Drug Discovery Case Study

Affinity initiated a collaboration with an emerging biotechnology company in the first quarter of 2019.

Hit Identification:

In Q4 2019, We initiated the project in a Fee-for-Service (FFS) format, and quickly accomplished the following:

• We synthesized tool compounds and reference compounds, each involving 10-25 steps, to assist the customer in setting up biological assays.
• Completed the synthesis of a small, focused library generated by molecular modeling, consisting of approximately 20-30 compounds with 15-25 steps per compound.
• Achieved the successful identification of initial hit compounds by the customer within a three-month timeframe.

Hit-to-Lead Exploration:

Q1 2020 -Q2 2020: Buoyed by the early success, the project transitioned rapidly to a Full-Time Equivalent (FTE) format.

It commenced with two FTEs for the initial two months, swiftly scaling up to six FTEs. Approximately 180 compounds were synthesized during this period, culminating in the discovery of the initial lead compound.

Lead Optimization:

Q3 2019 – Q1 2020: Throughout the subsequent three quarters, the project remained in the FTE format.

• Utilized 8 full-time equivalents (FTEs)
• Synthesized approximately 600-700 compounds at milligram scale
• Scaled up approximately 10-15 compounds to gram scale for PK/PD studies
• Identified lead compound for IND-enabling process

Process Development Services:

From Q1, 2020 to Q4, 2020, the project transitioned to process work under a Fee-for-Service arrangement. Key activities included:

• Developed a scalable process starting from readily available raw materials, involving a total of 35 steps.
• Utilized this process to produce 30 kg of cGMP starting materials.
• Preparation of GLP tox batches.
• Conducting salt screening and polymorph studies.

In Q1 2021, our customer's IND filing was accepted by the FDA.