MEDICINAL CHEMISTRY
or medium throughput screening technologies are unlikely to detect. Fragment screening has become an accepted and often primary screening approach for identifying target hits. Selcia has branded its CE fragment screening offer as CEfrag™, and can provide it alongside a novel fragment library partly derived from natural compounds. “In 2011, we established a facility in Hopkinton, Massachusetts, which retains the founding scientists of the technology who are expert in performing all aspects of CE-based fragment screening including both the initial assay development and interpretation and understanding of the data output,” says Saxby.
Selcia’s analytical laboratory features two GLP high-field NMR instruments for molecular characterisation in discovery studies.
package of chemistry and biology data led to a number of long-term collaborations and fee- for-service contracts with customers with which Selcia continues to develop compounds as potential clinical candidates,” says Saxby. “The reduction and closure of UK- based R&D facilities by many of the large pharma companies has enabled Selcia to recruit experienced and talented scientists who have added considerable weight to the company’s scientific credentials and expertise. “We also have a sound business model that allows customers to base one or more of their chemists in our facility to work on their discovery programmes alongside Selcia chemists. We have developed this ‘embedded chemist’ option in a way that ensures the complete confidentiality of other client projects. One significant advantage of the approach is that it allows embedded chemists to make programme decisions in real time. The clear benefit here is that the customer remains fully and regularly updated on progress and can be assured that its programme is proceeding efficiently.”
Supplying custom radiolabelling globally
Currently, Selcia is the world’s second-largest supplier of 14C custom radiolabelled compounds. It has a global customer base including Japan, which Saxby says is a strategically important and growing market. Currently, Selcia has a team of about 25 full time radiochemists. “We can react quickly to customer demands by adding resources from the discovery team when the need arises,” he says.
In October 2010, Selcia was certified by the
UK MHRA as a GMP-compliant radiolabelling facility. The company is one of just a few that can provide GMP radiolabelled APIs to customers and/or directly to clinics for in-vivo studies in man.
Although Selcia Radiolabelling and Selcia Discovery groups run separately from a business development perspective, both operate within Selcia as a single company. The businesses are entirely complementary and can utilise chemists from either group. Saxby says this means the company is well positioned to provide both discovery and 14C radiolabelling services to the same customers.
New investments, new collaborations
Selcia has established medicinal drug discovery collaborations in Europe and North America, most of which are confidential. These collaborations are mainly with SMEs and mid-size pharma companies, with the majority of the larger collaborations being with North American companies. The company intends to grow both divisions over the course of the next three years, with an expected increase in turnover of about 50 per cent. For the Discovery Division, the company has made a number of investments to achieve this goal:
First, the company acquired the rights to a screening technology using capillary electrophoresis (CE) from Cetek in Boston, Massachusetts, USA and subsequently adapted this technology to fragment screening. This technology can detect low- affinity binding interactions, particularly low- affinity protein-protein interactions, that high
Second, Selcia has established a dedicated business development team, led by Simon Bury, who has 20 years’ global business experience in medicinal chemistry. He will oversee the continued growth of the company’s discovery business. “As a result, we expect our CEfrag service offering to win fee-for-service screening contracts that will lead to longer-term international discovery contracts and/or collaborations,” says Saxby.
Mitochondrial pathophysiology discovery collaboration
Last September, Selcia and Swedish company NeuroVive Pharmaceutical AB signed a research collaboration to develop new medicines and drug compounds targeting mitochondrial physiology and pathophysiology. The agreement is focused on mitochondrial medicine, an emerging therapeutic modality that promises innovative treatments for chronic diseases ie cancer and obesity, and acute conditions such as stroke and heart failure. The joint investment combines Selcia’s medicinal and analytical chemistry expertise with NeuroVive’s advanced research and development programmes in mitochondrial medicine. “We have already assembled a team of medicinal chemists to support this collaboration, many of whom previously worked for Big Pharma,” says Saxby. “Additionally, we have developed an expertise in a class of targets called peptide bond isomerases. Inhibition of a mitochondrial member of this protein class, cyclophilin D, has been shown to result in cytoprotection. So it seemed natural to pair the strengths of Selcia and NeuroVive in collaborative programmes.” Currently, the companies are running two joint programmes: the first addresses a type of hereditary mitochondrial dysfunction, while. the second aims at drugs that stabilise mitochondria in situations of ischemia and prevent nerve damage resulting from it. At the
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