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- | Kerendia (finerenone) / Bayer, apararenone (MT-3995) / Mitsubishi Tanabe
Journal: Insights into drug development with quantitative systems pharmacology: A prospective case study of uncovering hyperkalemia risk in diabetic nephropathy with virtual clinical trials. (Pubmed Central) - Jun 22, 2024
A QSP model for generating virtual patients with diabetic nephropathy was used to quantitatively assess that the nonsteroidal MRAs, finerenone and apararenone, have a lower risk of hyperkalemia than the steroidal MRA, eplerenone. Prospective simulation studies using a QSP model are useful to prioritize pharmaceutical candidates in clinical development and validate mechanism-based pharmacological concepts related to the risk-benefit, before conducting large-scale clinical trials.
- || Clinical, Journal: Renal effects and safety between Asian and non-Asian chronic kidney disease and type 2 diabetes treated with nonsteroidal mineralocorticoid antagonists. (Pubmed Central) - May 16, 2024
Prospective simulation studies using a QSP model are useful to prioritize pharmaceutical candidates in clinical development and validate mechanism-based pharmacological concepts related to the risk-benefit, before conducting large-scale clinical trials. Nonsteroidal MRAs exhibited significant renal benefits by decreasing UACR and lowering SBP in Asian than that of non-Asian patients with CKD and T2DM, without increase of adverse events except hyperkalemia and eGFR decrease ?30%.
- || Minnebro (esaxerenone) / Daiichi Sankyo, Kerendia (finerenone) / Bayer, apararenone (MT-3995) / Mitsubishi Tanabe
Review, Journal: Non-steroidal mineralocorticoid receptor antagonists in patients with chronic kidney disease and type 2 diabetes. (Pubmed Central) - Jan 9, 2024
Hyperkalaemia was the most notable treatment-related adverse event and could generally be managed through serum potassium monitoring and dose adjustments. The nsMRAs are now an important component of recommended treatment for CKD associated with T2D, providing a significant reduction in the risk of cardiorenal progression beyond what can be achieved with glucose and blood pressure control.
- || Review, Journal: Cardiovascular and Renal Benefit of Novel Non-steroidal Mineralocorticoid Antagonists in Patients with Diabetes. (Pubmed Central) - Nov 22, 2023
Selected candidates of this drug class reduced UACR in patients with varying degrees of CKD and T2D and have shown convincing cardiorenal protection, in particular finerenone. Furthermore, finerenone is currently tested in patients with heart failure with preserved ejection fraction.
- | Minnebro (esaxerenone) / Daiichi Sankyo, Kerendia (finerenone) / Bayer, apararenone (MT-3995) / Mitsubishi Tanabe
Journal: Efficacy and safety assessment of mineralocorticoid receptor antagonists in patients with chronic kidney disease. (Pubmed Central) - Sep 7, 2023
Compared to placebo, Apararenone, Esaxerenone, and Finerenone might ameliorate albuminuria in CKD patients without causing elevated serum potassium levels. Remarkably, Finerenone conferred a cardiovascular benefit, and Spironolactone lowered blood pressure in CKD patients.
- || Review, Journal: Therapeutic perspective-evolving evidence of nonsteroidal mineralocorticoid receptor antagonists in diabetic kidney disease. (Pubmed Central) - Jun 5, 2023
This review summarizes the effects of pharmacological MR blockade on diabetes and diabetes-associated CKD, with a particular focus on the therapeutic mechanisms of NS-MRAs in preclinical studies and ongoing clinical studies. Further investigation of combined treatment with renoprotective drugs and NS-MRAs to improve treatment of DKD is needed.
- || Minnebro (esaxerenone) / Daiichi Sankyo, Kerendia (finerenone) / Bayer, apararenone (MT-3995) / Mitsubishi Tanabe
Clinical, Retrospective data, Review: Network meta-analysis of mineralocorticoid receptor antagonists for diabetic kidney disease. (Pubmed Central) - Oct 4, 2022
This Bayesian network meta-analysis was the first to explore the optimal alternative among MRAs in the treatment of DKD and revealed the superiority of 20 mg of finerenone among MRAs in treating DKD. Systematic Review Registration: PROSPERO, identifier (CRD42022313826).
