Manabu Abe
Daiichi Sankyo
CancerTargeted drug deliverySomatic cellInternalizationCellCytotoxic T cellAntibodyGene knockdownChemistryAutophagyIn vivoGrowth factor receptorGiSTRegorafenibPatritumabStromal tumorAntibody-drug conjugateImatinibBafilomycinSunitinibTrastuzumabTriple-negative breast cancerLysosomeExatecanPDGFRATyrosine kinaseCancer researchFlow cytometryCell growthMedicineIntracellularCell cultureCell biologyCancer cell
6Publications
1H-index
12Citations
Publications 6
Newest
#1Kenji Iida (Daiichi Sankyo)H-Index: 1
#2Amr H. Abdelhamid Ahmed (Harvard University)
Last. Toshinori Agatsuma (Daiichi Sankyo)H-Index: 12
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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
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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
#1Kumiko KoyamaH-Index: 8
#2Hirokazu Ishikawa (Daiichi Sankyo)H-Index: 1
Last. Masato MurakamiH-Index: 1
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Background: U3-1402, a novel HER3-targeting antibody-drug conjugate (ADC) composed of a fully human anti-HER3 antibody (patritumab), tetrapeptide-based linker, and topoisomerase I inhibitor payload, is currently being studied in clinical trials for patients with HER3-positive breast cancer (phase 1/2, NCT02980341) and NSCLC (phase 1, NCT03260491). HER3 is overexpressed in multiple human cancers and plays an important role in cell proliferation and survival. Furthermore, HER3 somatic mutations ha...
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#1Hashimoto Yuuri (Daiichi Sankyo)H-Index: 1
#2Kumiko Koyama (Daiichi Sankyo)H-Index: 8
Last. Toshinori Agatsuma (Daiichi Sankyo)H-Index: 12
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Purpose: HER3 is a compelling target for cancer treatment; however no HER3-targeted therapy is currently clinically available. Here, we produced U3-1402, an anti-HER3 antibody-drug conjugate with a topoisomerase I inhibitor exatecan -derivative (DXd), and systematically investigated its targeted drug delivery potential and antitumor activity in preclinical models. Experimental Design: In vitro pharmacological activities and the mechanisms of action of U3-1402 were assessed in several human cance...
19 CitationsSource
#1Manabu Abe (Daiichi Sankyo)H-Index: 1
#2Motoko Nagata (Daiichi Sankyo)H-Index: 2
Last. Masato Murakami (Daiichi Sankyo)H-Index: 1
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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...
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#1Kumiko Koyama (Daiichi Sankyo)H-Index: 8
#2Hashimoto Yuuri (Daiichi Sankyo)H-Index: 1
Last. Masato Murakami (Daiichi Sankyo)H-Index: 1
view all 15 authors...
Background: Human epidermal growth factor receptor 3 (HER3), a member of the ErbB receptor tyrosine kinase family, is overexpressed in a variety of human cancers and plays an important role in cell proliferation and survival. U3-1402 is a novel HER3-targeting antibody-drug conjugate (ADC) consisting of a fully human anti-HER3 antibody (patritumab), a tetrapeptide-based linker, and a topoisomerase I inhibitor payload. It is currently being investigated in clinical trials for HER3-positive breast ...
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