Peptide Drug Development

Peptide drug products are a rapidly growing area within the pharmaceutical industry for oncology, metabolic disease, rare and orphan indications, among other areas. However, the complexity and unique physicochemical properties of peptides present many challenges to drug developers.

We understand that each peptide is unique and that there is not just one, standard approach to formulation design. With over 35 years of experience working on a variety of peptide programs for a range of delivery routes, our scientists are skilled at developing strategies to reduce degradation and instability while maximizing absorption and bioavailability.

As polymers of amino acids, peptides are neither small molecules nor large molecules (biologics). Peptides are typically water soluble, hydrophilic, and charged, so they are poorly absorbed across the skin and mucosal membranes. 

Historically, peptides are mainly administered via injection, but recent advancements in enabling formulation technologies, alternative routes of drug delivery, such as oral dosage forms, are becoming more prevalent.

In this phase, we develop an experimental plan that is tailored to the stage of development, availability and purity of your drug substance, often using material-sparing approaches. This enables us to recommend a lead molecule and a drug delivery strategy to pursue for in-vivo animal studies.

• Analytical development using appropriate techniques
  • Liquid chromatography with mass spectrometry (LC-MS)
  • Reversed-phase high-performance liquid chromatography (HPLC)/ultra-performance liquid chromatography (UPLC) with ultraviolet (UV), size-exclusion, and charged aerosol detection
  • Light scattering methods
• Chemical stabilization (solid and solution state)
• Assessment of aggregation and binding
• Characterization in biorelevant conditions
• In-vitro permeability assessment
• Bioanalysis

Peptides often present unique stability and permeability challenges, so we provide a well-designed and adaptive plan for pre-clinical in-vivo screening and safety assessments that includes:

• Solution development for oral and IV dosing
• Animal model selection appropriate for the drug delivery strategy
• Permeability enhancement by use of excipients and targeted drug delivery
• Safety assessment and dose selection of permeation enhancers

The clinical performance of a peptide can deviate from the outcome predicted by pre-clinical data. For non-parenteral routes, such as oral and nasal delivery, a complex formulation approach may be required for the FIH trial.

Our scientists are experienced with:

• Formulation design for a wide range of FIH dosage forms
• Adaptive clinical trial design solutions that allow dose strength and/or functional excipient selection based on emerging pharmacokinetic (PK) data
• Use of controlled-release coatings and permeation-enhancing excipients for oral, nasal, and other non-parenteral formulations
• Imaging using gamma scintigraphy to evaluate dosage form performance in the gastrointestinal (GI) tract
• Sterile manufacturing of peptide products for IV, SC, and IM injection

Our unique Translational Pharmaceutics® platform accelerates peptide development by integrating formulation development, drug product manufacturing, and clinical testing, all under one organization and a single program manager. 

Flexible study protocols and rapid 'make-test' cycles enable formulation optimization in real-time based on arising clinical data, which reduces development risks, maximizes the probability of success, and saves time and costs.

Key applications:

• Accelerating molecules from FIH study to POC study
• Selecting and optimizing clinical formulations
• Optimizing formulations to minimize injection site reactions
• Managing route switches, e.g. parenteral to oral delivery