gsk2982772 clinical trial

b One participant did not comply with contraception requirements. The EU Clinical Trials Register currently displays 40154 clinical trials with a EudraCT protocol, of which 6573 are clinical trials conducted with subjects less than 18 years old. Brief Summary: This study is the first experience with GSK2982772, a receptor-interacting protein-1 (RIP1) kinase inhibitor, in subjects with active ulcerative colitis (UC). The study will evaluate the efficacy, safety, pharmacokinetic and pharmacodynamics profile of 960 milligram (mg) GSK2982772 administered as a once daily modified release (MR) formulation. The inspiration provided by biologically active natural products to conceive of hybrids, congeners, analogs and unnatural variants is discussed by experts in the field in 16 highly informative chapters. Epub 2018 May 24. Planned surgical procedure that makes the participant unsuitable for the study, in the opinion of the Investigator. History of sensitivity to any of the study treatments, or components thereof or a history of drug or other allergy that, in the opinion of the Investigator or Medical Monitor, contraindicates their participation. Found inside – Page 36Encouraged by favorable safety data, GSK has entered GSK2982772 into small phase 2 clinical trials for psoriasis, rheumatoid arthritis, and ulcerative ... GSK2982772 is a highly selective inhibitor of receptor‐interacting protein kinase 1 (RIPK1) being developed to treat chronic inflammatory diseases. U.S. Department of Health and Human Services, The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. (Clinical Trial), Participants will randomized in ratio of 2:1 to receive either 960 mg GSK2982772 or placebo, This is a double-blind study where sponsor will be unblinded, A Multicentre, Randomised, Double-blind, Placebo-controlled Study to Evaluate the Efficacy and Safety of GSK2982772 in Participants With Moderate to Severe Plaque Psoriasis, Experimental: Participants receiving GSK2982772 960 mg, Placebo Comparator: Participants receiving placebo, 18 Years to 75 Years (Adult, Older Adult), Surrey, British Columbia, Canada, V3R 6A7. Participants will receive GSK2982772 960 mg oral tablets once daily for 12 weeks. The RIPK1 inhibitor GSK2982772 developed by GlaxoSmithKline Pharmaceuticals is in Phase II clinical trials for the treatment of ulcerative colitis and psoriasis. Subjects who complete the Part A study will move to open label Part B study to receive GSK2982772 60 mg three times daily for an additional 42 Days (6 weeks). Fecal sample were collected to measure FCP. This study evaluated the PK and safety of the matrix MR formulations of GSK2982772 MT and MM to determine the feasibility of developing a QD regimen to optimize patient compliance. [1] Necrostatin-1 efficiently suppresses necroptotic cell death triggered by an array of stimuli in a variety of cell types. 3, No. Found inside – Page 116By 2018, two clinical candidates originated from DEL hits. ... GSK2982772 (75) was advanced to PIIa trials in 2017 for treating inflammatory disorders such ... Psoriatic lesions will be assessed using the PASI scoring system. Found insideTopics covered in this new volume include DELT, Oligos: ASO, siRNA, CRISPR, Micro-fluidic chemistry, High throughput screening, Kinase-centric computational drug development, Virtual Screening, Phenotypic screening, PROTACS, Chemical ... Participants whose value category was unchanged (e.g., High to High), or whose value became within range, were recorded in the 'To within Range or No Change' category. Safety, tolerability, pharmacokinetics (PK), RIPK1 target engagement (TE), and pharmacodynamics (PD) were assessed. In cases where the QuantiFERON or T-spot test is positive, but a follow-up chest x-ray, locally read by a radiologist, shows no evidence of current or previous pulmonary tuberculosis, the subject may be eligible for the study at the discretion of the Investigator and GlaxoSmithKline (GSK) Medical Monitor. RIP kinases: key decision makers in cell death and innate immunity. Participants between 18 and 75 years of age inclusive, at the time of signing the informed consent. In Part A, subjects in Cohorts 1 and 2 were randomizedâ¦, Part A. Females on hormone replacement therapy (HRT) and whose menopausal status is in doubt will be required to use one of the highly effective contraception methods if they wish to continue their HRT during the study. 