It’s been really noticeable in recent years that clients’ early-stage small molecules are getting increasingly complex. So many of the ‘easy win’ therapeutic targets have already been met that many of those being studied now are much more difficult to drug, and companies are having to make ever more complex molecules to hit those targets.

That complexity comes in multiple forms – the molecules might be difficult to make, they might be difficult to formulate, or they might even be both of these things. On the ‘make’ side, the molecule itself might include structural features that are challenging to synthesize, or the synthetic route might require many steps. 

When it comes to formulation, it’s now well recognized that most of the small molecules entering the development pipeline have poor solubility. This has a significant impact on their bioavailability, and formulation tricks are likely to be required to create a successful dosage form. 

Here at Lonza, we are well aware of the challenges, and have been investing in technologies and expertise that will allow us to address them. A good example on the ‘make’ side is our new Route Scouting offering. This combines our own in-house database of raw materials, reagents and reactions with AI tools that suggest potential synthetic routes we can test out in an automated system, regardless of how complicated the molecule itself might be. It supports our skilled process chemists by speeding up the whole route evaluation process significantly. 

When it comes to formulation, our expertise in solid form services is invaluable. No one answer will solve all formulation problems, and the skill lies in finding the right answer. It might involve finding the optimal crystal form or, perhaps, a co-crystal. Equally, an amorphous form might prove more successful, perhaps created via spray drying, or maybe hot melt extrusion would work better. Whatever proves the best option, the talented Lonza team has the skills to identify it, and then create a successful formulation for dosing to patients. 

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