DRUG DISCOVERY
companies and university groups. This means that ChemOvation has developed a broad range of chemistry experience working on nucleosides, natural and non-natural peptides and amino acids, DNA chelators, and porphyrins, for example. The company also has significant experience and expertise in fused heterocyclic chemistries, particularly for kinase and ion channel inhibition/binding. Synthetic chemistry expertise includes palladium cross-coupling chemistry (Suzuki, Heck, Negishi); organometallic chemistry (Li, Mg, Zn reactions); peptide coupling chemistry; heterocyclic chemistry; hydrogenation; and protecting groups chemistry. Some of this chemistry lends itself to particular therapeutic areas but ChemOvation has worked across many different areas from cancer and neurology to infectious diseases and respiratory diseases.
Taking on even the most difficult chemistry
“ChemOvation has good, all-round ability and a willingness to take on even the most difficult chemistry,” says Matthews. “We work hard on our communications with our customers and have built excellent relationships, as our testimonials will attest. Our operations director keeps our customers aware of what is happening with their projects on a regular basis, acting as the customers’ representative in the lab. ChemOvation is agile enough to be responsive to customers’ changing research requirements and we are building a reputation for fast turnaround times, starting with the quoting process and ending with delivery of materials. For large pieces of work, the entire team is aware of the whole project and where their work fits in. This gives flexibility for other chemists to take over, starting or completing
Successes at ChemOvation
Successful projects carried out by ChemOvation include: - A 2-FTE lead-hopping project (cognition to cancer) produced two patentable lead series and xenograph ‘proof of principle’ in three months - A 4-FTE chemistry project prepared over 100 pro-drugs for a biotechnology company within two years, supporting a $232 million licence agreement
- Production of a formulation for successful ‘proof of principle’ treatment of hepatic encephalopathy
- An unstable, poor hit was taken from an initial screen and a stable, low nanomolar compound with acceptable pharmacokinetics was synthesised within 6 months
ChemOvation medicinal chemistry has contributed to: - Two clinical candidates in oncology - One clinical candidate in immunosuppression - A preclinical lead series in neurology - A preclinical lead compound in inflammation - Eight patents since 2006 - Two papers published with Roche (USA)
ChemOvation’s LCMS, the basic workhorse of the lab. It is used routinely for high-throughput QC and reaction monitoring.
a reaction when necessary, which we feel is an outcome of our close teamwork. We are also competitively priced.
“The chemistry projects we generally undertake are customer-driven and the projects are either organic chemistry orientated, requiring just synthesis of the desired compound by the most efficient route, or medicinal chemistry focused – a much more collaborative approach. Here we work under a confidentiality agreement and there is disclosure of primary/secondary screening, which enables ChemOvation to have input into what molecules are made. We have also carried out some chemical and process development prior to compounds being
outsourced for cGMP synthesis, either stand- alone or as a continuation of a medicinal chemistry project.”
New drug discovery agreement ChemOvation recently entered into a drug discovery project agreement with MISSION Therapeutics, a speciality pharmaceutical company aimed at translating cutting-edge cell biology research on DNA repair into drugs. This partnership originated from previous work with the individuals now at MISSION, which, Matthews says, demonstrates ChemOvation’s impressive record of repeat business from its customers and reflects its good track record: “Access to our screening collection was also a key determinant and the hits that were garnered from the collection forms the basis of our current work. We hope this will follow the pattern of previous medicinal chemistry projects and develop into a long-term relationship where ChemOvation provides a significant portion of MISSION’s chemistry resource. This is typical of the types of relationship we want to establish in the future and is similar to others we referred to earlier. “Our aim is to establish longer-term working relationships with any company whether they are Big Pharma or small biotechs, as this obviously gives our business a stability it would not otherwise have,” he continues. “We do have a growing relationship with a large pharmaceutical company, so far only repeat business for individual pieces of work, but we are hopeful it can develop into something more consistent and sustainable.
July/August 2012 sp2 Inter-Active 29
Page 1 |
Page 2 |
Page 3 |
Page 4 |
Page 5 |
Page 6 |
Page 7 |
Page 8 |
Page 9 |
Page 10 |
Page 11 |
Page 12 |
Page 13 |
Page 14 |
Page 15 |
Page 16 |
Page 17 |
Page 18 |
Page 19 |
Page 20 |
Page 21 |
Page 22 |
Page 23 |
Page 24 |
Page 25 |
Page 26 |
Page 27 |
Page 28 |
Page 29 |
Page 30 |
Page 31 |
Page 32 |
Page 33 |
Page 34 |
Page 35 |
Page 36 |
Page 37 |
Page 38 |
Page 39 |
Page 40 |
Page 41 |
Page 42 |
Page 43 |
Page 44