The affinity (Ki) of LIT-001 for the human oxytocin receptor, where it acts as an agonist, is 61 to 226nM, and its half maximal effective concentration (EC50) is 25nM.[1][3] At the human vasopressin V1A receptor, where LIT-001 is an antagonist, its affinity (Ki) and half maximal inhibitory concentration (IC50) are 1,253nM and 5,900nM, respectively.[1][3] Finally, at the human vasopressin V2 receptor, where the drug functions as an agonist, its affinity (Ki) and EC50 are 1,666nM and 41nM, respectively.[3] Based on the preceding EC50 and IC50 values, LIT-001 shows 236-fold selectivity for activating the oxytocin receptor over antagonizing the V1A receptor, whereas it has no appreciable selectivity for activating the oxytocin receptor over activating the V2 receptor (only 1.64-fold greater preference).[3]
Hibert has disclosed that other more potent and selective small-molecule oxytocin receptor agonists have also since been discovered by his research group.[5] Formal development of these compounds is now being pursued.[5] In 2024, a new highly potent oxytocin receptor agonist called LIT-002 was described and is being developed by a new pharmaceutical company called Occentis Pharmaceuticals.[12][10][11] Potential therapeutic applications include treatment of autism, alcoholism and opioid addiction, and neuropathic pain.[12]
123456789Hibert M (2022). "Approches moléculaires et thérapeutiques des interactions entre l'ocytocine et son récepteur" [Oxytocin and its receptor: molecular and therapeutic approaches]. Biologie Aujourd'hui (in French). 216 (3–4): 125–130. doi:10.1051/jbio/2022013. PMID36744978.
12345678910111213Boutaud AS (9 January 2022). "Oxytocin, from love potion to medicine". CNRS News. Retrieved 15 October 2025. After twenty years of research, we finally managed to overcome this obstacle and identified a synthetic molecule, called LIT-001, which acts in the same way as oxytocin. This was the first one that could restore social interaction in an animal model of autism5 following peripheral administration. Other, more potent and specific molecules have since been discovered and will soon be patented; at best, their preclinical and clinical development potential will require eight to ten years of industrial investment.
12Hibert M, Zhao Q, Noel-Duchesneau L, Peron F, Brugoux A, Bolot F, etal. (2026). LIT-002, a highly potent and selective nonpeptide oxytocin receptor agonist that improves social interaction in mouse models of autism. doi:10.2139/ssrn.6624262.
12Hibert M (15 December 2025). "De l'amour au traitement de l'autisme: une histoire d'ocytocine"[From love to the treatment of autism: a story of oxytocin]. CNRS Le journal (in French). Ce n'est que très récemment que nous avons identifié un composé répondant aux critères attendus. Ce produit, le LIT-002, est plus puissant que l'ocytocine elle-même, in vitro et in vivo. À des concentrations extrêmement faibles, il améliore l'interaction sociale dans deux modèles animaux d'autisme. La molécule et ses analogues ont été brevetés56, et les brevets ont été licenciés par le CNRS et l'Université de Strasbourg pour créer une start-up, Occentis7. Société spécialisée dans le développement de médicaments pour le traitement des maladies neuropsychiatriques et neurocomportementales, elle vise à répondre aux besoins dans des domaines thérapeutiques tels que l'autisme, la dépendance à l'alcool et aux opioïdes, la douleur neuropathique… C'est elle qui prendra en charge les étapes suivantes du développement préclinique et clinique8, ce qui nécessitera comme toujours de 6 à 10 ans avant de pouvoir proposer un médicament aux patients qui le souhaitent.
