List of investigational analgesics

This is a dynamic list and may never be able to satisfy particular standards for completeness. You can help by adding missing items with reliable sources.

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 It is likely to become outdated with time.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. ^[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-HT_2C receptor antagonist. ^[3]
• Deumitragynine (KUR-101) – atypical μ-opioid receptor agonist related to mitragynine (found in kratom) ^{[4] [5] [6]}
• Lexanopadol  [ Wikidata ] (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 Na_v blocker, including Na_v1.7. ^[9]
• CC-8464 (ASP-1807) – selective Na_v1.7 blocker ^[10]
• Cenobamate (YKP-3089) – atypical voltage-gated sodium channel blocker. ^{[11] [12] : 5593–5605  [13]}
• DSP-2230 – selective Na_v1.7 and Na_v1.8 blocker. ^[14]
• Funapide (TV-45070, XEN402) – selective Na_v1.7 and Na_v1.8 blocker. ^[15]
• GDC-0276 (RG-7893) – selective Na_v1.7 blocker ^[16]
• GDC-0310 (RG-6029) – selective Na_v1.7 blocker ^[17]
• NKTR-171 – voltage-gated sodium channel blocker ^[18]
• PF-05089771 – selective Na_v1.7 and Na_v1.8 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 Na_v1.8 blocker ^[23]

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

• ABX-1431 – selective monoacylglycerol lipase inhibitor ^[38]
• Cannabidiol (CBD) – cannabinoid receptor modulator ^{[39] [40]}
• Cannabidivarin (CBDV; GWP-42006) – cannabinoid receptor modulator ^[41]
• CMX-020 – TRPV1 modulator as well as CB₁ and CB₂ receptor modulator ^[27]
• Dronabinol (Δ⁹-THC; ECP022A, Namisol) – CB₁ and CB₂ receptor agonist ^{[42] [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 (p75^NTR-Fc) – LNGF receptor (p75^NTR) 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]
• CR-4056 – imidazoline I₂ receptor agonist ^[59]
• E-52862 (MR-309; S1A; S1RA) – sigma-1 receptor antagonist ^[60]
• HSP-3150 – undefined mechanism of action ^[61]
• KCP-506 – nicotinic acetylcholine receptor antagonist ^[62]
• LATER – CRISPR-dCas9 gene-editing ^[63]
• PAX-01 – undefined mechanism of action ^[64]
• Opiranserin - Dual 5HT2A Receptor antagonist and GlyT2 inhibitor