- || Minnebro (esaxerenone) / Daiichi Sankyo, Kerendia (finerenone) / Bayer, apararenone (MT-3995) / Mitsubishi Tanabe
Retrospective data, Review: Efficacy and Safety of Non-Steroidal Mineralocorticoid Receptor Antagonists in Patients With Chronic Kidney Disease and Type 2 Diabetes: A Systematic Review Incorporating an Indirect Comparisons Meta-Analysis. (Pubmed Central) - Jul 6, 2022
Esaxerenone and apararenone may have better antihypertensive effects than finerenone. The head-to-head RCTs are still needed to compare the differences of the efficacy and safety in these non-steroidal MRAs.
- | apararenone (MT-3995) / Mitsubishi Tanabe
Journal: Discovery of Apararenone (MT-3995) as a Highly Selective, Potent, and Novel Nonsteroidal Mineralocorticoid Receptor Antagonist. (Pubmed Central) - Jun 25, 2022
We discovered that the novel 1,4-benzoxazin-3-one derivative 19 (apararenone: MT-3995) acted as a highly selective and potent nonsteroidal MRA. Apararenone exhibited a more potent antihypertensive and organ-protective activity than steroidal MRA eplerenone in a primary aldosteronism rat model obtained by infusing aldosterone in uninephrectomized rats.
- || Review, Journal: Novel Non-Steroidal Mineralocorticoid Receptor Antagonists in Cardiorenal Disease. (Pubmed Central) - Jun 11, 2022
To better understand the non-steroidal MRAs, this review provides information on the molecular pharmacology as well as relevant current preclinical and clinical data on cardiorenal outcomes. A comparative review of all compounds in the class is discussed with regard to clinical efficacy and safety as well as a perspective outlining their future use in clinical practice.
- || spironolactone / Generic mfg.
Review, Journal: Role of mineralocorticoid receptor antagonists in kidney diseases. (Pubmed Central) - Mar 30, 2022
Mineralocorticoid receptor (MR) antagonists, for example, spironolactone and eplerenone, are in clinical use to treat hypertension...Other nonsteroidal MRA such as apararenone, finerenone, AZD9977, and LY2623091 are in different clinical trials in patients with hypertension suffering from renal or hepatic fibrotic diseases...The new generation nonsteroidal MRAs like esaxerenone are less likely to cause hyperkalemia at therapeutic doses. It appears that the nonsteroidal MRAs can provide optimum therapeutic benefit for patients suffering from kidney diseases.
- || apararenone (MT-3995) / Mitsubishi Tanabe
Clinical, P1 data, PK/PD data, Journal: Phase 1 Studies to Define the Safety, Tolerability, and Pharmacokinetic and Pharmacodynamic Profiles of the Nonsteroidal Mineralocorticoid Receptor Antagonist Apararenone in Healthy Volunteers. (Pubmed Central) - Mar 25, 2022
Apararenone suppressed the decrease in urinary sodium and potassium ion ratio that occurs after loading with fludrocortisone. These studies support the mechanism of action of apararenone as an MRA, and further clinical development is warranted.
- | spironolactone / Generic mfg.
Journal, Combination therapy: Nonsteroidal Mineralocorticoid Receptor Antagonism for cardiovascular and renal disorders - new perspectives for combination therapy. (Pubmed Central) - Mar 3, 2022
Spironolactone was launched as the first antagonist of aldosterone 27 years before the MR was cloned...The second steroidal MR antagonist was eplerenone which was discovered at a time when the role of aldosterone and MR in cardiac fibrosis was rediscovered...Addition of the nonsteroidal MRA finerenone to optimal RAS blockade recently reduced CV and kidney outcomes in two large phase III trials in patients with chronic kidney disease (CKD) and type 2 diabetes (T2D). We provide an outlook on further opportunities for combination therapy of nonsteroidal MRA finerenone with RAS inhibitors and sodium-glucose cotransporter-2 inhibitors (SGLT2i).
