finerenone: a potent, selective, and orally available nonsteroidal mineralocorticoid receptor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 60150535 |
| SCHEMBL ID | 8157011 |
| MeSH ID | M0579256 |
| Synonym |
|---|
| bay 94-8862 |
| bay94-8862 |
| finerenone |
| bay-94-8862 |
| 1050477-31-0 |
| finerenone [usan:inn] |
| unii-de2o63yv8r |
| de2o63yv8r , |
| (4s)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide |
| finerenone [orange book] |
| finerenone [jan] |
| 1,6-naphthyridine-3-carboxamide, 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-1,4-dihydro-2,8-dimethyl-, (4s)- |
| finerenone [who-dd] |
| finerenone [inn] |
| finerenone [usan] |
| kerendia |
| SCHEMBL8157011 |
| finerenone (jan/usan/inn) |
| D10633 |
| gtpl8678 |
| AC-30916 |
| DTXSID10146928 , |
| 1,6-naphthyridine-3-carboxamide, 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-1,4-dihydro-2,8-dimethyl-, (4s)-;1,6-naphthyridine-3-carboxamide, 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-1,4-dihydro-2,8-dimethyl-, (4s)- |
| bay94-8862; bay 94-8862; bay-94-8862; bay948862; bay 948862; bay-948862 |
| BCP24177 |
| HY-111372 |
| EX-A2845 |
| finerenone (bay 94-8862) |
| Q21099046 |
| CS-0040097 |
| AMY9115 |
| F53302 |
| MS-26172 |
| bay 948862 |
| bay-948862 |
| bay948862 |
| finerenonum |
| dtxcid5069419 |
| finerenona |
| (s)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Administration of finerenone 20 mg once daily confers no risk of clinically relevant drug-drug interactions with substrates of cytochrome P450 enzymes." | ( Results from Drug-Drug Interaction Studies In Vitro and In Vivo Investigating the Effect of Finerenone on the Pharmacokinetics of Comedications. Bairlein, M; Gerisch, M; Heinig, R; Loewen, S; Nagelschmitz, J, 2020) | 0.56 |
| " Here, we report the development of a physiologically-based pharmacokinetic (PBPK) model for finerenone and its application as a victim drug of cytochrome P450 3A4 (CYP3A4)-mediated drug-drug interactions (DDIs) using the open-source PBPK platform PK-Sim, which has recently been qualified for this application purpose." | ( Physiologically-based pharmacokinetic modeling to predict CYP3A4-mediated drug-drug interactions of finerenone. Eissing, T; Frechen, S; Gerisch, M; Heinig, R; Wendl, T, 2022) | 0.72 |
| "Administration of finerenone 40 mg once daily confers no risk of clinically relevant drug-drug interactions with substrates of BCRP, OATP1B1, or OATP1B3." | ( Results From Drug-Drug Interaction Studies In Vitro and In Vivo Investigating the Inhibitory Effect of Finerenone on the Drug Transporters BCRP, OATP1B1, and OATP1B3. Fricke, R; Heinig, R; Loewen, S; Nagelschmitz, J; Wertz, S, 2022) | 0.72 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Study 2 was a relative bioavailability study comparing a finerenone 10 mg immediate-release (IR) tablet with finerenone 10 mg PEG solution in the fasted state, investigating the effect of a high-fat/high-calorie meal on the pharmacokinetics of the IR tablet and assessing a further dose escalation to finerenone 80 mg (eight × finerenone 10 mg IR tablets), in an open-label, fourfold crossover design (n = 15)." | ( Pharmacokinetics, safety and tolerability of the novel, selective mineralocorticoid receptor antagonist finerenone - results from first-in-man and relative bioavailability studies. Heinig, R; Kimmeskamp-Kirschbaum, N; Lentini, S; Wensing, G, 2016) | 0.43 |
| " In vivo and in vitro studies were performed to assess absolute bioavailability of finerenone, the effect of metabolic enzyme inhibitors on the pharmacokinetics of finerenone and its metabolites, the quantitative contribution of the involved enzymes cytochrome P450 (CYP) 3A4 and CYP2C8 and the relevance of gut wall versus liver metabolism." | ( Pharmacokinetics of the Novel, Selective, Non-steroidal Mineralocorticoid Receptor Antagonist Finerenone in Healthy Volunteers: Results from an Absolute Bioavailability Study and Drug-Drug Interaction Studies In Vitro and In Vivo. Engelen, A; Gerisch, M; Heinig, R; Loewen, S; Nagelschmitz, J, 2018) | 0.48 |
