List of investigational analgesics

Short description: none

This is a dynamic list and may never be able to satisfy particular standards for completeness. You can help by expanding it with reliably sourced entries.

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 It is likely to become outdated with time.

## Contents

* 1 Opioid receptor modulators
* 2 Sodium channel blockers
* 3 Calcium channel blockers
* 4 TRP channel modulators
* 5 Cannabinoid receptor modulators
* 6 Nerve growth factor inhibitors
* 7 Others
* 8 See also
* 9 References
* 10 External links

## 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.[1]
* Cebranopadol (GRT-6005) – non-selective μ-opioid receptor, nociceptin receptor, and δ-opioid receptor full agonist and κ-opioid receptor partial agonist[2]
* Desmetramadol (O-desmethyltramadol; Omnitram) – μ-opioid receptor agonist, norepinephrine reuptake inhibitor (NRI), and 5-HT2C receptor antagonist.[3]
* Deumitragynine (KUR-101) – atypical μ-opioid receptor agonist related to mitragynine (found in kratom)[4][5][6]
* Lexanopadol (GRT-6006, GRT13106G) – non-selective opioid receptor agonist[7]
* Oxycodone/naltrexone – combination of a μ-opioid receptor agonist and a μ- and κ-opioid receptor antagonist.[8]

## Sodium channel blockers

* BIIB-095 – state-dependent and use-dependent Nav blocker, including Nav1.7.[9]
* CC-8464 (ASP-1807) – selective Nav1.7 blocker[10]
* Cenobamate (YKP-3089) – atypical voltage-gated sodium channel blocker.[11][12]: 5593–5605 [13]
* DSP-2230 – selective Nav1.7 and Nav1.8 blocker.[14]
* Funapide (TV-45070, XEN402) – selective Nav1.7 and Nav1.8 blocker.[15]
* GDC-0276 (RG-7893) – selective Nav1.7 blocker [16]
* GDC-0310 (RG-6029) – selective Nav1.7 blocker [17]
* NKTR-171 – voltage-gated sodium channel blocker [18]
* PF-05089771 – selective Nav1.7 and Nav1.8 blocker [19]
* Ralfinamide (NW-1029) – non-selective voltage-gated sodium channel blocker, as well as other actions [20]
* Tetrodotoxin (9401-TTX; Tectin, Tetrodin, Tocudin) – non-selective voltage-gated sodium channel blocker [21]
* Vixotrigine (formerly raxatrigine; CNV1014802, GSK-1014802, BIIB 074) – non-selective voltage-gated sodium channel blocker [22][citation needed]
* VX-150 – selective Nav1.8 blocker [23]
* VX-993

## Calcium channel blockers

* HSK16149 - selective ligand of α2δ subunit of voltage-gated calcium channel [24]

## TRP channel modulators

* Capsaicin (Adlea, ALGRX-4975, CNTX-4975, VLNX-4975) – TRPV1 agonist [25]
* Capsaicin/diclofenac – combination of a TRPV1 agonist and a COX-2 inhibitor for topical application [26]
* CMX-020 – TRPV1 modulator as well as CB1 and CB2 receptor modulator [27]
* DWP-05195 (TR-1) – TRPV1 antagonist [28]
* GRC-6211 – TRPV1 agonist [29]
* JNJ-38893777 – TRPV1 antagonist [30]
* Mavatrep (JNJ‐39439335) – TRPV1 antagonist.[31]: 712–726 [32]
* NEO-6860 – TRPV1 antagonist [33]
* Parentide (DD-04107) – TRPV1 antagonist [34]
* Resiniferatoxin (RTX; MCP-101) – TRPV1 agonist [35]
* SAR-115740 – TRPV1 antagonist [36]
* Tivanisiran (SYL-1001) – TRPV1 antagonist [37]