- |||| FDA event: Posttest Poll 3⃣ Which nonsteroidal treatment option for #CKD associated with T2DM was recently FDA-approved? A. Finerenone B. Apararenone C. Esaxerenone D. Spironolactone (Twitter) - Jan 25, 2022
- ||| Minnebro (esaxerenone) / Daiichi Sankyo, Kerendia (finerenone) / Bayer, apararenone (MT-3995) / Mitsubishi Tanabe
Clinical, FDA event: New & Emerging Treatment Options May Improve Patient Outcomes in #CKD ➡️ Newer nonsteroidal agents = improvement vs steroidal agents ➡️ In US, FDA approved finerenone, July 2021 ➡️ Clinical trial data looks promising for 2 nonsteroidal agents: apararenone & esaxerenone (Twitter) - Jan 25, 2022
- ||| 3⃣ Which of the following nonsteroidal mineralocorticoid receptor agents was recently approved for treatment of adults w/ CKD associated w/ T2DM? A. Finerenone B. Apararenone C. Spironolactone D. Esaxerenone (Twitter) - Jan 18, 2022
- |||| Minnebro (esaxerenone) / Daiichi Sankyo, Kerendia (finerenone) / Bayer, apararenone (MT-3995) / Mitsubishi Tanabe
Clinical: ⚡️ Newer nonsteroidal agents = improvement vs steroidal agents as tx target for renal disease ⚡️ Clinical trial data appears promising for 2 emerging nonsteroidal agents: apararenone & esaxerenone ⚡️ Finerenone & esaxerenone approved for HTN in Japan #CKD (Twitter) - Jan 18, 2022
- || apararenone (MT-3995) / Mitsubishi Tanabe
Clinical, P2 data, Journal: Apararenone in patients with diabetic nephropathy: results of a randomized, double-blind, placebo-controlled phase 2 dose-response study and open-label extension study. (Pubmed Central) - Nov 4, 2021
P2
We provide an outlook on further opportunities for combination therapy of nonsteroidal MRA finerenone with RAS inhibitors and sodium-glucose cotransporter-2 inhibitors (SGLT2i). The UACR-lowering effect of apararenone administered once daily for 24 weeks in patients with stage 2 DN was confirmed, and the 52-week administration was safe and tolerable.
- || apararenone (MT-3995) / Mitsubishi Tanabe
Clinical, Journal: Efficacy and safety of apararenone (MT-3995) in patients with nonalcoholic steatohepatitis: A randomized controlled study. (Pubmed Central) - Jul 15, 2021
In patients with NASH, apararenone 10 mg/day for 72 weeks was effective in decreasing ALT levels, improved multiple potential fibrosis markers and was safe and well tolerated. Pathological findings showed anti-inflammatory and antifibrotic effects of apararenone.
- || spironolactone / Generic mfg.
Review, Journal: Mineralocorticoid Receptor Antagonists in Diabetic Kidney Disease. (Pubmed Central) - Jul 4, 2021
Non-steroidal MRA still block the damaging effects of mineralocorticoid receptor overactivation (extracellular fluid volume expansion, inflammation, fibrosis), but with fewer side effects (hormonal, hyperkalemia) than steroidal MRA. This review article summarizes the current knowledge and newer research conducted on MRA in DKD.
- | Minnebro (esaxerenone) / Daiichi Sankyo, finerenone (BAY-94-8862) / Bayer, apararenone (MT-3995) / Mitsubishi Tanabe
Review, Journal: New mineralocorticoid receptor antagonists: update on their use in chronic kidney disease and heart failure. (Pubmed Central) - Jun 8, 2021
For this reason, nonsteroidal MRA represent an interesting new therapeutic approach for the prevention of CHF and CKD progression. Some basic research findings also yielded interesting results in acute clinical settings such as myocardial infarction and acute kidney injury.
- || apararenone (MT-3995) / Mitsubishi Tanabe
Clinical, P1 data, Journal: Drug-Drug Interactions of the Nonsteroidal Mineralocorticoid Receptor Antagonist Apararenone with Midazolam, Warfarin, and Digoxin: A Phase 1 Studies in Healthy Volunteers. (Pubmed Central) - Apr 27, 2021
P1
The findings from this analysis of data from healthy volunteers suggest minimal risk for potential drug-drug interactions between apararenone and other drugs that are likely to be used concurrently in patients. ClinicalTrials.gov identifier: NCT02531568.