8600 Rockville Pike Geboes score is a 7-items instrument which classifies histologic changes and generates a score from 0 to 5.4. Weiselfi etfial BMJ Open Gastro 2218:e68 doi:11136bmjgast22168 1 A randomised, placebo-controlled study of RIPK1 inhibitor GSK2982772 in patients with active ulcerative colitis Kathy Weisel,1 Nicola Scott,2 Scott Berger,1 Susanne Wang,1 Kurt Brown,1 Marcy Powell,3 Matthijs Broer,4 Clarissa Watts,5 Debra J Tompson,6 Susan W Burriss,7 Simon Hawkins,8 Kathy Abbott-Banner ,9 Paul Peter Tak10 The body region scores are each multiplied by a weighted factor; and the sum of the region scores give the overall PASI score. Baseline is defined as the latest pre-dose assessment at Screening (within 30 days prior to Day 1). The clinical concern range for vital signs were: systolic blood pressure (SBP) (low: <85 and high: >160 millimeters of mercury [mmHg]); diastolic blood pressure (DBP) (low: <45 and high: >100 mmHg). History of receiving a live or attenuated vaccine within 30 days of randomization OR plan to receive a live or attenuated vaccination during the study until completion of the follow-up visit. Blood samples were collected to measure CRP. Positive serology for Human Immunodeficiency Virus (HIV) 1 or 2. Search Results A Study to Evaluate the Benefit and Safety of GSK2982772 in Moderate to Severe Psoriasis Participants These include Phase II trials enrolling patients with moderate to severe rheumatoid arthritis (NCT02858492), ulcerative colitis (NCT02903966), or plaque-type psoriasis (NCT02776033). A Complete Mayo Score of >=3 points and endoscopy sub score of 2 to 3 at screening, despite concurrent treatment with at least 1 of the following (oral corticosteroids or any oral 5-aminosalicylates (5-ASA) or purine analogues or all as defined): Oral 5-ASA at a stable dose (equivalent to >=2.4 grams per day (g/day) of Asacol) for at least 4 weeks prior to first dose. Contraceptive use by men or women should be consistent with local regulations regarding the methods of contraception for those participating in clinical studies. Namour F, Vanhoutte FP, Beetens J, Blockhuys S, De Weer M, Wigerinck P. Drugs R D. 2012 Sep 1;12(3):141-63. doi: 10.2165/11633120-000000000-00000. Subjects will receive GSK2982772 60 mg orally three times daily (approximately 8 hours apart) for 42 days (6 weeks). Current or history of renal disease or estimated glomerular filtration rate (GFR) by Chronic Kidney Disease Epidemiology Collaboration equation (CKD-EPI) calculation <60 milliliter per minute per 1.73 meter square (mL/min/1.73 m^2) at screening. Study record managers: refer to the Data Element Definitions if submitting registration or results information. Subject with current history of suicidal ideation behavior (SIB) as measures using the Columbia Suicide Severity Rating Scale (C-SSRS) or history of attempted suicide. You have reached the maximum number of saved studies (100). The Investigator is responsible for review of medical history, menstrual history, and recent sexual activity to decrease the risk for inclusion of a woman with an early undetected pregnancy. BL is defined as the latest pre-dose assessment. Trial registration: "Repurposing these drugs for the treatment of AAV seems reasonable." Discussions of the role of cell death in AIDS, inflammatory disease, lung and cardiac disease, and lupus each emphasize the importance of understanding and regulating inflammation and the production of apoptotic bodies. Presence of hepatitis C antibody at Screening. Participants will be randomized in a 2:1 ratio to receive either 960 mg GSK2982772 or placebo for 12 weeks. FOIA The EU Clinical Trials Register currently displays 40231 clinical trials with a EudraCT protocol, of which 6586 are clinical trials conducted with subjects less than 18 years old. Number of participants with worst-case clinically significant and not clinically significant abnormal ECG findings have been presented. G protein-coupled receptors (GPCRs) are a large protein family of transmembrane receptors vital in dictating cellular responses. GPCRs are involved in many diseases, but