Lead Optimisation


During the lead optimisation phase of a drug discovery project, our medicinal chemists endeavour to deliver compounds which meet the target candidate profile (TCP) agreed with the client. An efficient design, make, test, analyse cycle is vital at this stage in order facilitate the rapid advancement of a lead optimisation project towards pre-clinical development. Due to the co-location of our drug discovery departments we can minimise delays in generating key data and can usually produce all necessary in-vitro data within 7 days of compound registration; enabling rapid responses in target synthesis prioritization.

In vivo pharmacokinetic (PK) and ‘proof-of-concept’ data obtained from relevant in vivo disease models can provide invaluable information to guide this stage of a drug delivery project. An understanding of the aspects of these molecules which modulate the pharmacokinetic/pharmacodynamic (PK/PD) profile is established.

Sygnature can also scale-up drug candidates (up to 0.5Kg) for early non-GLP pre-clinical development, including route selection studies. Our scientists are frequently named as inventors on clients’ patents and they have been trusted to present client data at scientific conferences.


Close Cooperation

Close cooperation between Sygnature’s medicinal chemists, computational scientists, bioscientists and DMPK scientists; together with the client is essential to ensure delivery of a high quality development candidate (and back-up candidate, as appropriate) in the optimal timeframe, whilst building a strong intellectual property (IP) position.

One of our Core Strengths

Lead optimisation is one of Sygnature’s core strengths. This phase of a drug discovery project typically lasts for 12 to 18 months. Sygnature can also scale-up drug candidates (up to 0.5kg) for early non-GLP pre-clinical development, including route selection studies.



Recognised Expertise

The level of expertise of our scientists is such that they are frequently named as inventors on clients’ patents due to the considerable intellectual input they provide into drug discovery projects. They have also been trusted to present data generated for clients at scientific conferences.


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