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

• 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-HT_2C 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 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 blocker [1]
• GDC-0310 (RG-6029) – selective Na_v1.7 blocker [2]
• NKTR-171 – voltage-gated sodium channel blocker [3]
• PF-05089771 – selective Na_v1.7 and Na_v1.8 blocker [4]
• Ralfinamide (NW-1029) – non-selective voltage-gated sodium channel blocker, as well as other actions [5]
• Tetrodotoxin (9401-TTX; Tectin, Tetrodin, Tocudin) – non-selective voltage-gated sodium channel blocker [6]
• Vixotrigine (formerly raxatrigine; CNV1014802, GSK-1014802, BIIB 074) – non-selective voltage-gated sodium channel blocker [7]
• VX-150 – selective Na_v1.8 blocker [8]
• VX-548 – selective Na_v1.8 blocker

Calcium channel blockers

• HSK16149 – selective ligand of α2δ subunit of voltage-gated calcium channel [9]

TRP channel modulators

• Capsaicin (Adlea, ALGRX-4975, CNTX-4975, VLNX-4975) – TRPV1 agonist [10]
• Capsaicin/diclofenac – combination of a TRPV1 agonist and a COX-2 inhibitor for topical application [11]
• CMX-020 – TRPV1 modulator as well as CB₁ and CB₂ receptor modulator [12]
• DWP-05195 (TR-1) – TRPV1 antagonist [13]
• GRC-6211 – TRPV1 agonist [14]
• JNJ-38893777 – TRPV1 antagonist [15]
• Mavatrep (JNJ‐39439335) – TRPV1 antagonist.
• NEO-6860 – TRPV1 antagonist [16]
• Parentide (DD-04107) – TRPV1 antagonist [17]
• Resiniferatoxin (RTX; MCP-101) – TRPV1 agonist [18]
• SAR-115740 – TRPV1 antagonist [19]
• Tivanisiran (SYL-1001) – TRPV1 antagonist [20]

Cannabinoid receptor modulators

• ABX-1431 – selective monoacylglycerol lipase inhibitor[21]
• Cannabidiol (CBD) – cannabinoid receptor modulator [22][23]
• Cannabidivarin (CBDV; GWP-42006) – cannabinoid receptor modulator [24]
• CMX-020 – TRPV1 modulator as well as CB₁ and CB₂ receptor modulator [25]
• Dronabinol (Δ⁹-THC; ECP022A, Namisol) – CB₁ and CB₂ receptor agonist [26][27]
• Nabilone – CB₁ and CB₂ receptor agonist [28]
• NEO-1940 – CB₁ and CB₂ receptor agonist [29]
• Olorinab (APD-371) – CB₂ receptor agonist [30]

Nerve growth factor inhibitors

• Fasinumab (REGN-475, SAR-164877) – monoclonal antibody against nerve growth factor[31]
• Fulranumab (AMG-403, JNJ-42160443) – monoclonal antibody against nerve growth factor [32]
• GBR-900 – monoclonal antibody against TrkA[33]
• GZ-389988 – TrkA, TrkB, and TrkC kinase inhibitor[34]
• LEVI-04 (p75^NTR-Fc) – LNGF receptor (p75^NTR) fusion protein and decoy receptor for nerve growth factor [35]
• NRD135S-E1 – tyrosine kinase modulator[36][37]
• ONO-4474 – peripherally selective TrkA, TrkB, and TrkC kinase inhibitor[38]
• Ranevetmab (NV-01) – monoclonal antibody against nerve growth factor for dogs [39]
• Tanezumab (PF-4383119, RI-624, RN-624) – monoclonal antibody against nerve growth factor [40]
• VM-902A – selective, peripherally selective allosteric inhibitor of TrkA [41]

Others

• ALLOD-2 – undefined mechanism of action [42]
• CR-4056 – imidazoline I₂ receptor agonist [43]
• E-52862 (MR-309; S1A; S1RA) – sigma-1 receptor antagonist [44]
• HSP-3150 – undefined mechanism of action [45]
• KCP-506 – nicotinic acetylcholine receptor antagonist [46]
• LATER – CRISPR-dCas9 gene-editing
• PAX-01 – undefined mechanism of action [47]

See also

• List of investigational drugs

External links

• AdisInsight - Springer