vixotrigine: a sodium channel blocker [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 16046068 |
| CHEMBL ID | 3544913 |
| SCHEMBL ID | 310473 |
| MeSH ID | M000598720 |
| Synonym |
|---|
| SCHEMBL310473 |
| (5r)-5-(4-{[(2-fluorophenyl)methyl]oxy}phenyl)-l-prolinamide |
| (5r)-5-(4-[2-fluorobenzyloxy]phenyl)-l-prolinamide |
| JESCETIFNOFKEU-SJORKVTESA-N |
| biib 074,vixotrigine |
| gsk2 |
| (2s,5r)-5-(4-(2-fluorobenzyloxy)phenyl)pyrrolidine-2-carboxamide |
| vixotrigine [usan] |
| unii-qqs4j85k6y |
| vixotrigine |
| gsk-1014802 |
| cnv-1014802 |
| gsk1014802 |
| raxatrigine |
| raxatrigine [usan] |
| cnv 1014802 |
| 2-pyrrolidinecarboxamide, 5-(4-((2-fluorophenyl)methoxy)phenyl)-, (2s,5r)- |
| gsk 1014802 |
| biib 074 |
| biib074 |
| qqs4j85k6y , |
| cnv1014802 , |
| 934240-30-9 |
| AC-31665 |
| HY-12796 |
| (2s,5r)-5-(4-((2-fluorobenzyl)oxy)phenyl)pyrrolidine-2-carboxamide |
| CHEMBL3544913 |
| vixotrigine [inn] |
| (2s,5r)-5-(4-((2-fluorophenyl)methoxy)phenyl)pyrrolidine-2-carboxamide |
| vixotrigine [who-dd] |
| biib-074 |
| AKOS027324140 |
| bdbm50505255 |
| NCGC00386656-01 |
| DB11706 |
| raxatrigine (gsk1014802) |
| 934240-30-9 (free base). |
| gtpl12645 |
| raxatrigine (deleted inn) |
| compound 20 [pmid: 32945812] |
| cnv1014802; gsk-1014802; raxatrigine |
| EX-A2232 |
| Q18386159 |
| gsk-1014802;cnv1014802 |
| 2-pyrrolidinecarboxamide, 5-[4-[(2-fluorophenyl)methoxy]phenyl]-, (2s,5r)- |
| (2s,5r)-5-[4-[(2-fluorophenyl)methoxy]phenyl]pyrrolidine-2-carboxamide |
| N11408 |
| vixotrigine (usan/inn) |
| D11179 |
| (5r)-5-{4-[(2-fluorobenzyl)oxy]phenyl}-l-prolinamide;cnv1014802 |
| A857124 |
| AS-56210 |
| DTXSID901031867 |
| (2~{s},5~{r})-5-[4-[(2-fluorophenyl)methoxy]phenyl]pyrrolidine-2-carboxamide |
| TB4 , |
CNV1014802 is a novel sodium channel blocker that is being assessed in the treatment of trigeminal neuralgia.
