Capsule based machines for the automated synthesis of organic molecules for drug discovery and medicinal chemistry

Project Information

AutoCapSyn

Grant agreement ID: 874451

DOI

10.3030/874451

Project closed

EC signature date 4 September 2019

Start date 1 October 2019

End date 31 March 2020

Funded under

• INDUSTRIAL LEADERSHIP - Innovation In SMEs

Total cost

€ 71 429,00

EU contribution

€ 50 000,00

Coordinated by

SYNPLE CHEM AG
Switzerland

Periodic Reporting for period 1 - AutoCapSyn (Capsule based machines for the automated synthesis of organic molecules for drug discovery and medicinal chemistry)

Reporting period: 2019-10-01 to 2020-03-31

Summary of the context and overall objectives of the project

The discovery of new pharmaceuticals continues to rely on the synthesis of tiny amounts of thousands of candidate molecules using unpredictable protocols that require highly trained specialists. Despite years of research, it remains expensive, time-consuming, unsafe, and environmentally unfriendly. Declining productivity, high costs, and safety issues, have driven a large amount of chemical synthesis to lower cost countries but this introduces uncertainty and delays in the already lengthy drug discovery process, where the flexibility to rapidly prepare new molecules in response to biological data is critical to success. In order to meet the unmet medical needs and relieve societal burdens, all elements of the drug discovery and development are focussed on adopting new processes and technologies to increase productivity and shorten the time to patients.

The ETH SpinOff company Synple Chem AG (Synple) was founded in 2016 with the aim of changing the way chemical synthesis is done, and supporting chemical research and development organisations by greatly simplifying the way in which key chemical scaffolds are produced. Through the development of an innovative, fully automated, bench-top, capsule-based machine that efficiently synthesises unique organic molecules at the touch of a button, Synple offers significant timesaving, productivity enhancing, and safety benefits. Synple’s first instrument employs single-use capsules for a range of chemical reactions for the preparation of important chemical products, including saturated N-heterocycles currently the most desired motif for medicinal chemists in drug discovery, and PROTACs one of the hottest trends in drug discovery. To expand and sell more capsules, Synple plans to continue developing additional applications for highly desirable chemistries, based on feedback from drug discovery chemists.

The objective of this project was to assess the technical and commercial feasibility of the technology. An additional goal of this study was to gain a deeper insight into the market size and dynamics in order to establish the steps required for commercial launch, including design and manufacture of a commercial product, defining the supply chain and pricing structure, and identifying the most appropriate sales, marketing and distribution channels.

Work performed from the beginning of the project to the end of the period covered by the report and main results achieved so far

In order to determine the technical and commercial feasibility of the technology, feedback was collected from customers who used the technology during the pilot phase. By analysing this feedback and combining it with the learnings gained from providing technical support throughout the pilot phase, it was clear that customers did actually want and need this technology, and that with some relatively minor modifications, the technology would be both compatible with customer's existing work processes and robust enough for prolonged use in a customer environment.

By analysing customer feedback and feeding the outcome into a redesign processes, Synple have been able to develop the first commercial version of their machine (Synple 2), which has recently been launched. As part of the pre-commercialisation efforts, a fully market analysis was also carried out to determine who the primary customers for the technology are, and in which geographic locations the technology should be launched initially. In addition, an appropriate supply chain - including sourcing, manufacturing, sales, marketing and distribution - has been established and validated.

Progress beyond the state of the art and expected potential impact (including the socio-economic impact and the wider societal implications of the project so far)

As the sole provider of a cartridge-based automated synthesis technology that has generated a great deal of interest from potential customers, Synple is in a unique position to offer its productivity-enhancing and time saving technology to discovery research chemists, such as those working in the drug discovery field. Historically, the needs of such chemists have been poorly met with respect to automated synthesis technologies. The pharmaceutical industry is still facing ever increasing pressure to reduce spiralling costs and make new therapies available at a cost that payers can afford, in as short a timeframe as possible. As such, all stages of the drug discovery and development process are driven to explore and adopt new productivity-enhancing technologies. With synthetic chemistry still proving to be one of the bottle-necks in bringing new drugs to the market, the field is urgently seeking new automated synthesis solutions that really address their need for simple, easy to use solutions that enable them to rapidly prepare potential drug molecules in a safe and predictable way. Synple's technology offers such a solution and has the potential to achieve the long elusive productivity hike, without the associated increase in R&D spending.

Synple 2 and reaction applications