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[edit]
- 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]
- Difelikefalin (CR845, FE-202845) – peripherally selective κ-opioid receptor agonist [4]
- Lexanopadol (GRT-6006, GRT13106G) – non-selective opioid receptor agonist [5]
- NKTR-181 – selective μ-opioid receptor full agonist that slowly enters the brain [6]
- Oliceridine (TRV130) – μ-opioid receptor biased agonist[1][7]
- Oxycodone/naltrexone – combination of a μ-opioid receptor agonist and a μ- and κ-opioid receptor antagonist [8]
Sodium channel blockers[edit]
- CC-8464 (ASP-1807) – selective Nav1.7 blocker[9]
- Cenobamate (YKP-3089) – atypical voltage-gated sodium channel blocker [10][2][3]
- 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 [13]
- GDC-0310 (RG-6029) – selective Nav1.7 blocker [14]
- NKTR-171 – voltage-gated sodium channel blocker [15]
- PF-05089771 – selective Nav1.7 and Nav1.8 blocker [16]
- Ralfinamide (NW-1029) – non-selective voltage-gated sodium channel blocker, as well as other actions [17]
- Tetrodotoxin (9401-TTX; Tectin, Tetrodin, Tocudin) – non-selective voltage-gated sodium channel blocker [18]
- Vixotrigine (formerly raxatrigine; CNV1014802, GSK-1014802, BIIB 074) – non-selective voltage-gated sodium channel blocker [19][4]
- VX-150 – selective Nav1.8 blocker [20]
Calcium channel blockers[edit]
- Mirogabalin - α2δ subunit-selective voltage-dependent calcium channel blocker [21]
TRP channel modulators[edit]
- Capsaicin (Adlea, ALGRX-4975, CNTX-4975, VLNX-4975) – TRPV1 agonist [22]
- Capsaicin/diclofenac – combination of a TRPV1 agonist and a COX-2 inhibitor for topical application [23]
- CMX-020 – TRPV1 modulator as well as CB1 and CB2 receptor modulator [24]
- DWP-05195 (TR-1) – TRPV1 antagonist [25]
- GRC-6211 – TRPV1 agonist [26]
- JNJ-38893777 – TRPV1 antagonist [27]
- Mavatrep (JNJ‐39439335) – TRPV1 antagonist [5][6]
- NEO-6860 – TRPV1 antagonist [28]
- Parentide (DD-04107) – TRPV1 antagonist [29]
- Resiniferatoxin (RTX; MCP-101) – TRPV1 agonist [30]
- SAR-115740 – TRPV1 antagonist [31]
- Tivanisiran (SYL-1001) – TRPV1 antagonist [32]
Cannabinoid receptor modulators[edit]
- ABX-1431 – selective monoacylglycerol lipase inhibitor[33]
- Cannabidiol (CBD) – cannabinoid receptor modulator [34][35]
- Cannabidivarin (CBDV; GWP-42006) – cannabinoid receptor modulator [36]
- CMX-020 – TRPV1 modulator as well as CB1 and CB2 receptor modulator [37]
- Dronabinol (Δ9-THC; ECP022A, Namisol) – CB1 and CB2 receptor agonist [38][39]
- Nabilone – CB1 and CB2 receptor agonist [40]
- NEO-1940 – CB1 and CB2 receptor agonist [41]
- Olorinab (APD-371) – CB2 receptor agonist [42]
Nerve growth factor inhibitors[edit]
- Fasinumab (REGN-475, SAR-164877) – monoclonal antibody against nerve growth factor[43]
- Frunevetmab (NV-02) – monoclonal antibody against nerve growth factor for cats [44]
- Fulranumab (AMG-403, JNJ-42160443) – monoclonal antibody against nerve growth factor [45]
- GBR-900 – monoclonal antibody against TrkA[46]
- GZ-389988 – TrkA, TrkB, and TrkC kinase inhibitor[47]
- LEVI-04 (p75NTR-Fc) – LNGF receptor (p75NTR) fusion protein and decoy receptor for nerve growth factor [48]
- NRD135S-E1 – tyrosine kinase modulator[49][50]
- ONO-4474 – peripherally selective TrkA, TrkB, and TrkC kinase inhibitor[51]
- Ranevetmab (NV-01) – monoclonal antibody against nerve growth factor for dogs [52]
- Tanezumab (PF-4383119, RI-624, RN-624) – monoclonal antibody against nerve growth factor [53]
- VM-902A – selective, peripherally selective allosteric inhibitor of TrkA [54]
Others[edit]
- ALLOD-2 – undefined mechanism of action [55]
- CR-4056 – imidazoline I2 receptor agonist [56]
- E-52862 (MR-309; S1A; S1RA) – sigma-1 receptor antagonist [57]
- HSP-3150 – undefined mechanism of action [58]
- PAX-01 – undefined mechanism of action [59]
See also[edit]
References[edit]
- ^ Zhu L, et al. Novel Opioid-Receptor Agonists with Reduced Morphine-like Side Effects. Mini Rev Med Chem. 2018 Jul 16. . doi:10.2174/1389557518666180716124336. PMID 30009707. Missing or empty
|title=(help) - ^ 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
- ^ Keppel Hesselink, Jan M. (2017). "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 of Medicine and Therapeutics. 1 (1). doi:10.15761/JMT.1000104. ISSN 2399-9799.
- ^ 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.
- ^ 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.