## Cannabinoid receptor modulators

* Cannabidiol (CBD) – cannabinoid receptor modulator [38][39]
* Cannabidivarin (CBDV; GWP-42006) – cannabinoid receptor modulator [40]
* CMX-020 – TRPV1 modulator as well as CB1 and CB2 receptor modulator [27]
* Dronabinol (Δ9-THC; ECP022A, Namisol) – CB1 and CB2 receptor agonist [41][42]
* Elcubragistat (ABX-1431; Lu-AG06466) – selective monoacylglycerol lipase (MAGL) inhibitor[43]
* Nabilone – CB1 and CB2 receptor agonist [44]
* NEO-1940 – CB1 and CB2 receptor agonist [45]
* Olorinab (APD-371) – CB2 receptor agonist [46]

## Nerve growth factor inhibitors

* Fasinumab (REGN-475, SAR-164877) – monoclonal antibody against nerve growth factor[47]
* Fulranumab (AMG-403, JNJ-42160443) – monoclonal antibody against nerve growth factor [48]
* GBR-900 – monoclonal antibody against TrkA[49]
* GZ-389988 – TrkA, TrkB, and TrkC kinase inhibitor[50]
* LEVI-04 (p75NTR-Fc) – LNGF receptor (p75NTR) fusion protein and decoy receptor for nerve growth factor [51]
* NRD135S-E1 – tyrosine kinase modulator[52][53]
* ONO-4474 – peripherally selective TrkA, TrkB, and TrkC kinase inhibitor[54]
* Ranevetmab (NV-01) – monoclonal antibody against nerve growth factor for dogs [55]
* Tanezumab (PF-4383119, RI-624, RN-624) – monoclonal antibody against nerve growth factor [56]
* VM-902A – selective, peripherally selective allosteric inhibitor of TrkA [57]

## Others

* ALLOD-2 – undefined mechanism of action [58]
* CM-304 – sigma-1 receptor antagonist. Cold version of radiotracer [18F] FTC-146[59]
* CR-4056 – imidazoline I2 receptor agonist [60]
* E-52862 (MR-309; S1A; S1RA) – sigma-1 receptor antagonist [61]
* HSP-3150 – undefined mechanism of action [62]
* KCP-506 – nicotinic acetylcholine receptor antagonist [63]
* KNX-101 – 15-lipoxygenase (15-LOX; ALOX15) inhibitor
* LATER – CRISPR-dCas9 gene-editing[64]
* PAX-01 – undefined mechanism of action [65]
* Opiranserin \- Dual 5HT2A Receptor antagonist and GlyT2 inhibitor

