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New Lead Optimisation paper in collaboration with Esteve Pharmaceuticals

October 26th, 2020

The Journal of Medicinal Chemistry has recently reported the results obtained in our Lead Optimisation collaboration with Esteve Pharmaceuticals, aimed at the identification of novel dual ligands of the sigma-1 receptor (σ1R) and the μ-opioid receptor (MOR), as part of Esteve’s R&D activities to develop new, potent and safer analgesics.
The chemistry work was developed by Enantia’s Medicinal Chemistry team, led by Dr. Marina Virgili, in collaboration with Esteve Pharmaceuticals. Previous investigations carried out at Enantia established a suitable Lead, comprised of a spirocyclic morpholino-piperidine core identified using rational drug design strategies. Subsequent Lead Optimization has led to the discovery of EST73502, a clinical candidate undergoing Phase I clinical trials. The compound showed promising results in animal models with potent analgesic efficacy and improved safety compared to oxycodone.

Enantia offers a wide portfolio of drug discovery services for pharmaceutical and biotech companies, including the design and synthesis of new scaffolds and libraries of small molecules with potential biological activity, covering Hit finding, Hit-to-Lead and Lead Optimization programs. Additionally, Enantia can collaborate with Structure-Activity Relationship (SAR) and Drug Metabolism and Pharmacokinetics (DMPK) data analysis. Enantia has a long track record of collaborative research projects with the pharmaceutical industry, leading to more than 20 patent applications related to medicinal chemistry.
Besides the most common MedChem activities, Enantia can also contribute to the early stages of the drug development by preparing cold labelled compounds and metabolites of the candidates. Additionally, for later phases of development, our Solid State department counts with extensive expertise in identifying the best solid form of the candidate to be further developed.

You can read the full paper here.