This is a list of investigational

analgesic An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It ...

s, 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 parentheses.''

Opioid receptor modulators

* Axelopran/oxycodone – combination of a centrally active

μ-opioid receptor The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins. They are also referred to as μ(''mu'')-opioid peptide (MOP) receptors. The prototypical � ...

agonist and a

peripherally selective Peripherally selective drugs have their primary mechanism of action outside of the central nervous system (CNS), usually because they are excluded from the CNS by the blood–brain barrier. By being excluded from the CNS, drugs may act on the rest ...

μ-, κ-, and

δ-opioid receptor The δ-opioid receptor, also known as delta opioid receptor or simply delta receptor, abbreviated DOR or DOP, is an inhibitory 7-transmembrane G-protein coupled receptor coupled to the G protein Gi/G0 and has enkephalins as its endogenous lig ...

antagonist An antagonist is a character in a story who is presented as the chief foe of the protagonist. Etymology The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...

. *

Cebranopadol Cebranopadol (developmental code GRT-6005) is an opioid analgesic of the benzenoid class which is currently under development internationally by Grünenthal, a Germany, German pharmaceutical company, and its partner Depomed, a pharmaceutical comp ...

(GRT-6005) – non-selective μ-opioid receptor,

nociceptin receptor The nociceptin opioid peptide receptor (NOP), also known as the nociceptin/orphanin FQ (N/OFQ) receptor or kappa-type 3 opioid receptor, is a protein that in humans is encoded by the ''OPRL1'' (opioid receptor-like 1) gene. The nociceptin receptor ...

, and δ-opioid receptor

full agonist An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ago ...

and

κ-opioid receptor The κ-opioid receptor or kappa opioid receptor, abbreviated KOR or KOP, is a G protein-coupled receptor that in humans is encoded by the ''OPRK1'' gene. The KOR is coupled to the G protein Gi/G0 and is one of four related receptors that bind op ...

partial agonist In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic e ...

Desmetramadol Desmetramadol (), also known as ''O''-desmethyltramadol (''O''-DSMT), is an opioid analgesic and the main active metabolite of tramadol. Tramadol is demethylated by the liver enzyme CYP2D6 in the same way as codeine, and so similarly to the var ...

(''O''-desmethyltramadol; Omnitram) –

agonist,

norepinephrine reuptake inhibitor A norepinephrine reuptake inhibitor (NRI, NERI) or noradrenaline reuptake inhibitor or adrenergic reuptake inhibitor (ARI), is a type of drug that acts as a reuptake inhibitor for the neurotransmitters norepinephrine (noradrenaline) and epineph ...

(NRI), and 5-HT_2C receptor antagonist. * Lexanopadol (GRT-6006, GRT13106G) – non-selective

opioid receptor Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin. The opioid receptors are ~40% identical to somatostatin ...

agonist * Oxycodone/naltrexone – combination of a μ-opioid receptor agonist and a μ- and κ-opioid receptor antagonist.

Sodium channel blockers

* BIIB-095 – state-dependent and use-dependent Na_v blocker, including Na_v1.7. * CC-8464 (ASP-1807) – selective Na_v1.7 blocker * Cenobamate (YKP-3089) – atypical voltage-gated sodium channel blocker. *

DSP-2230 DSP-2230 is a selective small-molecule Nav1.7 and Nav1.8 voltage-gated sodium channel blocker which is under development by Dainippon Sumitomo Pharma for the treatment of neuropathic pain. As of June 2014, it is in phase I/ phase II clinical ...

– selective Na_v1.7 and Na_v1.8 blocker. *

Funapide Funapide ( INN) (former developmental code names TV-45070 and XEN402) is a novel analgesic under development by Xenon Pharmaceuticals (formerly in partnership with Teva Pharmaceutical Industries) for the treatment of a variety of chronic pain co ...

(TV-45070, XEN402) – selective Na_v1.7 and Na_v1.8 blocker. * GDC-0276 (RG-7893) – selective Na_v1.7 blocke

* GDC-0310 (RG-6029) – selective Na_v1.7 blocke

* NKTR-171 – voltage-gated sodium channel blocke

*

PF-05089771 PF-05089771 is a selective, small-molecule Nav1.7 and Nav1.8 voltage-gated sodium channel blocker under development by Pfizer as a novel analgesic. As of June 2014, it has completed phase II clinical trials for wisdom tooth removal and prim ...

– selective Na_v1.7 and Na_v1.8 blocke

*

Ralfinamide Ralfinamide (INN) (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 and other pain conditions such as post-operative dental pain. ...

(NW-1029) – non-selective

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, as well as other action

*

Tetrodotoxin Tetrodotoxin (TTX) is a potent neurotoxin. Its name derives from Tetraodontiformes, an order that includes pufferfish, porcupinefish, ocean sunfish, and triggerfish; several of these species carry the toxin. Although tetrodotoxin was discovered ...

