Ralfinamide (
INN
Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway. Before the advent of motorized transportation, they also provided accomm ...
; development codes NW-1029, FCE-26742A, and PNU-0154339E) is a
multimodal drug
A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via insufflation (medicine), inhalation, drug i ...
which is under investigation by
Newron Pharmaceuticals for the treatment of
neuropathic pain
Neuropathic pain is pain caused by a lesion or disease of the somatosensory nervous system. Neuropathic pain may be associated with abnormal sensations called dysesthesia or pain from normally non-painful stimuli (allodynia). It may have continuo ...
and other
pain conditions such as
post-operative dental pain
Toothaches, also known as dental pain or tooth pain,Segen JC. (2002). ''McGraw-Hill Concise Dictionary of Modern Medicine''. The McGraw-Hill Companies. is pain in the teeth or their supporting structures, caused by dental diseases or pain re ...
.
It has a relatively complex
pharmacology
Pharmacology is the science of drugs and medications, including a substance's origin, composition, pharmacokinetics, pharmacodynamics, therapeutic use, and toxicology. More specifically, it is the study of the interactions that occur betwee ...
, acting as a mixed
voltage-gated sodium channel
Voltage-gated sodium channels (VGSCs), also known as voltage-dependent sodium channels (VDSCs), are a group of voltage-gated ion channels found in the membrane of excitable cells (''e.g.'', muscle, glial cells, neurons, etc.) with a permeability t ...
blocker (including
Nav1.7),
N-type calcium channel
N-type calcium channels, also called Cav2.2 channels, are voltage gated calcium channels that are localized primarily on the nerve terminals and dendrites as well as neuroendocrine cells. The calcium N-channel consists of several subunits: the prim ...
blocker,
NMDA receptor antagonist
NMDA receptor antagonists are a class of drugs that work to receptor antagonist, antagonize, or inhibit the action of, the NMDA, ''N''-Methyl-D-aspartate receptor (NMDA receptor, NMDAR). They are commonly used as anesthetics for humans and anima ...
,
and
monoamine oxidase B inhibitor
Inhibitor or inhibition may refer to:
Biology
* Enzyme inhibitor, a substance that binds to an enzyme and decreases the enzyme's activity
* Reuptake inhibitor, a substance that increases neurotransmission by blocking the reuptake of a neurotransmi ...
.
As of 2020, it was in
phase III clinical trial
Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel v ...
s.
In 2010 it failed a phase II trial for lower back pain. Encouraging Phase II results have been announced for neuropathic pain.
See also
*
List of investigational analgesics
This is a list of investigational analgesics, or analgesics that are currently under development for clinical use but are not yet approved. ''Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in par ...
*
Safinamide
Safinamide, sold under the brand name Xadago, is a medication used as treatment for Parkinson's disease with "off" episodes; it has multiple modes of action, including the inhibition of monoamine oxidase B. SeFDA index page for NDA 207145for ...
, different fluorine position
*
Evenamide, structurally-related antipsychotic in development
*
Lacosamide, used for partial-onset seizures and diabetic neuropathic pain
*
Ziconotide
Ziconotide, sold under the brand name Prialt, also called intrathecal ziconotide (ITZ) because of its administration route, is an atypical analgesic agent for the amelioration of severe and chronic pain. Derived from '' Conus magus'', a cone sn ...
,
FDA
The United States Food and Drug Administration (FDA or US FDA) is a federal agency of the Department of Health and Human Services. The FDA is responsible for protecting and promoting public health through the control and supervision of food ...
approved
peptide
Peptides are short chains of amino acids linked by peptide bonds. A polypeptide is a longer, continuous, unbranched peptide chain. Polypeptides that have a molecular mass of 10,000 Da or more are called proteins. Chains of fewer than twenty am ...
for chronic neuropathic pain
References
External links
Ralfinamide - Newron Pharmaceuticals
{{Glutamatergics
Carboxamides
Analgesics
Calcium channel blockers
Monoamine oxidase inhibitors
NMDA receptor antagonists
2-Fluorophenyl compounds
Sodium channel blockers
Experimental drugs