Demand for early formulation work to tackle drug target ‘Wild West’

By Fiona Barry

- Last updated on GMT

The opening up of biological targets has created a formulation "Wild West", says Xceleron's CEO.
The opening up of biological targets has created a formulation "Wild West", says Xceleron's CEO.

Related tags: Molecular profiles

Sponsors are turning to outsourcing earlier for help with bioavailability formulation, say contract research organisations (CROs)

Efficacy is not just about the drug binding with the target, it’s about making sure it gets to the target in the first place,​” Michael Butler, CEO, Xceleron, told “We think that’s where the outsourcing’s going to be going much more than it is at the moment.​”

The mass spectrometry company was at the annual meeting of the American Association of Pharmaceutical Scientists (AAPS) in San Diego, announcing a collaboration with CDMO Molecular Profiles to provide a joint formulation service.

Xceleron analyses if the drug is getting into the body, and Molecular Profiles looks at how do you present it to the body in a way that will improve its chances of getting in,​” said MP’s Claire Madden-Smith.

Solvable solubles

Both firms agreed that newly discovered drugs are more challenging to deliver than previous generations as they are less soluble and permeable.

When you started looking for new drugs [decades ago] a lot of them were easily soluble. Nowadays over 70% of drugs coming through discovery are poorly water soluble – BCS Class II,​” said Madden-Smith.

Some new drugs, she said, are less soluble than marble – “we call them brick dust.​”

Poor solubility is in part related to the growing size of drug compounds – while still considered “small molecules”, not biopharmaceuticals, they are getting bigger: “That’s related to the higher throughput screens we’ve been using over the last 20 years.​”

‘Wild West’: outsourcing demand

The companies say drugmakers are increasingly outsourcing their formulation development to screen their compounds earlier in the development process.

We’re both hearing that pharmaceutics is becoming a much more critical quite early on – the study of formulation and how that affects the drug in the body,​” said Butler.

There are so many new biological targets with a lack of precedent – in other words with the old targets you kind of knew what was going to happen – what the off-target or toxicity effects might be – but with the new targets it’s the Wild West – how does chemistry interact with the target? That’s feeding into our business.​”

Molecular Profiles uses technologies to process the API to enhance its dissolution rate or present it in a solubilised form. “We look at techniques such as nanomilling, hot melt extrusion, spray drying, and microemulsions – covering it in something lipidic that’s more attractive to the body.

We also have cyclodextrins [a compound of sugar molecules which can solubilise hydrophobic drugs].​”

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