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Fenebrutinib Versus Placebo or Adalimumab in Rheumatoid Arthritis: A Randomized, Double‐Blind, Phase II Trial
Arthritis & Rheumatology, 2020 ObjectiveTo evaluate fenebrutinib, an oral and highly selective noncovalent inhibitor of Bruton's tyrosine kinase (BTK), in patients with active rheumatoid arthritis (RA).MethodsPatients with RA and an inadequate response to methotrexate (MTX) (cohort 1; n = 480) were randomized to receive fenebrutinib (50 mg once daily, 150 mg once daily, or 200 mg ...Cohen, Stanley, Tuckwell, Katie, Katsumoto, Tamiko R., Zhao, Rui, Galanter, Joshua, Lee, Chin, Rae, Julie, Toth, Balazs, Ramamoorthi, Nandhini, Hackney, Jason A., Berman, Alberto, Damjanov, Nemanja, Fedkov, Dmytro, Jeka, Slawomir, Chinn, Leslie W., Townsend, Michael J., Morimoto, Alyssa M., Genovese, Mark C., Berman, Alberto, Porto, Alejandro, Granel, Amelia, Asnal, Cecilia, Mysler, Eduardo Fabian, Testa, Gladys Alicia, Zamora, Jose Luis Velasco, Moreno, Jose Luis Cristian, Gulin, Juan Pablo, Hofman, Julio, Ulla, Maria Rosa, Sabelli, Mirtha, Mannucci, Pablo Alejandro, Maid, Pablo Jorge, Melazzi, Ana Cláudia Cauceglia, Scotton, Antônio Scafuto, Ximenes, Antônio Carlos, Funes, Elisete, Gimenez, Emerson Alves, Marcolino, Flora Maria D’Andrea, Neto, João Francisco Marques, Keiserman, Mauro Waldemar, Radominski, Sebastião Cézar, Lima, Sônia Maria Alvarenga Anti Loduca, Pavan, Thaís Rohde, Azevedo, Valderílio Feijó, Koleva, Aneliya, Toncheva, Antoaneta, Bichovska, Daniela, Ivanova, Delina, Penev, Dimitar, Dimitrov, Emil, Mihaylova, Mariyana, Kapandjieva, Nadezhda, Marinova, Natalia, Aleksieva, Tanya, Tsvetanova, Tanya, Petranova, Tsvetanka, Popova, Valentina, Spasov, Yuliy, Toro, Carlos Enrique, Arteaga Unigarro, Carlos Ernesto, Jauregui, Edwin, Hernandez, Javier Dario Marquez, Raad, Juan Jose Jaller, Sanchez, Patricia Julieta Velez, Lee, Chang Keun, Suh, Chang‐Hee, Lee, Eun Young, Lee, Sang‐Heon, Kang, Seong Wook, Lee, Shin‐Seok, Lee, Yun Jong, Montiel, Beatriz Elena Zazueta, Pinzon de la O, Blanca Irma, Friedmann, Daniel Xibille, Lopez, Francisco Rosas, Torres, Isaura Rodriguez, Quezada, Luis Jara, Ceceña, Marco Maradiaga, Hernandez, Miguel Cortes, Salinas, Miguel Saavedra, Rapa, Agnieszka, Pawtel, Agnieszka, Zielinska, Agnieszka, Dudek, Anna, Rychlewska‐Hanczewska, Anna, Strzelecka, Anna, Racewicz, Artur, Stasiuk, Barbara, Gruszecka, Katarzyna, Dworak, Krystyna, Jeka, Slawomir, Lowenhoff, Tomasz, Maslyanskiy, Alexey, Rebrov, Andrey, Krechikova, Diana, Zhugrova, Elena, Shmidt, Evgeniya, Matsievskaya, Galina, Vinogradova, Irina, Ler, Irina, Eliseeva, Larisa, Savina, Ludmila, Stanislav, Marina, Sandin, Mikhail, Zyablova, Natalia, Korshunov, Nikolay, Mosesova, Nino, Polovnikova, Oksana, Nesmeyanova, Olga, Samigullina, Ruzana, Moiseev, Sergey, Noskov, Sergey, Raskina, Tatiana, Popova, Tatiana, Marchenko, Valeriy, Jovanovski, Aleksandar, Stamenkovic, Bojana, Ristic, Gorica, Lazarevic, Milijanka, Veselinovic, Mirjana, Vujasinovic‐Stupar, Nada, Damjanov, Nemanja, Ostojic, Predrag, Yagensky, Andriy, Gnylorybov, Andriy, Rekalov, Dmytro, Reshotko, Dmytroo, Fedkov, Dmytro, Dzyak, Georgiy, Gasanov, Iurii, Khimion, Ludmila, Stanislavchuk, Mykola, Prykhodko, Natalya, Nadashkevych, Oleg, Bortkevych, Oleg, Abrahamovych, Orest, Yatsyshyn, Roman, Turyanytsya, Samvel, Smiyan, Svitlana, Vizir, Vadym, Kachur, Victoria, Tseluyko, Vira, Povoroznyuk, Vladyslav, Koshlia, Volodymyr, Zhdan, Vyacheslav, Lymar, Yurii, Mostovoy, Yuriy, Hawkes, Angela, Mabaquiao, Arthur, Chu, Cong‐Qiu, Scoville, Craig, Wyatt, David, Weinstein, Debra, McIlwain, Harris, Vo, Jacqueline, Poiley, Jeffrey, Forstot, Joseph, Dao, Kathryn, Turner, Mark, Genovese, Mark, Borofsky, Michael, Caldron, Paul, Waller, Philip, Levin, Robert, Metyas, Samy, Stein, Scott, Shroff, Sharukh, Pang, Shirley, Cohen, Stanley, Syed, Tauseef, Chindalore, Vishala +170 moreopenaire +2 more sourcesDrug-target interaction network for proteins associated with Alzheimer’s disease and docking poses for representative drug-target pairs calculated by Autodock Vina.
