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

JPRN-UMIN000037722

/ RecruitingNot ApplicableIIT

Safety and antihypertensive effect of switching from eplerenone to esaxerenone in hypertensive patients. - Safety and antihypertensive effect of switching from eplerenone to esaxerenone in hypertensive patients.

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

163

Literatures (Medical) associated with Esaxerenone

01 Feb 2025·HYPERTENSION RESEARCH

Home blood pressure-lowering effect of esaxerenone versus trichlormethiazide for uncontrolled hypertension: a predefined subanalysis of the EXCITE-HT randomized controlled trial by basal calcium channel blocker versus angiotensin receptor blocker

Article

Author: Katsuya, Tomohiro ; Taguchi, Takashi ; Ohishi, Mitsuru ; Itabashi, Naoki ; Hirano, Kunio ; Ohbayashi, Hiroyuki ; Hashimoto, Masami ; Kario, Kazuomi ; on behalf of the EXCITE-HT investigators ; Ishida, Hidenori ; Ebe, Yusuke ; Tanabe, Ayumi ; Miyamoto, Takahide ; Uchiyama, Kazuaki ; Nakamura, Noriko ; Shimosawa, Tatsuo ; Fukui, Toshiki ; Kato, Mitsutoshi ; Nagashima, Hirotaka ; Hatta, Tsuguru

Abstract:

This prespecified subanalysis of the multicenter, randomized, open-label, parallel-group EXCITE-HT study aimed to examine the non-inferiority of esaxerenone to trichlormethiazide as a second-line antihypertensive agent according to the basal antihypertensive agent used (angiotensin receptor blocker [ARB] or calcium channel blocker [CCB]). The primary endpoint, change in morning home systolic/diastolic blood pressure (SBP/DBP) from baseline to end of treatment was similar between the two groups (intergroup difference in least squares mean change [95% confidence interval]: −1.3 [−3.8, 1.3]/−0.2 [−1.6, 1.3] mmHg for ARB; −2.7 [−4.2, −1.2]/−0.8 [−1.7, 0.1] mmHg for CCB). The respective incidences of serum potassium levels <3.5 mEq/L and ≥5.5 mEq/L in the ARB subgroup were 3.4% and 4.2% for esaxerenone and 7.9% and 0% for trichlormethiazide; in the CCB subgroup, they were 2.8% and 0.6% for esaxerenone and 13.9% and 1.2% for trichlormethiazide, respectively. The incidence of uric acid level ≥7.0 mg/dL was numerically higher in the trichlormethiazide group than the esaxerenone group in both the ARB and CCB subgroups. The non-inferiority of esaxerenone to trichlormethiazide in lowering morning home BP was demonstrated regardless of whether the basal antihypertensive agent was an ARB or CCB. Esaxerenone with a CCB showed superiority to trichlormethiazide in lowering SBP, without any new safety concerns. Serum potassium levels tended to be higher when esaxerenone was combined with an ARB than with a CCB, but this can be mitigated if administered according to the package insert.

01 Feb 2025·HYPERTENSION RESEARCH

Evolution of mineralocorticoid receptor antagonists, aldosterone synthase inhibitors, and alternative treatments for managing primary aldosteronism

Review

Author: Yoshida, Yuichi ; Shibata, Hirotaka

Primary aldosteronism (PA) is a prevalent and curable secondary hypertensive disorder that accounts for 5-13% of all hypertension cases. The prevalence of resistant hypertension, cerebral and cardiovascular diseases, and renal complications is higher in PA patients than in those with essential hypertension. Appropriate diagnosis and treatment at an early stage may suppress cerebral and cardiovascular events. Lifestyle modifications recommended for essential hypertensive patients, including dietary salt restriction and appropriate calorie intake to avoid fat accumulation, play a crucial role in suppressing overactivation of the mineralocorticoid receptor (MR), which helps to control blood pressure and prevent end-organ damage. Esaxerenone is a safe mineralocorticoid receptor antagonist (MRA) with strong antihypertensive and anti-albuminuric effects. Aldosterone synthase inhibitors (ASIs) have been developed, which are antihypertensive agents with a new mechanism of action. The pharmacological mechanisms of MRAs and ASIs differ; MRAs block MR activity by preventing aldosterone and/or cortisol from binding to the MR, while ASIs block aldosterone secretion from the adrenal gland. Other new treatments, such as robot-assisted laparoscopic adrenalectomy, percutaneous computed tomography radiofrequency ablation, transvenous radiofrequency catheter ablation, and super-selective adrenal arterial embolization have been developed. Further research will lead to better treatments for PA patients and reduce the frequency of cerebral and cardiovascular events.

