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Biological and Environmental Research Ontology
| Id | http://purl.obolibrary.org/obo/NCIT_C132112
http://purl.obolibrary.org/obo/NCIT_C132112
|
|---|---|
| Preferred Name | Anti-HER2/Auristatin Payload Antibody-drug Conjugate XMT-1522 |
| Definitions |
An antibody-drug conjugate (ADC) composed of HT-19, a monoclonal antibody directed against the human epidermal growth factor receptor 2 (ERBB2; HER2), conjugated, via a proprietary biodegradable, hydrophilic polymer backbone and various linkers, to proprietary auristatin-derived payload molecules (about 15 per antibody), with potential antineoplastic activity. Upon administration of anti-HER2/auristatin payload ADC XMT-1522, the antibody moiety targets and binds to a unique epitope in the extracellular domain (ECD) of HER2. Upon internalization, cleavage and release of the cytotoxic molecules, the auristatin-derived molecules bind to tubulin and inhibit its polymerization, which results in G2/M phase arrest and induces apoptosis of HER2-expressing tumor cells. The attachment of multiple auristatin molecules to the backbone enables XMT-1522 to effectively kill tumors that express relatively low amounts of the HER2 protein; therefore, this agent shows increased therapeutic potential in tumors with low HER2 expression compared to other anti-HER2 antibody-based therapies. The polymer-based proprietary platform optimizes delivery of the cytotoxic drug payload and improves drug solubility.
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| Type | http://www.w3.org/2002/07/owl#Class |
All Properties
| definition | An antibody-drug conjugate (ADC) composed of HT-19, a monoclonal antibody directed against the human epidermal growth factor receptor 2 (ERBB2; HER2), conjugated, via a proprietary biodegradable, hydrophilic polymer backbone and various linkers, to proprietary auristatin-derived payload molecules (about 15 per antibody), with potential antineoplastic activity. Upon administration of anti-HER2/auristatin payload ADC XMT-1522, the antibody moiety targets and binds to a unique epitope in the extracellular domain (ECD) of HER2. Upon internalization, cleavage and release of the cytotoxic molecules, the auristatin-derived molecules bind to tubulin and inhibit its polymerization, which results in G2/M phase arrest and induces apoptosis of HER2-expressing tumor cells. The attachment of multiple auristatin molecules to the backbone enables XMT-1522 to effectively kill tumors that express relatively low amounts of the HER2 protein; therefore, this agent shows increased therapeutic potential in tumors with low HER2 expression compared to other anti-HER2 antibody-based therapies. The polymer-based proprietary platform optimizes delivery of the cytotoxic drug payload and improves drug solubility. |
|---|---|
| prefLabel | Anti-HER2/Auristatin Payload Antibody-drug Conjugate XMT-1522
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| label | Anti-HER2/Auristatin Payload Antibody-drug Conjugate XMT-1522
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| NCI_META_CUI | CL520319
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| PDQ_Closed_Trial_Search_ID | 786937
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| code | C132112
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| Has_Target | |
| prefixIRI | NCIT:C132112
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| in_subset |
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| Display_Name | Anti-HER2/Auristatin Payload Antibody-drug Conjugate XMT-1522
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| Preferred_Name | Anti-HER2/Auristatin Payload Antibody-drug Conjugate XMT-1522
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| Contributing_Source | CTRP
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| Maps_To | Anti-HER2/Auristatin Payload Antibody-drug Conjugate XMT-1522
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| NCI_Drug_Dictionary_ID | 786937
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| type | |
| Is_Value_For_GDC_Property | |
| subClassOf | |
| PDQ_Open_Trial_Search_ID | 786937
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| Semantic_Type | Pharmacologic Substance
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