GSK2982772 / GSK 
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  • ||||||||||  GSK2982772 / GSK
    Clinical, Journal:  Inhibition of Receptor-Interacting Protein Kinase (Pubmed Central) -  Feb 19, 2024   
    P1
    The active enantiomer proved to be kinase selective. Administration of the RIPK1 inhibitor GSK2982772 to patients with moderate to severe plaque psoriasis did not translate into meaningful clinical improvements.
  • ||||||||||  GSK2982772 / GSK
    Journal:  Potent and Selective RIPK1 Inhibitors Targeting Dual-Pockets for the Treatment of Systemic Inflammatory Response Syndrome and Sepsis. (Pubmed Central) -  Feb 11, 2022   
    The emerging biological understanding of the role of RIPK1 in sepsis has opened up an exciting opportunity to explore potent and selective RIPK1 inhibitors as an effective therapeutic strategy for SIRS and sepsis therapy. Herein, we synthesized a class of highly potent dual-mode RIPK1 inhibitors occupying both the allosteric and the ATP binding pockets, exemplified by compound 21 ( ZB-R-55 ) which is about 10-fold more potent than GSK2982772 , and exhibits excellent kinase selectivity, good oral pharmacokinetics and good therapeutic effects in the LPS-induced sepsis model, suggesting that compound ZB-R-55 is a highly promising preclinical candidate.
  • ||||||||||  GSK2982772 / GSK
    Trial completion, Phase classification:  A Study to Evaluate the Benefit and Safety of GSK2982772 in Moderate to Severe Psoriasis Participants (clinicaltrials.gov) -  Nov 11, 2021   
    P1,  N=29, Completed, 
    However, no significant differences in efficacy were observed between treatment groups, suggesting that GSK2982772 as monotherapy is not a promising treatment for patients with active UC. Active, not recruiting --> Completed | Phase classification: P1/2 --> P1
  • ||||||||||  RSL3 / Stanford University
    Journal, IO biomarker:  Necrostatin-1 Prevents Ferroptosis in a RIPK1- and IDO-Independent Manner in Hepatocellular Carcinoma. (Pubmed Central) -  Sep 29, 2021   
    Necrostatin-1 potentiated sulfasalazine-induced expression of xCT, a catalytic subunit of system xc- in these cells. These results demonstrated that necrostatin-1 blocked ferroptosis through a mechanism independent from RIPK1 and IDO inhibition in Huh7 and SK-HEP-1 cells, indicating that its antioxidant activity should be considered when using necrostatin-1 as a RIPK1 inhibitor.
  • ||||||||||  GSK2982772 / GSK
    Clinical, PK/PD data, Journal:  Comparison of the Pharmacokinetics of RIPK1 Inhibitor GSK2982772 in Healthy Western and Japanese Subjects. (Pubmed Central) -  Sep 25, 2021   
    P1
    The pharmacokinetics and tolerability of GSK2982772 were similar between Western and Japanese subjects, justifying inclusion of Japanese subjects in future global clinical studies to assess the therapeutic potential of RIPK1 inhibition for the treatment of IMIDs. Clinical Trials: NCT03305419 and NCT03590613 available from http://www.clinicaltrials.gov .
  • ||||||||||  GSK2982772 / GSK
    Clinical, Journal:  Response to inhibition of receptor-interacting protein kinase 1 (RIPK1) in active plaque psoriasis: a randomized placebo-controlled study. (Pubmed Central) -  May 25, 2021   
    The objective of this phase IIa multicenter, randomized, double-blind, placebo-controlled study was to evaluate safety, tolerability pharmacokinetics, pharmacodynamics, and preliminary efficacy of GSK2982772, a RIPK1 inhibitor, in plaque-type psoriasis...Reductions in epidermal thickness and infiltration by CD3+ T cells in epidermis and dermis were observed compared with placebo. Results support the rationale for additional studies on RIPK1 inhibition in IMIDs.
  • ||||||||||  GSK2982772 / GSK
    Journal:  RIPK1 inhibitor ameliorates colitis by directly maintaining intestinal barrier homeostasis and regulating following IECs-Immuno crosstalk. (Pubmed Central) -  Jul 21, 2020   
    As a candidate in clinical study, GSK2982772 is the most well-developed drug of RIPK1 inhibitors, and we chose it as our study object...Taken together, RIPK1 inhibitor exerts suppressive function in intestinal inflammatory response possibly via protecting the intestinal epithelial barrier and maintaining the homeostasis of immune microenvironments. Eventually, the positive feedback immune response which triggered progressive epithelial cells injury could be restrained.
  • ||||||||||  GSK2982772 / GSK
    Trial completion date, Trial initiation date, Trial primary completion date:  A Study to Evaluate the Benefit and Safety of GSK2982772 in Moderate to Severe Psoriasis Participants (clinicaltrials.gov) -  Apr 16, 2020   
    P1,  N=21, Not yet recruiting, 
    Eventually, the positive feedback immune response which triggered progressive epithelial cells injury could be restrained. Trial completion date: Feb 2021 --> Jul 2021 | Initiation date: May 2020 --> Sep 2020 | Trial primary completion date: Jan 2021 --> Jun 2021
  • ||||||||||  GSK2982772 / GSK
    Enrollment closed:  GSK2982772 Study in Subjects With Ulcerative Colitis (clinicaltrials.gov) -  Apr 16, 2019   
    P2,  N=36, Active, not recruiting, 
    We also analyzed structure-kinetic relationship (SKR) for our novel chemical series and discussed the importance of evaluating drug-target residence time for lead optimization. Recruiting --> Active, not recruiting
  • ||||||||||  GSK2982772 / GSK
    Enrollment change, Trial completion date, Trial suspension, Trial primary completion date:  A Safety and Pharmacokinetic (PK) Study of GSK2982772 in Healthy Subjects (clinicaltrials.gov) -  Mar 23, 2018   
    P1,  N=66, Suspended, 
    Active, not recruiting --> Recruiting | Trial completion date: Jul 2018 --> Jan 2019 | Trial primary completion date: Jul 2018 --> Jan 2019 N=48 --> 66 | Trial completion date: May 2018 --> Oct 2018 | Recruiting --> Suspended | Trial primary completion date: May 2018 --> Oct 2018
  • ||||||||||  GSK2982772 / GSK
    Trial primary completion date:  GSK2982772 Study in Subjects With Ulcerative Colitis (clinicaltrials.gov) -  Jul 7, 2017   
    P2,  N=36, Recruiting, 
    Not yet recruiting --> Recruiting Trial primary completion date: Nov 2018 --> Apr 2019