## See also

* List of investigational drugs

## 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. ↑ "KUR 101". 27 December 2022. https://adisinsight.springer.com/drugs/800059454.
5. ↑ "Delving into the Latest Updates on Deuterated Mitragynine with Synapse". 22 February 2025. https://synapse.patsnap.com/drug/415e14fb698a450198273fa1444a6e84.
6. ↑ "KUR-101 Drug Profile". 23 December 2022. https://pryzm.ozmosi.com/product/24882.
7. ↑ "Drug profile | Lexanopadol" (in en-US). AdisInsight. 2018-08-20. https://adisinsight.springer.com/drugs/800034083.
8. ↑ "Drug profile | Oxycodone/naltrexone" (in en-US). Elite Pharmaceuticals. 2021-04-16. https://adisinsight.springer.com/drugs/800019069.
9. ↑ "Drug profile | BIIB 095" (in en-US). Biogen. 2021-05-07. https://adisinsight.springer.com/drugs/800051479.
10. ↑ "Drug profile | CC 8464" (in en-US). Chromocell Corporation. 2019-11-28. https://adisinsight.springer.com/drugs/800048067.
11. ↑ "Drug profile | Cenobamate" (in en-US). SK biopharmaceuticals. 2019-11-28. https://adisinsight.springer.com/drugs/800023388.
12. ↑ 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.
13. ↑ 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.
14. ↑ "Drug profile | DSP 2230" (in en-US). Sumitomo Dainippon Pharma. 2022-04-04. https://adisinsight.springer.com/drugs/800036041.
15. ↑ "Drug profile | Funapide" (in en-US). Xenon Pharmaceuticals. 2022-09-06. https://adisinsight.springer.com/drugs/800025125.
16. ↑ "GDC 0276 - AdisInsight". https://adisinsight.springer.com/drugs/800041740.
17. ↑ "GDC 0310 - AdisInsight". https://adisinsight.springer.com/drugs/800043573.
18. ↑ "NKTR 171 - AdisInsight". https://adisinsight.springer.com/drugs/800039638.
19. ↑ "PF 5089771 - AdisInsight". https://adisinsight.springer.com/drugs/800026875.
20. ↑ "Ralfinamide - Newron Pharmaceuticals - AdisInsight". https://adisinsight.springer.com/drugs/800014979.
21. ↑ "Tetrodotoxin - WEX Pharmaceuticals - AdisInsight". https://adisinsight.springer.com/drugs/800016242.
22. ↑ "Vixotrigine - Biogen - AdisInsight". https://adisinsight.springer.com/drugs/800027679.
23. ↑ "VX 150 - AdisInsight". https://adisinsight.springer.com/drugs/800044114.
24. ↑ Gou, Xiaoli; Yu, Xiaojuan; Bai, Dongdong; Tan, Bowei; Cao, Pingfeng; Qian, Meilin; Zheng, Xiaoxiao; Chen, Lei et al. (2021). "Pharmacology and Mechanism of Action of HSK16149, a Selective Ligand of α 2 δ Subunit of Voltage-Gated Calcium Channel with Analgesic Activity in Animal Models of Chronic Pain". Journal of Pharmacology and Experimental Therapeutics 376 (3): 330–337. doi:10.1124/jpet.120.000315. PMID 33293377.
25. ↑ "Capsaicin - Centrexion Therapeutics - AdisInsight". https://adisinsight.springer.com/drugs/800018328.
26. ↑ "Capsaicin/Diclofenac - Boehringer Ingelheim - AdisInsight". https://adisinsight.springer.com/drugs/800044916.
27. ↑ 27.0 27.1 "CMX 020 - AdisInsight". https://adisinsight.springer.com/drugs/800042284.
28. ↑ "DWP 05195 - AdisInsight". https://adisinsight.springer.com/drugs/800029507.
29. ↑ "GRC 6211 - AdisInsight". https://adisinsight.springer.com/drugs/800024886.
30. ↑ "JNJ 38893777 - AdisInsight". https://adisinsight.springer.com/drugs/800043593.
31. ↑ 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.
32. ↑ 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.
33. ↑ "NEO 6860 - AdisInsight". https://adisinsight.springer.com/drugs/800039045.
34. ↑ "Parentide - DiverDrugs - AdisInsight". https://adisinsight.springer.com/drugs/800049435.
35. ↑ "Resiniferatoxin - Sorrento Therapeutics - AdisInsight". https://adisinsight.springer.com/drugs/800009782.
36. ↑ "SAR 115740 - AdisInsight". https://adisinsight.springer.com/drugs/800025854.
37. ↑ "Tivanisiran - Sylentis - AdisInsight". https://adisinsight.springer.com/drugs/800035022.
38. ↑ "Synthetic cannabidiol - Benuvia Therapeutics/Radius Health - AdisInsight". https://adisinsight.springer.com/drugs/800039721.
39. ↑ "Cannabidiol - ANANDA Scientific - AdisInsight". https://adisinsight.springer.com/drugs/800045903.
40. ↑ "Cannabidivarin - GW Pharmaceuticals - AdisInsight". https://adisinsight.springer.com/drugs/800038847.
41. ↑ "Dronabinol - Echo Pharmaceuticals - AdisInsight". https://adisinsight.springer.com/drugs/800033565.
42. ↑ "Dronabinol buccal - IntelGenx - AdisInsight". https://adisinsight.springer.com/drugs/800027102.
43. ↑ "Elcubragistat - Lundbeck A/S - AdisInsight". https://adisinsight.springer.com/drugs/800042817.
44. ↑ "Nabilone controlled release - AOP Orphan Pharmaceuticals - AdisInsight". https://adisinsight.springer.com/drugs/800039582.
45. ↑ "ART 2713 - AdisInsight". https://adisinsight.springer.com/drugs/800039083.
46. ↑ "Olorinab - Pfizer - AdisInsight". https://adisinsight.springer.com/drugs/800039670.
47. ↑ "Fasinumab - Mitsubishi Tanabe Pharma/Regeneron/Teva - AdisInsight". https://adisinsight.springer.com/drugs/800029842.
48. ↑ "Fulranumab - AdisInsight". https://adisinsight.springer.com/drugs/800024342.
49. ↑ "GBR 900 - AdisInsight". https://adisinsight.springer.com/drugs/800040743.
50. ↑ "GZ 389988 - AdisInsight". https://adisinsight.springer.com/drugs/800019397.
51. ↑ "LEVI 04 - AdisInsight". https://adisinsight.springer.com/drugs/800046945.
52. ↑ "NRD 135S E1 - AdisInsight". https://adisinsight.springer.com/drugs/800041985.
53. ↑ https://www.novaremed.com/index.php/technology-pipeline
54. ↑ "ONO 4474 - AdisInsight". https://adisinsight.springer.com/drugs/800042445.
55. ↑ https://www.nexvet.com/therapies/chronic-pain/nv-01/
56. ↑ "Tanezumab - Eli Lilly and Company/Pfizer - AdisInsight". https://adisinsight.springer.com/drugs/800019466.
57. ↑ "VM 902 - AdisInsight". https://adisinsight.springer.com/drugs/800043233.
58. ↑ "Acetaminophen/Naltrexone - Allodynic Therapeutics - AdisInsight". https://adisinsight.springer.com/drugs/800038509.
59. ↑ Mallory Burns, Sarah; Guadagnoli, Nicholas; McCurdy, Christopher (May 2023). "Advances with the discovery and development of novel Sigma 1 receptor antagonists for the management of pain". Expert Opinion on Drug Discovery (Taylor and Francis) 18 (2). doi:10.1080/17460441.2023.2216015. https://www.researchgate.net/publication/370895039_Advances_with_the_discovery_and_development_of_novel_Sigma_1_receptor_antagonists_for_the_management_of_pain. Retrieved January 22, 2026.
60. ↑ "CR 4056 - AdisInsight". https://adisinsight.springer.com/drugs/800036726.
61. ↑ "E 52862 - AdisInsight". https://adisinsight.springer.com/drugs/800031669.
62. ↑ "Diclofenac sodium transdermal patch - Hisamitsu Pharmaceuticals - AdisInsight". https://adisinsight.springer.com/drugs/800044788.
63. ↑ "KCP 506 - AdisInsight". https://adisinsight.springer.com/drugs/800059947.
64. ↑ 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.
65. ↑ "PAX 01 - AdisInsight". https://adisinsight.springer.com/drugs/800045525.