See also

• List of investigational drugs

References

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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. "KUR 101". AdisInsight. 27 December 2022. Retrieved 26 February 2025.
5. "Delving into the Latest Updates on Deuterated Mitragynine with Synapse". Synapse. 22 February 2025. Retrieved 26 February 2025.
6. "KUR-101 Drug Profile". Ozmosi. 23 December 2022. Retrieved 26 February 2025.
7. "Drug profile | Lexanopadol" . AdisInsight . 20 August 2018. Archived from the original on 25 December 2018. Retrieved 2 November 2022.
8. "Drug profile | Oxycodone/naltrexone" . AdisInsight . Elite Pharmaceuticals. 16 April 2021. Archived from the original on 14 November 2022. Retrieved 14 November 2022.
9. "Drug profile | BIIB 095" . AdisInsight . Biogen. 7 May 2021. Archived from the original on 14 November 2022. Retrieved 14 November 2022.
10. "Drug profile | CC 8464" . AdisInsight . Chromocell Corporation. 28 November 2019. Archived from the original on 15 March 2022. Retrieved 14 November 2022.
11. "Drug profile | Cenobamate" . AdisInsight . SK biopharmaceuticals. 28 November 2019. Archived from the original on 14 November 2022. Retrieved 14 November 2022.
12. Zaccara, Gaetano; Schmidt, D. (2017). "Antiepileptic Drugs in Clinical Development: Differentiate or Die?". Current Pharmaceutical Design . 23 (37). Bentham Science Publishers: 5593–5605. doi:10.2174/1381612823666170809100524. eISSN   1873-4286. ISSN   1381-6128. PMID   28799516. S2CID   3676340.
13. Nakamura, Michiko; Shin, Hyewon; Jang, Il-Sung (26 April 2018). "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. eISSN   1526-632X. ISSN   0028-3878. LCCN   55043902. OCLC   960771045. S2CID   80887455.
14. "Drug profile | DSP 2230" . AdisInsight . Sumitomo Dainippon Pharma. 4 April 2022. Archived from the original on 14 November 2022. Retrieved 14 November 2022.
15. "Drug profile | Funapide" . AdisInsight . Xenon Pharmaceuticals. 6 September 2022. Archived from the original on 14 November 2022. Retrieved 14 November 2022.
16. "GDC 0276 - AdisInsight". adisinsight.springer.com.
17. "GDC 0310 - AdisInsight". adisinsight.springer.com.
18. "NKTR 171 - AdisInsight". adisinsight.springer.com.
19. "PF 5089771 - AdisInsight". adisinsight.springer.com.
20. "Ralfinamide - Newron Pharmaceuticals - AdisInsight". adisinsight.springer.com.
21. "Tetrodotoxin - WEX Pharmaceuticals - AdisInsight". adisinsight.springer.com.
22. "Vixotrigine - Biogen - AdisInsight". adisinsight.springer.com.
23. "VX 150 - AdisInsight". adisinsight.springer.com.
24. Gou, Xiaoli; Yu, Xiaojuan; Bai, Dongdong; Tan, Bowei; Cao, Pingfeng; Qian, Meilin; Zheng, Xiaoxiao; Chen, Lei; Shi, Zongjun; Li, Yao; Ye, Fei; Liang, Yong; Ni, Jia (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". adisinsight.springer.com.
26. "Capsaicin/Diclofenac - Boehringer Ingelheim - AdisInsight". adisinsight.springer.com.
27. "CMX 020 - AdisInsight". adisinsight.springer.com.
28. "DWP 05195 - AdisInsight". adisinsight.springer.com.
29. "GRC 6211 - AdisInsight". adisinsight.springer.com.
30. "JNJ 38893777 - AdisInsight". adisinsight.springer.com.
31. Manitpisitkul, Prasarn; Shalayda, Kevin; Russell, Lucille; Sanga, Panna; Solanki, Bhavna; Caruso, Joseph; Iwaki, Yuki; Moyer, John A. (10 November 2017). "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. eISSN   2160-7648. ISSN   2160-763X. PMID   29125703. S2CID   11755963.
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". Clinical Pharmacology in Drug Development. 7 (7): 699–711. doi:10.1002/cpdd.412. ISSN   2160-7648. PMID   29125700. S2CID   32666782.
33. "NEO 6860 - AdisInsight". adisinsight.springer.com.
34. "Parentide - DiverDrugs - AdisInsight". adisinsight.springer.com.
35. "Resiniferatoxin - Sorrento Therapeutics - AdisInsight". adisinsight.springer.com.
36. "SAR 115740 - AdisInsight". adisinsight.springer.com.
37. "Tivanisiran - Sylentis - AdisInsight". adisinsight.springer.com.
38. "Elcubragistat - Lundbeck A/S - AdisInsight". adisinsight.springer.com.
39. "Synthetic cannabidiol - Benuvia Therapeutics/Radius Health - AdisInsight". adisinsight.springer.com.
40. "Cannabidiol - ANANDA Scientific - AdisInsight". adisinsight.springer.com.
41. "Cannabidivarin - GW Pharmaceuticals - AdisInsight". adisinsight.springer.com.
42. "Dronabinol - Echo Pharmaceuticals - AdisInsight". adisinsight.springer.com.
43. "Dronabinol buccal - IntelGenx - AdisInsight". adisinsight.springer.com.
44. "Nabilone controlled release - AOP Orphan Pharmaceuticals - AdisInsight". adisinsight.springer.com.
45. "ART 2713 - AdisInsight". adisinsight.springer.com.
46. "Olorinab - Pfizer - AdisInsight". adisinsight.springer.com.
47. "Fasinumab - Mitsubishi Tanabe Pharma/Regeneron/Teva - AdisInsight". adisinsight.springer.com.
48. "Fulranumab - AdisInsight". adisinsight.springer.com.
49. "GBR 900 - AdisInsight". adisinsight.springer.com.
50. "GZ 389988 - AdisInsight". adisinsight.springer.com.
51. "LEVI 04 - AdisInsight". adisinsight.springer.com.
52. "NRD 135S E1 - AdisInsight". adisinsight.springer.com.
53. https://www.novaremed.com/index.php/technology-pipeline
54. "ONO 4474 - AdisInsight". adisinsight.springer.com.
55. https://www.nexvet.com/therapies/chronic-pain/nv-01/
56. "Tanezumab - Eli Lilly and Company/Pfizer - AdisInsight". adisinsight.springer.com.
57. "VM 902 - AdisInsight". adisinsight.springer.com.
58. "Acetaminophen/Naltrexone - Allodynic Therapeutics - AdisInsight". adisinsight.springer.com.
59. "CR 4056 - AdisInsight". adisinsight.springer.com.
60. "E 52862 - AdisInsight". adisinsight.springer.com.
61. "Diclofenac sodium transdermal patch - Hisamitsu Pharmaceuticals - AdisInsight". adisinsight.springer.com.
62. "KCP 506 - AdisInsight". adisinsight.springer.com.
63. Moreno, Ana M.; Alemán, Fernando; Catroli, Glaucilene F.; Hunt, Matthew; Hu, Michael; et al. (10 March 2021). "Long-lasting analgesia via targeted in situ repression of NaV1.7 in mice". Science Translational Medicine . 13 (584). doi:10.1126/scitranslmed.aay9056. eISSN   1946-6242. ISSN   1946-6234. PMC   8830379 . PMID   33692134.
64. "PAX 01 - AdisInsight". adisinsight.springer.com.

External links

• AdisInsight - Springer