구조모아 (StructureMoa)항암 chemical structure spider web
방문프로그램 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) | zanidatamab (Ziihera, ZW25, zanidatamab-hrii) Jazz Pharmaceuticals / Zymeworks·HER2 (biparatopic) 35 trials·t½ ~7 days | ||
|---|---|---|---|---|
Overview Program | Herceptin (trastuzumab) | Enhertu (trastuzumab deruxtecan) | Disitamab Vedotin (RC48) | Ziihera (zanidatamab) |
Overview Company | Roche / Genentech | Daiichi Sankyo / AstraZeneca | RemeGen | Jazz Pharmaceuticals / Zymeworks |
Overview Modality | ANTIBODY | ADC | ADC | ANTIBODY |
Overview Target | HER2 | HER2 | HER2 | HER2 (biparatopic) |
Overview Indication | HER2+ breast cancer, HER2+ gastric/GEJ adenocarcinoma | HER2+ breast cancer, HER2-low, gastric | HER2+ urothelial, gastric, breast | First-line HER2-positive gastric, GEJ, or esophageal adenocarcinoma; previously treated HER2-positive biliary tract cancer |
Overview Phase | APPROVED | APPROVED | APPROVED | APPROVED |
Overview Status | APPROVED | APPROVED | ACTIVE | APPROVED |
Overview Content status | Curated Core | Curated Core | Curated Core | Curated Core |
Overview Data Confidence | Data Confidence · High | Data Confidence · High | Data Confidence · High | Data Confidence · High |
Overview Development Signal | Development Signal · Established | Development Signal · Established | Development Signal · Established | Development Signal · Established |
Overview Approval status | FDA approved | FDA approved | 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 | Novel anti-HER2 mAb with distinct epitope | Dual-epitope binding drives receptor clustering, faster internalization, and stronger signaling blockade than either monoclonal alone. In GEA the label splits IHC 3+ (chemo doublet) from IHC 3+ or 2+/ISH+ (chemo + Tevimbra). |
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. | resistance mechanisms, optimize payload delivery, and minimize off-target toxicity | HER2 heterogeneity, PI3K pathway activation, and bypass RTK signaling. |
Positioning Development positioning | — | Leading efficacy in HER2 ADC class | Lower ILD signal vs DXd in some datasets | Challenges the ToGA trastuzumab-chemo backbone in 1L HER2+ GEA; still the only HER2 agent with a dedicated BTC indication. |
Technology Payload | — | DXd (topo-I inhibitor) | MMAE | — |
Technology Linker | — | Cleavable tetrapeptide | Cleavable | — |
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. | Disitamab vedotin binds a distinct HER2 epitope (different from trastuzumab), internalizes, and releases MMAE via cleavable linker, causing microtubule disruption and apoptosis. | Simultaneous binding of two non-overlapping HER2 epitopes crosslinks adjacent receptors, causing receptor clustering, internalization, and degradation alongside ADCC and complement activity. |
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). | HER2 expression (IHC); activity in HER2+ urothelial and gastric cancers. | GEA: PATHWAY 4B5 IHC and VENTANA Dual ISH. IHC 3+ for chemo doublet; IHC 3+ or IHC 2+/ISH+ when Tevimbra is added. BTC: HER2 IHC 3+. |
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) | ~5 days (ADC, clinical PK) | ~7 days |
PK/PD Species | Mouse, OS in metastatic BC | Minipig, Pig, Human, Tumor response (ORR, PFS), ILD incidence rises with exposure | Mouse, ORR in HER2+ UC/gastric | Cynomolgus monkey, Human, OS and PFS in GEA, ORR and DOR in BTC |
PK/PD Animal (cat.) | Mouse, In vitro | Human, In vitro | Human, Mouse, In vitro | Human, NHP, In vitro |
PK/PD Experiment | Pharmacokinetic | Pharmacokinetic | pd | pd |
