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 parentheses.

Opioid receptor modulators[]

• – combination of a centrally active μ-opioid receptor agonist and a peripherally selective μ-, κ-, and δ-opioid receptor antagonist[1]
• Cebranopadol (GRT-6005) – non-selective μ-opioid receptor, nociceptin receptor, and δ-opioid receptor full agonist and κ-opioid receptor partial agonist[2]
• Desmetramadol (O-desmethyltramadol; Omnitram) – μ-opioid receptor agonist, norepinephrine reuptake inhibitor (NRI), and 5-HT_2C receptor antagonist [3]
• (GRT-6006, GRT13106G) – non-selective opioid receptor agonist [4]
• – combination of a μ-opioid receptor agonist and a μ- and κ-opioid receptor antagonist [5]

Sodium channel blockers[]

• – state-dependent and use-dependent Na_v blocker, including Na_v1.7[6]
• (ASP-1807) – selective Na_v1.7 blocker[7]
• Cenobamate (YKP-3089) – atypical voltage-gated sodium channel blocker [8]^[1][2]
• DSP-2230 – selective Na_v1.7 and Na_v1.8 blocker [9]
• Funapide (TV-45070, XEN402) – selective Na_v1.7 and Na_v1.8 blocker [10]
• (RG-7893) – selective Na_v1.7 blocker [11]
• (RG-6029) – selective Na_v1.7 blocker [12]
• – voltage-gated sodium channel blocker [13]
• PF-05089771 – selective Na_v1.7 and Na_v1.8 blocker [14]
• Ralfinamide (NW-1029) – non-selective voltage-gated sodium channel blocker, as well as other actions [15]
• Tetrodotoxin (9401-TTX; Tectin, Tetrodin, Tocudin) – non-selective voltage-gated sodium channel blocker [16]
• Vixotrigine (formerly raxatrigine; CNV1014802, GSK-1014802, BIIB 074) – non-selective voltage-gated sodium channel blocker [17]^{[citation needed]}
• – selective Na_v1.8 blocker [18]

Calcium channel blockers[]

• – selective ligand of α2δ subunit of voltage-gated calcium channel [19]

TRP channel modulators[]

• Capsaicin (Adlea, ALGRX-4975, CNTX-4975, VLNX-4975) – TRPV1 agonist [20]
• – combination of a TRPV1 agonist and a COX-2 inhibitor for topical application [21]
• – TRPV1 modulator as well as CB₁ and CB₂ receptor modulator [22]
• (TR-1) – TRPV1 antagonist [23]
• GRC-6211 – TRPV1 agonist [24]
• – TRPV1 antagonist [25]
• Mavatrep (JNJ‐39439335) – TRPV1 antagonist ^[3][4]
• – TRPV1 antagonist [26]
• (DD-04107) – TRPV1 antagonist [27]
• Resiniferatoxin (RTX; MCP-101) – TRPV1 agonist [28]
• – TRPV1 antagonist [29]
• (SYL-1001) – TRPV1 antagonist [30]

Cannabinoid receptor modulators[]

• – selective monoacylglycerol lipase inhibitor[31]
• Cannabidiol (CBD) – cannabinoid receptor modulator [32][33]
• Cannabidivarin (CBDV; GWP-42006) – cannabinoid receptor modulator [34]
• – TRPV1 modulator as well as CB₁ and CB₂ receptor modulator [35]
• Dronabinol (Δ⁹-THC; ECP022A, Namisol) – CB₁ and CB₂ receptor agonist [36][37]
• Nabilone – CB₁ and CB₂ receptor agonist [38]
• – CB₁ and CB₂ receptor agonist [39]
• Olorinab (APD-371) – CB₂ receptor agonist [40]

Nerve growth factor inhibitors[]

• Fasinumab (REGN-475, SAR-164877) – monoclonal antibody against nerve growth factor[41]
• (NV-02) – monoclonal antibody against nerve growth factor for cats [42]
• Fulranumab (AMG-403, JNJ-42160443) – monoclonal antibody against nerve growth factor [43]
• – monoclonal antibody against TrkA[44]
• – TrkA, TrkB, and TrkC kinase inhibitor[45]
• (p75^NTR-Fc) – LNGF receptor (p75^NTR) fusion protein and decoy receptor for nerve growth factor [46]
• – tyrosine kinase modulator[47][48]
• – peripherally selective TrkA, TrkB, and TrkC kinase inhibitor[49]
• (NV-01) – monoclonal antibody against nerve growth factor for dogs [50]
• Tanezumab (PF-4383119, RI-624, RN-624) – monoclonal antibody against nerve growth factor [51]
• – selective, peripherally selective allosteric inhibitor of TrkA [52]

Others[]

• – undefined mechanism of action [53]
• CR-4056 – imidazoline I₂ receptor agonist [54]
• E-52862 (MR-309; S1A; S1RA) – sigma-1 receptor antagonist [55]
• – undefined mechanism of action [56]
• – nicotinic acetylcholine receptor antagonist [57]
• – CRISPR-dCas9 gene-editing [58]
• – undefined mechanism of action [59]

See also[]

• List of investigational drugs

References[]

External links[]

• AdisInsight - Springer