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

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-HT_2C receptor antagonist
Difelikefalin (CR845, FE-202845) – peripherally selective κ-opioid receptor agonist
Lexanopadol (GRT-6006, GRT13106G) – non-selective opioid receptor agonist
Oxycodone/naltrexone – combination of a μ-opioid receptor agonist and a μ- and κ-opioid receptor antagonist

Sodium channel blockers

BIIB-095 – state-dependent and use-dependent Na_v blocker, including Na_v1.7
CC-8464 (ASP-1807) – selective Na_v1.7 blocker
Cenobamate (YKP-3089) – atypical voltage-gated sodium channel blocker [1][2]
DSP-2230 – selective Na_v1.7 and Na_v1.8 blocker
Funapide (TV-45070, XEN402) – selective Na_v1.7 and Na_v1.8 blocker
GDC-0276 (RG-7893) – selective Na_v1.7 blocker
GDC-0310 (RG-6029) – selective Na_v1.7 blocker
NKTR-171 – voltage-gated sodium channel blocker
PF-05089771 – selective Na_v1.7 and Na_v1.8 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 Na_v1.8 blocker

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 [3][4]
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 (p75^NTR-Fc) – LNGF receptor (p75^NTR) 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
PAX-01 – undefined mechanism of action

References

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.
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
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.
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.

External links

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[pmid28799516-1] 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.

[NakamuraShin2018-2] 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

[3] 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.

[4] 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.

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, pregabalin, mirogabalin, carbamazepine, oxcarbazepine, lacosamide, lamotrigine) Local anesthetics (e.g., lidocaine) Mexiletine TCAs (e.g., amitriptyline, nortriptyline, desipramine) Ziconotide
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)