are also the target of around half of all modern medicinal drugs. Erythema, induration, and scale are each graded on a 5-point scale (0-4), and the percent body Surface Area (BSA) affected is scored on a 7-point scale (0-6) for each of the 4 specified body regions (head, upper extremities, trunk, and lower extremities). Disclaimer, National Library of Medicine -, Degterev A, Hitomi J, Germscheid M, et al. These medical conditions should be stable at the time of screening and are expected to remain stable for the duration of the study. Gsk2982772 Supplier and Supplier and structural formula Gsk2982772 Supplier and Supplier and structural formula. Other medications (including vitamins, herbal and dietary supplements) will be considered on a case-by-case basis and will be allowed if the medication will not interfere with the study procedures or compromise participant safety, in the opinion of the Investigator. It covers the pipeline drug profiles, including clinical and . 2021 Mar 16;23(1):85. doi: 10.1186/s13075-021-02468-0. The most common adverse events (AEs) were contact dermatitis and headache. Found inside – Page iIn this comprehensive two-volume resource on the topic senior lead generation medicinal chemists present a coherent view of the current methods and strategies in industrial and academic lead generation. This does not include infections that may occur in immunocompetent individuals, such as fungal nail infections or vaginal candidiasis, unless it is of an unusual severity or recurrent nature. Hematology parameters with their PCI ranges were: hematocrit (high: >0.54 proportion of red blood cells in blood and low: change from BL<0.075); hemoglobin (high: >180 grams per liter [g/L] and low: change from BL<25 g/L); lymphocytes (low: <0.8 Giga cells/L); platelet count (low: <100 Giga cells/L and high: >550 Giga cells/L); neutrophil count (low: <1.5 Giga cells/L); white blood cell (WBC) count (low: <3 Giga cells/L and high: >20 Giga cells/L). Subject with fulminant UC, or UC limited to the rectum (disease extent <15 centimeters (cm) from the anal verge). Candidate for systemic therapy or phototherapy (includes naïve or previously treated), in the opinion of the Investigator. Participants whose value category was unchanged (e.g., High to High), or whose value became within range, were recorded in the 'To within Range or No Change' category. Participants were counted in the worst case category that their value changed to (low, within range or no change, or high) unless there was no change in their category. Cell Discov. GSK2982772 is the potential first oral, monoselective, ATP competitive, small-molecule inhibitor of RIPK1 and necroptosis to advance into human clinical studies. Clinical Trials Nct Page; GSK2982772 Study in Subjects With Ulcerative Colitis A Multicentre, Randomised, Double-blind (Sponsor Unblinded), Placebo-controlled Study With Open Label Extension to Investigate the Safety and Tolerability, Pharmacokinetics, Pharmacodynamics, and Efficacy of GSK2982772 in Subjects With Active Ulcerative Colitis -. Tunicamycin Inhibits N-linked Glycosylation, GlcNAc Phosphotransferase and Induces ER Stress. GSK2982772 binds in an allosteric pocket of the RIPK1 kinase domain and is a potent inhibitor of RIPK1-mediated cell death and cytokine production in preclinical models. Tompson DJ, Davies C, Scott NE, Cannons EP, Kostapanos M, Gross AS, Powell M, Ino H, Shimamura R, Ogura H, Nagakubo T, Igarashi H, Nakano A. Eur J Drug Metab Pharmacokinet. Methods. Individual sub-scales were vascular pattern (0=Normal, 1=Patchy loss, 2=Obliterated); bleeding (0=None, 1=Mucosal, 2=Luminal mild, 3=Luminal severe); erosions and ulcerations (0=None, 1=Erosions, 2=Superficial ulcer, 3=Deep ulcer). BMJ Open Gastroenterol. GSK2982772 is highly selective, binding to an allosteric pocket of the RIPK1 kinase domain to inhibit RIPK1-mediated cell death and cytokine production.11 The objective of the current study was to examine the safety, pharmacokinetic (PK), pharmacodynamic (PD), and preliminary efficacy of GSK2982772, a first-in-class, RIPK1 small-molecule inhibitor This study is the first experience with GSK2982772, a receptor-interacting protein-1 (RIP1) kinase inhibitor, in subjects with active ulcerative colitis (UC). Studies