| " Absolute bioavailability was assessed in volunteers receiving finerenone orally and by intravenous infusion (n = 15) and the effects of erythromycin (n = 15), verapamil (n = 13) and gemfibrozil (n = 16) on finerenone pharmacokinetics were investigated." | ( Pharmacokinetics of the Novel, Selective, Non-steroidal Mineralocorticoid Receptor Antagonist Finerenone in Healthy Volunteers: Results from an Absolute Bioavailability Study and Drug-Drug Interaction Studies In Vitro and In Vivo. Engelen, A; Gerisch, M; Heinig, R; Loewen, S; Nagelschmitz, J, 2018) | 0.48 |
| " Finerenone (FIN), a novel, nonsteroidal, potent, and selective mineralocorticoid receptor antagonist, improves endothelial dysfunction through enhancing nitric oxide (NO) bioavailability and decreasing superoxide anion levels due to an upregulation in vascular and renal superoxide dismutase activity." | ( Finerenone Reduces Intrinsic Arterial Stiffness in Munich Wistar Frömter Rats, a Genetic Model of Chronic Kidney Disease. Fernández-Alfonso, MS; Gil-Ortega, M; González-Blázquez, R; Kolkhof, P; Kreutz, R; Martín-Ramos, M; Pulido-Olmo, H; Ruilope, LM; Ruiz-Hurtado, G; Schulz, A; Somoza, B; Vega-Martín, E, 2020) | 0.56 |
| " MA from MWF-FIN exhibited higher NO bioavailability and reduced superoxide anion levels compared to MWF-C." | ( Finerenone Reduces Intrinsic Arterial Stiffness in Munich Wistar Frömter Rats, a Genetic Model of Chronic Kidney Disease. Fernández-Alfonso, MS; Gil-Ortega, M; González-Blázquez, R; Kolkhof, P; Kreutz, R; Martín-Ramos, M; Pulido-Olmo, H; Ruilope, LM; Ruiz-Hurtado, G; Schulz, A; Somoza, B; Vega-Martín, E, 2020) | 0.56 |
| " It is rapidly and completely absorbed and undergoes first-pass metabolism in the gut wall and liver resulting in a bioavailability of 43." | ( The Pharmacokinetics of the Nonsteroidal Mineralocorticoid Receptor Antagonist Finerenone. Eissing, T; Heinig, R, 2023) | 0.91 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Glucocorticoid receptor | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0000 | 0.4953 | 10.0000 | AID1440430 |
| Progesterone receptor | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0000 | 0.5807 | 10.0000 | AID1440426 |
| Mineralocorticoid receptor | Homo sapiens (human) | IC50 (µMol) | 0.0275 | 0.0003 | 0.7484 | 10.0000 | AID1440428; AID1440429; AID705916; AID722892 |
| Androgen receptor | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0000 | 0.8753 | 10.0000 | AID1440425 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1440422 | Ratio of IC50 for Gal4-fused human MR Ser810 mutant expressed in HEK293T cells to IC50 for Gal4-fused human MR expressed in HEK293T cells | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Modulating Mineralocorticoid Receptor with Non-steroidal Antagonists. New Opportunities for the Development of Potent and Selective Ligands without Off-Target Side Effects. |
| AID1440425 | Antagonist activity at GAL4-fused human AR LBD (667 to 919 residues) expressed in CHO-K1 cells assessed as inhibition of dihydrotestosterone-induced transactivation activity after 5 to 6 hrs by luciferase reporter gene assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Modulating Mineralocorticoid Receptor with Non-steroidal Antagonists. New Opportunities for the Development of Potent and Selective Ligands without Off-Target Side Effects. |
| AID722892 | Antagonist activity at mineralocorticoid receptor (unknown origin) | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Microwave-assisted synthesis of pyrimido[4,5-b][1,6]naphthyridin-4(3H)-ones with potential antitumor activity. |
