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

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 [5][6]
  • 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[7][8]

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 [9][10]
  • 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-THC; 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
  • Frunevetmab (NV-02) – monoclonal antibody against nerve growth factor for cats
  • 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
  • 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

See also

References
  1. "Drug profile | Axelopran/oxycodone". AdisInsight. Theravance Biopharma. 1 October 2021. Retrieved 29 October 2022.
  2. "Drug profile | Cebranopadol". AdisInsight. Tris Pharma. 14 August 2022. Retrieved 29 October 2022.
  3. "Drug profile | Desmetramadol". AdisInsight. Syntrix Biosystems. 5 October 2021. Retrieved 2 November 2022.
  4. "Drug profile | Lexanopadol". AdisInsight. 20 August 2018. Archived from the original on 25 December 2018. Retrieved 2 November 2022.
  5. Zaccara G, Schmidt D (2017). "Antiepileptic Drugs in Clinical Development: Differentiate or Die?". Curr. Pharm. Des. 23 (37): 5593–5605. doi:10.2174/1381612823666170809100524. PMID 28799516.
  6. Nakamura, M., Shin, H., & Jang, I. S. (2018). Mechanism of Action of Cenobamate: Preferential Inhibition of the Persistent Sodium Current (P5. 278). http://n.neurology.org/content/90/15_Supplement/P5.278
  7. Vertex Initiates Phase 2 Clinical Trial Program for VX-548 for the Treatment of Acute Pain
  8. Vertex’s non-opioid painkiller shows promise in people recovering from surgery
  9. Manitpisitkul, Prasarn; Shalayda, Kevin; Russell, Lucille; Sanga, Panna; Solanki, Bhavna; Caruso, Joseph; Iwaki, Yuki; Moyer, John A. (2018). "Pharmacokinetics and Safety of Mavatrep (JNJ-39439335), a TRPV1 Antagonist in Healthy Japanese and Caucasian Men: A Double-Blind, Randomized, Placebo-Controlled, Sequential-Group Phase 1 Study". Clinical Pharmacology in Drug Development. 7 (7): 712–726. doi:10.1002/cpdd.413. ISSN 2160-7648. PMID 29125703. S2CID 11755963.
  10. Manitpisitkul, Prasarn; Shalayda, Kevin; Russell, Lucille; Sanga, Panna; Williams, Yinka; Solanki, Bhavna; Caruso, Joseph; Moyer, John A. (2018). "Bioavailability and Pharmacokinetics of TRPV1 Antagonist Mavatrep (JNJ-39439335) Tablet and Capsule Formulations in Healthy Men: Two Open-Label, Crossover, Single-Dose Phase 1 Studies". Clinical Pharmacology in Drug Development. 7 (7): 699–711. doi:10.1002/cpdd.412. ISSN 2160-7648. PMID 29125700. S2CID 32666782.
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