- apararenone (MT-3995) / Mitsubishi Tanabe
[VIRTUAL] MT-3995, A NOVEL NON-STEROIDAL MINERALOCORTICOID RECEPTOR ANTAGONIST, HAS BENEFICIAL EFFECTS ON THE PROGRESSION OF NON-ALCOHOLIC STEATOHEPATITIS IN CHOLINE-DEFICIENT L-AMINO ACID-DEFINED DIET-FED F344 RATS AND TRANS-FAT DIET-FED OB/OB MICE. () - Nov 2, 2020 - Abstract #AASLD2020AASLD_2103;
We showed, for the first time, that MT-3995, a non-steroidal MR antagonist, has the beneficial effect on the development of steatohepatitis and hepatic fibrosis in rodent NASH models. MT-3995 could be a novel therapeutic approach for the treatment of NASH.
- | apararenone (MT-3995) / Mitsubishi Tanabe
Trial completion: Efficacy and Safety of MT-3995 in Patients With Non-Alcoholic Steatohepatitis(NASH) (clinicaltrials.gov) - Sep 6, 2019
P2, N=48, Completed, Sponsor: Mitsubishi Tanabe Pharma Corporation
MT-3995 could be a novel therapeutic approach for the treatment of NASH. Active, not recruiting --> Completed
- apararenone (MT-3995) / Mitsubishi Tanabe
Trial primary completion date: Efficacy and Safety of MT-3995 in Patients With Non-Alcoholic Steatohepatitis(NASH) (clinicaltrials.gov) - Dec 2, 2017
P2, N=40, Active, not recruiting, Sponsor: Mitsubishi Tanabe Pharma Corporation
Active, not recruiting --> Completed Trial primary completion date: Oct 2017 --> Mar 2018
- |||| apararenone (MT-3995) / Mitsubishi Tanabe
Trial completion, Trial primary completion date: An Extended Treatment Study of MT-3995 in Patients With Diabetic Nephropathy (clinicaltrials.gov) - Sep 18, 2017
P2, N=241, Completed, Sponsor: Mitsubishi Tanabe Pharma Corporation
Trial primary completion date: Oct 2017 --> Mar 2018 Active, not recruiting --> Completed | Trial primary completion date: Apr 2018 --> Aug 2017
- | apararenone (MT-3995) / Mitsubishi Tanabe
Enrollment closed: Efficacy and Safety of MT-3995 in Patients With Non-Alcoholic Steatohepatitis(NASH) (clinicaltrials.gov) - Sep 11, 2017
P2, N=40, Active, not recruiting, Sponsor: Mitsubishi Tanabe Pharma Corporation
Active, not recruiting --> Completed | Trial primary completion date: Apr 2018 --> Aug 2017 Recruiting --> Active, not recruiting
- |||| apararenone (MT-3995) / Mitsubishi Tanabe
Trial completion, Trial primary completion date: Efficacy and Safety of MT-3995 in Patients With Diabetic Nephropathy (clinicaltrials.gov) - Mar 3, 2017
P2, N=293, Completed, Sponsor: Mitsubishi Tanabe Pharma Corporation
Recruiting --> Active, not recruiting Active, not recruiting --> Completed | Trial primary completion date: Sep 2017 --> Nov 2016
- ||| apararenone (MT-3995) / Mitsubishi Tanabe
Enrollment closed: An Extended Treatment Study of MT-3995 in Patients With Diabetic Nephropathy (clinicaltrials.gov) - Feb 27, 2017
P2, N=280, Active, not recruiting, Sponsor: Mitsubishi Tanabe Pharma Corporation
Active, not recruiting --> Completed | Trial primary completion date: Sep 2017 --> Nov 2016 Recruiting --> Active, not recruiting
- apararenone (MT-3995) / Mitsubishi Tanabe
Trial completion: Mass Balance Study of MT-3995 (clinicaltrials.gov) - Jan 31, 2017
P1, N=9, Completed, Sponsor: Mitsubishi Tanabe Pharma Corporation
Recruiting --> Active, not recruiting Active, not recruiting --> Completed
- apararenone (MT-3995) / Mitsubishi Tanabe
Enrollment closed: Mass Balance Study of MT-3995 (clinicaltrials.gov) - Oct 13, 2016
P1, N=9, Active, not recruiting, Sponsor: Mitsubishi Tanabe Pharma Corporation
