A Phase 2, Proof-of-concept, Multi-center, Randomized, Double-blind, Placebo-controlled Study to Evaluate the Efficacy and Safety of AT-5214 in Subjects with Moderate to Severe Facial Acne Vulgaris

Start Date01 Aug 2024

Sponsor / Collaborator-

NCT04263623 / Unknown statusPhase 2

A Double-Blind, Randomized, Placebo-Controlled Study to Assess the Efficacy and Safety of AT-5214 in the Treatment of Subjects With Moderate to Severe Palmar Hyperhidrosis

This is a multicenter, randomized, double-blind, placebo-controlled, parallel group comparison study of AT-5214 in subjects with moderate to severe primary palmar hyperhidrosis (sweaty palms). This study will compare two different oral (tablet) doses of AT-5214 (study drug) versus a matched placebo. Approximately 120 subjects will be enrolled at approximately 10 study sites.

Start Date31 Jan 2020

Sponsor / Collaborator

Atacama Therapeutics, Inc.Startup

NCT03404570 / CompletedPhase 2

A Double-Blind, Randomized, Placebo-Controlled Exploratory Study to Assess the Efficacy and Safety of TC-5214 in the Treatment of Subjects With Moderate to Severe Palmar Hyperhidrosis

This is a pilot exploratory study to evaluate the safety and efficacy of TC-5214 in subjects with palmar hyperhidrosis.

Start Date21 Dec 2017

Sponsor / Collaborator

Atacama Therapeutics, Inc.Startup

100 Clinical Results associated with nAChR α4/β2/α5 x nAChRα3&β4

100 Translational Medicine associated with nAChR α4/β2/α5 x nAChRα3&β4

0 Patents (Medical) associated with nAChR α4/β2/α5 x nAChRα3&β4

Literatures (Medical) associated with nAChR α4/β2/α5 x nAChRα3&β4

01 Aug 1998·Molecular PharmacologyQ3 · MEDICINE

Rat α3/β4 Subtype of Neuronal Nicotinic Acetylcholine Receptor Stably Expressed in a Transfected Cell Line: Pharmacology of Ligand Binding and Function

Q3 · MEDICINE

Article

Author: Kenneth J. Kellar ; Jarda Wroblewski ; Yingxian Xiao ; Alexander Surin ; Erin L. Meyer ; Jessica M. Thompson

We stably transfected human kidney embryonic 293 cells with the rat neuronal nicotinic acetylcholine receptor (nAChR) alpha3 and beta4 subunit genes. This new cell line, KXalpha3 beta4R2, expresses a high level of the alpha3/beta4 receptor subtype, which binds (+/-)- [3H]epibatidine with a Kd value of 304+/-16 pM and a Bmax value of 8942 +/- 115 fmol/mg protein. Comparison of nicotinic drugs in competing for alpha3/beta4 receptor binding sites in this cell line and the binding sites in rat forebrain (predominantly alpha4/beta2 receptors) revealed marked differences in their Ki values, but similar rank orders of potency for agonists were observed, with the exception of anatoxin-A. The affinity of the competitive antagonist dihydro-beta-erythroidine is >7000 times higher at alpha4/beta2 receptors in rat forebrain than at the alpha3/beta4 receptors in these cells. The alpha3/beta4 nAChRs expressed in this cell line are functional, and in response to nicotinic agonists, 86Rb+ efflux was increased to levels 8-10 times the basal levels. Acetylcholine, (-)-nicotine, cytisine, carbachol, and (+/-)-epibatidine all stimulated 86Rb+ efflux, which was blocked by mecamylamine. The EC50 values for acetylcholine and (-)-nicotine to stimulate 86Rb+ effluxes were 114 +/- 24 and 28 +/- 4 microM, respectively. The rank order of potency of nicotinic antagonists in blocking the function of this alpha3/beta4 receptor was mecamylamine > d-tubocurarine > dihydro-beta-erythroidine > hexamethonium. Mecamylamine, d-tubocurarine, and hexamethonium blocked the function by a noncompetitive mechanism, whereas dihydro-beta-erythroidine blocked the function competitively. The KXalpha3 beta4R2 cell line should prove to be a very useful model for studying this subtype of nAChRs.

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