First-in-Man Studies

Timely Phase I Clinical Trials

In today’s market, pharmaceutical companies are struggling to do more with less. With diminishing resources, patent expiry, and increased competition, companies are under pressure to reach critical drug development milestones faster, in spite of candidate chemical and physical challenges. To make matters worse, oftentimes there are limited quantities of active pharmaceutical ingredient (API) available for adequate development in Phase 1. In light of this fact, CoreRx™ offers you several drug development approaches, customized to align with your corporate goals. It is more than just getting into the clinic faster. One must view drug development from a holistic perspective.

API in bottle, powder in bottle, API into capsule, and traditional formulations are all approaches to consider for “first-in-man” phase 1 clinical trials. CoreRx capabilities and scientific depth encompass all available drug development options for expedited first-in-man studies. Whether your compound API is in short supply, has excipient compatibility issues, is unstable, or has solubility issues, CoreRx scientists can effectively deliver the solution that meets your budgetary and more importantly, your timeline needs. Depending upon your unique situation, CoreRx can use the following approaches.

API in bottle

Advantages

  • No need for excipients
  • No formulation development
  • Minimal analytical development
  • Simplified stability testing
  • Minimized API usage
  • Wide range of dosage strengths

Disadvantages

  • Clinic preparation time
  • Solubility issues may arise
  • Taste Masking may be difficult
  • Patient convenience may be compromised
 

Powder in bottle

Advantages

  • Wide range of dosage strengths
  • Minimal API Characterization
  • Use with Limited API availability
  • Added excipients can help with
    stability and taste masking

Disadvantages

  • Longer Manufacturing Time
  • Clinic Preparation Time
  • Development of matching placebo needed
  • Additional analytical development required
 

API in capsule

A common approach for phase 1 supplies is weighing API into capsules. In many cases, the overall development timelines may be reduced by as much as six months, by reducing formulation time as well as some analytical development & stability testing. Additionally, placebo development is straightforward. Following this approach is common for many pharmaceutical companies, as it is a “quick fix” option for supplying drug product to meet aggressive Phase I clinical study start dates. Dispensing API in capsules can be done by hand, semi-automated (utilizing a Quantos® or Xcelodose® system), or have a fully automated approach using the Symyx Powdernium® benchtop*.

Although the API in capsule approach can be a timesaver, getting you into clinical studies sooner, but it will not eliminate the need to conduct formulation development and process optimization. It is therefore critical to weigh carefully the impact on the overall development plan (as well as cost and time) of using neat drug substance filled capsules/vials vs. a formulated product in early studies. To view a whitepaper discussing all these points, click here.

Advantages

  • Short Manufacturing Time
  • Minimal API Characterization
  • Use with Limited API availability
  • Taste masking not necessary
  • Minimal Analytical Development

Disadvantages

  • Increased overall drug development costs
  • Increase overall development time
  • Development of matching placebo needed
  • Not suitable for all API’s
  • Possible capsule compatibility issues
 

Formulated Product

Provided that there is ample time for prototype development, and the API synthesis does not change, a formulated product approach can have advantages. Having a formulated product in Phase 1 can ease the transition into Phase 2 studies, saving time. For controlled release formulations in Phase 1, developing a formulated product is the only option. For water insoluble compounds, liquid capsules or commonly utilized. As with all development work, upfront time & energy will be necessary, such as pre-formulation, excipient compatibility, analytical methods development, and stability testing. The downside is that the additional work will take time and money. It is a matter of pay now or pay later.

Advantages

  • Wide range of dosage strengths
  • Decreases overall development time
  • Decreased overall development costs
  • Added excipients can help with stability and taste masking

Disadvantages

  • Longer Development & Manufacturing Time
  • Excipient Compatibility & Preformulation needed
  • Development of matching placebo needed
  • Additional analytical development required
 

Unfortunately, there is no single formulation approach that will fit every API. CoreRx will help you evaluate the advantages and disadvantages of each approach, depending upon the compound in question, as well as your overall project goals regarding time, budget, and API availability.

Partner With CoreRx For Your Drug Formulation Needs

When you’re ready to get expertise, flexibility, and reliability with your pharmaceutical formulation project, call us or complete the form below. We’ll be happy to answer your questions, provide a tour of our facilities, and get your project started today.

Discover The Benefits Of Working With CoreRx

  • Our scientists have expertise in a virtually every dosage form so you can rest assured we can quickly and effectively create solutions to formulation dilemmas.
  • Our staff has over 200 years of combined experience in contract pharmaceutical development giving us a unique insight and deep understanding of the process.
  • CoreRx is founded on effective communication and active client involvement which ensures your timelines and expectations are met again and again.
  • Our facilities and teams are designed to provide you the greatest flexibility while maintaining quality which means even as your project requirements change, our services can keep up with your needs.
  • We’re fast! CoreRx has the experience to identify the most effective process and keep your project on schedule throughout it. Without sacrificing quality, we’ll get your product through manufacturing and on the market quickly.

Call, email, or complete the form to learn more about the benefits of partnering with CoreRx for your pharmaceutical development project.

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