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2017 3
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Page 1
Inhibition of Receptor-Interacting Protein Kinase 1 in Chronic Plaque Psoriasis: A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study.
Ludbrook VJ, Budd DC, Thorn K, Tompson D, Votta BJ, Walker L, Lee A, Chen X, Peppercorn A, Loo WJ. Ludbrook VJ, et al. Dermatol Ther (Heidelb). 2024 Feb;14(2):489-504. doi: 10.1007/s13555-024-01097-0. Epub 2024 Feb 19. Dermatol Ther (Heidelb). 2024. PMID: 38372938 Free PMC article.
Twenty-nine patients were randomized 2:1 to GSK2982772 (N = 19) or placebo (N = 10) for 12 weeks. RESULTS: GSK2982772 was well tolerated with trough concentrations greater than tenfold higher than the previous phase 1 study with immediate release. ...This study exam …
Twenty-nine patients were randomized 2:1 to GSK2982772 (N = 19) or placebo (N = 10) for 12 weeks. RESULTS: GSK2982772 was well …
Design, synthesis and biological evaluation of novel cyclic malonamide derivatives as selective RIPK1 inhibitors.
Petró JL, Bényei G, Bana P, Linke N, Horti F, Szabó JE, Szalai KK, Hornyánszky G, Greiner I, Éles J. Petró JL, et al. Bioorg Med Chem Lett. 2024 Mar 1;100:129643. doi: 10.1016/j.bmcl.2024.129643. Epub 2024 Feb 3. Bioorg Med Chem Lett. 2024. PMID: 38316369
RIPK1 is a well-established therapeutic target, due to the presence of a unique kinase-regulating allosteric pocket, which enables selective inhibition. Herein we used GSK2982772 as our starting point in our discovery campaign. Applying isosteric replacement, we successful …
RIPK1 is a well-established therapeutic target, due to the presence of a unique kinase-regulating allosteric pocket, which enables selective …
Small-Molecule Receptor-Interacting Protein 1 (RIP1) Inhibitors as Therapeutic Agents for Multifaceted Diseases: Current Medicinal Chemistry Insights and Emerging Opportunities.
Shi K, Zhang J, Zhou E, Wang J, Wang Y. Shi K, et al. J Med Chem. 2022 Nov 24;65(22):14971-14999. doi: 10.1021/acs.jmedchem.2c01518. Epub 2022 Nov 8. J Med Chem. 2022. PMID: 36346971 Review.
Therefore, small-molecule RIP1 inhibitors with precise targeting and good penetrability have recently been used in potentially therapeutic methods, attracting extensive researcher interest. GSK2982772, developed by GlaxoSmithKline (GSK), became the world's first RIP1 inhib …
Therefore, small-molecule RIP1 inhibitors with precise targeting and good penetrability have recently been used in potentially therapeutic m …
Development of a Once-Daily Modified-Release Formulation for the Short Half-Life RIPK1 Inhibitor GSK2982772 using DiffCORE Technology.
Tompson D, Whitaker M, Pan R, Johnson G, Fuller T, Zann V, McKenzie L, Abbott-Banner K, Hawkins S, Powell M. Tompson D, et al. Pharm Res. 2022 Jan;39(1):153-165. doi: 10.1007/s11095-021-03124-7. Epub 2022 Jan 5. Pharm Res. 2022. PMID: 34988780 Free PMC article.
PURPOSE: GSK2982772 is a selective inhibitor of receptor-interacting protein kinase-1 (RIPK1) with a short 2- to 3-h half-life. ...METHODS: Part A evaluated PK following single-dose (240 mg) fasted and fed (high-fat meal) administration of three DiffCORE MR formulations wi …
PURPOSE: GSK2982772 is a selective inhibitor of receptor-interacting protein kinase-1 (RIPK1) with a short 2- to 3-h half-life. ...ME …
Potent and Selective RIPK1 Inhibitors Targeting Dual-Pockets for the Treatment of Systemic Inflammatory Response Syndrome and Sepsis.
Yang X, Lu H, Xie H, Zhang B, Nie T, Fan C, Yang T, Xu Y, Su H, Tang W, Zhou B. Yang X, et al. Angew Chem Int Ed Engl. 2022 Jan 26;61(5):e202114922. doi: 10.1002/anie.202114922. Epub 2021 Dec 16. Angew Chem Int Ed Engl. 2022. PMID: 34851543
Herein, we have 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, go …
Herein, we have synthesized a class of highly potent dual-mode RIPK1 inhibitors occupying both the allosteric and the ATP binding pockets, e …
Necrostatin-1 Prevents Ferroptosis in a RIPK1- and IDO-Independent Manner in Hepatocellular Carcinoma.