PK/PD Biodistribution | — | Systemic exposure with tumor-selective HER2-mediated uptake | — | — |
Toxicology Species | Mouse, Rat | Cynomolgus monkey, NHP, Rat, Minipig, Pig, Hamster, Human | Cynomolgus monkey, Mouse | Human |
Toxicology Animal (cat.) | — | NHP | NHP | — |
Toxicology Major finding | Cardiotoxicity (LVEF decline, CHF risk especially with anthracyclines); infusion reactions; myelosuppression in combos. | ILD-like lung findings at high exposure | Hematologic toxicity and peripheral neuropathy class effects of MMAE; ILD reported at lower frequency than DXd ADCs in published datasets. | Embryo-fetal toxicity warning. Diarrhea, infusion-related reactions, and left ventricular dysfunction require monitoring, as with the HER2 antibody class. |
Toxicology CRS | N/A | Minimal | N/A | N/A |
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 | Hematologic toxicity and peripheral neuropathy class effects of MMAE; ILD reported at lower frequency than DXd ADCs in published datasets. | Embryo-fetal toxicity warning. Diarrhea, infusion-related reactions, and left ventricular dysfunction require monitoring, as with the HER2 antibody class. |
Clinical Selected reported efficacy | ORR 91.2% | ORR 79.7% | — | ORR 52% |
Clinical Reported ORR | 91.2% | 79.7% | — | 52% |
Clinical Reported PFS | — | NA | — | ~5.5 mo |
Clinical Reported OS | — | NA | — | 15.54 |
Clinical Result source | ClinicalTrials.gov NCT02149524 | ClinicalTrials.gov NCT03529110 | — | HERIZON-BTC-01 (NCT04466891) |
Clinical Program phase | APPROVED | APPROVED | APPROVED | APPROVED |
Clinical Trial activity | No active/completed counts | No active/completed counts | No active/completed counts | No active/completed counts |
Clinical Trial ref | NCT02149524 | NCT03529110 | — | NCT04466891 |
Preclinical Animal (cat.) | — | Human, Mouse, In vitro | — | Unknown |
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) | zanidatamab (Ziihera, ZW25, zanidatamab-hrii) Jazz Pharmaceuticals / Zymeworks·HER2 (biparatopic) 35 trials·t½ ~7 days | ||
|---|---|---|---|---|
Overview Program | Herceptin (trastuzumab) | Enhertu (trastuzumab deruxtecan) | Disitamab Vedotin (RC48) | Ziihera (zanidatamab) |
Overview Company | Roche / Genentech | Daiichi Sankyo / AstraZeneca | RemeGen | Jazz Pharmaceuticals / Zymeworks |
Overview Modality | ANTIBODY | ADC | ADC | ANTIBODY |
Overview Target | HER2 | HER2 | HER2 | HER2 (biparatopic) |
Overview Indication | HER2+ breast cancer, HER2+ gastric/GEJ adenocarcinoma | HER2+ breast cancer, HER2-low, gastric | HER2+ urothelial, gastric, breast | First-line HER2-positive gastric, GEJ, or esophageal adenocarcinoma; previously treated HER2-positive biliary tract cancer |
Overview Phase | APPROVED | APPROVED | APPROVED | APPROVED |
Overview Status | APPROVED | APPROVED | ACTIVE | APPROVED |
Overview Content status | Curated Core | Curated Core | Curated Core | Curated Core |
Overview Data Confidence | Data Confidence · High | Data Confidence · High | Data Confidence · High | Data Confidence · High |
Overview Development Signal | Development Signal · Established | Development Signal · Established | Development Signal · Established | Development Signal · Established |
Overview Approval status | FDA approved | FDA approved | 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 | Novel anti-HER2 mAb with distinct epitope | Dual-epitope binding drives receptor clustering, faster internalization, and stronger signaling blockade than either monoclonal alone. In GEA the label splits IHC 3+ (chemo doublet) from IHC 3+ or 2+/ISH+ (chemo + Tevimbra). |