| Excerpt | Reference | Relevance |
|---|---|---|
| "CNV1014802 is a novel sodium channel blocker that is being assessed in the treatment of trigeminal neuralgia." | ( Novel design for a phase IIa placebo-controlled, double-blind randomized withdrawal study to evaluate the safety and efficacy of CNV1014802 in patients with trigeminal neuralgia. Ettlin, DA; Giblin, GM; Gunn, K; Morisset, V; Obermann, M; Palmer, J; Tate, S; Zakrzewska, JM, 2013) | 1.32 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Safety and adverse event endpoints are described." | ( Novel design for a phase IIa placebo-controlled, double-blind randomized withdrawal study to evaluate the safety and efficacy of CNV1014802 in patients with trigeminal neuralgia. Ettlin, DA; Giblin, GM; Gunn, K; Morisset, V; Obermann, M; Palmer, J; Tate, S; Zakrzewska, JM, 2013) | 0.59 |
| " BIIB074 was well tolerated, with similar adverse events in the double-blind phase to placebo." | ( Safety and efficacy of a Nav1.7 selective sodium channel blocker in patients with trigeminal neuralgia: a double-blind, placebo-controlled, randomised withdrawal phase 2a trial. Bendtsen, L; Cruccu, G; Derjean, D; Estacion, M; Ettlin, DA; Giblin, GM; Gunn, K; Layton, G; Morisset, V; Obermann, M; Palmer, J; Tate, S; Waxman, SG; Zakrzewska, JM, 2017) | 0.46 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
| " The final model included covariates of age, weight and carbamazepine co-administration on clearance, weight on central volume of distribution, food on absorption rate constant and formulation and Japanese race on bioavailability." | ( Population Pharmacokinetics of Vixotrigine in Healthy Volunteers and Subjects with Trigeminal Neuralgia, Painful Lumbosacral Radiculopathy and Erythromelalgia. Bockbrader, H; Chapel, S; Cleall, S; Forrestal, F; Naik, H; Zhao, Y, 2021) | 0.62 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " Each dosing period was preceded by 1 inpatient visit and 1 outpatient baseline visit." | ( Effects of a State- and Use-Dependent Nav1.7 Channel Blocker on Ambulatory Blood Pressure: A Randomized, Controlled Crossover Study. Ballow, CH; Fong, R; Naik, H; Palmer, J; Steiner, D; White, WB, 2019) | 0.51 |
| " When sodium channel blockers cannot reach full dosage because of side effects, an add-on treatment with lamotrigine or baclofen should be considered." | ( Current and Innovative Pharmacological Options to Treat Typical and Atypical Trigeminal Neuralgia. Cruccu, G; Di Stefano, G; Truini, A, 2018) | 0.48 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 15.0916 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Sodium channel protein type 1 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 22.0000 | 0.0023 | 2.8296 | 9.0000 | AID1525388 |
| Sodium channel protein type 4 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0001 | 3.5075 | 10.0000 | AID1525391 |
| Sodium channel protein type 7 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 32.0000 | 0.0360 | 3.7335 | 9.0000 | AID1525384 |
| Sodium channel protein type 5 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 84.0000 | 0.0003 | 3.6484 | 9.2000 | AID1525392 |
| Sodium channel protein type 2 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 13.0000 | 0.0000 | 3.7401 | 10.0000 | AID1525389 |
| Sodium channel protein type 3 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 23.0000 | 0.0053 | 2.8085 | 9.0000 | AID1525390 |
| Sodium channel protein type 8 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 15.0000 | 0.0011 | 3.4705 | 9.0000 | AID1525393 |
| Sodium channel protein type 10 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 0.0080 | 3.1752 | 9.0000 | AID1525394 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1525399 | Selectivity index, ratio of IC50 for inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay to IC50 for inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19 | Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na |
| AID1525401 | Selectivity index, ratio of IC50 for inhibition of human Nav1.8 expressed in HEK293 cells by electrophysiology assay to IC50 for inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19 | Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na |
| AID1525389 | Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19 | Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na |
| AID1525394 | Inhibition of human Nav1.8 expressed in HEK293 cells by electrophysiology assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19 | Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na |
| AID1525384 | Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19 | Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na |
| AID1525397 | Selectivity index, ratio of IC50 for inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay to IC50 for inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19 | Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na |
| AID1525395 | Selectivity index, ratio of IC50 for inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay to IC50 for inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19 | Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na |
| AID1525392 | Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19 | Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na |
| AID1525388 | Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19 | Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na |
| AID1525396 | Selectivity index, ratio of IC50 for inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay to IC50 for inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19 | Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na |
| AID1525398 | Selectivity index, ratio of IC50 for inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay to IC50 for inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19 | Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na |
| AID1525393 | Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19 | Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na |
| AID1525400 | Selectivity index, ratio of IC50 for inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay to IC50 for inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19 | Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na |
| AID1525390 | Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19 | Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na |
| AID1525391 | Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19 | Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 10 (55.56) | 24.3611 |
| 2020's | 8 (44.44) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (19.05) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 5 (27.78%) | 5.53% |
| Reviews | 4 (22.22%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 9 (50.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||