 (22): 9114–9141. November 2017. doi:10.1021/acs.jmedchem.7b00965. PMID 29039668. 
  6. 6.0 6.1 "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. doi:10.1002/jdn.10297. PMID 37641183. 
  7. "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. doi:10.1016/S2215-0366(21)00429-6. PMID 35151410.