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. | resistance mechanisms, optimize payload delivery, and minimize off-target toxicity | HER2 heterogeneity, PI3K pathway activation, and bypass RTK signaling. |
Positioning Development positioning | — | Leading efficacy in HER2 ADC class | Lower ILD signal vs DXd in some datasets | Challenges the ToGA trastuzumab-chemo backbone in 1L HER2+ GEA; still the only HER2 agent with a dedicated BTC indication. |
Technology Payload | — | DXd (topo-I inhibitor) | MMAE | — |
Technology Linker | — | Cleavable tetrapeptide | Cleavable | — |
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. | Disitamab vedotin binds a distinct HER2 epitope (different from trastuzumab), internalizes, and releases MMAE via cleavable linker, causing microtubule disruption and apoptosis. | Simultaneous binding of two non-overlapping HER2 epitopes crosslinks adjacent receptors, causing receptor clustering, internalization, and degradation alongside ADCC and complement activity. |
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). | HER2 expression (IHC); activity in HER2+ urothelial and gastric cancers. | GEA: PATHWAY 4B5 IHC and VENTANA Dual ISH. IHC 3+ for chemo doublet; IHC 3+ or IHC 2+/ISH+ when Tevimbra is added. BTC: HER2 IHC 3+. |
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) | ~5 days (ADC, clinical PK) | ~7 days |
PK/PD Species | Mouse, OS in metastatic BC | Minipig, Pig, Human, Tumor response (ORR, PFS), ILD incidence rises with exposure | Mouse, ORR in HER2+ UC/gastric | Cynomolgus monkey, Human, OS and PFS in GEA, ORR and DOR in BTC |
PK/PD Animal (cat.) | Mouse, In vitro | Human, In vitro | Human, Mouse, In vitro | Human, NHP, In vitro |
PK/PD Experiment | Pharmacokinetic | Pharmacokinetic | pd | pd |
PK/PD Biodistribution | — | Systemic exposure with tumor-selective HER2-mediated uptake | — | — |
Toxicology Species | Mouse, Rat | Cynomolgus monkey, NHP, Rat, Minipig, Pig, Hamster, Human | Cynomolgus monkey, Mouse | Human |
Toxicology Animal (cat.) | — | NHP | NHP | — |
Toxicology Major finding | Cardiotoxicity (LVEF decline, CHF risk especially with anthracyclines); infusion reactions; myelosuppression in combos. | ILD-like lung findings at high exposure | Hematologic toxicity and peripheral neuropathy class effects of MMAE; ILD reported at lower frequency than DXd ADCs in published datasets. | Embryo-fetal toxicity warning. Diarrhea, infusion-related reactions, and left ventricular dysfunction require monitoring, as with the HER2 antibody class. |
Toxicology CRS | N/A | Minimal | N/A | N/A |
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 | Hematologic toxicity and peripheral neuropathy class effects of MMAE; ILD reported at lower frequency than DXd ADCs in published datasets. | Embryo-fetal toxicity warning. Diarrhea, infusion-related reactions, and left ventricular dysfunction require monitoring, as with the HER2 antibody class. |
Clinical Selected reported efficacy | ORR 91.2% | ORR 79.7% | — | ORR 52% |
Clinical Reported ORR | 91.2% | 79.7% | — | 52% |
Clinical Reported PFS | — | NA | — | ~5.5 mo |
Clinical Reported OS | — | NA | — | 15.54 |
Clinical Result source | ClinicalTrials.gov NCT02149524 | ClinicalTrials.gov NCT03529110 | — | HERIZON-BTC-01 (NCT04466891) |
Clinical Program phase | APPROVED | APPROVED | APPROVED | APPROVED |
Clinical Trial activity | No active/completed counts | No active/completed counts | No active/completed counts | No active/completed counts |
Clinical Trial ref | NCT02149524 | NCT03529110 | — | NCT04466891 |
Preclinical Animal (cat.) | — | Human, Mouse, In vitro | — | Unknown |
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