Prolonged and tunable residence time using reversible covalent kinase inhibitors

J. Michael Bradshaw, Jesse M. McFarland, Ville O. Paavilainen, +20

Nature Chemical Biology

Medicinal ChemistryBiochemistryMedicineNatural SciencesTunable Residence Time +3

Preclinical Efficacy and Anti-Inflammatory Mechanisms of Action of the Bruton Tyrosine Kinase Inhibitor Rilzabrutinib for Immune-Mediated Disease

Claire L. Langrish, J. Michael Bradshaw, Michelle Francesco, +11

The Journal of Immunology

Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-<i>d</i>]pyrimidin-7(8<i>H</i>)-one (PRN1371) for the Treatment of Solid Tumors

Ken A. Brameld, Timothy D. Owens, Erik Verner, +13

Journal of Medicinal Chemistry

Drug TargetSolid TumorsPharmacotherapyFgf/fgfr PathwayPotent Fgfr1-4 Inhibitor +18

Discovery of Reversible Covalent Bruton’s Tyrosine Kinase Inhibitors PRN473 and PRN1008 (Rilzabrutinib)

Timothy D. Owens, Ken A. Brameld, Erik Verner, +21

Journal of Medicinal Chemistry

Phase 1 clinical trial evaluating safety, exposure and pharmacodynamics of BTK inhibitor tolebrutinib (PRN2246, SAR442168)

Timothy D. Owens, Patrick F. Smith, Andrew Redfern, +8

Clinical and Translational Science

Chemoprevention StrategyTyrosine KinaseImmunologyPharmacotherapyImmunotherapy +18

A multicenter phase 2 trial of camrelizumab plus famitinib for women with recurrent or metastatic cervical squamous cell carcinoma

Lingfang Xia, Qi Zhou, Yunong Gao, +8

Nature Communications

Cervical CancerMedicineMulticenter Phase 2PharmacologyClinical Trials +11

Humoral immune responses against tumor‐associated antigen OVA66 originally defined by serological analysis of recombinant cDNA expression libraries and its potentiality in cellular immunity

Jin Shu, Ying Wang, Yong Zhang, +5

Cancer Science

Preclinical Mechanisms of Topical PRN473, a Bruton Tyrosine Kinase Inhibitor, in Immune-Mediated Skin Disease Models

Yan Xing, Katherine A. Chu, Jyoti Wadhwa, +11

ImmunoHorizons

Licochalcone A inhibits IgE-mediated allergic reaction through PLC/ERK/STAT3 pathway

Jin Shu, Xu Cui, Xin Liu, +4

International Journal of Immunopathology and Pharmacology

Rilzabrutinib, a reversible covalent Bruton's tyrosine kinase inhibitor: Absorption, metabolism, excretion, and absolute bioavailability in healthy participants

Sibel Ucpinar, Patrick F. Smith, Long Li, +7

Clinical and Translational Science