N-desethyloxybutynin is a novel active metabolite of oxybutynin chloride, an FDA-approved anticholinergic indicated for the treatment of overactive bladder. NT502 is a new chemical entity and selective anticholinergic agent that we are developing as an oral, once- or twice-daily treatment to reduce chronic sialorrhea in patients with neurological conditions associated with excessive salivation and drooling. Based on preclinical data, NT502 has been shown to be preferential for blocking muscarinic receptors in the salivary glands and may offer the potential for an improved tolerability profile and an easier-to-dose oral formulation compared to currently approved chronic sialorrhea treatment options. The NT502 Phase 1 trial was a single-dose open-label, randomized, parallel study assessing the systemic exposure and safety of four ion-resin, modified-release ODT formulations of NT502 and oxybutynin in 30 healthy patients. The top-line results from this study confirmed a N-desethyloxybutynin formulation for further clinical development.
About Chronic Sialorrhea
Patients with neurological disease experience sialorrhea due to decreased intra-oral salivary clearance associated with neuromuscular dysfunction. Anatomic abnormalities and side effects from certain medications including anticonvulsants and antipsychotics can also cause chronic, excessive drooling. Chronic sialorrhea can lead to significant physical and psychosocial complications, including perioral chapping, dehydration, infection, foul odor, stigmatization, and increased dependency and level of care, all of which can create an additional burden for these medically complicated patients. Current anticholinergic agents are associated with treatment-limiting adverse events and require titration and dosing up to three times per day, presenting complexity and inconvenience to patients and caregivers. As such a significant unmet medical need remains for chronic sialorrhea patients.
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