구조모아 (StructureMoa)항암 chemical structure spider web
방문타깃 · 모달리티 · 임상 근거 · 비임상 맥락으로 최대 5개 프로그램을 나란히 비교합니다. · 다음 갱신 D-6 · 마지막 9월 2일
현재 선택: 2개 · Data Tier에서 열림
프로그램 상세에서 관심 등록 후 2개 이상 모으면 여기서 한 번에 비교할 수 있습니다.
표가 넓으면 좌우로 스크롤하세요. 핵심 비교 모드에서는 중요 항목만 표시됩니다.
| 항목 | trastuzumab deruxtecan (Enhertu, T-DXd, DS-8201) Daiichi Sankyo / AstraZeneca·HER2 240 trials·t½ ADC ~5.8 days; total antibody ~6.1 days; released DXd ~2.7 days (5.4 mg/kg q3w) | |
|---|---|---|
Overview Program | Herceptin (trastuzumab) | Enhertu (trastuzumab deruxtecan) |
Overview Company | Roche / Genentech | Daiichi Sankyo / AstraZeneca |
Overview Modality | ANTIBODY | ADC |
Overview Target | HER2 | HER2 |
Overview Indication | HER2+ breast cancer, HER2+ gastric/GEJ adenocarcinoma | HER2+ breast cancer, HER2-low, gastric |
Overview Phase | APPROVED | APPROVED |
Overview Status | APPROVED | APPROVED |
Overview Content status | Curated Core | Curated Core |
Overview Data Confidence | Data Confidence · High | Data Confidence · High |
Overview Development Signal | Development Signal · Established | Development Signal · Established |
Overview Approval status | FDA approved | FDA approved |
Positioning Key differentiator | novel bifunctional chelator (2E-C-NETA) for applications in 177 Lu-based TRT | High DAR (~8), bystander effect, HER2-low activity |
Positioning Known limitation | resistance to trastuzumab-based targeted therapy and limited intratumoral antibody penetration continue to restrict clinical outcomes | HER2 antigen loss/downregulation, payload efflux, and dose-limiting ILD/pneumonitis leading to discontinuation. |
Positioning Development positioning | — | Leading efficacy in HER2 ADC class |
Technology Payload | — | DXd (topo-I inhibitor) |
Technology Linker | — | Cleavable tetrapeptide |
MoA Mechanism | Trastuzumab binds domain IV of HER2, inhibiting ligand-independent HER2 signaling, mediating ADCC via Fcγ receptors, and inducing internalization/degradation of HER2. | Fam-trastuzumab deruxtecan is a HER2-directed antibody-drug conjugate: humanized anti-HER2 IgG1 linked via a cleavable tetrapeptide linker to DXd, a membrane-permeable topoisomerase I inhibitor. After binding HER2 on tumor cells, the conjugate is internalized; lysosomal proteases cleave the linker and release DXd, causing DNA damage and apoptosis. Released DXd can exert a bystander effect in neighboring cells. |
MoA Biomarker | HER2 IHC 3+ or ISH amplified (ASCO/CAP guidelines). | HER2 expression (IHC/ISH per indication); higher systemic exposure associated with greater ILD incidence (FDA label §12.2). |
PK/PD Half-life | 4 h | ADC ~5.8 days; total antibody ~6.1 days; released DXd ~2.7 days (5.4 mg/kg q3w) |
PK/PD Species | Mouse, OS in metastatic BC | Minipig, Pig, Human, Tumor response (ORR, PFS), ILD incidence rises with exposure |
PK/PD Animal (cat.) | Mouse, In vitro | Human, In vitro |
PK/PD Experiment | Pharmacokinetic | Pharmacokinetic |
PK/PD Biodistribution | — | Systemic exposure with tumor-selective HER2-mediated uptake |
Toxicology Species | Mouse, Rat | Cynomolgus monkey, NHP, Rat, Minipig, Pig, Hamster, Human |
Toxicology Animal (cat.) | — | NHP |
Toxicology Major finding | Cardiotoxicity (LVEF decline, CHF risk especially with anthracyclines); infusion reactions; myelosuppression in combos. | ILD-like lung findings at high exposure |
Toxicology CRS | N/A | Minimal |
Toxicology NOAEL | — | 10 mg/kg |
Clinical Safety signal | Cardiotoxicity (LVEF decline, CHF risk especially with anthracyclines); infusion reactions; myelosuppression in combos. | ILD-like lung findings at high exposure |
Clinical Selected reported efficacy | ORR 91.2% | ORR 79.7% |
Clinical Reported ORR | 91.2% | 79.7% |
Clinical Reported PFS | — | NA |
Clinical Reported OS | — | NA |
Clinical Result source | ClinicalTrials.gov NCT02149524 | ClinicalTrials.gov NCT03529110 |
Clinical Program phase | APPROVED | APPROVED |
Clinical Trial activity | No active/completed counts | No active/completed counts |
Clinical Trial ref | NCT02149524 | NCT03529110 |
Preclinical Animal (cat.) | — | Human, Mouse, In vitro |
타깃 · 모달리티 · 임상 근거 · 비임상 맥락으로 최대 5개 프로그램을 나란히 비교합니다. · 다음 갱신 D-6 · 마지막 9월 2일
현재 선택: 2개 · Data Tier에서 열림
프로그램 상세에서 관심 등록 후 2개 이상 모으면 여기서 한 번에 비교할 수 있습니다.
