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
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. 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-548 – selective Nav1.8 blocker
Calcium channel blockers
HSK16149 – selective ligand of α2δ subunit of voltage-gated calcium channel
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
ABX-1431 – selective monoacylglycerol lipase inhibitor
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-; ECP022A, Namisol) – CB1 and CB2 receptor agonist
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