## External links

* AdisInsight - Springer

* v
* t
* e

Analgesics (N02A, N02B)

Opioids|

| Opiates/opium|

* Codeine# (+paracetamol, +aspirin)
* Morphine# (+naltrexone)
* Opium
* Laudanum
* Paregoric

|

Semisynthetic|

* Acetyldihydrocodeine
* Benzylmorphine
* Buprenorphine (+naloxone)
* Desomorphine
* Diamorphine (heroin)
* Dihydrocodeine (+paracetamol)
* Dihydromorphine
* Ethylmorphine
* Hydrocodone (+paracetamol, +ibuprofen, +aspirin)
* Hydromorphinol
* Hydromorphone
* Nicocodeine
* Nicodicodine
* Nicomorphine
* Oxycodone (+paracetamol, +aspirin, oxycodone/ibuprofen

Synthetic|

* Alfentanil
* Alphaprodine
* Anileridine
* Butorphanol
* Carfentanil
* Dextromoramide
* Dextropropoxyphene
* Dezocine
* Fentanyl# (+fluanisone)
* Ketobemidone
* Levorphanol
* Lofentanil
* Meptazinol
* Methadone#
* Nalbuphine
* NFEPP
* Pentazocine
* Pethidine (meperidine)
* Phenadoxone
* Phenazocine
* Piminodine
* Piritramide
* Propiram
* Remifentanil
* Sufentanil
* Tapentadol
* Tilidine
* Tramadol

