2Hit Identification

Purpose of Each Stage

Narrowing down promising compounds that act on identified drug discovery targets

Cycle Time

9 months (from system construction with general target to hit identification); additional 3 months (profiling, initial synthetic development, and evaluation)

Axcelead Solution

Axcelead enjoys a higher than 90% hit rate that ensures we are able to efficiently obtain high-quality hit compound information, backed by accumulated drug discovery data and more than 600 screenings

• Vast Pharma-origin library with high-quality and diverse structure, holding over 1.5 million compounds
• High-throughput screening (HTS) using an automated system
• Comprehensive end to end support from strategic planning to material preparation, system construction, HTS, profiling and crystal structural analysis
• Scope includes a wide range of target classes including enzymes, GPCR, nuclear receptors, transporters, channels, protein-protein interactions, nucleic acids + platforms suitable for phenotypic screening, mass spectrometry, high content assay, qRT-PCR, HTS utilizing SyncoPatch
• Virtual screening using In Silico Medicinal Chemistry technology
• One-stop shop: high-throughput ADME-Tox evaluation, SAR analysis performed by experienced chemists and generation of Advanced Hit compounds with several approaches to prioritize your hit chemotype.
• HTS (click here for further details)

Recently Added Service

High-throughput screening — compound binding assay using affinity selection mass spectrometry (ASMS)

3Lead Generation

Purpose of Each Stage

Generate a compound with an appropriate profile that qualifies as a lead compound

Cycle Time

9 months

Axcelead Solution

Axcelead offer integrated capabilities spanning the Lead Generation process. Our scientists, with their wealth of knowledge and experience, keep the project moving forward through high-level “design, synthesis, evaluation and analysis” cycle.
navigate_next All-in-One Solutions for Candidates Generation

• Axcelead’s experts in medicinal chemistry can resolve multiple issues that may arise during the lead generation process, using a high level drug discovery platform
• One-stop shop: broad range, multifaceted evaluations including discovery DMPK, physicochemical properties, pharmacological evaluation, exploratory toxicity, other
• Supports PK/PD analysis and PoM
• The Axcelead Hit Identified Target (A-HiT) Project promises to significantly save the time and cost associated with the initial state of drug discovery research
  navigate_next Case study: Otsuka Pharmaceutical and Axcelead Drug Discovery Partners undertake collaborative drug discovery research in the area of central nervous system diseases

4Lead Optimization

Purpose of Each Stage

Optimize compounds and select the promising candidates with good efficacy, DMPK, and safety for clinical development

Cycle Time

12 months

Axcelead Solution

Cross-functionality supported by specialized teams, the primary one being our chemists who have considerable drug discovery experience, all who work in tandem to keep the project moving forward by rapidly putting the compounds through the “design, synthesis, evaluation and analysis” cycle
navigate_next All-in-One Solutions for Candidates Generation

• Delivered over 50 preclinical / clinical candidates
• Experts in medicinal chemistry determine the balance between drug efficacy, physicochemical properties, DMPK, and safety, etc., and provide candidate compounds for development that have undergone precise structural conversion
• Full support for PK/PD/efficacy analysis and acquisition of PoM/POC
• The A-HiT Project can be initiated at the lead optimization stage (The assets owned by Axcelead present lead compounds and a primary assay system specific to drug discovery targets)

5Candidate Selection

Purpose of Each Stage

Based on the multiple compound evaluation results, coupled with the in-house development strategy, select candidate compounds suitable to move forward to the IND application stage

Cycle Time

6 months

Axcelead Solution

Given our experience in a pharmaceutical company, advancing many projects to the IND/NDA application stage, we are able to support the selection of candidate compounds for development using a multi-disciplinary approach to evaluation

• Achieve efficient evaluation of compounds through collaboration between our pharmacology, pharmacokinetics, safety, and synthesis departments
  ・Use disease animal models to evaluate drug efficacy and effective dosage
  ・Predict human PK, effective concetration and dose based on the PK/PD analysis in disease animal models
  ・Based on the results of the human prediction, develop a plan for preliminary toxicity study
• Our professionals in all fields, leveraging their considerable drug discovery experience, will hold a series of discuss with the client so as to both reach and fully support the optimum decision that is tailored for nature of the compound and the client's strategy

6Non-Clinical Development

Purpose of Each Stage

Secure necessary data for the IND application, prepare and submit application documents, follow up as required with the regulatory agency, etc.

Cycle Time

12 months

Axcelead Solution

Drawing on our considerable experience in processing many IND applications in Japan, Europe, and the United States, not to mention our experience previously garnered while either working directly in a pharmaceutical company or as a consultant, we are confident in our ability to provide total support and smooth handling of your IND application and/or out-license

• Our pharmacokinetics, safety, pharmacology, and chemistry departments coordinate their efforts to ensure compounds are evaluated across multi-disciplines. We propose optimal non-clinical development strategies for individual projects
  navigate_next By paying especial attention to the safety of the compound for development we ensure efficiency up to the time the IND application is processed
• Achieve efficient non-clinical development by consistently tackling development issues from suggestion of data packages for the IND application to the study management
• Our experience in successfully handling over 100 IND and 20 NDA applications to date gives us the confidence to address such concerns as toxicity and metabolites, and respond to the regulatory authorities
• In collaboration with Leiden Experts on Advanced Pharmacokinetics & Pharmacodynamics Consultants BV (LAP&P) support translational research including human PK/PD predictive modeling and simulation, biomarker search