, 2023 (a) Drug-target interaction network predicted by PortalCG. Yellow rectangles and green ovals represent drugs and targets, respectively. (b) Docking pose and ligand binding interactions between protein TIR domain-containing adapter molecule 2 (Uniprot ...Hari Krishna Namballa (14445584), Muge Chen (14445578), Shuo Zhang (30844), Tian Cai (4227052), Michael Dorogan (14445587), Yang Liu (4829), Di He (791903), Wayne W. Harding (1612909), Cameron Mura (243164), Li Xie (108913), Philip E. Bourne (5755), Amitesh Badkul (14445581), Lei Xie (61344) +12 morecore +1 more sourceBruton’s Tyrosine Kinase Inhibition for the Treatment of Rheumatoid Arthritis
ImmunoTargets and Therapy, 2021 Laura C Arneson,1,* Kristen J Carroll,1,* Eric M Ruderman2 1Department of Medicine, Northwestern University Feinberg School of Medicine, Chicago, IL, USA; 2Department of Medicine, Division of Rheumatology, Northwestern University Feinberg School ...Arneson LC, Carroll KJ, Ruderman EMdoaj Bruton's tyrosine kinase inhibition—An emerging therapeutic strategy in immune‐mediated dermatological conditions [PDF]
, 2022 Bruton's tyrosine kinase (BTK), a member of the Tec kinase family, is critically involved in a range of immunological pathways. The clinical application of BTK inhibitors for B-cell malignancies has proven successful, and there is strong rationale for ...Frischbutter, Stefan, Brasileiro, Ana, Mendes-Bastos, Pedro, Pavel Kolkhir, Moñino‐Romero, S, Maurer, Marcus, Mendes‐Bastos, P, Kolkhir, Pavel, Marcus Maurer, Scheffel, Jörg, Pedro Mendes‐Bastos, Brasileiro, A., Ana Brasileiro, Mendes-Bastos, P., Mendes‐Bastos, Pedro, Kolkhir, P, Brasileiro, A, Sherezade Moñino‐Romero, Maurer, M, Moñino-Romero, Sherezade, Scheffel, J, Moñino‐Romero, Sherezade, Jörg Scheffel, Frischbutter, S, Stefan Frischbutter +24 morecore +1 more sourceFenebrutinib reduces disease activity in a mouse model of inflammatory multiple sclerosis, which is associated with reduced microglial activation
, 2021 Weber, M. S., Harp, C., Goodyear, A., Yuen, T., Durk, M., Kappos, L. +5 morecore +4 more sourcesOP0233 EFFICACY, SAFETY, AND PHARMACODYNAMIC EFFECTS OF THE BRUTON'S TYROSINE KINASE INHIBITOR, FENEBRUTINIB (GDC-0853), IN MODERATE TO SEVERE SYSTEMIC LUPUS ERYTHEMATOSUS IN A PHASE 2 CONTROLLED STUDY [PDF]
Annals of the Rheumatic Diseases, 2020 Background: Fenebrutinib (GDC-0853, FEN) is an oral, non-covalent, and selective inhibitor of Bruton’s tyrosine kinase (BTK) in clinical development for autoimmune diseases. Objectives: This was a randomized, placebo-controlled, multi-center study to evaluate the efficacy, safety, and pharmacodynamic effects of FEN in patients with moderate-to ...D. Isenberg, R. Furie, N.S. Jones, P. Guibord, J. Galanter, C. Lee, A. Mcgregor, B. Toth, J. Rae, O. Hwang, A. Lokku, P. Miranda, V. De Souza, J. Jaller-Raad, A. Maura Fernandes, R. Garcia Salinas, L. Chinn, M.J. Townsend, A. Morimoto, K. Tuckwell +19 moreopenaire +1 more sourceEmerging B-Cell Therapies in Systemic Lupus Erythematosus
Therapeutics and Clinical Risk Management, 2021 Ayse Bag-Ozbek,1 Joyce S Hui-Yuen2– 4 1Division of Rheumatology, Renaissance School of Medicine, Stony Brook University Medical Center, Stony Brook, NY, USA; 2Division of Pediatric Rheumatology, Steven and Alexandra Cohen Children Medical Center ...Bag-Ozbek A, Hui-Yuen JSdoaj