A Multicentric, Randomized, Prospective, Double Blind, Parallel Group, Comparative, Active Controlled, Phase III Clinical Study to Evaluate the Efficacy, Safety And Tolerability Of Esaxerenone 5mg Versus Eplerenone 50mg In Patients With Uncontrolled Or Resistant Hypertension. - NIL

Start Date13 Feb 2025

Sponsor / Collaborator

Eris Lifesciences Ltd.

[+1]

CTRI/2024/12/077633

/ Not yet recruitingNot Applicable

A Randomized, open label, balanced, two treatments, two period, two sequence, single dose, crossover, bioequivalence study of Test product (T) Esaxerenone Tablet 5 mg of Eris Lifesciences Limited India with Reference product (R) MINNEBRO (Esaxerenone) Tablets 5 mg of Daiichi Sankyo Company, Limited in normal, healthy, adult, human subjects under fasting condition. - NIL

Start Date16 Dec 2024

Sponsor / Collaborator

Eris Lifesciences Ltd.

[+1]

JPRN-UMIN000037721

/ RecruitingNot ApplicableIIT

Effects of adding esaxerenone to calcium channel blocker in patients with essential hypertension. - Effects of adding esaxerenone to calcium channel blocker in patients with essential hypertension.

Start Date15 May 2024

Sponsor / Collaborator

Tokyo Women's Medical University Educational Association

100 Clinical Results associated with Esaxerenone

100 Translational Medicine associated with Esaxerenone

100 Patents (Medical) associated with Esaxerenone

173

Literatures (Medical) associated with Esaxerenone

01 Jul 2025·LIFE SCIENCES

Fibroblast to macrophage-like cell transition in renal inflammatory injury through the MR/CSF1 pathway induced by aldosterone

Article

Author: Lv, Ruyan ; Yang, Fan ; Zhang, Boya ; Qiang, Panpan ; Guo, Haixia ; Xiong, Yunzhao ; Gao, Xiaomeng ; Shimosawa, Tatsuo ; Hao, Juan ; Xu, Qingyou ; Peng, Yunsong ; Liu, Ziqian ; Wang, Xiangting ; Chang, Yi ; Wang, Xuan

AIMS:

Inflammatory injury promotes the chronic kidney disease (CKD) progression，with renal macrophage accumulation and proliferation of as typical manifestations of inflammatory injury. We aimed to verify fibroblast to macrophage-like cell transition as a new source of macrophages that participate in renal inflammatory injury.

MATERIALS AND METHODS:

Wistar rats were divided into Sham, ALD (aldosterone infusion for 12 weeks), and ESA (aldosterone infusion and esaxerenone by diet for 12 weeks) groups. Rat kidney interstitial fibroblast (RKF) were cultured, induced with aldosterone or CSF1, and treated with antagonists in vitro. The proportions of FSP-1⁺ F4/80⁺ cells in the rat kidney and RKF, including M1 marker iNOS/CD86 and M2 marker CD206/CD163 were assessed by flow cytometry and immunofluorescence staining. Single-cell RNA sequencing was used to assess the origin of macrophages in the rat kidneys and related gene expression. Additionally, immunofluorescence was used to detect FSP-1⁺ F4/80⁺ cells in kidney biopsy samples from CKD patients.

KEY FINDINGS:

Fibroblast to macrophage-like cell transition was observed in both the kidneys of aldosterone-infused rats and in vitro aldosterone-treated RKF, with a predominant differentiation into the M1 phenotype. This transformation was mediated through the MR/CSF1 signalling pathway, revealing a novel source of macrophages and providing significant insights into the mechanisms underlying organ fibrosis.

SIGNIFICANCE:

Aldosterone induces fibroblast to macrophage-like cell transition through the MR/ CSF1 pathway.

01 May 2025·CURRENT OPINION IN NEPHROLOGY AND HYPERTENSION

Targeting aldosterone to improve cardiorenal outcomes: from nonsteroidal mineralocorticoid receptor antagonists to aldosterone synthase inhibitors

Review

Author: Hundemer, Gregory L. ; Helmeczi, Wryan

Purpose of review:

Aldosterone dysregulation plays a major role in the pathogenesis of hypertension, cardiovascular disease, and kidney disease. Traditionally, steroidal mineralocorticoid receptor (MR) antagonists, namely spironolactone and eplerenone, have been the only available options to target aldosterone. Over recent years, a host of promising novel aldosterone-targeted pharmacologic agents have been developed thereby providing new options to mitigate aldosterone-mediated cardiovascular and kidney disease.

