MRGPRX4

Existing investor Sanofi Ventures came back for Escient's series C fundraise, throwing money in the pot to support the ultimate goal of creating new small molecule therapeutics. Escient Pharmaceuticals has scored $120 million, a much heftier sum than its series B haul from a few years ago and once again snagging support from Big Pharma Sanofi’s VC arm. The series C financing round was co-led by new investors New Enterprise Associates, Abingworth and Forge Life Science Partners, with existing investors Sanofi Ventures and 5AM Ventures in tow, among others. The San Diego biotech’s fundraise follows a $77.5 million series B in September 2020, a round that occurred alongside Escient’s first in-human tests. Now, the $120 million will help the biotech push forward investigational small molecule therapeutics for several neurosensory-inflammatory disorders, with a focus on lead candidates EP547 and EP262. The assets are designed to inhibit cell surface receptors called Mas-related G protein-coupled receptors, or MRGPRs, which mediate the neuro-immune overactivation associated with many chronic disorders. By using small molecules to specifically block MRGPRX2 and MRGPRX4 activation, the company aims to develop oral medications for neurosensory-inflammatory diseases without the serious side effects tied to other approaches, Escient CEO Joshua Grass said in a Nov. 28 release. The $120 million financing will help the company advance its pipeline to clinical proof-of-concept in multiple indications. EP547 targets MRGPRX4 with the aim of treating cholestatic and uremic pruritus, a form of severe itching resulting from liver or kidney disease. The asset is being evaluated in phase 2 and phase 1 trials, respectively, and Escient is exploring its potential in other unnamed indications. EP262 is a MRGPRX2 antagonist in preclinical studies for chronic spontaneous urticaria, chronic inducible urticaria and atopic dermatitis.

SAN DIEGO--( BUSINESS WIRE )--Escient Pharmaceuticals, a clinical-stage company advancing novel small molecule therapeutics for the potential treatment of a broad range of neurosensory-inflammatory disorders, today announced the initiation of a Phase 2 clinical study of EP547 in subjects with cholestatic pruritus. EP547 is a highly selective antagonist of MRGPRX4, a cell surface receptor expressed on sensory neurons that is activated by bile acids, bilirubin and other heme metabolites and thought to be a key mediator of the often intense itch experienced by patients with cholestatic liver disease. The Phase 2 study, PACIFIC, is a randomized, double-blind, placebo-controlled study designed to assess the efficacy, safety and tolerability of EP547 in subjects with cholestatic pruritus due to primary biliary cholangitis (PBC) or primary sclerosing cholangitis (PSC). “ Intense, unrelenting itch is a common and often debilitating symptom for people living with PBC, PSC and other cholestatic liver diseases. There remains a large unmet need for safe and more efficacious treatments,” said Gideon Hirschfield, FRCP, PhD, Chair in Autoimmune Liver Disease Research, Professor, Division of Gastroenterology and Hepatology, University of Toronto, and a lead investigator of the PACIFIC study. “ Accumulation of bile acids and other bile components in the skin has long been implicated as a potential cause of cholestatic pruritus, and blocking the activation of sensory itch neurons by bile acids with EP547 thus represents a promising, mechanistically targeted therapeutic approach. It really is quite exciting and innovative to be testing the concept that cholestatic itch is in part a neurosensory-inflammatory process.” “ Building upon the excellent safety, tolerability and PK profile of EP547 in our previously completed Phase 1 study, we are excited to initiate the Phase 2 PACIFIC study, designed to establish definitive clinical proof-of-concept of MRGPRX4 antagonism in cholestatic pruritus,” said Christian Weyer, MD, President and Chief Medical Officer at Escient Pharmaceuticals. “ While the initial focus of our clinical program is focused on PBC and PSC, we believe EP547 has broad potential as a targeted anti-pruritic treatment for other forms of intra- and extrahepatic cholestasis.” The Phase 2 PACIFIC study will enroll approximately 58 patients with moderate-to-severe pruritus due to PBC or PSC. The study comprises a 6-week double-blind treatment period in which subjects are randomized 1:1 to 100mg EP547 or placebo, dosed orally once daily, followed by a 6-week open label extension period in which all subjects receive EP547. The primary efficacy endpoint is the change from baseline to week 6 in itch intensity. Visit www.pacificitchstudy.com to learn more. About Escient Pharmaceuticals Escient Pharmaceuticals is a clinical-stage company focused on developing novel therapeutics to address a broad range of neurosensory-inflammatory disorders. The company’s pipeline includes two first-in-class small molecule antagonists targeting MRGPRX2 for the treatment of various mast cell mediated disorders and MRGPRX4 for cholestatic pruritus. Based in San Diego, California, Escient is led by an experienced management and scientific team and funded by top-tier life science investors. Visit www.escientpharma.com to learn more.

