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Details

Stereochemistry ACHIRAL
Molecular Formula C21H20FN3O4
Molecular Weight 397.3996
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of RADIPRODIL

SMILES

FC1=CC=C(CC2CCN(CC2)C(=O)C(=O)NC3=CC=C4NC(=O)OC4=C3)C=C1

InChI

InChIKey=GKGRZLGAQZPEHO-UHFFFAOYSA-N
InChI=1S/C21H20FN3O4/c22-15-3-1-13(2-4-15)11-14-7-9-25(10-8-14)20(27)19(26)23-16-5-6-17-18(12-16)29-21(28)24-17/h1-6,12,14H,7-11H2,(H,23,26)(H,24,28)

HIDE SMILES / InChI

Description

RGH-896 (radiprodi) is orally active and selective NMDA NR2B antagonist, a potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions. It blocks pain signaling without interacting with other NMDA receptor subtypes thus potentially improving therapeutic index and side effect profile. RGH-896 is the first of this group and is currently in early clinical development. Forest and Richter initiated a Phase IIb study in neuropathic pain in the United Stated in the second half of 2006. The drug did not produce significant reductions in patient-reported pain scores for all the dosages tested. Forest says that it and Gedeon Richter will review the findings before making a decision about the further development of radiprodil. In addition to neuropathic pain, the companies intend to investigate various other pain conditions and possibly CNS indications not related to pain. Forest will pay Richter undisclosed upfront and milestone payments in addition to royalties and will have exclusive rights in the U.S. and Canada. The two companies will jointly fund the development program. RGH-896 has patent applications that provide patent protection until at least 2022.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
89.4 ng/mL
30 mg single, oral
RADIPRODIL plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
2042 ng × h/mL
30 mg single, oral
RADIPRODIL plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
15.8 h
30 mg single, oral
RADIPRODIL plasma
Homo sapiens

Doses

PubMed

Sample Use Guides

In Vivo Use Guide
45 mg capsules three times a day, 14 weeks
Route of Administration: Oral
In Vitro Use Guide
Unknown