31 Jan 2025·International Heart Journal

Esaxerenone Attenuates Cardiac Hypertrophy in a Pressure Overload Model in Mice

Article

Author: Fukuda, Daiju ; Ishikawa, Hirotoshi ; Hayashi, Ou ; Izumiya, Yasuhiro ; Hayashi, Hiroya

Esaxerenone, a non-steroidal mineralocorticoid receptor (MR) blocker, exhibits high selectivity for MR. While clinically used as an anti-hypertensive drug, its impact on cardiac remodeling remains poorly understood. This study investigated the effect of esaxerenone on pressure overload-induced cardiac hypertrophy in mice.Eight-week-old C57BL/6 mice underwent either transverse aortic constriction (TAC) or sham surgery. Animals were divided into 2 groups: 0.003% (3.0 mg/kg) Esaxerenone-fed (EX) and normal-fed (CNT) groups (n = 64, Sham/CNT = 12, Sham/EX = 13, TAC/CNT = 18, TAC/EX = 21). Cardiac gene expressions were analyzed using quantitative real-time PCR.Food intake and body weight variations showed no significant differences between CNT and EX groups during the 2-week experimental period. The mortality rate from 24 hours after TAC surgery to the end of the experiment was 30.8% in the CNT group, however, all mice survived following TAC surgery in EX group. CNT group showed a remarkable increase in heart weight/tibial length ratio 2 weeks after TAC compared with the Sham group. The EX group demonstrated a significant decrease in HW/TL following TAC surgery (-23.4%, P = 0.041). Masson's trichrome staining revealed that the TAC/CNT group had a significantly higher proportion of fibrotic area than the Sham/CNT group. However, the TAC/EX group had a slightly lower proportion of fibrotic area than the TAC/CNT group. In cardiac gene expression analysis, ANP and Collagen 3a1 were upregulated in the TAC group but were significantly reduced following treatment with esaxerenone.Esaxerenone attenuates cardiac hypertrophy and hypertrophy-related gene expression, resulting in improved survival in a pressure overload model in mice.

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
Hypertension, severe	Phase 3	Japan	Daiichi Sankyo Co., Ltd.	01 Jun 2016
Essential Hypertension	Phase 3	Japan	Daiichi Sankyo Co., Ltd.	01 Mar 2016
Diabetes Mellitus, Noninsulin-Dependent, 2	Phase 2	Japan	Daiichi Sankyo, Inc.	01 Jan 2015
Diabetic Nephropathies	Phase 2	Japan	Daiichi Sankyo, Inc.	01 Jan 2015

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	zlcpbyyhjp(rivsmxvjik) = cylwcmgglw lizheogffh (pfwulbidzq, 10) View more	Positive	01 Nov 2022
ODP190 (ENDO2022)	Not Applicable	Diabetes Mellitus, Type 2 \| Hypertension	-	Amlodipine	zlcpbyyhjp(rivsmxvjik) = jrhpcpqcda lizheogffh (pfwulbidzq, 14) View more	Positive	01 Nov 2022
NCT02722265 (Pubmed) Manual	Phase 3	Essential Hypertension	25	esaxerenone	uvajrqsiko(cqczdauwwt) = pzrjzmbxfk aenshtvngh (emvhwcmpfi ) View more	Positive	17 Aug 2022
NCT02807987 (Pubmed \| Hypertens Res) Manual	Phase 3	Hypertension	91	Esaxerenone	xcgjajzgxw(mtrdgmryon) = nxeufxweqt jzxnfnploe (adswmcdgsq ) View more	Positive	01 May 2021
ESH2021	Not Applicable	Hypertensive Nephropathy Add-on	91	Esaxerenone monotherapy	sczrojsyut(asnplqzuak) = vszvobdnkt ywtviyedmn (cfshabiyse ) View more	Positive	01 Apr 2021
ESH2021	Not Applicable	Hypertensive Nephropathy Add-on	91	Esaxerenone add-on therapy to RAS inhibitor	sczrojsyut(asnplqzuak) = hdrkoibplx ywtviyedmn (cfshabiyse ) View more	Positive	01 Apr 2021
NCT04019652 (Pubmed)	Phase 1	-	55	Moxifloxacin 400 mg	tvxsqsdlnl(bbsukbjrqn) = zwvwctbuat etdvvhkmzh (bnowcqwkmf )	-	01 Aug 2020
SUN-176 (ENDO2020)	Not Applicable	Adrenocortical Adenoma	-	Esaxerenone	bzhzgtatbm(ipuelrcwka) = pataydpdjb cimdsubhyn (ozrqxweger ) View more	-	08 May 2020
NCT02722265 (Pubmed \| Hypertens Res) Manual	Phase 3	Diabetes Mellitus, Type 2 \| Hypertension \| Albuminuria	51	Esaxerenone	rbhzqdhoch(mpegbvsspf) = tvcwyduths nfmobdovmd (svahzhgpak ) View more	Positive	01 Oct 2019

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