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2022 2
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Brepocitinib, Zimlovisertib, and Ropsacitinib in Hidradenitis Suppurativa.
Kimball AB, Peeva E, Forman S, Moiin A, Khattri S, Porter ML, Mangold AR, Ghosh P, Banfield C, Oemar B. Kimball AB, et al. NEJM Evid. 2024 Mar;3(3):EVIDoa2300155. doi: 10.1056/EVIDoa2300155. Epub 2024 Feb 9. NEJM Evid. 2024. PMID: 38335032 Clinical Trial.
Kinase Inhibitors for Hidradenitis SuppurativaThree kinase inhibitor immunomodulators (daily oral brepocitinib, zimlovisertib, and ropsacitinib) were evaluated in this randomized, placebo-controlled trial of 194 patients with hidradenitis suppurativa. ...
Kinase Inhibitors for Hidradenitis SuppurativaThree kinase inhibitor immunomodulators (daily oral brepocitinib, zimlovisertib, and ro …
A Phase 1 Study to Assess Mass Balance and Absolute Bioavailability of Zimlovisertib in Healthy Male Participants Using a (14) C-Microtracer Approach.
Singh RSP, Dowty ME, Salganik M, Brodfuehrer JI, Walker GS, Sharma R, Beebe JS, Danto SI. Singh RSP, et al. Clin Pharmacol Drug Dev. 2022 Jul;11(7):815-825. doi: 10.1002/cpdd.1109. Epub 2022 May 4. Clin Pharmacol Drug Dev. 2022. PMID: 35506501 Free PMC article. Clinical Trial.
All six participants received 300 mg (14) C-zimlovisertib with lower radioactivity per mass unit orally in Period A, then unlabeled zimlovisertib 300 mg orally and (14) C-zimlovisertib 135 mug intravenously (IV) in Period B. Study objectives included extent a …
All six participants received 300 mg (14) C-zimlovisertib with lower radioactivity per mass unit orally in Period A, then unlabeled …
Binding Energy Partition of Promising IRAK-4 Inhibitor (Zimlovisertib) for the Treatment of COVID-19 Pneumonia.
Zapata-Acevedo CA, Guevara-Vela JM, Popelier PLA, Rocha-Rinza T. Zapata-Acevedo CA, et al. Chemphyschem. 2022 Dec 16;23(24):e202200455. doi: 10.1002/cphc.202200455. Epub 2022 Oct 18. Chemphyschem. 2022. PMID: 36044560 Free PMC article.
We investigated the interactions of different fragments of ligands and Interleukin-1 Receptor-Associated Kinase 4 (IRAK-4) throughout the FBDD design of Zimlovisertib, a promising anti-inflammatory, currently in trials to be used for the treatment of COVID-19 pneumonia. .. …
We investigated the interactions of different fragments of ligands and Interleukin-1 Receptor-Associated Kinase 4 (IRAK-4) throughout the FB …
In Retrospect: Root-Cause Analysis of Structure-Activity Relationships in IRAK4 Inhibitor Zimlovisertib (PF-06650833).
Wright SW, Farley KA, Han S, Knafels JD, Lee KL. Wright SW, et al. ACS Med Chem Lett. 2024 Mar 21;15(4):540-545. doi: 10.1021/acsmedchemlett.4c00036. eCollection 2024 Apr 11. ACS Med Chem Lett. 2024. PMID: 38628800
In this paper, we disclose insights on the root causes of three structure-activity relationship (SAR) observations encountered in the discovery of the IRAK4 inhibitor Zimlovisertib (PF-06650833). The first is a nonlinear potency SAR encountered with the isoquinoline ether …
In this paper, we disclose insights on the root causes of three structure-activity relationship (SAR) observations encountered in the discov …