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RG7314 is an investigational drug candidate developed by Hoffman-La Roche for the potential treatment of autism spectrum disorder (ASD). It is a nonpeptide vasopressin receptor antagonist (vaptan) with reported selectivity for the vasopressin V1a receptor. RG7314 is the first vaptan drug to be tested in psychiatry, and its therapeutic potential is yet unknown. The drug is currently undergoing a phase II clinical trial in adult males with ASD for the alleviation of core ASD symptoms. To date, data on the safety or efficacy of RG7314 have not been published.
Vasopressin, also known as antidiuretic hormone, is a small peptide produced in the hypothalamus. It is a major physiological regulator of water homeostasis, affecting urine concentration and blood volume. Vasopressin binds to three different receptors, V1a, V1b (also called V3), and V2. Activation of V1a receptors on vascular smooth muscle causes vasoconstriction, and activation of V2...
References and Readings
A Phase 1, Randomized, Double-blind, Placebo-controlled Crossover Study of RG7314 on the Potential Regulation of Higher Brain Functions in Healthy Male Participants: Proof of Mechanism. (2014). Retrieved from https://clinicaltrials.gov/show/NCT02205073 (Identification no. NCT02205073).
Ali, F., Guglin, M., Vaitkevicius, P., & Ghali, J. K. (2007). Therapeutic potential of vasopressin receptor antagonists. Drugs, 67(6), 847–858.
Baribeau, D. A., & Anagnostou, E. (2015). Oxytocin and vasopressin: Linking pituitary neuropeptides and their receptors to social neurocircuits. Frontiers in Neuroscience, 9, 335.
Bolognani, F., del Valle Rubido, M., Squassante, L., Wandel, C., Liogier D’ardhuy, X., Boak, L., … Umbricht, D. (2017, May). Results of a phase 2 randomized double-blind Placebo controlled study (VANILLA) investigating the efficacy and safety of a V1a antagonist (RG7314) in adult men with ASD. Paper presented at the international meeting for autism research, San Francisco.
Meyer-Lindenberg, A., Domes, G., Kirsch, P., & Heinrichs, M. (2011). Oxytocin and vasopressin in the human brain: Social neuropeptides for translational medicine. Nature Reviews Neuroscience, 12(9), 524–538.
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Williams, Z., McPartland, J.C. (2017). RG7314. In: Volkmar, F. (eds) Encyclopedia of Autism Spectrum Disorders. Springer, New York, NY. https://doi.org/10.1007/978-1-4614-6435-8_102135-1
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DOI: https://doi.org/10.1007/978-1-4614-6435-8_102135-1
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Balovaptan- Published:
- 21 March 2018
DOI: https://doi.org/10.1007/978-1-4614-6435-8_102135-2
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RG7314- Published:
- 29 July 2017
DOI: https://doi.org/10.1007/978-1-4614-6435-8_102135-1