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API Development for Phase I and II Clinical Supplies

Developing complex, chiral drug candidates for early‑stage clinical programs often presents significant synthetic and scalability challenges. A U.S.-based biotech partner, with whom Sai Life Sciences shares an eight‑year relationship, sought support in optimizing an intricate 11‑step medicinal chemistry route for a sensitive non‑natural peptide.

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Sai Life Sciences partnered with a long-standing U.S. biotech client to optimize a complex 11‑step synthesis for a sensitive, chiral non‑natural peptide. The aim was to improve yield, streamline manufacturing, and ensure reliable API supply for early clinical studies.

Overview & Objective

A long-standing U.S.-based biotech partner engaged Sai Life Sciences to optimize an 11‑step medicinal chemistry route for a highly sensitive, chiral molecule. The objectives were to improve the overall process yield, streamline manufacturing of a non-natural peptide, and ensure consistent API supply to support toxicology, Phase I, and Phase II clinical studies.

Approach

The molecule posed significant synthetic and purification challenges due to its three chiral centers, formation of eight possible stereoisomers, and the need for three chromatographic purifications.

Sai Life Sciences employed a systematic and science-driven approach to overcome these hurdles:

  • Eliminated column chromatography across all three stages of the process
  • Conducted extensive screening of coupling reagents to enhance reaction efficiency
  • Modified work-up procedures and implemented telescoping strategies with robust process controls
  • Successfully scaled up the optimized process to deliver the required API quantities for Tox and Phase I studies
  • Confirmed the absolute configuration of four diastereomeric process impurities using single-crystal X‑ray analysis

Outcome / Results / Evidence

The process enhancements delivered several significant improvements:

  • Yield Improvement: Overall yield increased from 15% to 22%
  • Operational Efficiency: Delivery timelines for kilogram-scale API batches were substantially shortened
  • Process Understanding: Stereochemical configuration of key impurities was fully characterized and controlled
  • Successful Clinical Supply: API manufactured and supplied on time for both Toxicology and Phase I studies

Key Takeaways / Impact

  • The molecule has successfully progressed to Phase II clinical studies
  • Raw material cost (RMC) has been reduced by 30% due to process improvements
  • The success of this program led the client to award two additional projects involving similar molecular motifs for Tox and Phase I supply

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