revefenacin: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 11753673 |
| CHEMBL ID | 3833319 |
| SCHEMBL ID | 356480 |
| MeSH ID | M0587924 |
| Synonym |
|---|
| S5258 |
| SCHEMBL356480 |
| CS-7743 |
| yupelri |
| gsk-1160724 |
| 1-(2-(4-((4-carbamoylpiperidin-1-yl)methyl)-n-methylbenzamido)ethyl)piperidin-4-yl n-((1,1'-biphenyl)-2-yl)carbamate |
| revefenacin [who-dd] |
| revefenacin [mi] |
| biphenyl-2-ylcarbamic acid, 1-(2-((4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl)methylamino)ethyl)piperidin-4-yl ester |
| revefenacin [inn] |
| revefenacin [usan] |
| G2AE2VE07O , |
| revefenacin |
| 864750-70-9 |
| revefenacin [orange book] |
| carbamic acid, n-(1,1'-biphenyl)-2-yl-, 1-(2-((4-((4-(aminocarbonyl)-1-piperidinyl)methyl)benzoyl)methylamino)ethyl)-4-piperidinyl ester |
| td-4208 |
| gsk1160724 |
| revefenacin [usan:inn] |
| biphenyl-2-ylcarbamic acid 1-(2-((4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl)methylamino)ethyl)piperidin-4-yl ester |
| revefenacin [usan:inn:who-dd] |
| unii-g2ae2ve07o |
| CHEMBL3833319 |
| 1-(2-(3-((4-carbamoylpiperidin-1-yl)methyl)-n-methylbenzamido)ethyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate |
| D10978 |
| revefenacin (usan/inn) |
| EX-A1722 |
| td-4208; gsk-1160724;[1-[2-[[4-[(4-carbamoylpiperidin-1-yl)methyl]benzoyl]-methylamino]ethyl]piperidin-4-yl] n-(2-phenylphenyl)carbamate |
| 1-(2-(4-((4-carbamoylpiperidin-1-yl)methyl)-n-methylbenzamido)ethyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate |
| HY-15851 |
| DB11855 |
| revefenacin;gsk1160724 |
| revefenacin; td 4208; td4208; gsk-1160724; gsk1160724; gsk 1160724 |
| BCP15793 |
| 864750-70-9 (free base) |
| BS-18189 |
| [1-[2-[[4-[(4-carbamoylpiperidin-1-yl)methyl]benzoyl]-methylamino]ethyl]piperidin-4-yl] n-(2-phenylphenyl)carbamate |
| gtpl10129 |
| td4208 |
| AMY16789 |
| SB17262 |
| HMS3886K17 |
| CCG-270187 |
| Q27278649 |
| A903445 |
| td-4208; td 4208; td4208; gsk-1160724; gsk1160724;1-(2-(4-((4-carbamoylpiperidin-1-yl)methyl)-n-methylbenzamido)ethyl)piperidin-4-yl n-((1,1'-biphenyl)-2-yl)carbamate |
| AKOS037649398 |
| DTXSID701027775 |
| revefenacine |
| revefenacinum |
| revefenacina |
| r03bb08 |
| 1-[2-(1-{4-[(4-carbamoylpiperidin-1-yl)methyl]phenyl}-n-methylformamido)ethyl]piperidin-4-yl n-{[1,1'-biphenyl]-2-yl}carbamate |
| EN300-20352165 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Treatment-emergent adverse events (AEs) were comparable across all treatment groups (n [%] patients; revefenacin 88 μg, 272 [74." | ( Revefenacin, a once-daily, lung-selective, long-acting muscarinic antagonist for nebulized therapy: Safety and tolerability results of a 52-week phase 3 trial in moderate to very severe chronic obstructive pulmonary disease. Barnes, CN; Crater, G; Dean, L; Donohue, JF; Haumann, B; Kerwin, E; Moran, EJ; Pendyala, S; Sethi, S, 2019) | 0.51 |
| " There were four major adverse cardiac events (MACEs) in Study 0126 (one, two, and one in the placebo, revefenacin 88 μg, and revefenacin 175 μg groups, respectively), no MACEs in Study 0127 and 26 MACEs in Study 0128 (9, 10 and 7 in the revefenacin 88 μg, revefenacin 175 μg and tiotropium groups, respectively)." | ( Cardiovascular safety of revefenacin, a once-daily, lung-selective, long-acting muscarinic antagonist for nebulized therapy of chronic obstructive pulmonary disease: Evaluation in phase 3 clinical trials. Barnes, CN; Bourdet, D; Crater, G; Donohue, JF; Feldman, G; Pendyala, S; Sethi, S, 2019) | 0.51 |
| " Combined results showed that there were no significant differences between COPD patients receiving 175 μg revefenacin and those receiving a placebo, concerning the risk of discontinuation due to adverse events (AEs), any all-grade AE, or any serious AE." | ( Safety evaluation of revefenacin at the approved dose in patients with chronic obstructive pulmonary disease: A meta-analysis. Liu, B; Luo, W; Zan, S, ) | 0.13 |
