Endothelin Receptor Antagonist - Pipeline Insight, 2025

The “Endothelin Receptor Antagonist - Pipeline Insight, 2025” report provides comprehensive insights about 10+ companies and 15+ pipeline drugs in Endothelin Receptor Antagonist pipeline landscape. It covers the pipeline drug profiles, including clinical and nonclinical stage products. It also covers the therapeutics assessment by product type, stage, route of administration, and molecule type. It further highlights the inactive pipeline products in this space.

Geography Covered

• Global coverage

Endothelin Receptor Antagonist: Understanding

Endothelin Receptor Antagonist: Overview

Endothelin receptor antagonists (ERAs) are a class of medications designed to block the effects of endothelins, which are potent vasoconstrictive peptides that play a crucial role in regulating vascular tone, cellular proliferation, and inflammation. Endothelins bind to two main receptor types: endothelin receptor A (ET-A) and endothelin receptor B (ET-B). ET-A receptors primarily mediate vasoconstriction and smooth muscle proliferation, while ET-B receptors promote vasodilation and facilitate endothelin clearance. Dysregulation of the endothelin system has been linked to various cardiovascular and pulmonary diseases.

ERAs are categorized into two types: selective and dual receptor antagonists. Selective ERAs primarily block the ET-A receptor, reducing vasoconstriction and preventing adverse cardiovascular remodeling. Examples include ambrisentan and sitaxentan. Dual ERAs, such as bosentan and macitentan, inhibit both ET-A and ET-B receptors, providing a broader therapeutic effect by simultaneously addressing vasoconstriction and endothelin clearance.

One of the primary clinical applications of ERAs is in the management of pulmonary arterial hypertension (PAH), a condition characterized by elevated blood pressure in the pulmonary arteries, leading to right heart failure. By blocking the endothelin pathway, ERAs help reduce vascular resistance and improve blood flow, thereby enhancing exercise capacity and slowing disease progression. Studies have demonstrated that ERAs can significantly improve hemodynamic parameters and reduce clinical worsening in PAH patients.

Beyond PAH, ERAs have potential applications in other cardiovascular and renal conditions, such as heart failure and chronic kidney disease. Endothelin-mediated vasoconstriction and inflammation contribute to disease progression in these conditions. Clinical trials have explored the use of ERAs to mitigate organ damage and improve outcomes in these patient populations. However, challenges such as fluid retention and liver toxicity have limited their widespread adoption in these indications. Adverse effects associated with ERAs include liver function abnormalities, peripheral edema, and anemia. Therefore, regular monitoring of liver enzymes and careful dose adjustments are essential for patient safety. ERAs are also contraindicated in pregnancy due to their teratogenic potential. The development of newer ERAs with improved safety profiles remains an active area of research.

In summary, endothelin receptor antagonists play a vital role in the management of PAH and hold promise for other cardiovascular and renal disorders. Ongoing research aims to optimize their therapeutic potential while minimizing adverse effects. Their ability to target a key pathway in vascular biology makes them a valuable addition to the arsenal of treatments for complex diseases involving endothelin dysregulation.

“Endothelin Receptor Antagonist - Pipeline Insight, 2025" report outlays comprehensive insights of present scenario and growth prospects across the mechanism of action. A detailed picture of the Endothelin Receptor Antagonist pipeline landscape is provided which includes the disease overview and Endothelin Receptor Antagonist treatment guidelines. The assessment part of the report embraces, in depth Endothelin Receptor Antagonist commercial assessment and clinical assessment of the pipeline products under development. In the report, detailed description of the drug is given which includes mechanism of action of the drug, clinical studies, NDA approvals (if any), and product development activities comprising the technology, Endothelin Receptor Antagonist collaborations, licensing, mergers and acquisition, funding, designations and other product related details.

Report Highlights

The companies and academics are working to assess challenges and seek opportunities that could influence Endothelin Receptor Antagonist R&D. The therapies under development are focused on novel approaches to treat/improve Endothelin Receptor Antagonist.

Endothelin Receptor Antagonist Emerging Drugs Chapters

This segment of the Endothelin Receptor Antagonist report encloses its detailed analysis of various drugs in different stages of clinical development, including phase II, I, preclinical and Discovery. It also helps to understand clinical trial details, expressive pharmacological action, agreements and collaborations, and the latest news and press releases.

