The High Potent Pathway

The demand for sterile dosage forms is rising, but oral solid dosage forms remain a significant growth driver in the pharmaceutical industry.

In 2023, the OSD market was approximately $36.5bn and is poised to register a compound annual growth rate (CAGR) of around 6% by the year 2030. Within this space, the main drivers for growth include oncology, diabetes, and obesity drugs, the latter experiencing a boom due to the recent use of GLP-1 therapies in weight loss management.

This article explores the role of a CDMO in the delivery of these life changing therapies to patients around the globe. It outlines the main touchpoints, including the earliest stages of technical transfer and new product introduction, through formulation development and scalable manufacture, and finally ensuring that these potent products are packaged in a safe environment before global distribution to clinic or market.

New Product Introduction (NPI) and Technical Transfer (TT)

As drug products containing highly potent APIs (HPAPIs) become more prevalent, a robust approach to TT and NPI is essential. Around 41% of new drug compounds are considered highly potent, which is unsurprising considering that oncology and GLP-1 therapies are among the industry’s major growth drivers, and those molecules tend to be highly potent. In a multi-product OSD facility, the NPI/TT processes for HPAPIs involve complex risk management and safety controls to ensure operator protection, drug product integrity, and, ultimately, patient safety.

Handling HPAPIs demands specialized facilities and expertise, with CDMOs required to navigate complex risk management scenarios, including accurate risk categorization, containment, and preventing cross-contamination. The lack of standardized guidelines for NPI and TT further complicates these tasks, making meticulous planning and robust process controls essential. Effective TT involves detailed risk assessments, incorporating exposure modeling, and designing material segregation and cross-contamination prevention controls, whilst implementing validated cleaning procedures and engineering controls is vital to mitigate risks, reducing reliance on personal protective equipment (PPE) alone.
Regulatory landscapes for HPAPIs are continuously evolving, with significant discrepancies in occupational exposure limits and the impact of chemical bans on supply chains. Additionally, artificial intelligence (AI) offers potential enhancements in risk assessment and toxicology, although its integration remains uncertain.

Maintaining rigorous scientific standards and leveraging AI advancements can improve process safety and efficiency in HPAPI manufacturing. Successful NPI and TT require advanced safety protocols, comprehensive risk management, and effective collaboration between sponsors and CDMOs to ensure the production of safe and effective pharmaceutical products.

Analytical Method Development (AMD)

AMD is critical for analyzing drug substances (DS) and drug products (DP), ensuring methods are fit for purpose, provide necessary data for product development, and enable validation according to ICH guidelines. Understanding the development objective and collecting relevant data—such as degradation products, solubility, pKa, and molecular stability—are fundamental, and leveraging existing pharmacopoeial methods where possible can expedite the development timeline.
When navigating the drug development lifecycle, getting drugs to patients as quickly as possible is a high priority. This is why CDMOs that are able to conduct AMD alongside formulation development activities are such a valuable asset in the pharmaceutical supply chain. To act quickly on AMD for highly potent drug products, a CDMO should not only have vast experience in handling HPAPIs, it should also boast an in-house laboratory with essential equipment, including HPLC/UPLC systems, dissolution apparatus, spectrophotometers, and Karl Fischer titration equipment. Equally important is a highly trained analytical team capable of troubleshooting and resolving development issues.
Regulatory authorities, such as the FDA, MHRA, and EMA, mandate that AMD processes adhere to ICH guidelines, ensuring methods are specific, accurate, reproducible, and robust. For high-potent active pharmaceutical ingredients (HPAPIs), this involves meticulous method validation to detect and quantify trace levels of potent compounds, prevent cross-contamination, and ensure product safety and efficacy. Methods must be stability-indicating to monitor degradation products and confirm product shelf-life. Detailed standard operating procedures (SOPs) are required for method validation, incorporating protocols for out-of-expectation (OOE) and out-of-specification (OOS) results investigation. The CDMO must also ensure comprehensive documentation, including validation reports and raw data, to support regulatory submissions. The use of advanced equipment such as HPLC/UPLC systems, dissolution apparatus, and spectrophotometers, coupled with a highly trained analytical team, is essential to meet stringent regulatory standards. The CDMO’s experience with specific dosage forms and their ability to handle HPAPIs safely is crucial, as it ensures that analytical methods are developed and validated efficiently, supporting the timely approval and commercialization of high-potent drug products.