Los Angeles, USA , July 13, 2021 (GLOBE NEWSWIRE) -- Uremic Pruritus Pipeline Shows Rapid Progress in Clinical Trials Around 6+ key companies are developing Uremic Pruritus therapies. The drug candidate Difelikefalin by Cara Therapeutics has been accepted and granted priority review by the US Food and Drug Administration. DelveInsight’s “Uremic Pruritus Pipeline Insight” report provides comprehensive insights about 6+ companies and 6+ pipeline drugs in the Uremic Pruritus pipeline landscapes. It comprises Uremic Pruritus pipeline drug profiles, including clinical and non-clinical stage products. It also includes the Uremic Pruritus therapeutics assessment by product type, stage, route of administration, and molecule type and further highlights the inactive Uremic Pruritus pipeline products. Some of the key takeaways from the Uremic Pruritus Pipeline Report Get an overview of pipeline landscape @ Uremic Pruritus Clinical Trials Analysis Uremic Pruritus is also called chronic kidney disease-associated pruritus (CKD-associated pruritus). Uremia refers to excessive urea in the blood and occurs when both kidneys stop working. Pruritus, or itch, is a common problem for patients with chronic renal failure or end-stage renal disease. Uremic Pruritus Emerging Drugs HSK 21542 is an opioid kappa receptor agonist being developed and investigated in Phase II clinical trial to treat Uremic pruritus by Haisco Pharmaceutical. The main objective is to evaluate the safety, pharmacokinetics, and efficacy of HSK21542 injection in subjects undergoing hemodialysis. It is being investigated to be administered via the parenteral route of administration. Lumos Therapeutics’ LT 5001 is a drug candidate for Uremic Pruritus. The drug has secured Taiwan FDA approval for conducting an Ib/2 trial. It is being developed to be applied topically. It is a partial mu-opioid antagonist and kappa-opioid agonist. The formulation is considered to have the ability to modulate opioid receptors on immune cells and sensory nerves. EP547 is an MRGPRX4 targeted product candidate to treat cholestatic and uremic pruritus being evaluated by Escient Pharmaceuticals. The Phase I/Ib trial of EP547 is a randomized, double-blind, placebo-controlled study to assess the safety, tolerability, and pharmacokinetics of single and multiple ascending doses of EP547 in healthy subjects and subjects with cholestatic or uremic pruritus. For further information, refer to the detailed report @ Uremic Pruritus Pipeline Therapeutics Scope of Uremic Pruritus Pipeline Drug Insight ·       Uremic Pruritus Therapies Late-stage (Phase III)  ·       Uremic Pruritus Therapies Mid-stage (Phase II)·       Uremic Pruritus Therapies Early-stage (Phase I) ·       Uremic Pruritus Pre-clinical stage and Discovery candidates     ·       Discontinued and Inactive candidates ·       Opioid kappa receptor agonists ·       Kappa-opioid receptor agonist ·       Natural metabolites·       Monoclonal Antibody  ·      Small molecule ·     Intravenous ·      Oral·     Subcutaneous ·      Intramuscular ·       Monotherapy·       Combination·       Mono/Combination Key Questions regarding Current Uremic Pruritus Treatment Landscape and Emerging Therapies Answered in the Pipeline Report Table of Contents Get a customized pipeline report @ Uremic Pruritus Drugs Pipeline Report Related Reports About DelveInsightDelveInsight is a leading Business Consultant, and Market Research firm focused exclusively on life sciences. It supports Pharma companies by providing comprehensive end-to-end solutions to improve their performance. It also provides Healthcare Consulting services comprising credible market analysis that will help accelerate the business growth and overcome challenges with a practical approach.