Endothelin Receptor Antagonist Emerging Drugs

• Zibotentan: Astrazeneca

Zibotentan is a novel once daily tablet and works by blocking the endothelin pathway. As prostate cancer advances, this pathway becomes uncontrolled, which then drives the spread of cancer growth. By blocking the endothelin receptor in this pathway, zibotentan can slow tumour growth and the spread of cancer cells. Zibotentan is under development for the treatment of diabetic nephropathy, chronic kidney disease (CKD), cirrhosis with features of portal hypertension and microvascular angina. The drug candidate is administered orally in the form of tablet and capsule. It was also under development for intermittent claudication in peripheral artery disease, patients with non-metastatic castrate resistant prostate cancer, epithelial ovarian cancer, fallopian tube cancer, primary serous peritoneal cancer and non-small cell lung cancer. Currently it is being investigated in Phase III stage of development for the treatment of patients with Chronic Kidney Disease.

• SC0062: Biocity Biopharmaceutics

SC0062 is an ETA highly selective receptor small molecule antagonist developed for chronic kidney disease, dedicated to improving the long-term drug safety of patients with chronic diseases. Preclinical studies have shown that SC0062 has good activity and can effectively improve the pathological scores of acute kidney injury and chronic kidney disease models. In the completed clinical phase I study, SC0062 showed good safety, tolerability and pharmacokinetic characteristics, and no side effects such as water and sodium retention were found, and it is expected to become a potential "Best-in-Class" drug. Currently the drug is in Phase II stage of its development for the treatment of for

Diabetic kidney disease and IgA Nephropathy.

• GMA301: Gmax Biopharm

GMA301 is a humanized monoclonal antibody against endothelin receptor A, may become the first long-lasting PAH drug with better efficacy and less adverse effects. Endothelin receptor A/endothelin-1 axis is associated with pulmonary artery hypertension (PAH) and has been targeted for the treatment of PAH. Orphan drug designation has been granted by FDA. Currently the drug is in Phase I stage of clinical trial evaluation for the treatment of Pulmonary Arterial Hypertension.

Endothelin Receptor Antagonist: Therapeutic Assessment

This segment of the report provides insights about the different Endothelin Receptor Antagonist drugs segregated based on following parameters that define the scope of the report, such as:

Major Players in Endothelin Receptor Antagonist

There are approx. 10+ key companies which are developing the therapies for Endothelin Receptor Antagonist. The companies which have their Endothelin Receptor Antagonist drug candidates in the most advanced stage, i.e. Phase III include, Astrazeneca.

Phases

The report covers around 15+ products under different phases of clinical development like

• Late stage products (Phase III)
• Mid-stage products (Phase II)
• Early-stage product (Phase I) along with the details of
• Pre-clinical and Discovery stage candidates
• Discontinued & Inactive candidates

Route of Administration

Endothelin Receptor Antagonist pipeline report provides the therapeutic assessment of the pipeline drugs by the Route of Administration. Products have been categorized under various ROAs such as

• Intra-articular
• Intraocular
• Intrathecal
• Intravenous
• Oral
• Parenteral
• Subcutaneous
• Topical
• Transdermal

Molecule Type

Products have been categorized under various Molecule types such as

• Oligonucleotide
• Peptide
• Small molecule

Product Type

Drugs have been categorized under various product types like Mono, Combination and Mono/Combination.

Endothelin Receptor Antagonist: Pipeline Development Activities

The report provides insights into different therapeutic candidates in phase II, I, preclinical and discovery stage. It also analyses Endothelin Receptor Antagonist therapeutic drugs key players involved in developing key drugs.

Pipeline Development Activities

The report covers the detailed information of collaborations, acquisition and merger, licensing along with a thorough therapeutic assessment of emerging Endothelin Receptor Antagonist drugs.

Endothelin Receptor Antagonist Report Insights

• Endothelin Receptor Antagonist Pipeline Analysis
• Therapeutic Assessment
• Unmet Needs
• Impact of Drugs

Endothelin Receptor Antagonist Report Assessment

• Pipeline Product Profiles
• Therapeutic Assessment
• Pipeline Assessment
• Inactive drugs assessment
• Unmet Needs

Key Questions

Current Treatment Scenario and Emerging Therapies:

• How many companies are developing Endothelin Receptor Antagonist drugs?
• How many Endothelin Receptor Antagonist drugs are developed by each company?
• How many emerging drugs are in mid-stage, and late-stage of development for the treatment of Endothelin Receptor Antagonist?
• What are the key collaborations (Industry-Industry, Industry-Academia), Mergers and acquisitions, licensing activities related to the Endothelin Receptor Antagonist therapeutics?
• What are the recent trends, drug types and novel technologies developed to overcome the limitation of existing therapies?
• What are the clinical studies going on for Endothelin Receptor Antagonist and their status?
• What are the key designations that have been granted to the emerging drugs?

Key Players

• Astrazeneca
• Biocity Biopharmaceutics
• Gmax Biopharm
• ENB Therapeutics
• Alchemedicine
• Lassogen

Key Products

• Zibotentan
• SC0062
• GMA301
• GMA131
• ENB-003
• ENB-004
• ETA antagonist
• Lassotides

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