Recent findings:

Recently, a number of nonsteroidal MR antagonists (finerenone, esaxerenone, and ocedurenone) and highly specific aldosterone synthase inhibitors (baxdrostat, lorundrostat, dexfadrostat, and vicadrostat) have been developed. The early clinical data for these novel medications looks promising regarding their efficacy in improving blood pressure control, preventing adverse cardiovascular outcomes, and slowing chronic kidney disease progression. Moreover, they appear to be generally safe and well tolerated.

Summary:

In the coming years, nonsteroidal MR antagonists and aldosterone synthase inhibitors are likely to play an increasingly large role in routine medical practice to help improve cardiovascular and kidney outcomes.

24 Apr 2025·BIOLOGICAL & PHARMACEUTICAL BULLETIN

Esaxerenone Improves Vascular Endothelial Dysfunction by Reducing Serum and Glucocorticoid-Regulated Kinase 1 Activity and Enhancing the Akt Pathway in Type 2 Diabetic Mice

Article

Author: Matsumoto, Takayuki ; Kobayashi, Tsuneo ; Taguchi, Kumiko ; Furukawa, Tomoya

Mineralocorticoid receptor (MR) blockers reduce cardiovascular complications as MRs play a crucial role in cardiovascular regulation. Diabetic cardiovascular complications are caused by vascular endothelial dysfunction. This study used a type 2 diabetic mouse model (DM) to investigate whether esaxerenone (ESAX), an MR blocker, ameliorates vascular endothelial dysfunction. ESAX (3 mg/kg/d) was administered via diet to KK-Ay mice or C57BL/6J mice, a nondiabetic control (Control), for 8 weeks, and metabolic parameters and blood pressure were measured. Vascular responses of the aortic segments were analyzed with acetylcholine, sodium nitroprusside, UK14304, or phenylephrine (PE). The other aortas were used for Western blot analysis. DM mice exhibited higher plasma glucose, insulin, metabolic parameters, and blood pressure levels than those of the Control mice. Parameters that did not include blood pressure were unaltered by DM or ESAX-administered DM (DM + ESAX). However, DM impaired UK14304-induced endothelial-dependent relaxation and nitric oxide production and elevated PE-induced contraction. ESAX administration ameliorated endothelial dysfunction and improved the protein kinase B (Akt) phosphorylation under α₂-agonist UK14304 stimulation in the aorta from DM mice compared with that of the Control mice. However, ESAX did not recover the increased G protein-coupled receptor kinase 2 (GRK2) expression and activity in the DM aorta. Furthermore, the DM-induced phosphorylation of serum and glucocorticoid-regulated kinase 1 (SGK1) was inhibited by ESAX. Overall, ESAX attenuates the development of DM-induced endothelial dysfunction by reducing SGK1 activity and enhancing Akt activity without affecting the GRK2 pathway. These results suggest that the vascular protective effects of ESAX could be employed for diabetic vascular complications.

News (Medical) associated with Esaxerenone

18 Apr 2023

·www.prnewswire.com

Ocedurenone: A Novel Therapy for Uncontrolled Hypertension in Advanced Chronic Kidney Disease

