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.

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 It is likely to become outdated with time.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-HT_2C 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 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
• GDC-0310 (RG-6029) – selective Na_v1.7 blocker
• NKTR-171 – voltage-gated sodium channel blocker
• PF-05089771 – selective Na_v1.7 and Na_v1.8 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 Na_v1.8 blocker
• VX-993

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

• 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
• 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 (p75^NTR-Fc) – LNGF receptor (p75^NTR) 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
• 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