Endothelin Receptor Antagonist - Pipeline Insight, 2024

This “Endothelin Receptor (ET) Antagonist - Pipeline Insight, 2024” report provides comprehensive insights about 8+ companies and 8+ pipeline drugs in Endothelin Receptor (ET) 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 (ET) Antagonist Understanding

Endothelin Receptor (ET) Antagonist: Overview

In mammals, the endothelin (ET) family comprises three endogenous isoforms, ET-1, ET-2 and ET-3, and the receptors that mediate their effects have been classified as the endothelin ETA and ETB receptors. Endothelin is able to activate a number of signal transduction processes including phospholipase (PL) A2, PLC and PLD, as well as cytosolic protein kinase activation.

Function - Endothelin receptors are widely expressed in all tissues, consistent with the physiological role of endothelins as ubiquitous endothelium-derived vasoactive peptides, contributing to the maintenance of vascular tone. Receptors are also localised to non-vascular structures such as epithelial cells as well as occurring in the central nervous system (CNS) on glia and neurones. Both ETA and ETB receptors are widely distributed, particularly in blood vessels. In human vessels, ETA receptors are mainly located on vascular smooth muscle cells, with ETB receptors being present on endothelial cells lining the vessel wall. ETB receptors may play a role in the release of endothelium-derived relaxing factors such as nitric oxide (NO) and prostanoids from endothelial cells where all three isoforms have a similar potency. ETA receptors present on smooth muscle cells are mainly responsible for contraction, but in animals this can vary depending on the species and vascular bed.

Endothelin Receptor (ET) Antagonists - Endothelin Receptor (ET) Antagonists (ERAs) are a type of targeted therapy used to treat people with pulmonary hypertension (PH). Targeted therapies slow the progression of PH and may even reverse some of the damage to the heart and lungs. ERAs work by reducing the amount of a substance called endothelin in the blood. Endothelin is made in the layer of cells that line the heart and blood vessels. It causes the blood vessels to constrict (become narrower). In people with PH the body produces too much endothelin. This causes the blood vessels in the lungs to become narrow, increasing the blood pressure in the pulmonary arteries. ERAs reduce the amount of endothelin in the blood, therefore limiting the harm an excess of endothelin can cause.

Endothelin Receptor (ET) Antagonist Emerging Drugs Chapters

This segment of the Endothelin Receptor (ET) Antagonist report encloses its detailed analysis of various drugs in different stages of clinical development, including phase III, 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 (ET) Antagonist Emerging Drugs

Aprocitentan: Idorsia Pharmaceuticals Aprocitentan is an orally active dual Endothelin Receptor (ET) Antagonist that is being investigated for patients whose hypertension is uncontrolled despite the use of at least three anti-hypertensive drugs (called resistant hypertension in the medical community). Currently, it is in phase 3 stage of development for the treatment of Resistant hypertension.

Atrasentan: Chinook Therapeutics Atrasentan is a highly potent and selective endothelin receptor A antagonist (ETA) that is currently being evaluated in a phase 3 registration trial (ALIGN) for IgA nephropathy and a phase 2 basket trial (AFFINITY) of primary glomerular diseases, including FSGS and Alport Syndrome.

Sparsentan: Travere Therapeutics Sparsentan is a first-in-class, orally active, single molecule that functions as a high affinity dual-acting antagonist of both endothelin type A (ETA) and angiotensin II subtype 1 (AT1) receptors which are associated with kidney disease progression. Currently, it is Phase 3 stage of development for the treatment of focal segmental glomerulosclerosis (FSGS).

Endothelin Receptor (ET) Antagonist: Therapeutic Assessment

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

Major Players working on Endothelin Receptor (ET) Antagonist

There are approx. 8+ key companies which are developing the Endothelin Receptor (ET) Antagonist. The companies which have their Endothelin Receptor (ET) Antagonist drug candidates in the most advanced stage, i.e. phase III include, Idorsia Pharmaceuticals.

Phases

This report covers around 8+ products under different phases of clinical development like

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

Route of Administration

Endothelin Receptor (ET) 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

• Infusion
• Intradermal
• Intramuscular
• Intranasal
• Intravaginal
• Oral
• Parenteral
• Subcutaneous
• Topical.

Molecule Type

Products have been categorized under various Molecule types such as

• Vaccines
• Monoclonal Antibody
• Peptides
• Polymer
• Small molecule

Product Type

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

Endothelin Receptor (ET) 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 (ET) 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 (ET) Antagonist drugs.

Report Highlights

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

Endothelin Receptor (ET) Antagonist Report Insights

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

Endothelin Receptor (ET) Antagonist Report Assessment

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

Key Questions

Current Scenario and Emerging Therapies:

• How many companies are developing Endothelin Receptor (ET) Antagonist drugs?
• How many Endothelin Receptor (ET) Antagonist drugs are developed by each company?
• How many emerging drugs are in mid-stage, and late-stage of development for Endothelin Receptor (ET) Antagonist?
• What are the key collaborations (Industry-Industry, Industry-Academia), Mergers and acquisitions, licensing activities related to the Endothelin Receptor (ET) 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 (ET) Antagonist and their status?
• What are the key designations that have been granted to the emerging drugs?

Key Players

• Idorsia Pharmaceuticals
• Travere Therapeutics
• Chinook Therapeutics
• Actelion Pharmaceuticals
• Gmax Biopharm
• Noorik Biopharmaceuticals
• Timber Pharmaceuticals
• Spectrum Pharmaceuticals
• Pharmazz

Key Products

• Aprocitentan
• Sparsentan
• Atrasentan
• Bosentan
• Macitentan
• Getagozumab
• Ambrisentan
• Sovateltide
• Sitaxentan
• BQ-123
• Clazosentan

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