(9401-TTX; Tectin, Tetrodin, Tocudin) – non-selective voltage-gated sodium channel blocke

*

Vixotrigine Vixotrigine (, ), formerly known as raxatrigine (, ), is an analgesic which is under development by Convergence Pharmaceuticals for the treatment of lumbosacral radiculopathy (sciatica) and trigeminal neuralgia (TGN). Vixotrigine was originally c ...

(formerly raxatrigine; CNV1014802, GSK-1014802, BIIB 074) – non-selective voltage-gated sodium channel blocke

* VX-150 – selective Na_v1.8 blocke

* VX-548 – selective Na_v1.8 blocker

Calcium channel blockers

* HSK16149 – selective ligand of α2δ subunit of voltage-gated calcium channe

channel modulators

Capsaicin Capsaicin (8-methyl-''N''-vanillyl-6-nonenamide) ( or ) is an active component of chili peppers, which are plants belonging to the genus ''Capsicum''. It is a chemical irritant for mammals, including humans, and produces a sensation of burning ...

(Adlea, ALGRX-4975, CNTX-4975, VLNX-4975) –

TRPV1 The transient receptor potential cation channel subfamily V member 1 (TrpV1), also known as the capsaicin receptor and the vanilloid receptor 1, is a protein that, in humans, is encoded by the ''TRPV1'' gene. It was the first isolated member of th ...

agonis

* Capsaicin/diclofenac – combination of a TRPV1 agonist and a

COX-2 inhibitor COX-2 inhibitors are a type of nonsteroidal anti-inflammatory drug (NSAID) that directly targets cyclooxygenase-2, COX-2, an enzyme responsible for inflammation and pain. Targeting selectivity for COX-2 reduces the risk of peptic ulceration and i ...

for topical applicatio

* CMX-020 – TRPV1

modulator In electronics and telecommunications, modulation is the process of varying one or more properties of a periodic waveform, called the ''carrier signal'', with a separate signal called the ''modulation signal'' that typically contains informatio ...

as well as CB₁ and CB₂ receptor modulato

* DWP-05195 (TR-1) – TRPV1 antagonis

* GRC-6211 – TRPV1 agonis

* JNJ-38893777 – TRPV1 antagonis

* Mavatrep (JNJ‐39439335) – TRPV1 antagonist. * NEO-6860 – TRPV1 antagonis

* Parentide (DD-04107) – TRPV1 antagonis

*

Resiniferatoxin Resiniferatoxin (RTX) is a naturally occurring chemical found in resin spurge (''Euphorbia resinifera''), a cactus-like plant commonly found in Morocco, and in '' Euphorbia poissonii'' found in northern Nigeria.

(RTX; MCP-101) – TRPV1 agonis

* SAR-115740 – TRPV1 antagonis

* Tivanisiran (SYL-1001) – TRPV1 antagonis

Cannabinoid receptor modulators

* ABX-1431 – selective

monoacylglycerol lipase Monoacylglycerol lipase (EC 3.1.1.23; systematic name glycerol-ester acylhydrolase, also known as MAG lipase, acylglycerol lipase, MAGL, MGL or MGLL) is an enzyme that, in humans, is encoded by the ''MGLL'' gene. MAGL is a 33-kDa, membrane-associ ...

inhibitor

*

Cannabidiol Cannabidiol (CBD) is a phytocannabinoid discovered in 1940. It is one of 113 identified cannabinoids in cannabis plants, along with tetrahydrocannabinol (THC), and accounts for up to 40% of the plant's extract. , clinical research on CBD incl ...

(CBD) –

cannabinoid receptor Cannabinoid receptors, located throughout the body, are part of the endocannabinoid system a class of cell membrane receptors in the G protein-coupled receptor superfamily. As is typical of G protein-coupled receptors, the cannabinoid recepto ...

modulato

http://adisinsight.springer.com/drugs/800045903] *

Cannabidivarin Cannabidivarin (CBDV, GWP42006) is a non-psychoactive cannabinoid found in ''Cannabis''. It is a homolog (chemistry) of cannabidiol (CBD), with the side-chain shortened by two methylene bridges (CH2 units). Although cannabidivarin (CBDV) is us ...

(CBDV; GWP-42006) – cannabinoid receptor modulato

* CMX-020 – TRPV1 modulator as well as CB₁ and CB₂ receptor modulato

*

Dronabinol The International Nonproprietary Name Dronabinol, also known as delta-9-tetrahydrocannabinol, or under the trade names Marinol, Syndros, Reduvo and Adversa, is a generic name for the molecule of delta-9-tetrahydrocannabinol in the pharmaceutica ...

(Δ⁹-; ECP022A, Namisol) – CB₁ and CB₂ receptor agonis

http://adisinsight.springer.com/drugs/800027102] *

Nabilone Nabilone, sold under the brand name Cesamet among others, is a synthetic cannabinoid with therapeutic use as an antiemetic and as an adjunct analgesic for neuropathic pain. It mimics tetrahydrocannabinol (THC), the primary psychoactive compound ...

