Chemistry:List of investigational analgesics

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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.[6]
  • CC-8464 (ASP-1807) – selective Nav1.7 blocker[7]
  • Cenobamate (YKP-3089) – atypical voltage-gated sodium channel blocker.[8][9]:5593–5605[10]
  • DSP-2230 – selective Nav1.7 and Nav1.8 blocker.[11]
  • Funapide (TV-45070, XEN402) – selective Nav1.7 and Nav1.8 blocker.[12]
  • GDC-0276 (RG-7893) – selective Nav1.7 blocker [1]
  • GDC-0310 (RG-6029) – selective Nav1.7 blocker [2]
  • NKTR-171 – voltage-gated sodium channel blocker [3]
  • PF-05089771 – selective Nav1.7 and Nav1.8 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][citation needed]
  • VX-150 – selective Nav1.8 blocker [8]
  • VX-548 – selective Nav1.8 blocker[13][14]

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.[15]:712-726[16]
  • 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

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 (p75NTR-Fc) – LNGF receptor (p75NTR) 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[17]
  • PAX-01 – undefined mechanism of action [47]

See also

References

  1. ↑ "Drug profile | Axelopran/oxycodone". Theravance Biopharma. 2021-10-01. http://adisinsight.springer.com/drugs/800041868. 
  2. ↑ "Drug profile | Cebranopadol". Tris Pharma. 2022-08-14. http://adisinsight.springer.com/drugs/800030045. 
  3. ↑ "Drug profile | Desmetramadol". Syntrix Biosystems. 2021-10-05. https://adisinsight.springer.com/drugs/800041025. 
  4. ↑ "Drug profile | Lexanopadol" (in en-US). AdisInsight. 2018-08-20. https://adisinsight.springer.com/drugs/800034083. 
  5. ↑ "Drug profile | Oxycodone/naltrexone" (in en-US). Elite Pharmaceuticals. 2021-04-16. https://adisinsight.springer.com/drugs/800019069. 
  6. ↑ "Drug profile | BIIB 095" (in en-US). Biogen. 2021-05-07. https://adisinsight.springer.com/drugs/800051479. 
  7. ↑ (in en-US) Drug profile | CC 8464. Chromocell Corporation. 2019-11-28. https://adisinsight.springer.com/drugs/800048067. Retrieved 2022-11-14. 
  8. ↑ "Drug profile | Cenobamate" (in en-US). SK biopharmaceuticals. 2019-11-28. https://adisinsight.springer.com/drugs/800023388. 
  9. ↑ Zaccara, Gaetano; Schmidt, D. (2017). "Antiepileptic Drugs in Clinical Development: Differentiate or Die?". Current Pharmaceutical Design (Bentham Science Publishers) 23 (37): 5593–5605. doi:10.2174/1381612823666170809100524. ISSN 1381-6128. PMID 28799516. 
  10. ↑ Nakamura, Michiko; Shin, Hyewon; Jang, Il-Sung (2018-04-26). "Mechanism of Action of Cenobamate: Preferential Inhibition of the Persistent Sodium Current (P5.278)". Neurology 90 (15 Supplement). doi:10.1212/WNL.90.15_supplement.P5.278. ISSN 0028-3878. OCLC 960771045. 
  11. ↑ "Drug profile | DSP 2230" (in en-US). Sumitomo Dainippon Pharma. 2022-04-04. https://adisinsight.springer.com/drugs/800036041. 
  12. ↑ (in en-US) Drug profile | Funapide. Xenon Pharmaceuticals. 2022-09-06. https://adisinsight.springer.com/drugs/800025125. Retrieved 2022-11-14. 
  13. ↑ Nichols, Heather (19 July 2021). "Vertex Initiates Phase 2 Clinical Trial Program for VX-548 for the Treatment of Acute Pain". Vertex Pharmaceuticals (Press Release). Retrieved 14 November 2022. Vertex Pharmaceuticals Incorporated (Nasdaq: VRTX) today announced that it has begun a Phase 2 proof-of-concept (POC) study in acute pain following bunionectomy surgery with the selective NaV1.8 inhibitor VX-548 and that it expects to commence a second Phase 2 study in acute pain following abdominoplasty surgery in the coming weeks.
  14. ↑ Cross, Ryan (2022-03-31). "Vertex's non-opioid painkiller shows promise in people recovering from surgery" (in en-US). The Boston Globe. ISSN 0743-1791. OCLC 66652431. https://www.bostonglobe.com/2022/03/31/business/vertexs-non-opioid-painkiller-shows-promise-people-recovering-surgery/. ""There is an enormous need for novel non-opioid analgesics with no abuse liability," and Vertex's results are an "important advance," said Dr. Clifford J. Woolf, director of the F.M. Kirby Neurobiology Center and Boston Children's Hospital. It will be important for Vertex to determine whether the drug also works for patients with chronic pain, such as diabetic neuropathy and low back pain, "where the clinical need is highest," he added." 
  15. ↑ Manitpisitkul, Prasarn; Shalayda, Kevin; Russell, Lucille; Sanga, Panna; Solanki, Bhavna; Caruso, Joseph; Iwaki, Yuki; Moyer, John A. (2017-11-10). "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 2160-763X. PMID 29125703. 
  16. ↑ 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" (in en). Clinical Pharmacology in Drug Development 7 (7): 699–711. doi:10.1002/cpdd.412. ISSN 2160-7648. PMID 29125700. 
  17. ↑ Moreno, Ana M.; Alemán, Fernando; Catroli, Glaucilene F.; Hunt, Matthew; Hu, Michael et al. (2021-03-10). "Long-lasting analgesia via targeted in situ repression of NaV1.7 in mice". Science Translational Medicine 13 (584). doi:10.1126/scitranslmed.aay9056. ISSN 1946-6234. PMID 33692134. 

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