Drug Discovery and Kilo Lab Services

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Apertus offers medicinal and synthetic organic chemistry solutions on milligram to kilogram scale. Our chemistry team brings experience from previous employment in the fine chemical, pharma and biotech industries and can help you at any stage in your development process. Our style is highly collaborative, stressing close contact, open communication and full disclosure of progress – both accomplishments and roadblocks/issues, to enable rapid decision making and project success.

Apertus can help with early stage hit confirmation and expansion by:

  • Lead optimization through chemical modification of hit structures leading to a larger pool of active compounds
  • Supplying milligram to gram quantities of lead compounds for primary screening studies
  • Manufacturing gram scale quantities for primary screening confirmation, dose-response curves, orthogonal testing and secondary screenings
  • Evaluation of synthetic route feasibility and detailed cost estimation for each hit
  • Working with your legal team to evaluate freedom to operate and patentability

Apertus can continue to provide kilo-lab service beyond lead optimization by:

  • Providing route selection and optimization services
  • cGMP synthesis of targets for pre-clinical and clinical studies
  • Documenting process design work for regulatory filings
  • Performing validation batches and writing associated validation reports
  • Conducting stability and forced degradation studies
  • Co-developing stability-indicating analytical methods
  • Identifying and synthesizing process impurities and degradants
  • Manufacturing your NME for delivery to your selected forumlator
  • Providing tech transfer support if a larger manufacturing facility is required

Case Study

Project Objective: Provide synthesis services and med-chem consulting on a novel non-alkaloid analgesic.

Discussion: Starting with a plant-derived natural product, a hit optimization study was completed resulting in over a 10000 fold improvement in the receptor binding affinity of the target scaffold. Several iterations of pharmacophores, synthesis and testing led to a group of leads that are currently undergoing further in-vitro and in-vivo testing. Apertus aided in design and route selection then provided all synthesis services, and scale up for testing.

Outcome: A first round of hit optimization led to a substantial increase in target receptor affinity. Over 50 compounds were synthesized, isolated and tested.

Patent pending.