Pharmacokinetic characteristics of vactosertib, a new activin receptor-like kinase 5 inhibitor, in patients with advanced solid tumors in a first-in-human phase 1 study

TGFβ drives immune evasion in genetically reconstituted colon cancer metastasis

(2018) Daniele V. F. Tauriello et al.   NATURE

Sustained-release ruxolitinib: Findings from a phase 1 study in healthy subjects and a phase 2 study in patients with myelofibrosis

(2018) Srdan Verstovsek et al.   HEMATOLOGICAL ONCOLOGY

Association of TGF-β responsive signature with anti-tumor effect of vactosertib, a potent, oral TGF-β receptor type I (TGFBRI) inhibitor in patients with advanced solid tumors.

(2018) Vicki Leigh Keedy et al.   JOURNAL OF CLINICAL ONCOLOGY

TGFβ attenuates tumour response to PD-L1 blockade by contributing to exclusion of T cells

(2018) Sanjeev Mariathasan et al.   NATURE

Transforming growth factor-β: A therapeutic target for cancer

(2017) Sulsal Haque et al.   Human Vaccines & Immunotherapeutics

Critical parameters in targeted drug development: the pharmacological audit trail

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TCR signaling intensity controls CD8+ T cell responsiveness to TGF- 

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Targeting the TGFβ pathway for cancer therapy

(2015) Cindy Neuzillet et al.   PHARMACOLOGY & THERAPEUTICS

Pharmacokinetic, pharmacodynamic and biomarker evaluation of transforming growth factor-β receptor I kinase inhibitor, galunisertib, in phase 1 study in patients with advanced cancer

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Discovery of N-((4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): A Highly Potent, Selective, and Orally Bioavailable Inhibitor of TGF-β Type I Receptor Kinase as Cancer Immunotherapeutic/Antifibrotic Agent

(2014) Cheng Hua Jin et al.   JOURNAL OF MEDICINAL CHEMISTRY

EW-7197, a Novel ALK-5 Kinase Inhibitor, Potently Inhibits Breast to Lung Metastasis

(2014) J. Y. Son et al.   MOLECULAR CANCER THERAPEUTICS

Early phase clinical trials to identify optimal dosing and safety

(2014) Natalie Cook et al.   Molecular Oncology

Determining the optimal dose in the development of anticancer agents

(2014) Ron H. J. Mathijssen et al.   Nature Reviews Clinical Oncology

Targeting the Transforming Growth Factor-β Signaling in Cancer Therapy

(2013) Yhun Yhong Sheen et al.   Biomolecules & Therapeutics

Defining a therapeutic window for the novel TGF-β inhibitor LY2157299 monohydrate based on a pharmacokinetic/pharmacodynamic model

(2013) Ivelina Gueorguieva et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Oral Anticancer Drugs: Mechanisms of Low Bioavailability and Strategies for Improvement

(2013) Frederik E. Stuurman et al.   CLINICAL PHARMACOKINETICS

Activin receptor-like kinase5 inhibition suppresses mouse melanoma by ubiquitin degradation of Smad4, thereby derepressing eomesodermin in cytotoxic T lymphocytes

(2013) Jeong-Hwan Yoon et al.   EMBO Molecular Medicine

Formulation approaches in mitigating toxicity of orally administrated drugs

(2013) Irina Kadiyala et al.   PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY

Phase I, Dose-Escalation Trial of the Oral Cyclin-Dependent Kinase 4/6 Inhibitor PD 0332991, Administered Using a 21-Day Schedule in Patients with Advanced Cancer

(2011) K. T. Flaherty et al.   CLINICAL CANCER RESEARCH

Dose Escalation Methods in Phase I Cancer Clinical Trials

(2009) Christophe Le Tourneau et al.   JNCI-Journal of the National Cancer Institute