At Oakwood Labs, we’re proud to contribute to the development of cancer pharmaceuticals through our continuous work manufacturing long-acting injectables (LAIs). That’s why we’ve compiled an informational guide showcasing our ongoing work in the healthcare field, as well as the numerous benefits of LAIs for oncology treatment.

Advantages of Long-Acting Injectables to Treat Cancer

There are numerous advantages to the use of LAIs as pharmaceuticals to treat cancer. To start, Bruton tyrosine kinase (BTK) inhibitors are established standards of care in multiple B-cell malignancies including chronic lymphocytic leukemia, mantle cell lymphoma, and Waldenstrom macroglobulinemia. LAI formulations of BTK inhibitors offer certain advantages in terms of pharmacokinetics (PK) and patient adherence. For example, ibrutinib (Imbruvica) has a very short half-life of 4-6 hours. Hence, relatively large doses of the oral form are required to target plasma levels within the therapeutic range.

The PK profile is marked by large peaks and valleys, sometimes exceeding the therapeutic level, and sometimes falling below. The PK profile of the LAI formulation is much “smoother,” having no significant peaks and valleys. Also, the oral bioavailability of ibrutinib is only 3% and varies among patients. The LAI formulation, meanwhile, is 100% bioavailable and therefore can be administered at much lower per-day doses.

These factors above could reduce side effects caused by off-target receptor interactions, while maintaining efficacy, and result in fewer cases in which the medication needs to be discontinued. The LAI formulations of two weeks and one month ensure patient adherence for these periods, possibly enhancing efficacy in clinical practice.

Similar benefits may be possible with other immunomodulatory cancer pharmaceuticals, such as the thalidomide analog pomalidomide (Pomalyst), indicated for multiple myeloma. The recommended dose for multiple myeloma is 4 mg per day taken orally on days 1 through 21 of repeated 28-day cycles. The half-life is approximately 7.5 hours and oral bioavailability is estimated to be approximately 75%. The LAI formulation reduces the peaks and valleys of drug exposure, enables a reduction in the total amount of drug administered, reduces the frequency of doses, possibly reduces side effects, and ensures patient adherence.

Additional Benefits to Highlight

Along with administration approaches and the long-term effects on the body, LAIs as oncology pharmaceuticals possess several key advantages for the patient, including:

• Reduced treatment burden
• Increased patient compliance
• Sustained stable hormone suppression

How Oakwood Labs Is Contributing to Cancer Drug Development

Alongside working with external partners who have been seeking out LAIs for their own initiatives, our team is also currently in the process of creating internal programs that utilize our very own microparticle technology. The goal of these internal initiatives is to convert an existing product into an LAI formulation to extend the duration of drug release to what is currently on the market, achieving patient compliance and ease of use.

More specifically, Oakwood Labs has used its internal technology to progress its formulations that are focused on treating mantle cell lymphoma, small lymphocytic lymphoma, chronic lymphocytic leukemia, and multiple myeloma with release durations ranging anywhere between two and four weeks. Our LAI oncology drug development has led to significant benefits for patients, such as:

• Reducing the amount of drug administered to the patient
• Decreasing the number of doses needing to be injected
• Diminishing more adverse reactions and side effects from dosages

Partnership Opportunities

At this point in the cancer drug development process, our team is actively seeking an external partner to help further develop our internal program. Key responsibilities in this area include funding ongoing development activities as well as phases one through three of clinical trials and registration/commercialization efforts.

If you’re interested in learning more about this opportunity, please contact our team directly, as we would be happy to provide additional details or answer any questions you may have.

FAQs About Oncology Pharmaceuticals, Development, and More

Can you provide me a brief history of oncology pharmaceutical development and its breakthroughs?

Though it is estimated that the preliminary study and treatment of cancer was initially recorded as early as 520 BCE when Persian queen Atossa was treated for a breast tumor, modern-day pharmaceuticals for treating cancer did not surface until relatively recently. Just some of the pivotal findings in this scientific journey include:

• The 1840s – Physician Rudolf Virchow is well-known for his observation of cancer cells during this time, in which he defined their key characteristics. This led to the future of cancer treatment protocols by the start of the 20^th
• 1895 – Once German physicist Wilhelm Conrad Röntgen first correctly identified the waves of radiation that we all now know as X-rays, this equipment was then used in radiotherapy cancer treatment shortly thereafter.
• The 1940s – Based on the discovery that nitrogen mustard contains anticancer properties during World War II, researchers were able to develop various cytotoxic drugs to directly target dividing cancer cells, which later led to today’s chemotherapy practices.

Can you tell me more about the work Oakwood Labs does to develop LAIs?

Oakwood Labs performs LAI development through our technology platform Chroniject™, and some characteristics of products we have made with this system including the following:

• The duration of release is one week to one year
• LAIs are easily syringable with 18- to 23-gauge needles
• Products are reconstituted immediately with sterile water
• LAIs are filled aseptically and terminally sterilized if feasible
• Products have proven content uniformity and good stability characteristics
• LAIs are free of foreign particulate matter

Additionally, Chroniject™ is microsphere-based and has biodegradable polymers such as PLA, PLGA, and other polymers with demonstrated low toxicity and sourced from multiple suppliers. Plus, the finished dosage form typically consists of a lyophilized vial containing microspheres, a suspending agent, and other excipients.

What are the current barriers to an LAI entering this particular space?

The barrier to entry is that LAI formulations are extremely difficult to develop and require a high degree of technical expertise. Once developed, you then need to scale up the process to be able to manufacture in an aseptic GMP facility. The Oakwood Labs team can work with you to overcome key challenges.

What are some common trends in the development of drugs to treat cancer?

As healthcare professionals and pharmaceutical developers continue to produce different types of drugs for treating cancer, numerous trends have emerged from their discoveries, such as:

• Targeted drugs for treatment
• Immunotherapy
• Monoclonal antibodies
• Small molecule-targeted agents
• CRISPR
• Biomaterials, such as chitosan oligosaccharide (COS)

These recent practices have significantly advanced the oncology field, leading to longer, happier, and healthier lives for patients undergoing treatment.

Contact Oakwood Labs for More Information

If you have any additional questions about the oncology drug development process, or if you’re looking to get in touch with us regarding a potential partnership opportunity, please contact our team today. We look forward to assisting you.