Laxxon has received a grant by Freistaat Thüringen and the ESF Plus (European Social Fund) for the further development of LXM.2. LXM.2 is Laxxon's oral GLP-1 agonist asset, offering adult and pediatric patients a non-invasive, once-daily treatment designed to transform the treatment landscape for diabetes, metabolic syndrome and weight loss.
LXM.2 is produced by Laxxon's proprietary 3D screen printing technology platform, SPID®. LXM.2 is an enteric coated oral tablet of a GLP-1 agonist combined with a permeation enhancer to offer better bioavailability upon intake, offering an oral alternative to GLP-1 injections currently on the market.
SPID®-Technology: Manufacturing traditionally fragile molecules
SPID® (Screen Printed Innovation Drug) Technology is Laxxon Medical’s disruptive 3D screen printing (3DSP) additive manufacturing process and technology platform.
SPID® enables the development and production of smart drug delivery system (DDS) oral dosage forms with tailored pharmacokinetics based on complex novel formulations and geometric structures which optimize the release profiles of common pharmaceuticals and new chemical entities. In addition, it enables the processing of substances into dosage forms that cannot be processed by conventional methods.
The sophisticated, additive layer-by-layer production of SPID® enables a new generation of smart DDS’s through the heterogenous distribution of active pharmaceutical ingredients (APIs) and excipients, allowing for a range of innovate drug forms, including micro tablets and multi-compartment tablets.
SPID® is capable of scaling from R&D batches to mass production for commercialization (> 1 million tablets per day per unit) with no change in the manufacturing process.
Laxxon's first cGMP manufacturing unit is installed at its CDMO partner Adare's CGMP facilities in Pessano, Italy.
A patent-protected manufacturing process
Laxxon owns the exclusive worldwide rights for the development, production, and
commercialization products developed with SPID®-Technology. SPID® is a special additive manufacturing, 3D screen printing (3DSP) process based on the classic flatbed screen printing process widely used in electronic, automotive, and aerospace industries.
The company together with its technology provider Exentis has 230+ patents and patent applications (both in-licensed and owned) worldwide with 5,000+ patent claims. All products produced by SPID®-Technology are patent protected until at least 2037.
The production capacity of traditional 3DP technologies is limited and typically used for R&D-sized batches. SPID® is capable of scaling from R&D batches to mass production for commercialization (> million tablets per day per unit) with no change in the manufacturing process.
LXM.2 - An oral GLP-1 made possible by SPID®
Proteins and polypeptides like GLP-1s are difficult to formulate for oral drug delivery due to their:
Poor solubility – many peptides are poorly soluble in water which can decrease the amount of drug that enters the bloodstream through the intestinal wall.
Size and nature – their large size may them poorly absorbable and their nature renders them susceptible to degradation by digestive enzymes, both leading to poor bioavailability. Laxxon has carefully chosen a combination of ingredients to combat the low bioavailability of oral GLP-1s. The enteric coating protects the molecules from degradation in the stomach so that the active ingredient can pass into the small intestine. The permeation enhancer then will act to increase the amount of GLP-1 absorbed into the bloodstream. Each component plays a crucial role in increasing the bioavailability of the GLP-1. Key is the production of a stable core harboring permeation enhancers and GLP-1 with stable physical properties, which is only possible due to SPID®-Technology.
Designed with the patient in mind
GLP-1 agonists approved for weight loss are currently only available in injectable formulations. Patients must either inject themselves daily or weekly. These products also must be stored at specific conditions and have limited shelf lives.
LXM.2 is designed to provide patients with a once-daily oral medication to replace the daily or weekly injections. In its form of the multi-compartment micro tablets, LMX.2 addresses particularly the needs of pediatric patients.
Oral GLP-1 is as effective as the injectable version
A 2021 research review looked at several clinical studies on GLP-1s and concluded that once-a-day oral semaglutide is as or more effective for weight loss than injectable versions of semaglutide. Other recent research points to oral tablets having a distinguishing feature, allowing for “similar or better efficacy and similar tolerability” compared with most of the injectable GLP-1s.
Laxxon has carefully chosen a combination of ingredients to combat the low bioavailability of oral GLP-1s:
The enteric coating protects the molecules from degradation in the stomach so that the active ingredient can pass into the small intestine.
The permeation enhancer then will act to increase the amount of GLP-1 absorbed into the bloodstream.
Each component plays a crucial role in increasing the bioavailability of the GLP-1 Agonist. Key is the production of a stable core harboring permeation enhancers and GLP-1 with stable physical properties with the combination of these ingredient, which is only possible in an oral solid formulation with Laxxon’s SPID® Technology
Enhancing Permeability for Improved Absorption
A key goal of pharmaceutical research is the development of oral dosage forms for conditions such as diabetes, reducing the need for frequent injections.
Peptide-based drugs like GLP-1 Agonists have low bioavailability due to their poor permeability. Laxxon's LXM.2 enhances peptide absorption by utilizing a permeation enhancer in the construction of the tablet. Upon tablet dissolution in the intestine, this enhancer temporarily opens tight junctions in the intestinal epithelium, increasing the permeability of large molecules and thereby facilitating their absorption. This approach can significantly improve patient compliance by offering a more convenient and less invasive alternative to injections.
Pilot PK data for LXM.2 identified lead candidates with a 10-fold increase in bioavailability over published results for competing products.
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