– CB₁ and CB₂ receptor agonis

* NEO-1940 – CB₁ and CB₂ receptor agonis

* Olorinab (APD-371) – CB₂ receptor agonis

Nerve growth factor inhibitors

Fasinumab Fasinumab is a human monoclonal antibody designed for the treatment of acute sciatic pain. This drug was developed in collaboration by Teva Pharmaceutical Industries and Regeneron Pharmaceuticals. It is currently at Phase III trials (NCT03245008 ...

(REGN-475, SAR-164877) – monoclonal antibody against nerve growth factor

* Frunevetmab (NV-02) – monoclonal antibody against nerve growth factor for cat

*

Fulranumab Fulranumab is a monoclonal antibody against nerve growth factor. It was designed for the treatment of pain. Johnson & Johnson licensed the drug from Amgen in a deal valued at around US$425 million in 2008. In 2016 Johnson & Johnson discontin ...

(AMG-403, JNJ-42160443) – monoclonal antibody against nerve growth facto

* GBR-900 –

monoclonal antibody A monoclonal antibody (mAb, more rarely called moAb) is an antibody produced from a cell Lineage made by cloning a unique white blood cell. All subsequent antibodies derived this way trace back to a unique parent cell. Monoclonal antibodies ca ...

against TrkA

* GZ-389988 – TrkA,

TrkB Tropomyosin receptor kinase B (TrkB), also known as tyrosine receptor kinase B, or BDNF/NT-3 growth factors receptor or neurotrophic tyrosine kinase, receptor, type 2 is a protein that in humans is encoded by the ''NTRK2'' gene. TrkB is a recepto ...

, and

TrkC Tropomyosin receptor kinase C (TrkC), also known as NT-3 growth factor receptor, neurotrophic tyrosine kinase receptor type 3, or TrkC tyrosine kinase is a protein that in humans is encoded by the ''NTRK3'' gene. TrkC is the high affinity catalyt ...

kinase inhibitor

* LEVI-04 (p75^NTR-Fc) – LNGF receptor (p75^NTR)

fusion protein Fusion proteins or chimeric (kī-ˈmir-ik) proteins (literally, made of parts from different sources) are proteins created through the joining of two or more genes that originally coded for separate proteins. Translation of this ''fusion gene'' r ...

and

decoy receptor A decoy receptor is a receptor that is able to recognize and bind specific growth factors or cytokines efficiently, but is not structurally able to signal or activate the intended receptor complex. It acts as an inhibitor, binding a ligand and keep ...

for nerve growth facto

* NRD135S-E1 – tyrosine kinase modulator

http://www.novaremed.com/index.php/technology-pipeline] * ONO-4474 – peripherally selective TrkA,

, and

kinase inhibitor

* Ranevetmab (NV-01) – monoclonal antibody against nerve growth factor for dog

*

Tanezumab Tanezumab (INN, codenamed RN624) is a monoclonal antibody against nerve growth factor as a treatment for pain via a novel mechanisms different from conventional pain-killer drugs. Tanezumab was discovered and developed by Rinat Neuroscience and ...

(PF-4383119, RI-624, RN-624) – monoclonal antibody against nerve growth facto

* VM-902A – selective, peripherally selective allosteric inhibitor of Trk

Others

* ALLOD-2 – undefined mechanism of actio

*

CR-4056 CR-4056 is an analgesic drug candidate with a novel mechanism of action, acting as a ligand for the imidazoline receptor I2. It showed promising results in animal studies against various types of neuropathic pain, and has reached Phase II human c ...

– imidazoline I₂ receptor agonis

* E-52862 (MR-309; S1A; S1RA) –

sigma-1 receptor The sigma-1 receptor (σ1R), one of two sigma receptor subtypes, is a chaperone protein at the endoplasmic reticulum (ER) that modulates calcium signaling through the IP3 receptor. In humans, the σ1 receptor is encoded by the ''SIGMAR1'' gene. ...

antagonis

* HSP-3150 – undefined mechanism of actio

* KCP-506 –

nicotinic acetylcholine receptor Nicotinic acetylcholine receptors, or nAChRs, are receptor polypeptides that respond to the neurotransmitter acetylcholine. Nicotinic receptors also respond to drugs such as the agonist nicotine. They are found in the central and peripheral ne ...

antagonis

*

LATER Later may refer to: * Future, the time after the present Television * ''Later'' (talk show), a 1988–2001 American talk show * '' Later... with Jools Holland'', a British music programme since 1992 * ''The Life and Times of Eddie Roberts'', or ...

– CRISPR-dCas9 gene-editing * PAX-01 – undefined mechanism of actio

References

External links

AdisInsight - Springer
{{Neuropathic pain and fibromyalgia pharmacotherapies Analgesics Analgesics, investigational Experimental drugs