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Early Phase Drug Product Development
From a solid with unknown properties to an IND-ready formulation, usually in 8 to 12 weeks.
The developability problem
A compound that is active in the assay may not dissolve, may not be stable in solution, or may need a dose that will not fit in a capsule a patient can swallow.
Each of those is a formulation problem, and the technology chosen to solve it is difficult to change once the IND-enabling work has started.
The IND-enabling preformulation package
An integrated developability assessment that ends with an IND-ready formulation, typically in 8 to 12 weeks.
- Bioavailability technologies screened in parallel, so the selection is made by direct comparison
- An animal PK study included, which gives a measured exposure figure
- In vitro, in vivo and in silico work in one place, with one point of contact
- High-potency compounds, PROTACs, peptides and oligonucleotides run through the same assessment
Solid-state development
The solid form taken forward is difficult to change later, and it determines the product’s stability profile and part of its patent position.
We run salt, co-crystal and polymorph screening for toxicology and clinical development, and the full polymorph study an NDA filing needs. That includes crystal structure analysis, solid form quantitative methods, and simulation and modeling where experiment alone is inconclusive.
Powder characterization covers flowability, particle size, morphology, surface area and density. Material science adds SEM-EDS, micro-CT, Raman, wettability and texture analysis — the techniques that explain why a powder will not compress.
Formulation development
Profiling first: pKa, LogP, thermal transitions, solubility, supersaturation, forced degradation, solution and solid stability, photostability, excipient compatibility. Then preclinical formulation screening and selection, and the formulations used for PK and toxicology studies.
Where bioavailability needs enhancing, the options are spray-dried dispersion, hot melt extrusion, lipid-based emulsion, nano suspension and micronization by jet milling.
In silico work runs alongside: developability prediction, DCS and BCS classification, food-effect and acid-reducing-agent interaction prediction, and GastroPlus modeling, used to decide which experiments are worth running.
Parenteral formulation development
For injectables, the questions are different: solution or lyophilized powder, suspension or emulsion, and whether an advanced formulation (liposome, lipid nanoparticle, nanoparticle) is needed at all. All of these formats are developed at WuXi STA and manufactured on the same site network.
IND and IMPD-enabling manufacturing
The first GMP drug product batches, with the analytical and stability package that goes into the filing. The package supports both an IND for the United States and an IMPD for Europe.