Active, not recruiting --> Completed Recruiting --> Active, not recruiting
- | apararenone (MT-3995) / Mitsubishi Tanabe
New P2 trial: Efficacy and Safety of MT-3995 in Patients With Non-Alcoholic Steatohepatitis(NASH) (clinicaltrials.gov) - Oct 4, 2016
P2, N=40, Recruiting, Sponsor: Mitsubishi Tanabe Pharma Corporation
- ||| apararenone (MT-3995) / Mitsubishi Tanabe
Enrollment closed: Efficacy and Safety of MT-3995 in Patients With Diabetic Nephropathy (clinicaltrials.gov) - Oct 4, 2016
P2, N=280, Active, not recruiting, Sponsor: Mitsubishi Tanabe Pharma Corporation
Recruiting --> Active, not recruiting Recruiting --> Active, not recruiting
- apararenone (MT-3995) / Mitsubishi Tanabe
New P1 trial: Mass Balance Study of MT-3995 (clinicaltrials.gov) - Sep 14, 2016
P1, N=9, Recruiting, Sponsor: Mitsubishi Tanabe Pharma Corporation
- ||||| apararenone (MT-3995) / Mitsubishi Tanabe
New P2 trial: An Extended Treatment Study of MT-3995 in Patients With Diabetic Nephropathy (clinicaltrials.gov) - Feb 8, 2016
P2, N=280, Recruiting, Sponsor: Mitsubishi Tanabe Pharma Corporation
- | apararenone (MT-3995) / Mitsubishi Tanabe
Trial completion: Drug Interaction Study of Warfarin and MT-3995 (clinicaltrials.gov) - Oct 9, 2015
P1, N=20, Completed, Sponsor: Mitsubishi Tanabe Pharma Corporation
Recruiting --> Active, not recruiting Active, not recruiting --> Completed
- | apararenone (MT-3995) / Mitsubishi Tanabe
Trial completion: Safety, Tolerability and Pharmacokinetic Study of MT-3995 at a Low Dose in Subjects With Diabetic Nephropathy (clinicaltrials.gov) - Sep 16, 2015
P2, N=31, Completed, Sponsor: Mitsubishi Tanabe Pharma Corporation
Active, not recruiting --> Completed Active, not recruiting --> Completed
- | apararenone (MT-3995) / Mitsubishi Tanabe
New P1 trial: Drug Interaction Study of Warfarin and MT-3995 (clinicaltrials.gov) - Aug 24, 2015
P1, N=20, Active, not recruiting, Sponsor: Mitsubishi Tanabe Pharma Corporation
- ||||| apararenone (MT-3995) / Mitsubishi Tanabe
New P2 trial: Efficacy and Safety of MT-3995 in Patients With Diabetic Nephropathy (clinicaltrials.gov) - Aug 7, 2015
P2, N=280, Recruiting, Sponsor: Mitsubishi Tanabe Pharma Corporation
- | apararenone (MT-3995) / Mitsubishi Tanabe
Enrollment closed: Safety, Tolerability and Pharmacokinetic Study of MT-3995 at a Low Dose in Subjects With Diabetic Nephropathy (clinicaltrials.gov) - Apr 14, 2015
P2, N=30, Active, not recruiting, Sponsor: Mitsubishi Tanabe Pharma Corporation
Active, not recruiting --> Completed Recruiting --> Active, not recruiting
- | apararenone (MT-3995) / Mitsubishi Tanabe
Trial completion, Enrollment change, Trial primary completion date: A Study to Evaluate Pharmacodynamics, Safety, Tolerability and Pharmacokinetics of MT-3995 in Type II Diabetic Nephropathy Subjects With Albuminuria and Moderately Decreased GFR (clinicaltrials.gov) - Feb 9, 2015
P2, N=49, Completed, Sponsor: Mitsubishi Tanabe Pharma Corporation
Recruiting --> Active, not recruiting Active, not recruiting --> Completed | N=90 --> 49 | Trial primary completion date: Jan 2015 --> Sep 2014
- |||| apararenone (MT-3995) / Mitsubishi Tanabe
Trial completion, Enrollment change, Trial primary completion date: A Study to Evaluate Pharmacodynamics, Safety, Tolerability and Pharmacokinetics of MT-3995 in Type II Diabetic Nephropathy Subjects With Albuminuria (clinicaltrials.gov) - Feb 9, 2015
