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词条 List of investigational analgesics
释义

  1. Opioid receptor modulators

  2. Sodium channel blockers

  3. Calcium channel blockers

  4. {{abbr|TRP|Transient receptor potential}} channel modulators

  5. Cannabinoid receptor modulators

  6. Nerve growth factor inhibitors

  7. Others

  8. See also

  9. References

  10. External links

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.

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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  
  • Difelikefalin (CR845, FE-202845) – peripherally selective κ-opioid receptor agonist  
  • Lexanopadol (GRT-6006, GRT13106G) – non-selective opioid receptor agonist  
  • NKTR-181 – selective μ-opioid receptor full agonist that slowly enters the brain  
  • Oliceridine (TRV130) – μ-opioid receptor biased agonist[1] 
  • Oxycodone/naltrexone – combination of a μ-opioid receptor agonist and a μ- and κ-opioid receptor antagonist  

Sodium channel blockers

  • CC-8464 (ASP-1807) – selective Nav1.7 blocker 
  • Cenobamate (YKP-3089) – atypical voltage-gated sodium channel blocker  [2][3]
  • 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  [4]
  • VX-150 – selective Nav1.8 blocker  

Calcium channel blockers

  • Mirogabalin - α2δ subunit-selective voltage-dependent calcium channel blocker  

{{abbr|TRP|Transient receptor potential}} 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 [5][6]
  • 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-{{abbr|THC|tetrahydrocannabinol}}; 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  
  • PAX-01 – undefined mechanism of action  

See also

  • List of investigational drugs

References

1. ^Zhu L, et al. Novel Opioid-Receptor Agonists with Reduced Morphine-like Side Effects. Mini Rev Med Chem. 2018 Jul 16. {{Cite journal|doi= 10.2174/1389557518666180716124336|pmid=30009707}}
2. ^{{cite journal | vauthors = Zaccara G, Schmidt D | title = Antiepileptic Drugs in Clinical Development: Differentiate or Die? | journal = Curr. Pharm. Des. | volume = 23 | issue = 37 | pages = 5593–5605 | date = 2017 | pmid = 28799516 | doi = 10.2174/1381612823666170809100524 | url = }}
3. ^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
4. ^{{cite journal|last1=Keppel Hesselink|first1=Jan M.|title=Moving targets in sodium channel blocker development: the case of raxatrigine: from a central NaV1.3 blocker via a peripheral NaV1.7 blocker to a less selective sodium channel blocker|journal=Journal of Medicine and Therapeutics|volume=1|issue=1|year=2017|issn=2399-9799|doi=10.15761/JMT.1000104}}
5. ^{{Cite journal|last=Manitpisitkul|first=Prasarn|last2=Shalayda|first2=Kevin|last3=Russell|first3=Lucille|last4=Sanga|first4=Panna|last5=Solanki|first5=Bhavna|last6=Caruso|first6=Joseph|last7=Iwaki|first7=Yuki|last8=Moyer|first8=John A.|date=2018|title=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|url=https://accp1.onlinelibrary.wiley.com/doi/abs/10.1002/cpdd.413|journal=Clinical Pharmacology in Drug Development|language=en|volume=7|issue=7|pages=712–726|doi=10.1002/cpdd.413|issn=2160-7648}}
6. ^{{Cite journal|last=Manitpisitkul|first=Prasarn|last2=Shalayda|first2=Kevin|last3=Russell|first3=Lucille|last4=Sanga|first4=Panna|last5=Williams|first5=Yinka|last6=Solanki|first6=Bhavna|last7=Caruso|first7=Joseph|last8=Moyer|first8=John A.|date=2018|title=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|url=https://accp1.onlinelibrary.wiley.com/doi/abs/10.1002/cpdd.412|journal=Clinical Pharmacology in Drug Development|language=en|volume=7|issue=7|pages=699–711|doi=10.1002/cpdd.412|issn=2160-7648}}

External links

  • AdisInsight - Springer
{{Analgesics}}{{Neuropathic pain and fibromyalgia pharmacotherapies}}

3 : Analgesics|Drug-related lists|Experimental drugs
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