구조모아 (StructureMoa)항암 chemical structure spider web
방문타깃 · 모달리티 · 임상 근거 · 비임상 맥락으로 최대 5개 프로그램을 나란히 비교합니다. · 다음 갱신 D-5 · 마지막 9월 2일
현재 선택: 5개 · 차세대 보드에서 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) | ado-trastuzumab emtansine (Kadcyla, T-DM1, ado-trastuzumab emtansine / T-DM1) Roche / Genentech·HER2 178 trials·t½ 4 h | sacituzumab govitecan (Trodelvy, IMMU-132, sacituzumab-govitecan-hziy) Gilead / Immunomedics·TROP2 242 trials·t½ ADC ~16 h; free SN-38 ~18 h | ||
|---|---|---|---|---|---|
Overview Program | Herceptin (trastuzumab) | Enhertu (trastuzumab deruxtecan) | Kadcyla (ado-trastuzumab emtansine / T-DM1) | Disitamab Vedotin (RC48) | Trodelvy (sacituzumab govitecan) |
Overview Company | Roche / Genentech | Daiichi Sankyo / AstraZeneca | Roche / Genentech | RemeGen | Gilead / Immunomedics |
Overview Modality | ANTIBODY | ADC | ADC | ADC | ADC |
Overview Target | HER2 | HER2 | HER2 | HER2 | TROP2 |
Overview Indication | HER2+ breast cancer, HER2+ gastric/GEJ adenocarcinoma | HER2+ breast cancer, HER2-low, gastric | HER2+ breast cancer | HER2+ urothelial, gastric, breast | Metastatic triple-negative breast cancer, pretreated HR+/HER2− breast cancer |
Overview Phase | APPROVED | APPROVED | APPROVED | APPROVED | APPROVED |
Overview Status | APPROVED | APPROVED | APPROVED | ACTIVE | APPROVED |
Overview Content status | Curated Core | Curated Core | Curated Core | Curated Core | Curated Core |
Overview Data Confidence | Data Confidence · High | 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 | Development Signal · Established |
Overview Approval status | FDA approved | 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 | Stable linker, DAR ~3.5 | Novel anti-HER2 mAb with distinct epitope | Very high DAR plus a deliberately unstable linker — extracellular SN-38 release gives bystander killing in TROP2-heterogeneous tumors. |
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. | HER2 downregulation, lysosomal trapping, and efflux; superseded in 2L HER2+ mBC by trastuzumab deruxtecan (DESTINY-Breast03). | resistance mechanisms, optimize payload delivery, and minimize off-target toxicity | TROP2 downregulation, TOP1 mutation, and ABC-transporter payload efflux. |
Positioning Development positioning | — | Leading efficacy in HER2 ADC class | Established SOC before Enhertu head-to-head | Lower ILD signal vs DXd in some datasets | TROP2 class leader by approval history; now facing Datroway and other TROP2 ADCs. |
Technology Payload | — | DXd (topo-I inhibitor) | MMAE (maytansinoid) | MMAE | SN-38 (topoisomerase I inhibitor) |
Technology Linker | — | Cleavable tetrapeptide | Non-cleavable SMCC | Cleavable | Hydrolyzable CL2A, DAR ~7.6 |
Technology DAR | — | — | — | — | DAR 7.6 |
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. | Ado-trastuzumab emtansine (T-DM1) binds HER2 on tumor cells, is internalized, and MMAE is released after lysosomal degradation of the antibody in the non-cleavable SMCC linker system. MMAE disrupts microtubules, causing G2/M arrest and apoptosis. | Disitamab vedotin binds a distinct HER2 epitope (different from trastuzumab), internalizes, and releases MMAE via cleavable linker, causing microtubule disruption and apoptosis. | Anti-TROP2 antibody binds and internalizes; the hydrolyzable linker releases SN-38 both intracellularly and in the tumor microenvironment, inhibiting topoisomerase I and causing lethal DNA double-strand breaks. |
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 overexpression/amplification (IHC 3+ or ISH+ per label). | HER2 expression (IHC); activity in HER2+ urothelial and gastric cancers. | TROP2 is broadly expressed in epithelial tumors; no companion diagnostic is required in the label. |
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) | 4 h | ~5 days (ADC, clinical PK) | ADC ~16 h; free SN-38 ~18 h |
PK/PD Species | Mouse, OS in metastatic BC | Minipig, Pig, Human, Tumor response (ORR, PFS), ILD incidence rises with exposure | Mouse, Tumor response | Mouse, ORR in HER2+ UC/gastric | Mouse, ORR and PFS, ctDNA dynamics exploratory |