P2, N=67, Completed, Sponsor: Mitsubishi Tanabe Pharma Corporation
Active, not recruiting --> Completed | N=90 --> 49 | Trial primary completion date: Jan 2015 --> Sep 2014 Active, not recruiting --> Completed | N=90 --> 67 | Trial primary completion date: Nov 2014 --> Aug 2014
- |||| apararenone (MT-3995) / Mitsubishi Tanabe
Trial completion: Safety, Tolerability and Pharmacokinetic Study of MT-3995 in Subjects With Diabetic Nephropathy (clinicaltrials.gov) - Jan 28, 2015
P2, N=51, Completed, Sponsor: Mitsubishi Tanabe Pharma Corporation
Active, not recruiting --> Completed | N=90 --> 67 | Trial primary completion date: Nov 2014 --> Aug 2014 Active, not recruiting --> Completed
- ||| apararenone (MT-3995) / Mitsubishi Tanabe
Enrollment closed, Trial primary completion date: A Study to Evaluate Pharmacodynamics, Safety, Tolerability and Pharmacokinetics of MT-3995 in Type II Diabetic Nephropathy Subjects With Albuminuria and Moderately Decreased GFR (clinicaltrials.gov) - Sep 28, 2014
P2, N=90, Active, not recruiting, Sponsor: Mitsubishi Tanabe Pharma Corporation
Active, not recruiting --> Completed Recruiting --> Active, not recruiting | Trial primary completion date: Dec 2013 --> Jan 2015
- ||| apararenone (MT-3995) / Mitsubishi Tanabe
Enrollment closed, Trial primary completion date: A Study to Evaluate Pharmacodynamics, Safety, Tolerability and Pharmacokinetics of MT-3995 in Type II Diabetic Nephropathy Subjects With Albuminuria (clinicaltrials.gov) - Sep 28, 2014
P2, N=90, Active, not recruiting, Sponsor: Mitsubishi Tanabe Pharma Corporation
Recruiting --> Active, not recruiting | Trial primary completion date: Dec 2013 --> Jan 2015 Recruiting --> Active, not recruiting | Trial primary completion date: Dec 2013 --> Nov 2014
- | apararenone (MT-3995) / Mitsubishi Tanabe
Enrollment closed: Safety, Tolerability and Pharmacokinetic Study of MT-3995 in Subjects With Diabetic Nephropathy (clinicaltrials.gov) - Aug 19, 2014
P2, N=45, Active, not recruiting, Sponsor: Mitsubishi Tanabe Pharma Corporation
Recruiting --> Active, not recruiting | Trial primary completion date: Dec 2013 --> Nov 2014 Recruiting --> Active, not recruiting
- | apararenone (MT-3995) / Mitsubishi Tanabe
New P2 trial: Safety, Tolerability and Pharmacokinetic Study of MT-3995 at a Low Dose in Subjects With Diabetic Nephropathy (clinicaltrials.gov) - Aug 1, 2014
P2, N=30, Recruiting, Sponsor: Mitsubishi Tanabe Pharma Corporation
- | apararenone (MT-3995) / Mitsubishi Tanabe
Enrollment change: Safety, Tolerability and Pharmacokinetic Study of MT-3995 in Subjects With Diabetic Nephropathy (clinicaltrials.gov) - Feb 10, 2014
P2, N=45, Recruiting, Sponsor: Mitsubishi Tanabe Pharma Corporation
Recruiting --> Active, not recruiting N=30 --> 45
- | apararenone (MT-3995) / Mitsubishi Tanabe
Enrollment open: Safety, Tolerability and Pharmacokinetic Study of MT-3995 in Subjects With Diabetic Nephropathy (clinicaltrials.gov) - Aug 5, 2013
P2, N=45, Recruiting, Sponsor: Mitsubishi Tanabe Pharma Corporation
N=30 --> 45 Not yet recruiting --> Recruiting
- | apararenone (MT-3995) / Mitsubishi Tanabe
New P2 trial: Safety, Tolerability and Pharmacokinetic Study of MT-3995 in Subjects With Diabetic Nephropathy (clinicaltrials.gov) - Jun 26, 2013
P2, N=45, Recruiting, Sponsor: Mitsubishi Tanabe Pharma Corporation