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 accommo ...
) (code names NW-1029, FCE-26742A, PNU-0154339E) is a
multimodal drug which is under investigation by
Newron Pharmaceuticals for the treatment of
neuropathic pain
Neuropathic pain is pain caused by damage or disease affecting the somatosensory system. Neuropathic pain may be associated with abnormal sensations called dysesthesia or pain from normally non-painful stimuli (allodynia). It may have continuous ...
and other
pain conditions such as
post-operative dental pain
Toothache, also known as dental 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 referred to the te ...
.
It has a relatively complex
pharmacology, acting as a mixed
voltage-gated sodium channel
Sodium channels are integral membrane proteins that form ion channels, conducting sodium ions (Na+) through a cell's membrane. They belong to the superfamily of cation channels and can be classified according to the trigger that opens the channel ...
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 prima ...
blocker,
NMDA receptor antagonist
NMDA receptor antagonists are a class of drugs that work to antagonize, or inhibit the action of, the ''N''-Methyl-D-aspartate receptor ( NMDAR). They are commonly used as anesthetics for animals and humans; the state of anesthesia they induce ...
,
and
monoamine oxidase B
Monoamine oxidase B, also known as MAOB, is an enzyme that in humans is encoded by the ''MAOB'' gene.
The protein encoded by this gene belongs to the flavin monoamine oxidase family. It is an enzyme located in the outer mitochondrial membrane. I ...
inhibitor.
It has thus far progressed as far as
phase IIb
The phases of clinical research are the stages in which scientists conduct experiments with a health intervention to obtain sufficient evidence for a process considered effective as a medical treatment. For drug development, the clinical phases ...
/
phase III clinical trial
Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, diet ...
s.
In 2010 it failed a phase II trial for lower back pain. Encouraging Phase II results have been announced for neuropathic pain.
Newron Announces Positive Results With Ralfinamide From Phase II Trial in Neuropathic Pain
/ref>
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 pare ...
* Safinamide, different fluorine position
* Evenamide, structurally-related antipsychotic in development
* Lacosamide
Lacosamide, sold under the brand name Vimpat among others, is a medication used for the treatment of partial-onset seizures and primary generalized tonic-clonic seizures. It is used by mouth or intravenously.
It is available as a generic medic ...
, used for partial-onset seizures and diabetic neuropathic pain
* Ziconotide
Ziconotide (SNX–111; 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 snail, it is the ...
, 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. Long chains of amino acids are called proteins. Chains of fewer than twenty amino acids are called oligopeptides, and include dipeptides, tripeptides, and tetrapeptides.
...
for chronic neuropathic pain
References
External links
Ralfinamide - Newron Pharmaceuticals
Carboxamides
Analgesics
Calcium channel blockers
Monoamine oxidase inhibitors
NMDA receptor antagonists
Fluoroarenes
Sodium channel blockers
Experimental drugs
{{analgesic-stub