Nav1.7 blockers(Sodium channel protein type IX alpha subunit blockers), Nav1.8 blockers(Sodium channel protein type X alpha subunit blockers), Nav1.9 inhibitors(SCN11A sodium channel subunit inhibitors)

Therapeutic Areas

Nervous System Diseases

Active Indication-

Inactive Indication

NeuralgiaPain

Originator Organization

Sumitomo Pharma Co., Ltd.

Active Organization-

Inactive Organization

Sumitomo Pharma Co., Ltd.

Alphanavi Pharma KKStartup

Drug Highest PhasePendingPhase 1/2

First Approval Date-

Regulation-

Structure

Molecular FormulaC20H20F3N5O2

InChIKeyHHXCJIMPEJSJTG-JTQLQIEISA-N

CAS Registry1233231-30-5

Clinical Trials associated with DSP-2230

JPRN-jRCT2061200046 / RecruitingPhase 1/2IIT

An exploratory Phase I/II study of ANP-230 to evaluate the safety, efficacy and pharmacokinetics in patients with infantile episodic limb pain

Start Date18 Jan 2021

Sponsor / Collaborator-

ISRCTN02543559 / CompletedPhase 1

A phase 1 study to investigate the effect of single and repeated doses of DSP-2230/placebo on renal function in healthy subjects

Start Date03 Oct 2013

Sponsor / Collaborator

Sunovion Pharmaceuticals Europe Ltd.

ISRCTN80154838 / CompletedNot Applicable

A randomised, double-blind, placebo-controlled, four-way crossover, two-part study investigating the pharmacodynamic effect of DSP-2230 using the ID Capsaicin and UVB models in healthy male subjects, using pregabalin and ibuprofen lysine as positive controls.

Start Date07 Jan 2013

Sponsor / Collaborator

Sunovion Pharmaceuticals Europe Ltd.

100 Clinical Results associated with DSP-2230

100 Translational Medicine associated with DSP-2230

100 Patents (Medical) associated with DSP-2230

Literatures (Medical) associated with DSP-2230

01 Aug 2024·Biochemical and Biophysical Research Communications

Unique electrophysiological property of a novel Nav1.7, Nav1.8, and Nav1.9 sodium channel blocker, ANP-230

Article

Author: Kudo, Takehiro ; Takada, Yoshinori ; Ishibashi, Fumiaki ; Oyamada, Yoshihiro ; Maezawa, Yasuyo ; Ikeda, Kazuhito ; Honda, Shigeyuki ; Kamei, Tatsuya ; Yamane, Hana

Voltage-gated sodium channel subtypes, Nav1.7, Nav1.8, and Nav1.9 are predominantly expressed in peripheral sensory neurons. Recent genetic studies have revealed that they are involved in pathological pain processing and that the blockade of Nav1.7, Nav1.8, or Nav1.9 will become a promising pharmacotherapy especially for neuropathic pain. A growing number of drug discovery programs have targeted either of the subtypes to obtain a selective inhibitor which can provide pain relief without affecting the cardiovascular and central nervous systems, though none of them has been approved yet. Here we describe the in vitro characteristics of ANP-230, a novel sodium channel blocker under clinical development. Surprisingly, ANP-230 was shown to block three pain-related subtypes, human Nav1.7, Nav1.8, and Nav1.9 with similar potency, but had only low inhibitory activity to human cardiac Nav1.5 channel and rat central Nav channels. The voltage clamp experiments using different step pulse protocols revealed that ANP-230 had a "tonic block" mode of action without state- and use-dependency. In addition, ANP-230 caused a depolarizing shift of the activation curve and decelerated gating kinetics in human Nav1.7-stably expressing cells. The depolarizing shift of activation curve was commonly observed in human Nav1.8-stably expressing cells as well as rat dorsal root ganglion neurons. These data suggested a quite unique mechanism of Nav channel inhibition by ANP-230. Finally, ANP-230 reduced excitability of rat dorsal root ganglion neurons in a concentration dependent manner. Collectively, these promising results indicate that ANP-230 could be a potent drug for neuropathic pain.

01 Apr 2023·Heliyon

Reduced pain sensitivity of episodic pain syndrome model mice carrying a Nav1.9 mutation by ANP-230, a novel sodium channel blocker

Article

Author: Okuda, Hiroko ; Oyamada, Yoshihiro ; Inoue, Sumiko ; Youssefian, Shohab ; Koizumi, Akio

The sodium channel Nav1.9 is expressed in the sensory neurons of small diameter dorsal root ganglia that transmit pain signals, and gain-of-function Nav1.9 mutations have been associated with both painful and painless disorders. We initially determined that some Nav1.9 mutations are responsible for familial episodic pain syndrome observed in the Japanese population. We therefore generated model mice harboring one of the more painful Japanese mutations, R222S, and determined that dorsal root ganglia hyperexcitability was the cause of the associated pain. ANP-230 is a novel non-opioid drug with strong inhibitory effects on Nav1.7, 1.8 and 1.9, and is currently under clinical trials for patients suffering from familial episodic pain syndrome. However, little is known about its mechanism of action and effects on pain sensitivity. In this study, we therefore investigated the inhibitory effects of ANP-230 on the hypersensitivity of Nav1.9 p.R222S mutant model mouse to pain. In behavioral tests, ANP-230 reduced the pain response of the mice, particularly to heat or mechanical stimuli, in a concentration- and time-dependent manner. Furthermore, ANP-230 suppressed the repetitive firing of dorsal root ganglion neurons of these mutant mice. Our results clearly demonstrate that ANP-230 is an effective analgesic for familial episodic pain syndrome resulting from DRG neuron hyperexcitability, and that such analgesic effects are likely to be of clinical significance.

100 Deals associated with DSP-2230

External Link

KEGG	Wiki	ATC	Drug Bank
-	DSP-2230	-	-

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Pain	Phase 2	JP	Alphanavi Pharma KKStartup	30 Dec 2020
Neuralgia	Phase 2	GB	Sumitomo Pharma Co., Ltd.	-
Neuralgia	Phase 2	JP	Sumitomo Pharma Co., Ltd.	-
Neuralgia	Phase 2	US	Sumitomo Pharma Co., Ltd.	-

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