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Sparian Pipeline

Arylepoxamide Receptor (AEAr) Agonists

Acute and Chronic Pain

MOR/DOR Modulators

Opioid Use Disorder 

Irreversible MOR Antagonists

Opioid Overdose

Peripheral DOR Bitopic Agonists

Neuropathic Pain

Stimulant Use Disorder

Peripheral DOR Bitopic Agonists

Neuropathic Pain

SBS-406

Peripheral DOR Bitopic Agonists

Neuropathic Pain

Discovery

Lead Optimization

CMC/IND Enabling Studies

Phase 1 

SBS-1000 IV/SC

SBS-1001 Oral

SBS-226 Oral

SBS-371 IV/SC

SBS-406

SBS-518

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AEAr Agonists

SBS-1000 IND-enabling Studies

SBS-1001 Lead Optimization

Acute and Chronic Pain

Arylepoxamides are first in class compounds which bind to the newly discovered receptor, the AEAr. In preclinical studies, arylepoxamides demonstrate potent analgesia for acute and chronic pain and a clean safety profile lacking respiratory depression, physical dependence, and reward behavior. 

 

MOR Agonist/
DOR Antagonist

SBS-226 Lead Optimization

Opioid Use Disorder

Our MOR Agonist/DOR Antagonists are synthetic compounds that are structurally similar to mitragynine pseudoindoxyl - one of the primary alkaloids in Kratom. SBS-226 is a new chemical entity (NCE) synthesized and developed in the Majumdar Lab. SBS-226 is a very weak MOR agonist and potent DOR antagonist. Preclinically, SBS-226 can ameliorate opioid withdrawal but does not demonstrate abuse potential, respiratory depression, or physical dependence.  

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Irreversible MOR Antagonists

SBS-371 Lead Optimization

Opioid Overdose 

SBS-371 is a first in class irreversible MOR antagonist being developed for the acute treatment and prophylaxis of opioid overdose. The opioid epidemic has transformed to a fentanyl epidemic and urgently demands more potent, longer lasting MOR antagonists. Preclinically, SBS-371 can prevent and reverse a synthetic opioid overdose (e.g. fentanyl and fentanyl derivatives). 

 
 

Peripheral DOR Bitopic Agonists

SBS-406 Discovery

 

Neuropathic Pain

Our peripherally acting bitopic DOR agonists bind to the orthostatic and allosteric sites of delta opioid receptors (DOR). Preclinically, SBS-406 alleviates neuropathic pain and does not elicit the side effects seen with centrally acting DOR agonists. 

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Sigma Antagonist / DAT Inhibitor

SBS-518 Lead Optimization

 

Stimulant Use Disorder (Cocaine and Methamphetamine)

Our dual acting sigma antagonist / dopamine active transporter (DAT) inhibitor is a first in class compound to treat stimulant use disorder (StUD). There are ~3.2 M people with StUD and ~57 K StUD overdose related deaths per year. Preclinically, SBS-518 reduces cocaine self-administration and reduces cocaine-induced extracellular dopamine increases.