Paracetamol-type|

* Acetanilide‡
* Bucetin‡
* Butacetin‡
* Paracetamol (acetaminophen)#
* Parapropamol‡
* Phenacetin‡
* Propacetamol‡

NSAIDs|

| Propionates|

* Fenoprofen
* Flurbiprofen
* Ibuprofen#
* Ketoprofen
* Naproxen
* Oxaprozin

|

Oxicams|

* Meloxicam
* Piroxicam

Acetates|

* Diclofenac
* Indometacin
* Ketorolac
* Nabumetone
* Sulindac
* Tolmetin

COX-2 inhibitors|

* Celecoxib
* Etoricoxib
* Lumiracoxib
* Parecoxib
* Rofecoxib ‡
* Valdecoxib ‡

Fenamates|

* Meclofenamic acid
* Mefenamic acid

Salicylates|

* Aspirin (acetylsalicylic acid)# (+paracetamol/caffeine)
* Benorylate
* Diflunisal
* Ethenzamide
* Magnesium salicylate
* Salicin
* Salicylamide
* Salsalate
* Wintergreen (methyl salicylate)

Pyrazolones|

* Aminophenazone‡
* Ampyrone
* Metamizole (dipyrone)
* Nifenazone
* Phenazone
* Propyphenazone (+paracetamol/caffeine)

Others|

* Glafenine

Cannabinoids|

* Cannabidiol
* Cannabis
* Nabilone
* Nabiximols
* Tetrahydrocannabinol (dronabinol)

Ion channel
modulators|

| Calcium blockers|

* Gabapentin
* Gabapentin enacarbil
* Mirogabalin
* Pregabalin
* Ziconotide

|

Sodium blockers|

* Carbamazepine
* Lacosamide
* Local anesthetics (e.g., cocaine, lidocaine)
* Mexiletine
* Nefopam
* Tricyclic antidepressants (e.g., amitriptyline#)

* Nav1.7/1.8-selective: DSP-2230§
* Funapide§
* PF-05089771§

Potassium openers|

* Flupirtine

Myorelaxants|

* Carisoprodol
* Chlorzoxazone
* Cyclobenzaprine
* Mephenoxalone
* Methocarbamol
* Orphenadrine

Others|

* Analgesic adjuvant
* Analgecine
* Camphor
* Capsaicin
* Clonidine
* Ketamine
* Menthol
* Methoxyflurane
* Nefopam
* Proglumide
* Tricyclic antidepressants (e.g., amitriptyline#)

* #WHO-EM
* ‡Withdrawn from market
* Clinical trials:
* †Phase III
* §Never to phase III

* v
* t
* e

Neuropathic pain and fibromyalgia pharmacotherapies

Monoaminergics|

* SNRIs (e.g., duloxetine, milnacipran)
* TCAs (e.g., amitriptyline, nortriptyline, dosulepin)
* Opioid MRIs (e.g., tapentadol, tramadol)

Ion channel blockers|

* Anticonvulsants (e.g., gabapentin, Chemistry:Pregabalin

Others|

* Alpha lipoic acid
* Benfotiamine
* Botulinum toxin A
* Bupropion
* Cannabinoids (e.g., cannabis, dronabinol, nabilone)
* NMDA receptor antagonists (e.g., ketamine, dextromethorphan, methadone)
* Opioids (e.g., hydrocodone, morphine, oxycodone, methadone, buprenorphine, tramadol, tapentadol)
* Sodium oxybate (GHB)

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Retrieved from "https://handwiki.org/wiki/index.php?title=Chemistry:List_of_investigational_analgesics&oldid=4531819"
*[TRP]: Transient receptor potential
*[THC]: tetrahydrocannabinol
*[v]: View this template
*[t]: Discuss this template
*[e]: Edit this template
*[SNRIs]: Serotonin–norepinephrine reuptake inhibitor
*[TCAs]: Tricyclic antidepressants
*[MRIs]: monoamine reuptake inhibitors
*[GHB]: γ-hydroxybutyric acid