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) | ado-trastuzumab emtansine (Kadcyla, T-DM1, ado-trastuzumab emtansine / T-DM1) Roche / Genentech·HER2 178 trials·t½ 4 h | |
|---|---|---|---|
Overview Program | Enhertu (trastuzumab deruxtecan) | Kadcyla (ado-trastuzumab emtansine / T-DM1) | Disitamab Vedotin (RC48) |
Overview Company | Daiichi Sankyo / AstraZeneca | Roche / Genentech | RemeGen |
Overview Modality | ADC | ADC | ADC |
Overview Target | HER2 | HER2 | HER2 |
Overview Indication | HER2+ breast cancer, HER2-low, gastric | HER2+ breast cancer | HER2+ urothelial, gastric, breast |
Overview Phase | APPROVED | APPROVED | APPROVED |
Overview Status | APPROVED | APPROVED | ACTIVE |
Overview Content status | Curated Core | Curated Core | Curated Core |
Overview Data Confidence | Data Confidence · High | Data Confidence · High | Data Confidence · High |
Overview Development Signal | Development Signal · Established | Development Signal · Established | Development Signal · Established |
Overview Approval status | FDA approved | FDA approved | FDA approved |
Positioning Key differentiator | High DAR (~8), bystander effect, HER2-low activity | Stable linker, DAR ~3.5 | Novel anti-HER2 mAb with distinct epitope |
Positioning Known limitation | 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 | HER2 downregulation, lysosomal trapping, and efflux; superseded in 2L HER2+ mBC by trastuzumab deruxtecan (DESTINY-Breast03).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 |
Positioning Development positioning | Leading efficacy in HER2 ADC class | Established SOC before Enhertu head-to-head | Lower ILD signal vs DXd in some datasets |
Technology Payload | DXd (topo-I inhibitor) | MMAE (maytansinoid) | MMAE |
Technology Linker | Cleavable tetrapeptide | Non-cleavable SMCC | Cleavable |
MoA Mechanism | 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. |
MoA Biomarker | 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. |
PK/PD Half-life | 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) |
PK/PD Species | Minipig, Pig, Human, Tumor response (ORR, PFS), ILD incidence rises with exposure | Mouse, Tumor response | Mouse, ORR in HER2+ UC/gastric |
PK/PD Animal (cat.) | Human, In vitro | Mouse, In vitro | Human, Mouse, In vitro |
PK/PD Experiment | Pharmacokinetic | Pharmacokinetic | pd |
PK/PD Biodistribution | Systemic exposure with tumor-selective HER2-mediated uptake | — | — |
Toxicology Species | Cynomolgus monkey, NHP, Rat, Minipig, Pig, Hamster, Human | Cynomolgus monkey, Mouse, Rat | Cynomolgus monkey, Mouse |
Toxicology Animal (cat.) | NHP | NHP | NHP |
Toxicology Major finding | 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. |
Toxicology CRS | Minimal | Minimal | N/A |
Toxicology NOAEL | 10 mg/kg | — | — |
Clinical Safety signal | 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. |
Clinical Selected reported efficacy | ORR 79.7% | ORR 43.6% | — |
Clinical Reported ORR | 79.7% | 43.6% (EMILIA) | — |
Clinical Reported PFS | NA | 9.6 mo | — |
Clinical Reported OS | NA | 30.9 mo | — |
Clinical Result source | ClinicalTrials.gov NCT03529110 | EMILIA | — |
Clinical Program phase | APPROVED | APPROVED | APPROVED |
Clinical Trial activity | No active/completed counts | No active/completed counts | No active/completed counts |
Clinical Trial ref | NCT03529110 | EMILIA | — |
Preclinical Animal (cat.) | Human, Mouse, In vitro | In vitro | — |
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 | |
|---|---|---|---|
Overview Program | Enhertu (trastuzumab deruxtecan) | Kadcyla (ado-trastuzumab emtansine / T-DM1) | Disitamab Vedotin (RC48) |
Overview Company | Daiichi Sankyo / AstraZeneca | Roche / Genentech | RemeGen |
Overview Modality | ADC | ADC | ADC |
Overview Target | HER2 | HER2 | HER2 |
Overview Indication | HER2+ breast cancer, HER2-low, gastric | HER2+ breast cancer | HER2+ urothelial, gastric, breast |
Overview Phase | APPROVED | APPROVED | APPROVED |
Overview Status | APPROVED | APPROVED | ACTIVE |
Overview Content status | Curated Core | Curated Core | Curated Core |
Overview Data Confidence | Data Confidence · High | Data Confidence · High | Data Confidence · High |
Overview Development Signal | Development Signal · Established | Development Signal · Established | Development Signal · Established |
Overview Approval status | FDA approved | FDA approved | FDA approved |
Positioning Key differentiator | High DAR (~8), bystander effect, HER2-low activity | Stable linker, DAR ~3.5 | Novel anti-HER2 mAb with distinct epitope |
Positioning Known limitation | 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 |
Positioning Development positioning | Leading efficacy in HER2 ADC class | Established SOC before Enhertu head-to-head | Lower ILD signal vs DXd in some datasets |
Technology Payload | DXd (topo-I inhibitor) | MMAE (maytansinoid) | MMAE |
Technology Linker | Cleavable tetrapeptide | Non-cleavable SMCC | Cleavable |
MoA Mechanism | 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. |
MoA Biomarker | 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. |
PK/PD Half-life | 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) |
PK/PD Species | Minipig, Pig, Human, Tumor response (ORR, PFS), ILD incidence rises with exposure | Mouse, Tumor response | Mouse, ORR in HER2+ UC/gastric |
PK/PD Animal (cat.) | Human, In vitro | Mouse, In vitro | Human, Mouse, In vitro |
PK/PD Experiment | Pharmacokinetic | Pharmacokinetic | pd |
PK/PD Biodistribution | Systemic exposure with tumor-selective HER2-mediated uptake | — | — |
Toxicology Species | Cynomolgus monkey, NHP, Rat, Minipig, Pig, Hamster, Human | Cynomolgus monkey, Mouse, Rat | Cynomolgus monkey, Mouse |
Toxicology Animal (cat.) | NHP | NHP | NHP |
Toxicology Major finding | 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. |
Toxicology CRS | Minimal | Minimal | N/A |
Toxicology NOAEL | 10 mg/kg | — | — |
Clinical Safety signal | 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. |
Clinical Selected reported efficacy | ORR 79.7% | ORR 43.6% | — |
Clinical Reported ORR | 79.7% | 43.6% (EMILIA) | — |
Clinical Reported PFS | NA | 9.6 mo | — |
Clinical Reported OS | NA | 30.9 mo | — |
Clinical Result source | ClinicalTrials.gov NCT03529110 | EMILIA | — |
Clinical Program phase | APPROVED | APPROVED | APPROVED |
Clinical Trial activity | No active/completed counts | No active/completed counts | No active/completed counts |
Clinical Trial ref | NCT03529110 | EMILIA | — |
Preclinical Animal (cat.) | Human, Mouse, In vitro | In vitro | — |
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