Satoru Yasuda
Daiichi Sankyo
PharmacokineticsCancerInternalizationDNA damageAntigenCellGene expressionMolecular biologyGene knockdownKnockout mouseChemistryApoptosisCaco-2ConjugateIn vitroAutophagyIn vivoGrowth factor receptorGiSTRegorafenibStromal tumorVerapamilOral administrationAntibody-drug conjugateImatinibBafilomycinSmall intestineFluvastatinP-glycoproteinLucifer yellowSunitinibGrowth inhibitionTrastuzumabUssing chamberLysosomeFamotidineTrophoblast cellDNA Topoisomerase IIntestinal absorptionSurface proteinPharmacology toxicologyPDGFRATyrosine kinaseATP-binding cassette transporterCancer researchAbcg2Monoclonal antibodyPotencyParacellular transportCell growthMedicineIntracellularCell cultureCell biologyPharmacology
Publications 8
#1Kenji Iida (Daiichi Sankyo)H-Index: 1
#2Amr H. Abdelhamid Ahmed (Harvard University)
Last. Toshinori Agatsuma (Daiichi Sankyo)H-Index: 12
view all 24 authors...
Currently, the only approved treatments for gastrointestinal stromal tumor (GIST) are tyrosine kinase inhibitors (TKIs), which eventually lead to development of secondary resistance mutations in KIT or PDGFRA and disease progression. Herein, we identified G protein-coupled receptor 20 (GPR20) as a novel non-TK target in GIST, developed new GPR20 immunohistochemistry, assessed GPR20 expression in cell lines, PDXs & clinical samples from 2 institutes (USA & Japan). We studied GPR20 expression stra...
3 CitationsSource
#1Kenji IidaH-Index: 1
#2Amr Hesham Abdelhamid (Harvard University)H-Index: 2
Last. Toshinori AgatsumaH-Index: 12
view all 23 authors...
More than 85% of GISTs are driven by activating mutations in KIT proto-oncogene receptor tyrosine kinase (KIT) or platelet-derived growth factor receptor alpha (PDGFRA). Currently, the only approved treatments for GIST are KIT directed tyrosine kinase inhibitors (TKIs). However, treatment with approved TKIs eventually results in disease progression most often due to the development of secondary resistance mutations in KIT. In addition, these agents have limited activity in PDGFRA mutant GIST and...
2 CitationsSource
#1Satoru Yasuda (Daiichi Sankyo)H-Index: 3
#2Daisuke Okajima (Daiichi Sankyo)H-Index: 4
Last. Masato Murakami (Daiichi Sankyo)H-Index: 1
view all 9 authors...
Background: DS-1062a is a TROP2-targeting antibody-drug conjugate with Daiichi-Sankyo DXd technology. DS-1062a is expected to deliver DXd, a derivative of Exatecan, to TROP2 highly expressed tumors such as epithelial cancers with stronger anti-tumor effect and safer profile than the systemic chemotherapy. SLFN11 has been reported as a sensitivity biomarkers of DNA topoisomerase I inhibitors in several cancers. In this research, we elucidated the potency of combination of TROP2 and SLFN11 as a se...
#1Daisuke Okajima (Daiichi Sankyo)H-Index: 4
#2Junko Yamaguchi (Daiichi Sankyo)H-Index: 5
Last. Toshinori Agatsuma (Daiichi Sankyo)H-Index: 12
view all 15 authors...
Background: A trophoblast cell surface antigen 2 (TROP2) is a 36-kDa single-pass transmembrane protein overexpressed in various epithelial tumors including non-small cell lung cancer (NSCLC) with relatively low and restricted expression in normal tissues, and is associated with aggressive tumor behavior. Therefore, TROP2 could be an attractive target for cancer therapy. We created DS-1062a, TROP2-targeting antibody-drug conjugate (ADC) with Daiichi Sankyo DXd technology using a novel DNA topoiso...
#1Manabu Abe (Daiichi Sankyo)H-Index: 1
#2Motoko Nagata (Daiichi Sankyo)H-Index: 2
Last. Masato Murakami (Daiichi Sankyo)H-Index: 1
view all 13 authors...
Background of the study: [fam-] trastuzumab deruxtecan (DS-8201a) is a HER2-targeting antibody-drug conjugate (ADC) with a humanized anti-HER2 monoclonal antibody attached to a topoisomerase I inhibitor payload by a peptide-based cleavable linker. [fam-] trastuzumab deruxtecan has been shown to be highly effective in preclinical and clinical studies. In addition to payload potency, drug-to-antibody ratio and linker stability, the effectiveness of the ADC is expected to be defined by intracellula...
#1Daisuke Okajima (Daiichi Sankyo)H-Index: 4
#2Satoru Yasuda (Daiichi Sankyo)H-Index: 3
Last. Toshinori Agatsuma (Daiichi Sankyo)H-Index: 12
view all 16 authors...
e24206Background: DS-1062a is a trophoblast cell surface protein 2 (TROP2)-targeting antibody-drug conjugate (ADC) comprised of a humanized anti-TROP2 monoclonal antibody, enzymatically cleavable p...
5 CitationsSource
#1Tsuyoshi Karibe (Daiichi Sankyo)H-Index: 4
#2Rie Hagihara-Nakagomi (Daiichi Sankyo)H-Index: 1
Last. Takashi Izumi (Daiichi Sankyo)H-Index: 17
view all 10 authors...
Purpose To evaluate whether the impact of functional modulation of the breast cancer resistance protein (BCRP, ABCG2 421C>A) on human pharmacokinetics after oral administration is predictable using Bcrp knockout mice and cynomolgus monkeys pretreated with a BCRP inhibitor, elacridar.
18 CitationsSource
#1Veronika Rozehnal (Daiichi Sankyo)H-Index: 3
#2Daisuke Nakai (Daiichi Sankyo)H-Index: 11
Last. Juergen Mueller (Daiichi Sankyo)H-Index: 4
view all 8 authors...
Abstract The purpose of this study was to validate human small intestinal and colonic tissue mounted in the Ussing chamber as a tool for predicting the oral drug absorption in humans with the main focus on moderately and poorly permeable compounds. The obtained apparent permeability coefficient (Papp) of eleven test compounds was compared to their fraction absorbed (Fa) in humans taken from the literature. Beside the conventional Papp a new parameter, the apparent permeability coefficient total ...
84 CitationsSource