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 It is likely to become outdated with time.
Opioid receptor modulators Axelopran/oxycodone – combination of a centrally active μ-opioid receptor agonist and a peripherally selective μ-, κ-, and δ-opioid receptor antagonist. Cebranopadol (GRT-6005) – non-selective μ-opioid receptor, nociceptin receptor, and δ-opioid receptor full agonist and κ-opioid receptor partial agonist Desmetramadol (O-desmethyltramadol; Omnitram) – μ-opioid receptor agonist, norepinephrine reuptake inhibitor (NRI), and 5-HT2C receptor antagonist. Deumitragynine (KUR-101) – atypical μ-opioid receptor agonist related to mitragynine (found in kratom) Lexanopadol (GRT-6006, GRT13106G) – non-selective opioid receptor 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 Nav blocker, including Nav1.7. CC-8464 (ASP-1807) – selective Nav1.7 blocker Cenobamate (YKP-3089) – atypical voltage-gated sodium channel blocker. DSP-2230 – selective Nav1.7 and Nav1.8 blocker. Funapide (TV-45070, XEN402) – selective Nav1.7 and Nav1.8 blocker. GDC-0276 (RG-7893) – selective Nav1.7 blocker GDC-0310 (RG-6029) – selective Nav1.7 blocker NKTR-171 – voltage-gated sodium channel blocker PF-05089771 – selective Nav1.7 and Nav1.8 blocker Ralfinamide (NW-1029) – non-selective voltage-gated sodium channel blocker, as well as other actions Tetrodotoxin (9401-TTX; Tectin, Tetrodin, Tocudin) – non-selective voltage-gated sodium channel blocker Vixotrigine (formerly raxatrigine; CNV1014802, GSK-1014802, BIIB 074) – non-selective voltage-gated sodium channel blocker VX-150 – selective Nav1.8 blocker VX-993
Calcium channel blockers HSK16149 – selective ligand of α2δ subunit of voltage-gated calcium channel
TRP channel modulators Capsaicin (Adlea, ALGRX-4975, CNTX-4975, VLNX-4975) – TRPV1 agonist Capsaicin/diclofenac – combination of a TRPV1 agonist and a COX-2 inhibitor for topical application CMX-020 – TRPV1 modulator as well as CB1 and CB2 receptor modulator DWP-05195 (TR-1) – TRPV1 antagonist GRC-6211 – TRPV1 agonist JNJ-38893777 – TRPV1 antagonist Mavatrep (JNJ‐39439335) – TRPV1 antagonist. NEO-6860 – TRPV1 antagonist Parentide (DD-04107) – TRPV1 antagonist Resiniferatoxin (RTX; MCP-101) – TRPV1 agonist SAR-115740 – TRPV1 antagonist Tivanisiran (SYL-1001) – TRPV1 antagonist
Cannabinoid receptor modulators Cannabidiol (CBD) – cannabinoid receptor modulator Cannabidivarin (CBDV; GWP-42006) – cannabinoid receptor modulator CMX-020 – TRPV1 modulator as well as CB1 and CB2 receptor modulator Dronabinol (Δ9-THC; ECP022A, Namisol) – CB1 and CB2 receptor agonist Elcubragistat (ABX-1431; Lu-AG06466) – selective monoacylglycerol lipase (MAGL) inhibitor Nabilone – CB1 and CB2 receptor agonist NEO-1940 – CB1 and CB2 receptor agonist Olorinab (APD-371) – CB2 receptor agonist
Nerve growth factor inhibitors Fasinumab (REGN-475, SAR-164877) – monoclonal antibody against nerve growth factor Fulranumab (AMG-403, JNJ-42160443) – monoclonal antibody against nerve growth factor GBR-900 – monoclonal antibody against TrkA GZ-389988 – TrkA, TrkB, and TrkC kinase inhibitor LEVI-04 (p75NTR-Fc) – LNGF receptor (p75NTR) fusion protein and decoy receptor for nerve growth factor NRD135S-E1 – tyrosine kinase modulator ONO-4474 – peripherally selective TrkA, TrkB, and TrkC kinase inhibitor Ranevetmab (NV-01) – monoclonal antibody against nerve growth factor for dogs Tanezumab (PF-4383119, RI-624, RN-624) – monoclonal antibody against nerve growth factor VM-902A – selective, peripherally selective allosteric inhibitor of TrkA
Others ALLOD-2 – undefined mechanism of action CM-304 – sigma-1 receptor antagonist. Cold version of radiotracer [18F] FTC-146 CR-4056 – imidazoline I2 receptor agonist E-52862 (MR-309; S1A; S1RA) – sigma-1 receptor antagonist HSP-3150 – undefined mechanism of action KCP-506 – nicotinic acetylcholine receptor antagonist KNX-101 – 15-lipoxygenase (15-LOX; ALOX15) inhibitor LATER – CRISPR-dCas9 gene-editing PAX-01 – undefined mechanism of action Opiranserin - Dual 5HT2A Receptor antagonist and GlyT2 inhibitor
See also List of investigational drugs
References
External links AdisInsight - Springer
