Delving into the Latest Updates on PF-05020182 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

Mechanism

KCNQ5 modulators(KCNQ voltage-gated potassium channel-5 modulators), Kv7.2 modulators(Voltage-gated potassium channel subunit Kv7.2 modulators), Kv7.3 modulators(KCNQ voltage-gated potassium channel-3 modulators)

+ [1]

Therapeutic Areas

Nervous System Diseases

Active Indication-

Inactive Indication

Epilepsy

Originator Organization

Pfizer Inc.

Active Organization-

Inactive Organization

Pfizer Inc.

Drug Highest PhasePendingDiscovery

First Approval Date-

Regulation-

Author: Serpa, Kevin A ; Arora, Gaurav ; Rogers, Bruce N ; Stolyar, Polina ; Baker, Karen ; Claffey, Michelle M ; Duplantier, Allen J ; Wright, Ann S ; Butler, Christopher R ; Boscoe, Brian P ; Rong, SuoBao ; Reese, Matthew R ; DeNinno, Shari L ; Tse, Karen ; Snow, Sheri L ; Zhang, Lei ; Drozda, Susan E ; Schuyten, Katherine ; Moine, Ludivine ; Clark, Alan J ; Whisman, Tammy L ; Weber, Mark L ; Rong, Haojing ; Lowe, John A ; Mather, Robert J ; Davoren, Jennifer E ; Chenard, Lois

Facilitating activation, or delaying inactivation, of the native Kv7 channel reduces neuronal excitability, which may be beneficial in controlling spontaneous electrical activity during epileptic seizures. In an effort to identify a compound with such properties, the structure-activity relationship (SAR) and in vitro ADME for a series of heterocyclic Kv7.2-7.5 channel openers was explored. PF-05020182 (2) demonstrated suitable properties for further testing in vivo where it dose-dependently decreased the number of animals exhibiting full tonic extension convulsions in response to corneal stimulation in the maximal electroshock (MES) assay. In addition, PF-05020182 (2) significantly inhibited convulsions in the MES assay at doses tested, consistent with in vitro activity measure. The physiochemical properties, in vitro and in vivo activities of PF-05020182 (2) support further development as an adjunctive treatment of refractory epilepsy.

100 Deals associated with PF-05020182

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