PK/PD Animal (cat.) | Mouse, In vitro | Human, In vitro | Mouse, In vitro | Human, Mouse, In vitro | Human, Mouse, In vitro |
PK/PD Experiment | Pharmacokinetic | 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, Rat | Cynomolgus monkey, Mouse | Cynomolgus monkey, Mouse, Hamster |
Toxicology Animal (cat.) | — | NHP | 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 | Thrombocytopenia, hepatotoxicity | Hematologic toxicity and peripheral neuropathy class effects of MMAE; ILD reported at lower frequency than DXd ADCs in published datasets. | Boxed warning for severe neutropenia and severe diarrhea. Nausea, alopecia, fatigue, and rare hypersensitivity are common. |
Toxicology CRS | N/A | Minimal | 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 | Thrombocytopenia, hepatotoxicity | Hematologic toxicity and peripheral neuropathy class effects of MMAE; ILD reported at lower frequency than DXd ADCs in published datasets. | Boxed warning for severe neutropenia and severe diarrhea. Nausea, alopecia, fatigue, and rare hypersensitivity are common. |
Clinical Selected reported efficacy | ORR 91.2% | ORR 79.7% | ORR 43.6% | — | ORR 44% |
Clinical Reported ORR | 91.2% | 79.7% | 43.6% (EMILIA) | — | 44.0% |
Clinical Reported PFS | — | NA | 9.6 mo | — | — |
Clinical Reported OS | — | NA | 30.9 mo | — | — |
Clinical Result source | ClinicalTrials.gov NCT02149524 | ClinicalTrials.gov NCT03529110 | EMILIA | — | ClinicalTrials.gov NCT04916002 |
Clinical Program phase | APPROVED | APPROVED | APPROVED | APPROVED | APPROVED |
Clinical Trial activity | No active/completed counts | No active/completed counts | No active/completed counts | No active/completed counts | No active/completed counts |
Clinical Trial ref | NCT02149524 | NCT03529110 | EMILIA | — | NCT04916002 |
Preclinical Animal (cat.) | — | Human, Mouse, In vitro | In vitro | — | Mouse |
타깃 · 모달리티 · 임상 근거 · 비임상 맥락으로 최대 5개 프로그램을 나란히 비교합니다. · 다음 갱신 D-5 · 마지막 9월 2일
현재 선택: 5개 · 차세대 보드에서 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) | ado-trastuzumab emtansine (Kadcyla, T-DM1, ado-trastuzumab emtansine / T-DM1) Roche / Genentech·HER2 178 trials·t½ 4 h | sacituzumab govitecan (Trodelvy, IMMU-132, sacituzumab-govitecan-hziy) Gilead / Immunomedics·TROP2 242 trials·t½ ADC ~16 h; free SN-38 ~18 h | ||
|---|---|---|---|---|---|
Overview Program | Herceptin (trastuzumab) | Enhertu (trastuzumab deruxtecan) | Kadcyla (ado-trastuzumab emtansine / T-DM1) | Disitamab Vedotin (RC48) | Trodelvy (sacituzumab govitecan) |
Overview Company | Roche / Genentech | Daiichi Sankyo / AstraZeneca | Roche / Genentech | RemeGen | Gilead / Immunomedics |
Overview Modality | ANTIBODY | ADC | ADC | ADC | ADC |
Overview Target | HER2 | HER2 | HER2 | HER2 | TROP2 |
Overview Indication | HER2+ breast cancer, HER2+ gastric/GEJ adenocarcinoma | HER2+ breast cancer, HER2-low, gastric | HER2+ breast cancer | HER2+ urothelial, gastric, breast | Metastatic triple-negative breast cancer, pretreated HR+/HER2− breast cancer |
Overview Phase | APPROVED | APPROVED | APPROVED | APPROVED | APPROVED |
Overview Status | APPROVED | APPROVED | APPROVED | ACTIVE | APPROVED |
Overview Content status | Curated Core | Curated Core | Curated Core | Curated Core | Curated Core |
Overview Data Confidence | Data Confidence · High | 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 | Development Signal · Established |
Overview Approval status | FDA approved | 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 | Stable linker, DAR ~3.5 | Novel anti-HER2 mAb with distinct epitope | Very high DAR plus a deliberately unstable linker — extracellular SN-38 release gives bystander killing in TROP2-heterogeneous tumors. |