a U.S. FDA-regulated Drug Product: Studies a U.S. FDA-regulated Device Product: Percentage of participants who achieve >=75 percent improvement from Baseline in Psoriasis Area Severity Index (PASI) score at Week 12 [ Time Frame: Baseline and Week 12 ], Percentage of participants who achieve >=50 percent improvement from Baseline in PASI score at Week 12 [ Time Frame: Baseline and Week 12 ], Percentage of participants who achieve >=90 percent improvement from Baseline in PASI score at Week 12 [ Time Frame: Baseline and Week 12 ], Percentage of participants who achieved >=100 percent improvement from Baseline in PASI score at Week 12 [ Time Frame: Baseline and Week 12 ], Change from Baseline PASI scores at Week 12 [ Time Frame: Baseline and Week 12 ], Percentage of participants who have a Static Investigator's Global Assessment (sIGA) score of 0 or 1 at Week 12 [ Time Frame: At Week 12 ], Change from Baseline in psoriatic BSA at Week 12 [ Time Frame: Baseline and Week 12 ]. New life-saving treatments for ulcerative colitis in clinical trial on A multicentre randomised double-blind (sponsor-unblinded) placebo-controlled study with open label extension to investigate the safety and tolerability pharmacokinetics pharmacodynamics and efficacy of GSK2982772 in subjects with active ulcerative colitis It is either machine-read or manually over-read. Within 30 Days of screening visit, subjects will be randomized to receive either GSK2982772 60 mg or placebo orally three times daily for 42 Days (6 weeks) in a 2:1 ratio in Part A study. Expert Opin Ther Pat. Privacy, Help For information about participating in this trial, including eligibility criteria, email Heather Dufficy Lampone at heather.dufficylampone@nyulangone.org. Pharmaceuticals R&D expenditure was £3,348 million, up 19% AER, 16% CER, with a significant increase in study and clinical trial material investment in Oncology compared with 2018 reflecting the progression of assets from the Tesaro acquisition, primarily Zejula and dostarlimab, and a number of other programmes, including belantamab mafodotin . An AE is any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. The 4 sub-scores are stool frequency (0=normal number of stools; 1=1 to 2 stools/day more than normal; 2=3 to 4 stools/day more than normal; 3= >4 stools/day more than normal); rectal bleeding (0=no blood seen; 1=visible blood with stools less than half the time; 2= visible blood with stool half the time or more; 3=passing blood alone); findings at endoscopy (0=normal or inactive disease; 1=mild disease [erythema, decreased vascular pattern, mild friability]; 2=moderate disease [marked erythema, lack of vascular pattern, friability, erosions]; 3=severe disease [spontaneous bleeding, ulceration]); and PGA (0=normal; 1=mild; 2=moderate; 3=severe). 9 GSK2982772 possesses high in vitro potency and excellent kinase selectivity, which combined with has highly favorable physicochemical and pharmacokinetic . -, Kopalli SR, Kang TB, Koppula S. Necroptosis inhibitors as therapeutic targets in inflammation mediated disorders â a review of the current literature and patents. This volume will be useful to transplant cardiologists, cardiovascular surgeons, cardiac pathologists and transplant scientists who seek to prolong the lifespan and improve the quality of life of their transplant recipients. This first‐in‐human study evaluated safety, tolerability, pharmacokinetics (PK), and exploratory pharmacodynamics (PD) of GSK2982772 administered orally to healthy male volunteers. Unable to load your collection due to an error, Unable to load your delegates due to an error, Study design. Hereditary or acquired immunodeficiency disorder, including immunoglobulin deficiency unless subject has a documented history of selective immunoglobulin A (IgA) deficiency. A 5-point scoring system will be used to measure the severity of psoriatic lesions over the entire body at the time of evaluation. GSK 2982772 is a receptor-interacting protein-1 (RIP1) kinase inhibitor, that is being devloped by GlaxoSmithKline, for the treatment of inflammatory bowel Where participation in the study would result in donation of blood or blood products in excess of 500 mL within 3 months. GSK2982772 will be available as MR tablet at a unit dose strength of 480 mg. PA Harris et al. Participants whose value was unchanged (e.g., Trace to Trace), or whose value was decreased, were recorded in the 'No change or Decreased' category. 