Krakow, Poland – 20 August 2019 – Selvita and Sandoz researchers have recently jointly published an article: Mini-Review: The Chemistry of Vorapaxar – Is There Any Room for Improvement Left?, which appeared in the Heterocycles, an International Journal for Reviews and Communications in Heterocyclic Chemistry, published online by The Japan Institute of Heterocyclic Chemistry.
The publication, based on the case of Vorapaxar, describes the key role of an early chemistry effort to enable rapid discovery of an optimal synthetic route to a commercially important product. The intramolecular Diels-Alder (IMDA) reaction developed by scientists from Schering to make natural product Himbacine in mid-‘90s allowed formation of the Vorapaxar’s backbone almost 10 years later. Since then this strategy has been followed by all companies. Additional improvements by Schering to the synthesis of Vorapaxar greatly limited the opportunities for generic manufacturers to secure new intellectual property. Most of the chemistry presented in this review comes from the patent applications and as such has not been subjected to rigorous peer review, but in our opinion this paper may serve as helpful information for readers in the area of drug discovery.
The authors of the publication are Piotr Graczyk from Selvita S.A. and Sven Nerdinger from Sandoz GmbH.
Selvita is a drug discovery and development partner for the pharmaceutical and biotechnology industries. It provides integrated drug discovery support starting from hit identification, hit to lead, lead optimization phase up to nomination of a preclinical candidate. The broad range of services includes medicinal and computational chemistry, custom synthesis and scale-up, in vitro pharmacology, structural biology, protein chemistry, ADME/DMPK as well as a comprehensive offer of analytical testing for APIs and drug products. In addition, Selvita has extensive expertise in comparability studies of biosimilar drugs. Its laboratories are both GLP- and GMP-certified.
Selvita is headquartered in Krakow, Poland, with offices in the U.S (Greater Boston, San Francisco Bay), and in the U.K. (Cambridge). The company is listed on the Warsaw Stock Exchange (WSE:SLV).