| "Revefenacin at the approved dose is generally well-tolerated and safe with minimal AEs, which supports its use as a once-daily nebulized LAMA for the treatment of moderate to severe stable COPD." | ( Safety evaluation of revefenacin at the approved dose in patients with chronic obstructive pulmonary disease: A meta-analysis. Liu, B; Luo, W; Zan, S, ) | 0.13 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Here we report pharmacokinetic (PK) and safety results from two multicenter, open-label, single-dose trials evaluating revefenacin in subjects with severe renal impairment (NCT02578082) and moderate hepatic impairment (NCT02581592)." | ( Pharmacokinetics and safety of revefenacin in subjects with impaired renal or hepatic function. Barnes, CN; Borin, MT; Bourdet, DL; Lo, A; Pendyala, S, 2019) | 0.51 |
| " The objectives of this analysis were to evaluate the pharmacokinetics of revefenacin and its major metabolite (THRX-195518) in patients with chronic obstructive pulmonary disease, and identify significant covariates affecting revefenacin disposition using a population pharmacokinetic approach based on plasma concentration-time data obtained after single- and repeated-dose once-daily administration in three phase II and two phase III studies." | ( Population Pharmacokinetics of Revefenacin in Patients with Chronic Obstructive Pulmonary Disease. Borin, MT; Bourdet, DL; Lo, A, 2021) | 0.62 |
| " Pharmacokinetic parameters for THRX-195518 were estimated using a sequential approach, where the concentration-time profiles were fit to a combined model." | ( Population Pharmacokinetics of Revefenacin in Patients with Chronic Obstructive Pulmonary Disease. Borin, MT; Bourdet, DL; Lo, A, 2021) | 0.62 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " The estimated 24-hour potency (expressed as concentration of dosing solution) was 45." | ( In vivo pharmacological characterization of TD-4208, a novel lung-selective inhaled muscarinic antagonist with sustained bronchoprotective effect in experimental animal models. Hegde, SS; Jaw-Tsai, S; Ji, Y; Martin, WJ; McNamara, A; Obedencio, GP; Pulido-Rios, MT, 2013) | 0.65 |
| " Revefenacin is the first once-daily dosed nebulized long-acting muscarinic antagonist indicated for the maintenance treatment of patients with COPD." | ( Revefenacin for the treatment of chronic obstructive pulmonary disease. Li, F; Yang, J, 2019) | 0.51 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | Ki | 0.0050 | 0.0000 | 0.6902 | 10.0000 | AID1341905; AID1341906 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | Ki | 0.0050 | 0.0000 | 0.5405 | 7.7600 | AID1341904; AID1341907 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| G protein-coupled acetylcholine receptor activity | Muscarinic acetylcholine receptor M2 | Homo sapiens (human) |
| arrestin family protein binding | Muscarinic acetylcholine receptor M2 | Homo sapiens (human) |
| G protein-coupled serotonin receptor activity | Muscarinic acetylcholine receptor M2 | Homo sapiens (human) |
| phosphatidylinositol phospholipase C activity | Muscarinic acetylcholine receptor M3 | Homo sapiens (human) |
| protein binding | Muscarinic acetylcholine receptor M3 | Homo sapiens (human) |
| G protein-coupled acetylcholine receptor activity | Muscarinic acetylcholine receptor M3 | Homo sapiens (human) |
| signaling receptor activity | Muscarinic acetylcholine receptor M3 | Homo sapiens (human) |
| acetylcholine binding | Muscarinic acetylcholine receptor M3 | Homo sapiens (human) |
| G protein-coupled serotonin receptor activity | Muscarinic acetylcholine receptor M3 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| 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 | 11 (55.00) | 24.3611 |
| 2020's | 9 (45.00) | 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 (16.28) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 7 (29.17%) | 5.53% |
| Reviews | 7 (29.17%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 10 (41.67%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||