PRINCETON, N.J., April 17, 2023 /PRNewswire/ -- EMJ Nephrology interviewed two World-renowned experts in nephrology and cardiology, George Bakris and Faiez Zannad, regarding the challenges of treating uncontrolled hypertension (uHTN) in patients with advanced chronic kidney disease (CKD), a large unmet need for safe, effective therapies, and the potential of one therapy, Ocedurenone, to address this need. Original article: EMJ-8.1-2023-1.pdf (emg-health.com) Large Unmet Need Patients with advanced CKD have a high burden of disease, compounded by serious comorbidities, most commonly hypertension. Controlling hypertension is vital in these patients to reduce the associated risks of morbidity and mortality, as well as reducing cardiorenal risk, but treatment options are limited due to safety concerns with the use of existing agents. Current Options Bakris:"The PATHWAY-2 trial showed that in people with resistant hypertension without advanced CKD, spironolactone produced a greater reduction in blood pressure than a β-blocker and an α-blocker. However, it presents safety risks to patients when administered." "Then there is eplerenone, given twice a day, while safe, has a much weaker effect on blood pressure reduction than spironolactone. That's all we've got, so that's what people use." Dr Bakris also mentioned two existing nonsteroidal MRAs, esaxerenone which is "approved exclusively in Japan, for which there are no placebo-controlled comparisons", and Finerenone which "reduces blood pressure (placebo subtracted) variously from 3 mmHg (ARTS-DN, FIGARO-DKD, and FIDELIO-DKD studies) to approximately 8 mmHg (subset analysis from ARTS-DN study, eGFR of approximately 68, though office blood pressure from the same study showed around 3 mmHg reduction)". Future Option - Ocedurenone Bakris:"Now, Ocedurenone, a non-steroidal MRA, shows clear promise in patients whose standard of care includes two, three, or more drugs. Ocedurenone is the only drug that has consistently steadied resistant hypertension in people with advanced CKD." In the first dedicated study of patients with uncontrolled hypertension and advanced CKD (BLOCK-CKD), Ocedurenone demonstrated efficacy in lowering blood pressure, together with a favorable safety profile. The experts were optimistic that it could provide a much-needed treatment option for these patients, with the added potential for reduction in the risk of cardiorenal outcomes. "This study showed that Ocedurenone reduces SBP by 11 mmHg (placebo-subtracted), a reduction that could lead to potential approval. No other agent to date has steadied blood pressure as well in this group of patients. And the point is that these are the patients who need the most help." Zannad reinforced the importance of the hyperkalemia data for the clinical safety of Ocedurenone:"With Ocedurenone, we may for the first time have an MRA that is both safe and efficacious." Bakris added:"A Phase 3 study (CLARION-CKD) of Ocedurenone in a similar patient population is ongoing. I remain optimistic that the signal seen in the BLOCK-CKD study will be seen in this larger study." "I remain excited about Ocedurenone. Its tolerability and efficacy in lowering blood pressure in a very high-risk group will have a significant impact on morbidity." "Mineralocorticoid receptors are so ubiquitous which may allow for indications beyond CKD and cardiovascular conditions. This is likely just the beginning for Ocedurenone." About Ocedurenone (KBP-5074) KBP Biosciences is a global, clinical-stage biotechnology company, headquartered in Princeton, NJ, focused on discovering, developing, and commercializing innovative small-molecule therapeutics for the treatment of serious cardiorenal and infectious diseases with large unmet medical needs. Ocedurenone (KBP-5074) is a non-steroidal MRA discovered and developed by KBP Biosciences. At present, the Phase 3 clinical trial of the first indication for Ocedurenone, advanced CKD and uncontrolled hypertension, is underway. About KBP Biosciences, please visit . SOURCE KBP Biosciences

Phase 3Clinical ResultDrug Approval

10 Jan 2023

·www.biospace.com

Ajinomoto and Exelixis Enter Into a License Agreement to Discover and Develop Novel Antibody-Drug Conjugates for the Treatment of Cancer

