By: Pharma Solutions Editors
The demand for novel pharmaceutical candidates and expanded therapeutic options continues to grow, driven by the increasing need to address patient convenience and compliance – and elevate global health. To pave the way for more treatment possibilities that will provide relief from ailments so that patients can live life to the fullest, the scientific community has turned its attention to cannabinoids, cannabidiol (CBD) in particular. That includes dsm-firmenich.
This month, we reached a new milestone in the cannabinoid landscape with the launch of CBtru®, a first-ever CBD drug product intermediate. The intermediate is a formulation of the CBD active pharmaceutical ingredient (API) – the component responsible for the medicine’s efficacy – with enhanced properties, ready for further development into a finished product. As a result of its advanced properties, CBtru® enables the manufacture of oral solid dosage forms. We interviewed Athanasia Kanli, Global Business Development Manager for Pharma at dsm-firmenich, to understand why it was the right time to introduce a formulated CBD solution to the market and what it means for future advancements in the space.
Cannabinoids hold immense therapeutic potential – demonstrating promising benefits in several broad therapeutic areas, like central nervous system (CNS) diseases (such as epilepsy), chronic pain management, mood disorders, cancer, brain health and more. That’s why we were drawn to cannabinoids. However, our experts quickly recognized that bioavailability was a recurring challenge for drug innovators formulating with these molecules.
Existing CBD-based formulations exhibit very limited bioavailability – as low as 6%1 – and therefore efficacy. This is due to the highly lipophilic nature and poor solubility of CBD, which reduces its absorption in the body. On top of that, CBD undergoes significant pre-systemic elimination in the liver, further decreasing bioavailability. Consequently, despite the promise of this drug candidate, its full therapeutic potential was not being realized.
We saw an opportunity to change this. After assessing approximately 200 prototypes and drug delivery technologies, we finally discovered a solution that would accelerate the path to optimized CBD bioavailability and therefore more patient-friendly medicines – CBtru®.
The application of CBD has been limited to oil-based preparations due to its low bioavailability and physical and chemical instability. These formulations require large doses and several administrations a day for any real therapeutic effectiveness. This isn’t very pleasant to ingest or convenient for patients; potentially affecting medicine acceptance and compliance. Take CBD for epilepsy as an example. The daily dosage required to treat drug resistant epilepsy with CBD varies between 5-20 mg/kg body weight.2 In adults, this can translate to more than 1 g of active ingredient in 10 mL of oil . Not only is this inconvenient, but such large doses also increase the risk of unwanted adverse effects linked to frequent and sizeable carrier oil consumption.
CBtru® mitigates these issues by enabling higher active loading, improved stability and optimized pharmacokinetic performance. Our internal research demonstrated that CBtru® facilitates formulations with three-to-four times higher drug loading than existing commercially available products. This in turn, reduces the dosage, making it more cost-effective and lowering the probability of side effects.
Our formulated drug product intermediate is pioneering in the cannabinoid market because it paves the way for faster-acting therapies and more patient-friendly delivery systems, like tablets, including orally disintegrating tables (ODTs) and chewables. By enabling the delivery of CBD in novel dosage forms, CBtru® represents a new era in cannabinoid-based medicines where patients can avoid having to administer higher dosages of the active in unpleasant delivery formats – promoting better compliance and ultimately improved therapeutic outcomes. We see this being especially beneficial for individuals who may struggle with traditional oil-based formulations due to their taste, texture and the large volumes required.
There are benefits for CBD innovators too. A key advantage of increasing the bioavailability of CBD is the ability to alter its therapeutic window, i.e. reduce the amount needed to achieve therapeutic effects. These adjustments increase the likelihood that clinical trials will successfully reach their primary endpoints, thereby validating the effectiveness of treatments, supporting regulatory approval and informing healthcare decisions – not to mention mitigating costs associated with trial failures.
The next step is to establish long-term strategic partnerships to explore the therapeutic applications of our trial-ready intermediate drug product. We see CBtru® having the most immediate impact in the realm of insomnia treatment, where we already have a project underway with our partner Oz Medicann Group (OMG) Pharma. We are also interested in the solution’s potential for pain management, brain health and CNS diseases. However, we envision a broad spectrum of applications for CBtru® due to its unique properties and the growing interest in cannabinoid-based therapies. Given this, we are eager to collaborate with strategic partners who share our vision for unlocking new frontiers in medical treatment with patient-first innovation.
Our CBD offering for pharma applications goes beyond CBtru®, because we understand that entering early-stage drug development in the cannabinoid space is complex. Together with Brains Bioceutical, manufacturer of high-quality pharma-grade cannabinoids, we can help drug developers navigate the cannabinoid drug development journey with confidence. Our unique innovation platform combines a robust cannabinoids portfolio, expert services – including leading-edge technical capabilities, global regulatory knowledge and clinical study proficiency – plus customized solutions to elevate cannabinoid-based research and development.
Together, we can prevent and treat diseases to support better quality of life. Download our case study to learn more about how CBtru® is paving the way for elevated patient care in the realm of insomnia treatment.
26 June 2024
5 min read
1 Perucca and Bialer. Critical aspects affecting cannabidiol oral bioavailability and metabolic elimination, and related clinical implications. Cannabinoids in Neurology and Psychiatry, 2020;34(8):795-800.
2 Lawson et al. Expert advice for prescribing cannabis medicines for patients with epilepsy—drawn from the Australian clinical experience. BJCP, 2022;88(7):3101-3113.