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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.
This list was last comprehensively updated in June 2017. It is likely to become outdated with time.
- Axelopran/oxycodone – 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-HT2C receptor antagonist.[3]
- Lexanopadol (GRT-6006, GRT13106G) – non-selective opioid receptor agonist[4]
- Oxycodone/naltrexone – combination of a μ-opioid receptor agonist and a μ- and κ-opioid receptor antagonist.[5]
- BIIB-095 – state-dependent and use-dependent Nav blocker, including Nav1.7.[6]
- CC-8464 (ASP-1807) – selective Nav1.7 blocker[7]
- Cenobamate (YKP-3089) – atypical voltage-gated sodium channel blocker.[8][9]: 5593–5605 [10]
- DSP-2230 – selective Nav1.7 and Nav1.8 blocker.[11]
- Funapide (TV-45070, XEN402) – selective Nav1.7 and Nav1.8 blocker.[12]
- GDC-0276 (RG-7893) – selective Nav1.7 blocker [13]
- GDC-0310 (RG-6029) – selective Nav1.7 blocker [14]
- NKTR-171 – voltage-gated sodium channel blocker [15]
- PF-05089771 – selective Nav1.7 and Nav1.8 blocker [16]
- Ralfinamide (NW-1029) – non-selective voltage-gated sodium channel blocker, as well as other actions [17]
- Tetrodotoxin (9401-TTX; Tectin, Tetrodin, Tocudin) – non-selective voltage-gated sodium channel blocker [18]
- Vixotrigine (formerly raxatrigine; CNV1014802, GSK-1014802, BIIB 074) – non-selective voltage-gated sodium channel blocker [19][citation needed]
- VX-150 – selective Nav1.8 blocker [20]
- VX-548 – selective Nav1.8 blocker[21][22]
- Capsaicin (Adlea, ALGRX-4975, CNTX-4975, VLNX-4975) – TRPV1 agonist [24]
- Capsaicin/diclofenac – combination of a TRPV1 agonist and a COX-2 inhibitor for topical application [25]
- CMX-020 – TRPV1 modulator as well as CB1 and CB2 receptor modulator [26]
- DWP-05195 (TR-1) – TRPV1 antagonist [27]
- GRC-6211 – TRPV1 agonist [28]
- JNJ-38893777 – TRPV1 antagonist [29]
- Mavatrep (JNJ‐39439335) – TRPV1 antagonist.[30]: 712–726 [31]
- NEO-6860 – TRPV1 antagonist [32]
- Parentide (DD-04107) – TRPV1 antagonist [33]
- Resiniferatoxin (RTX; MCP-101) – TRPV1 agonist [34]
- SAR-115740 – TRPV1 antagonist [35]
- Tivanisiran (SYL-1001) – TRPV1 antagonist [36]
- ABX-1431 – selective monoacylglycerol lipase inhibitor[37]
- Cannabidiol (CBD) – cannabinoid receptor modulator [38][39]
- Cannabidivarin (CBDV; GWP-42006) – cannabinoid receptor modulator [40]
- CMX-020 – TRPV1 modulator as well as CB1 and CB2 receptor modulator [26]
- Dronabinol (Δ9-THC; ECP022A, Namisol) – CB1 and CB2 receptor agonist [41][42]
- Nabilone – CB1 and CB2 receptor agonist [43]
- NEO-1940 – CB1 and CB2 receptor agonist [44]
- Olorinab (APD-371) – CB2 receptor agonist [45]
- Fasinumab (REGN-475, SAR-164877) – monoclonal antibody against nerve growth factor[46]
- Fulranumab (AMG-403, JNJ-42160443) – monoclonal antibody against nerve growth factor [47]
- GBR-900 – monoclonal antibody against TrkA[48]
- GZ-389988 – TrkA, TrkB, and TrkC kinase inhibitor[49]
- LEVI-04 (p75NTR-Fc) – LNGF receptor (p75NTR) fusion protein and decoy receptor for nerve growth factor [50]
- NRD135S-E1 – tyrosine kinase modulator[51][52]
- ONO-4474 – peripherally selective TrkA, TrkB, and TrkC kinase inhibitor[53]
- Ranevetmab (NV-01) – monoclonal antibody against nerve growth factor for dogs [54]
- Tanezumab (PF-4383119, RI-624, RN-624) – monoclonal antibody against nerve growth factor [55]
- VM-902A – selective, peripherally selective allosteric inhibitor of TrkA [56]
- ALLOD-2 – undefined mechanism of action [57]
- CR-4056 – imidazoline I2 receptor agonist [58]
- E-52862 (MR-309; S1A; S1RA) – sigma-1 receptor antagonist [59]
- HSP-3150 – undefined mechanism of action [60]
- KCP-506 – nicotinic acetylcholine receptor antagonist [61]
- LATER – CRISPR-dCas9 gene-editing[62]
- PAX-01 – undefined mechanism of action [63]
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