TOKYO, Jan. 10, 2023 /PRNewswire/ -- Ajinomoto Co., Inc. ("Ajinomoto Co.") today announced a license agreement with Exelixis, Inc. ("Exelixis") to incorporate AJICAP®, Ajinomoto Co.'s proprietary site-specific bioconjugation and linker technologies, in the development of certain of Exelixis' antibody-drug conjugate (ADC) programs. Exelixis is a commercially successful, oncology-focused biotechnology company that strives to accelerate the discovery, development and commercialization of new medicines for difficult-to-treat cancers. Utilizing its network of biotherapeutics collaborations, the company is developing next generation ADCs for the treatment of various cancers. Ajinomoto Co. is a leading technology provider for biopharmaceuticals and the owner of CDMO Ajinomoto Bio-Pharma Services. AJICAP® is Ajinomoto Co.'s proprietary site-specific bioconjugation and stable linker technologies compatible with commonly used antibody isotypes. AJICAP technology includes its "off-the-shelf" feature, allowing any therapeutic antibody at any stage of development to be conjugated to drug-payloads of choice without the need for antibody engineering or cell line development, and stable/hydrophilic linkers to generate antibody-drug conjugates with an enhanced therapeutic window. As part of the license agreement, Exelixis will have the right to use the AJICAP technology to support its aim of advancing multiple ADCs with the potential for higher efficacy and lower toxicity than currently available options. Ajinomoto Co. is eligible to receive development, regulatory and commercial milestone payments as well as royalties on commercial sales. Dr. Tatsuya Okuzumi, General Manager, Business Development Group, Bio-Pharma Services Department, Ajinomoto Co., expressed: "We are very excited to support Exelixis, a leader in oncology drug discovery, development, and commercialization, in the development of novel antibody-drug conjugates. The combination of Exelixis' antibodies and payloads with Ajinomoto Co.'s AJICAP opens up a wide range of oncology applications and may be harnessed to provide a clinical benefit to patients." About Ajinomoto Co. and Ajinomoto Bio-Pharma Services Based on the corporate message "Eat Well, Live Well.", Ajinomoto Co., Inc. has been scientifically pursuing the possibilities of amino acids to aim for future growth by creating new value through sustainable and innovative solutions for communities and society. For additional information about Ajinomoto Co. (TYO: 2802), please visit . As its pharmaceutical arm, Ajinomoto Bio-Pharma Services is a fully integrated contract development and manufacturing organization (CDMO) with sites in Belgium, United States, Japan, and India, providing comprehensive development, cGMP manufacturing, and aseptic fill finish services for small and large molecule APIs and intermediates. For more information about Ajinomoto Bio-Pharma Services, please visit . In addition, Ajinomoto Co. and Ajinomoto Bio-Pharma Services offer a broad range of innovative platform technologies and capabilities for pre-clinical and pilot programs to commercial quantities, including AJIPHASE® oligonucleotide manufacturing technology, CORYNEX® and TALAMAX® protein expression systems, AJICAP® site-specific conjugation and linker technologies for ADCs, continuous flow manufacturing and more. For additional information on the platform technologies, please visit . About Exelixis, Inc. Founded in 1994, Exelixis, Inc. (Exelixis) is a commercially successful, oncology-focused biotechnology company that strives to accelerate the discovery, development and commercialization of new medicines for difficult-to-treat cancers. Following early work in model system genetics, Exelixis established a broad drug discovery and development platform that has served as the foundation for our continued efforts to bring new cancer therapies to patients in need. Exelixis' discovery efforts have resulted in four commercially available products, CABOMETYX® (cabozantinib), COMETRIQ® (cabozantinib), COTELLIC® (cobimetinib) and MINNEBRO® (esaxerenone), and Exelixis has entered into partnerships with leading pharmaceutical companies to bring these important medicines to patients worldwide. Supported by revenues from marketed products and collaborations, Exelixis is committed to prudently reinvesting in our business to maximize the potential of our pipeline. Exelixis is supplementing existing therapeutic assets with targeted business development activities and internal drug discovery — all to deliver the next generation of Exelixis medicines and help patients recover stronger and live longer. Exelixis is a member of the Standard & Poor's (S&P) MidCap 400 index, which measures the performance of profitable mid-sized companies. For more information about Exelixis, please visit , follow @ExelixisInc on Twitter or like Exelixis, Inc. on Facebook. Company Codes: Tokyo:2802, OTC-PINK:AJINY

License out/inOligonucleotide

03 Jan 2023

·www.businesswire.com

Exelixis to Present at the 41st Annual J.P. Morgan Healthcare Conference on January 9, 2023 — Presentation to be webcast on www.exelixis.com —

ALAMEDA, Calif.--( BUSINESS WIRE )--Exelixis, Inc. (Nasdaq: EXEL) today announced that Michael M. Morrissey, Ph.D., the company’s President and Chief Executive Officer, will provide a corporate overview at the 41 st Annual J.P. Morgan Healthcare Conference on Monday, January 9, 2023 at 8:15pm ET / 5:15pm PT. To access the webcast link, log onto www.exelixis.com and proceed to the News & Events / Event Calendar page under the Investors & Media heading. Please connect to the company’s website at least 15 minutes prior to the presentation to ensure adequate time for any software download that may be required to listen to the webcast. A replay will also be available at the same location for at least 30 days. About Exelixis Founded in 1994, Exelixis, Inc. (Nasdaq: EXEL) is a commercially successful, oncology-focused biotechnology company that strives to accelerate the discovery, development and commercialization of new medicines for difficult-to-treat cancers. Following early work in model system genetics, we established a broad drug discovery and development platform that has served as the foundation for our continued efforts to bring new cancer therapies to patients in need. Our discovery efforts have resulted in four commercially available products, CABOMETYX ® (cabozantinib), COMETRIQ ® (cabozantinib), COTELLIC ® (cobimetinib) and MINNEBRO ® (esaxerenone), and we have entered into partnerships with leading pharmaceutical companies to bring these important medicines to patients worldwide. Supported by revenues from our marketed products and collaborations, we are committed to prudently reinvesting in our business to maximize the potential of our pipeline. We are supplementing our existing therapeutic assets with targeted business development activities and internal drug discovery – all to deliver the next generation of Exelixis medicines and help patients recover stronger and live longer. Exelixis is a member of the Standard & Poor’s (S&P) MidCap 400 index, which measures the performance of profitable mid-sized companies. For more information about Exelixis, please visit www.exelixis.com , follow @ExelixisInc on Twitter or like Exelixis, Inc. on Facebook. Exelixis, the Exelixis logo, CABOMETYX, COMETRIQ and COTELLIC are registered U.S. trademarks. MINNEBRO is a registered Japanese trademark.