| AID1440428 | Antagonist activity at Gal4-fused human MR LBD (734 to 985 residues) expressed in CHO-K1 cells after 5 to 6 hrs by luciferase reporter gene assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Modulating Mineralocorticoid Receptor with Non-steroidal Antagonists. New Opportunities for the Development of Potent and Selective Ligands without Off-Target Side Effects. |
| AID705911 | Binding affinity to Ca2+ channel L type by radioligand binding assay | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18 | Mineralocorticoid receptor antagonists for the treatment of hypertension and diabetic nephropathy. |
| AID1440427 | Ratio of IC50 for Gal4-fused human MR A773 mutant expressed in HEK293T cells to IC50 for Gal4-fused human MR expressed in HEK293T cells | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Modulating Mineralocorticoid Receptor with Non-steroidal Antagonists. New Opportunities for the Development of Potent and Selective Ligands without Off-Target Side Effects. |
| AID1440430 | Antagonist activity at GAL4-fused human GR LBD (443 to 777 residues) expressed in CHO-K1 cells assessed as inhibition of dexamethasone-induced transactivation activity after 5 to 6 hrs by luciferase reporter gene assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Modulating Mineralocorticoid Receptor with Non-steroidal Antagonists. New Opportunities for the Development of Potent and Selective Ligands without Off-Target Side Effects. |
| AID705916 | Antagonist activity against human mineralocorticoid receptor expressed in CHOK1 cells after 10 to 30 mins by luciferase reporter gene assay | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18 | Mineralocorticoid receptor antagonists for the treatment of hypertension and diabetic nephropathy. |
| AID1440426 | Antagonist activity at GAL4-fused human PR LBD (680 to 933 residues) expressed in CHO-K1 cells assessed as inhibition of progesterone-induced transactivation activity after 5 to 6 hrs by luciferase reporter gene assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Modulating Mineralocorticoid Receptor with Non-steroidal Antagonists. New Opportunities for the Development of Potent and Selective Ligands without Off-Target Side Effects. |
| AID1440452 | Induction of improvement in urinary albumin-creatinine ratio in patient with diabetic nephropathy receiving ACE inhibitor or angiotensin receptor blocker at 7.5 to 20 mg/day during latter phase II trial | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Modulating Mineralocorticoid Receptor with Non-steroidal Antagonists. New Opportunities for the Development of Potent and Selective Ligands without Off-Target Side Effects. |
| AID1440429 | Antagonist activity at Gal4-fused human MR LBD expressed in HEK293T cells assessed as inhibition of aldosterone-induced transactivation activity after 16 hrs by luciferase reporter gene assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Modulating Mineralocorticoid Receptor with Non-steroidal Antagonists. New Opportunities for the Development of Potent and Selective Ligands without Off-Target Side Effects. |
| AID1346902 | Human Mineralocorticoid receptor (3C. 3-Ketosteroid receptors) | 2012 | ChemMedChem, Aug, Volume: 7, Issue:8 | Discovery of BAY 94-8862: a nonsteroidal antagonist of the mineralocorticoid receptor for the treatment of cardiorenal diseases. |
| [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 | 46 (25.70) | 24.3611 |
| 2020's | 133 (74.30) | 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 (23.01) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 37 (20.22%) | 5.53% |
| Reviews | 55 (30.05%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 3 (1.64%) | 0.25% |
| Other | 88 (48.09%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||