Formulation Development

Successful high potent formulation development requires the collaboration of highly skilled teams across various disciplines, including analytical, manufacturing, quality assurance and control, and formulation development. These multidisciplinary teams must possess a deep understanding of their equipment and processes, along with a keen awareness of alternative development and manufacturing methods. Such expertise allows them to assess how different formulation attributes can affect the final drug product, both positively and negatively, and provide informed guidance to their sponsors throughout the development process.
In terms of manufacturing technology, partnering with a CDMO that has facilities designed for small-scale operations but also offers scalability for large-scale clinical and commercial manufacturing is advantageous. This flexibility enables a CDMO to meet diverse product requirements and adapt to varying formulation challenges. Access to a wide array of equipment and processes ensures that various challenges can be tackled, and the most appropriate solution for each unique project can be identified.
Roller compaction offers numerous advantages in pharmaceutical formulation development, especially for highly potent active pharmaceutical ingredients (APIs) and heat or moisture-sensitive materials. This dry granulation technique bypasses the need for liquid binders and high-temperature drying, making it ideal for formulations containing APIs that are sensitive to moisture and heat. By applying controlled pressure through counter-rotating rollers, roller compaction densifies powders into uniform ribbons, which are subsequently milled into granules. These granules exhibit improved flow properties and compressibility, essential for consistent tablet production.
For highly potent APIs, roller compaction significantly reduces the risk of airborne contamination and cross-contamination, ensuring a safer working environment and enhancing operator safety. The process parameters, such as roll pressure, roll speed, and gap width, can be precisely adjusted, enabling the fine-tuning of granule properties to meet specific formulation requirements. This adaptability is crucial during the development phase, where optimizing the balance between excipients and APIs determines the final product’s efficacy and stability. Additionally, roller compaction supports a scalable development approach, where the optimized parameters can be directly transferred to larger production scales, ensuring product consistency and quality from lab-scale prototypes to commercial manufacturing. The method’s ability to maintain the integrity and potency of sensitive APIs, combined with its flexibility and scalability, makes roller compaction a valuable tool in pharmaceutical formulation development.


Scalable Manufacturing

Pharma organizations that outsource to CDMOs are increasingly keen to work with fewer suppliers, driven mainly by the desire to simplify and de-risk their supply chain. Finding a CDMO that is able to scale their manufacturing processes alongside the drug product’s growth trajectory is a key factor that could – or should – influence outsourcing decisions.
Scalability in high potent OSD manufacturing can be achieved via geometrically scalable equipment trains, which enable seamless transition from small-scale clinical batches up to large-scale batches for Phase III and Commercial supply. This ability removes the need to initiate another technical transfer out to a site with large-scale capabilities. CDMOs with geometric scalability built into their equipment trains also benefit hugely from a high degree of flexibility in their manufacturing processes. For example, using small and large intermediate bulk containers (IBCs) with the same split butterfly valves, and contained within the same size frame, enables rapid scalability and allows the CDMO to adapt to an ever-changing workflow, which is vital in a facility that handles products at both the clinical and commercial scale.
Whereas roller compaction plays a major role in the development stages, as mentioned above, the versatility of this technology also has a great influence over later-stage manufacturing activities. One of its primary advantages is the ability to handle and process HPAPIs safely and efficiently due to its engineered containment and dry granulation process, which minimizes dust and airborne contamination, thereby protecting both operators and the environment. Furthermore, roller compaction facilitates seamless scale-up from laboratory to commercial production by allowing direct adjustments of key parameters such as roll pressure and speed, ensuring consistent granule quality and uniformity. This method enhances material flow and compressibility, leading to reliable tablet formation without the need for solvents or drying steps, thus reducing processing time and operational costs. Additionally, the continuous nature of roller compaction supports high throughput manufacturing, which is essential for meeting the demands of large-scale production while maintaining stringent quality control standards. By integrating Process Analytical Technology (PAT) for real-time monitoring, roller compaction ensures consistent product quality and regulatory compliance, making it an ideal choice for manufacturing pharmaceutical products with highly potent APIs.

Conclusion

The ongoing growth in oncology and obesity research is expected to persist, with many therapies such as GLP-1s involving highly potent molecules. Consequently, outsourcing drug product manufacturing to specialist Contract Development and Manufacturing Organizations (CDMOs) is becoming increasingly vital.
Recent advances in the molecular understanding of cancer, alongside a heightened focus on developing targeted therapies and regulatory support for expedited market entry of new treatments, have transformed the outsourcing landscape for highly potent oncology drugs. Biopharmaceutical companies now recognize the critical importance of selecting the right partner for the development, manufacturing, packaging, and commercialization of oncology products containing highly potent active pharmaceutical ingredients.
Given the growing complexities associated with the safe handling of these molecules and the corresponding regulatory scrutiny, companies looking to outsource must conduct thorough due diligence. They need to identify specialist CDMOs that provide safe, regulatory-compliant, scalable, and flexible processes; offer additional in-house services; and deliver end-to-end solutions tailored to evolving needs throughout the development lifecycle and global commercial supply.


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