100 Deals associated with Esaxerenone

External Link

KEGG	Wiki	ATC	Drug Bank
D10892	Esaxerenone	C02	DB15207

R&D Status

Approved

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Hypertension	Japan	Daiichi Sankyo Co., Ltd.	08 Jan 2019

Developing

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Albuminuria	Phase 3	Japan	Daiichi Sankyo Co., Ltd.	01 Jun 2016
Diabetes Mellitus, Type 2	Phase 3	Japan	Daiichi Sankyo Co., Ltd.	01 Jun 2016
Hypertension, Renal	Phase 3	Japan	Daiichi Sankyo Co., Ltd.	01 Jun 2016
Essential Hypertension	Phase 3	Japan	Daiichi Sankyo Co., Ltd.	01 Mar 2016
Diabetic Nephropathies	Phase 2	Japan	Daiichi Sankyo Co., Ltd.	01 Jan 2015
Hyperaldosteronism	Clinical	Japan	Daiichi Sankyo Co., Ltd.	01 Sep 2016

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ODP190 (ENDO2022)	Not Applicable	Diabetes Mellitus, Type 2 \| Hypertension	-	Esaxerenone	betkggacwp(zwcfpmxmnk) = tuybqmzfbx izwyonifkc (ieuyktzmmt, 10) View more	Positive	01 Nov 2022
ODP190 (ENDO2022)	Not Applicable	Diabetes Mellitus, Type 2 \| Hypertension	-	Amlodipine	betkggacwp(zwcfpmxmnk) = cnvnnuwdlz izwyonifkc (ieuyktzmmt, 14) View more	Positive	01 Nov 2022
NCT02722265 (Pubmed) Manual	Phase 3	Essential Hypertension	25	esaxerenone	spigmqibga(ffcywltmyv) = jtchkuuyih dhnwcsfskz (yuocbxolqc ) View more	Positive	17 Aug 2022
NCT02807987 (Pubmed \| Hypertens Res) Manual	Phase 3	Hypertension	91	Esaxerenone	svdelfrheu(rvmuxqwsji) = nkrvbttmri idxpbnskbh (liwivivvdj ) View more	Positive	01 May 2021
ESH2021	Not Applicable	Hypertensive Nephropathy Add-on	91	Esaxerenone monotherapy	ydmoihtvmm(kgmbeqojgm) = wwjohenkcn oxaezhttti (kdlsnmqlpa ) View more	Positive	01 Apr 2021
ESH2021	Not Applicable	Hypertensive Nephropathy Add-on	91	Esaxerenone add-on therapy to RAS inhibitor	ydmoihtvmm(kgmbeqojgm) = jryfzdgkii oxaezhttti (kdlsnmqlpa ) View more	Positive	01 Apr 2021
ESH2021	Not Applicable	Add-on	230	Esaxerenone add-on group	uiuuegqocl(zsrlljubwh) = xbtjshukuh afupkrzwak (ysvsrhndob, 12) View more	Positive	01 Apr 2021
ESH2021	Not Applicable	Add-on	230	Esaxerenone replacement group	aojturnmzi(cnhdcdfiyn) = auxhgbrxge wnfmgoayll (yyriwbwbmn, 14)	Positive	01 Apr 2021
NCT04019652 (Pubmed)	Phase 1	-	55	Moxifloxacin 400 mg	ovdfsyykpa(vlzifmxdew) = rqmqrlwend jdfskjeoio (iknyxqavcr )	-	01 Aug 2020
SUN-176 (ENDO2020)	Not Applicable	Adrenocortical Adenoma	-	Esaxerenone	vtoybeyixx(afqufagysy) = kgvjgfdprw jgfkfeciqc (ufedeclyxc ) View more	-	08 May 2020
NCT02722265 (Pubmed \| Hypertens Res) Manual	Phase 3	Diabetes Mellitus, Type 2 \| Hypertension \| Albuminuria	51	Esaxerenone	huxuatnlsz(pqhjgopodr) = qyotlywbxc navqgyvgiq (imjutrldky ) View more	Positive	01 Oct 2019

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