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 o ...

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, ri ...

. * Cebranopadol (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 a ...

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 ...

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 antagonis ...

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 varia ...

(''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 ep ...

(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 – selective Na_v1.7 and Na_v1.8 blocker. * Funapide (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 – selective Na_v1.7 and Na_v1.8 blocke

* Ralfinamide (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 discovere ...

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

* Vixotrigine (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 burnin ...

(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 in ...

(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 recep ...

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 pharmaceutic ...

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

http://adisinsight.springer.com/drugs/800027102] * Nabilone – CB₁ and CB₂ receptor agonis

* NEO-1940 – CB₁ and CB₂ receptor agonis

* Olorinab (APD-371) – CB₂ receptor agonis

Nerve growth factor inhibitors

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

*

Frunevetmab Frunevetmab, sold under the brand name Solensia, is a medication used to treat pain associated with osteoarthritis in cats. It is the first monoclonal antibody new animal drug approved by the U.S. Food and Drug Administration (FDA) for use in ...

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

* Fulranumab (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 ...

against TrkA

* GZ-389988 – TrkA, TrkB, 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'' ...

and decoy receptor for nerve growth facto

* NRD135S-E1 – tyrosine kinase modulator

http://www.novaremed.com/index.php/technology-pipeline] * ONO-4474 – peripherally selective TrkA, TrkB, 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 In biochemistry, allosteric regulation (or allosteric control) is the regulation of an enzyme by binding an effector molecule at a site other than the enzyme's active site. The site to which the effector binds is termed the ''allosteric site ...

of Trk

Others

* ALLOD-2 – undefined mechanism of actio

* CR-4056 – 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'' gen ...

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 ner ...

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