4 295. Keywords: This book draws together contributions from an international group of scientists and clinicians from diverse disciplines, ranging from epidemiology to immunology, cell biology, molecular oncology, molecular medicine and pharmacology to ... eCollection 2021 Jun 1. History of hypertrophic or keloid scarring. Targeting a cell-death regulator to treat autoimmune diseases. This was a Phase I, randomized, placebo‐controlled, double . This book starts with an introduction that reviews the general characteristics of apoptosis, its regulation and its role in physiology and disease. Next, the book focuses on three areas as they relate to inflammatory cells and diseases. The clinical concern range for vital signs were: SBP (low: <85 and high: >160 mmHg); DBP (low: <45 and high: >100 mmHg). After the open label (Part B) treatment period, subjects will enter the Follow-up period which lasts for 28 Days (+/- 3 Days) post the last administration of study medication. MRS Score ranges from 0 to 7, with higher scores indicates more severity. Psoriatic lesions will be assessed using the PASI scoring system. This timely guide to kinase inhibitor drug development is the first to cover the entire drug pipeline, from target identification to compound development and clinical application. Although no formal hypothesis will be tested, these endpoints will enable a broader understanding of the mechanism of action and potential for clinical efficacy of GSK2982772 in UC. Clinical trial for Rheumatoid Arthritis , Safety and Tolerability Pharmacokinetics (PK) Pharmacodynamics (PD) and Efficacy of Repeat Doses of GSK2982772 in Subjects With Moderate to Severe Rheumatoid Arthritis (RA) -, Zhou W, Yuan J. Necroptosis in health and diseases. All subjects will receive GSK2982772 60 mg three times daily (approximately 8 hours apart) for 42 days (6 weeks). Found inside – Page 16ripK1 inhibitor, gsK2982772 (19), has advanced into phase 2a clinical trials for the treatment of psoriasis, ulcerative colitis, and rheumatoid arthritis.44 ... The use of these direct target engagement assays in pharmaceutical development can support mechanism of action h 2019 Emerging Investigators Please refer to this study by its ClinicalTrials.gov identifier (NCT number): NCT04316585. Greater than 90% RIPK1 TE was achieved over a 24-hour period for the 60-mg and 120-mg BID dosing regimens. Body mass index (BMI) within the range of 18.5 to 40.0 kilogram (kg)/meter square (m^2). The 4 sub-scores are stool frequency (0=normal number of stools; 1=1 to 2 stools/day more than normal; 2=3 to 4 stools/day more than normal; 3= >4 stools/day more than normal); rectal bleeding (0=no blood seen; 1=visible blood with stools less than half the time; 2= visible blood with stool half the time or more; 3=passing blood alone); findings at endoscopy (0=normal or inactive disease; 1=mild disease [erythema, decreased vascular pattern, mild friability]; 2=moderate disease [marked erythema, lack of vascular pattern, friability, erosions]; 3=severe disease [spontaneous bleeding, ulceration]); and PGA (0=normal; 1=mild; 2=moderate; 3=severe). These include Phase II trials enrolling patients with moderate to severe rheumatoid arthritis (NCT02858492), ulcerative colitis (NCT02903966), or plaque‐type psoriasis (NCT02776033). UCEIS was used as an additional tool to assess disease activity based on 3 sub-scales: 'endoscopic vascular pattern, bleeding, erosions and ulcerations'. GSK2982772 psoriasis RIP1 kinase inhibitor viral COPD exacerbations PI4K beta inhibitor uncomplicated urinary tract infection (uUTI) gonorrhea (GC) BLENREP COVID-19 SCB-2019 (Clover Biopharmaceuticals) Ɨ SARS-CoV-2 vaccine (Sanofi) Ɨ Coronavirus-like particle COVID-19 vaccine (Medicago) Ɨ recombinant protein-adjuvanted GSK2982772 matching placebo tablets will be administered via the oral route. Support progression into Phase II clinical trials for psoriasis, special populations, and colitis. Beats per min [ bpm ] and high > 100 bpm ) as a positive QuantiFERON-TB test! 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