표가 넓으면 좌우로 스크롤하세요. 핵심 비교 모드에서는 중요 항목만 표시됩니다.
| 항목 | trastuzumab deruxtecan (Enhertu, T-DXd, DS-8201) Daiichi Sankyo / AstraZeneca·HER2 240 trials·t½ ADC ~5.8 days; total antibody ~6.1 days; released DXd ~2.7 days (5.4 mg/kg q3w) | |
|---|---|---|
Overview Program | Herceptin (trastuzumab) | Enhertu (trastuzumab deruxtecan) |
Overview Company | Roche / Genentech | Daiichi Sankyo / AstraZeneca |
Overview Modality | ANTIBODY | ADC |
Overview Target | HER2 | HER2 |
Overview Indication | HER2+ breast cancer, HER2+ gastric/GEJ adenocarcinoma | HER2+ breast cancer, HER2-low, gastric |
Overview Phase | APPROVED | APPROVED |
Overview Status | APPROVED | APPROVED |
Overview Content status | Curated Core | Curated Core |
Overview Data Confidence | Data Confidence · High | Data Confidence · High |
Overview Development Signal | Development Signal · Established | Development Signal · Established |
Overview Approval status | FDA approved | FDA approved |
Positioning Key differentiator | novel bifunctional chelator (2E-C-NETA) for applications in 177 Lu-based TRT | High DAR (~8), bystander effect, HER2-low activity |
Positioning Known limitation | resistance to trastuzumab-based targeted therapy and limited intratumoral antibody penetration continue to restrict clinical outcomes | HER2 antigen loss/downregulation, payload efflux, and dose-limiting ILD/pneumonitis leading to discontinuation. |
Positioning Development positioning | — | Leading efficacy in HER2 ADC class |
Technology Payload | — | DXd (topo-I inhibitor) |
Technology Linker | — | Cleavable tetrapeptide |
MoA Mechanism | Trastuzumab binds domain IV of HER2, inhibiting ligand-independent HER2 signaling, mediating ADCC via Fcγ receptors, and inducing internalization/degradation of HER2. | Fam-trastuzumab deruxtecan is a HER2-directed antibody-drug conjugate: humanized anti-HER2 IgG1 linked via a cleavable tetrapeptide linker to DXd, a membrane-permeable topoisomerase I inhibitor. After binding HER2 on tumor cells, the conjugate is internalized; lysosomal proteases cleave the linker and release DXd, causing DNA damage and apoptosis. Released DXd can exert a bystander effect in neighboring cells. |
MoA Biomarker | HER2 IHC 3+ or ISH amplified (ASCO/CAP guidelines). | HER2 expression (IHC/ISH per indication); higher systemic exposure associated with greater ILD incidence (FDA label §12.2). |
PK/PD Half-life | 4 h | ADC ~5.8 days; total antibody ~6.1 days; released DXd ~2.7 days (5.4 mg/kg q3w) |
PK/PD Species | Mouse, OS in metastatic BC | Minipig, Pig, Human, Tumor response (ORR, PFS), ILD incidence rises with exposure |
PK/PD Animal (cat.) | Mouse, In vitro | Human, In vitro |
PK/PD Experiment | Pharmacokinetic | Pharmacokinetic |
PK/PD Biodistribution | — | Systemic exposure with tumor-selective HER2-mediated uptake |
Toxicology Species | Mouse, Rat | Cynomolgus monkey, NHP, Rat, Minipig, Pig, Hamster, Human |
Toxicology Animal (cat.) | — | NHP |
Toxicology Major finding | Cardiotoxicity (LVEF decline, CHF risk especially with anthracyclines); infusion reactions; myelosuppression in combos. | ILD-like lung findings at high exposure |
Toxicology CRS | N/A | Minimal |
Toxicology NOAEL | — | 10 mg/kg |
Clinical Safety signal | Cardiotoxicity (LVEF decline, CHF risk especially with anthracyclines); infusion reactions; myelosuppression in combos. | ILD-like lung findings at high exposure |
Clinical Selected reported efficacy | ORR 91.2% | ORR 79.7% |
Clinical Reported ORR | 91.2% | 79.7% |
Clinical Reported PFS | — | NA |
Clinical Reported OS | — | NA |
Clinical Result source | ClinicalTrials.gov NCT02149524 | ClinicalTrials.gov NCT03529110 |
Clinical Program phase | APPROVED | APPROVED |
Clinical Trial activity | No active/completed counts | No active/completed counts |
Clinical Trial ref | NCT02149524 | NCT03529110 |
Preclinical Animal (cat.) | — | Human, Mouse, In vitro |
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