Yuk H, Abdullah M, Kim DH, Lee H, Lee SJ. Yuk H, et al. Antioxidants (Basel). 2021 Aug 25;10(9):1347. doi: 10.3390/antiox10091347. Antioxidants (Basel). 2021. PMID: 34572979 Free PMC article.
Necrostatin-1, ferrostatin-1, and deferoxamine repressed sulfasalazine-provoked membrane permeabilization, as detected by 7-aminoactinomycin D staining and lipid peroxidation measured using a C11-BODIPY probe. However, other RIPK1 inhibitors (necrostatin-1s and GSK2982772) …
Necrostatin-1, ferrostatin-1, and deferoxamine repressed sulfasalazine-provoked membrane permeabilization, as detected by 7-aminoactinomycin …
A randomised, placebo-controlled study of RIPK1 inhibitor GSK2982772 in patients with active ulcerative colitis.
Weisel K, Scott N, Berger S, Wang S, Brown K, Powell M, Broer M, Watts C, Tompson DJ, Burriss SW, Hawkins S, Abbott-Banner K, Tak PP. Weisel K, et al. BMJ Open Gastroenterol. 2021 Aug;8(1):e000680. doi: 10.1136/bmjgast-2021-000680. BMJ Open Gastroenterol. 2021. PMID: 34389633 Free PMC article. Clinical Trial.
RESULTS: Thirty-six patients were randomised (n=12, placebo/open-label GSK2982772; n=24, GSK2982772/open-label GSK2982772). Most adverse events were mild, with headache reported the most frequently across groups (placebo/open-label GSK2982772, n=2 (17% …
RESULTS: Thirty-six patients were randomised (n=12, placebo/open-label GSK2982772; n=24, GSK2982772/open-label GSK2982772 …
Development of a Prototype, Once-Daily, Modified-Release Formulation for the Short Half-Life RIPK1 Inhibitor GSK2982772.
Tompson DJ, Whitaker M, Pan R, Johnson G, Fuller T, McKenzie L, Zann V, Powell M, Abbott-Banner K, Hawkins S. Tompson DJ, et al. Pharm Res. 2021 Jul;38(7):1235-1245. doi: 10.1007/s11095-021-03059-z. Epub 2021 Jun 16. Pharm Res. 2021. PMID: 34136987 Free PMC article. Clinical Trial.
PURPOSE: GSK2982772 is a selective inhibitor of receptor-interacting protein kinase-1, with a 2-3 h half-life. This study evaluated if a once-daily modified-release formulation of GSK2982772 could be developed with no significant food effect. METHODS: Part A evaluat …
PURPOSE: GSK2982772 is a selective inhibitor of receptor-interacting protein kinase-1, with a 2-3 h half-life. This study evaluated i …
A randomized, placebo-controlled experimental medicine study of RIPK1 inhibitor GSK2982772 in patients with moderate to severe rheumatoid arthritis.
Weisel K, Berger S, Thorn K, Taylor PC, Peterfy C, Siddall H, Tompson D, Wang S, Quattrocchi E, Burriss SW, Walter J, Tak PP. Weisel K, et al. Arthritis Res Ther. 2021 Mar 16;23(1):85. doi: 10.1186/s13075-021-02468-0. Arthritis Res Ther. 2021. PMID: 33726834 Free PMC article. Clinical Trial.
RESULTS: A total of 52 patients were randomized (placebo, 18; GSK2982772, 34). Adverse events (AEs) were reported in 13 (72%) in patients in the placebo group (n = 3 b.i.d; n = 10 t.i.d.) and 20 (61%) in the GSK2982772 group (n = 3 b.i.d; n = 17 t.i.d.). ...CONCLUSI …
RESULTS: A total of 52 patients were randomized (placebo, 18; GSK2982772, 34). Adverse events (AEs) were reported in 13 (72%) in pati …
Comparison of the Pharmacokinetics of RIPK1 Inhibitor GSK2982772 in Healthy Western and Japanese Subjects.
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. Tompson DJ, et al. Eur J Drug Metab Pharmacokinet. 2021 Jan;46(1):71-83. doi: 10.1007/s13318-020-00652-2. Eur J Drug Metab Pharmacokinet. 2021. PMID: 33165774 Free PMC article. Clinical Trial.
Part B subjects (N = 47) received GSK2982772 120 mg TID, 240 mg TID, or placebo TID for 14 days. Japanese subjects in Study 2 (N = 13) (NCT03590613) were randomly assigned to receive TID doses of GSK2982772 60, 120, 240 mg TID or placebo TID for 1 day. RESULTS: G …
Part B subjects (N = 47) received GSK2982772 120 mg TID, 240 mg TID, or placebo TID for 14 days. Japanese subjects in Study 2 (N = 13 …
18 results