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Small Pharma Expands Potential of Commercial Portfolio With DMT-Based Psychedelic Assets - Seite 2
SPL028 Update
Small Pharma has advanced its proprietary deuterated DMT candidate SPL028 through preclinical studies. The goal is to deliver a treatment with an extended psychedelic experience, as compared to SPL026, but still significantly shorter than the experience of other psychedelics, such as psilocybin and LSD. Through SPL028, Small Pharma is exploring whether an extended duration could offer a DMT treatment tailored for other mental health conditions. Additionally, the pharmacokinetic profile of SPL028 offers the opportunity for optimizing alternative routes of administration beyond IV.
The final candidate of SPL028 was selected after screening a range of deuterated DMT compounds through in vitro and in vivo studies. Importantly, preclinical studies suggest that SPL028 offers a similar safety and pharmacological profile to SPL026, while being differentiated by its pharmacokinetics, to offer a potentially extended psychedelic experience as compared to SPL026.
Key parameters include:
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Safety profile: SPL028 has the potential for a similar safety profile to SPL026 in the clinic.
- In vitro and ex vivo binding: data suggest a similar binding affinity across a range of receptors including 5-HT receptor subtypes (5HT2A included), which are believed to induce psychoactive effects.
- Toxicology: SPL028 found to be safe and well-tolerated in vivo at all doses tested, demonstrating significant safety margins for progressing into first-in-human trials.
- Behavioral effects: Similar but prolonged behaviors induced by SPL028 in a number of preclinical models were observed in vivo, suggesting the potential for a similar but longer psychedelic experience as compared to SPL026.
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Pharmacokinetic profile: In vitro data of SPL028 demonstrated a reduction in clearance rate and significant extension in half-life compared to SPL026. Following IM
administration in vivo, SPL028 demonstrated a marked decrease in clearance from the body, resulting in higher blood concentrations for an extended period of time versus SPL026.
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Dr. Carol Routledge continued, “The rapid effects of DMT, as highlighted in recent Phase I data, offers the flexibility to engineer alternative DMT candidates that could deliver extended yet convenient and accessible in-clinic treatment options for a broader range of mental health conditions. SPL028’s promising preclinical data demonstrates its similarities to DMT from a safety and behavioral perspective, allowing for a potentially expedited route to the clinic.”