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. | HER2 downregulation, lysosomal trapping, and efflux; superseded in 2L HER2+ mBC by trastuzumab deruxtecan (DESTINY-Breast03). | resistance mechanisms, optimize payload delivery, and minimize off-target toxicity | TROP2 downregulation, TOP1 mutation, and ABC-transporter payload efflux. |
Positioning Development positioning | — | Leading efficacy in HER2 ADC class | Established SOC before Enhertu head-to-head | Lower ILD signal vs DXd in some datasets | TROP2 class leader by approval history; now facing Datroway and other TROP2 ADCs. |
Technology Payload | — | DXd (topo-I inhibitor) | MMAE (maytansinoid) | MMAE | SN-38 (topoisomerase I inhibitor) |
Technology Linker | — | Cleavable tetrapeptide | Non-cleavable SMCC | Cleavable | Hydrolyzable CL2A, DAR ~7.6 |
Technology DAR | — | — | — | — | DAR 7.6 |
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. | Ado-trastuzumab emtansine (T-DM1) binds HER2 on tumor cells, is internalized, and MMAE is released after lysosomal degradation of the antibody in the non-cleavable SMCC linker system. MMAE disrupts microtubules, causing G2/M arrest and apoptosis. | Disitamab vedotin binds a distinct HER2 epitope (different from trastuzumab), internalizes, and releases MMAE via cleavable linker, causing microtubule disruption and apoptosis. | Anti-TROP2 antibody binds and internalizes; the hydrolyzable linker releases SN-38 both intracellularly and in the tumor microenvironment, inhibiting topoisomerase I and causing lethal DNA double-strand breaks. |
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 overexpression/amplification (IHC 3+ or ISH+ per label). | HER2 expression (IHC); activity in HER2+ urothelial and gastric cancers. | TROP2 is broadly expressed in epithelial tumors; no companion diagnostic is required in the label. |
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) | 4 h | ~5 days (ADC, clinical PK) | ADC ~16 h; free SN-38 ~18 h |
PK/PD Species | Mouse, OS in metastatic BC | Minipig, Pig, Human, Tumor response (ORR, PFS), ILD incidence rises with exposure | Mouse, Tumor response | Mouse, ORR in HER2+ UC/gastric | Mouse, ORR and PFS, ctDNA dynamics exploratory |
PK/PD Animal (cat.) | Mouse, In vitro | Human, In vitro | Mouse, In vitro | Human, Mouse, In vitro | Human, Mouse, In vitro |
PK/PD Experiment | Pharmacokinetic | 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, Rat | Cynomolgus monkey, Mouse | Cynomolgus monkey, Mouse, Hamster |
Toxicology Animal (cat.) | — | NHP | 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 | Thrombocytopenia, hepatotoxicity | Hematologic toxicity and peripheral neuropathy class effects of MMAE; ILD reported at lower frequency than DXd ADCs in published datasets. | Boxed warning for severe neutropenia and severe diarrhea. Nausea, alopecia, fatigue, and rare hypersensitivity are common. |
Toxicology CRS | N/A | Minimal | 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 | Thrombocytopenia, hepatotoxicity | Hematologic toxicity and peripheral neuropathy class effects of MMAE; ILD reported at lower frequency than DXd ADCs in published datasets. | Boxed warning for severe neutropenia and severe diarrhea. Nausea, alopecia, fatigue, and rare hypersensitivity are common. |
Clinical Selected reported efficacy | ORR 91.2% | ORR 79.7% | ORR 43.6% | — | ORR 44% |
Clinical Reported ORR | 91.2% | 79.7% | 43.6% (EMILIA) | — | 44.0% |
Clinical Reported PFS | — | NA | 9.6 mo | — | — |
Clinical Reported OS | — | NA | 30.9 mo | — | — |
Clinical Result source | ClinicalTrials.gov NCT02149524 | ClinicalTrials.gov NCT03529110 | EMILIA | — | ClinicalTrials.gov NCT04916002 |
Clinical Program phase | APPROVED | APPROVED | APPROVED | APPROVED | APPROVED |
Clinical Trial activity | No active/completed counts | No active/completed counts | No active/completed counts | No active/completed counts | No active/completed counts |
Clinical Trial ref | NCT02149524 | NCT03529110 | EMILIA | — | NCT04916002 |
Preclinical Animal (cat.) | — | Human, Mouse, In vitro | In vitro | — | Mouse |
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