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: 4개 · 임상 갱신 필요 2개
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 | Tisotumab Vedotin | Erbitux | Enhertu (trastuzumab deruxtecan) | Toripalimab |
Overview Company | Genmab / Pfizer | Eli Lilly / Merck KGaA | Daiichi Sankyo / AstraZeneca | Junshi Biosciences |
Overview Modality | ADC | ANTIBODY | ADC | ANTIBODY |
Overview Target | Solid Malignancies | Colorectal Cancer | HER2 | Gastric Cancer |
Overview Indication | Colorectal Neoplasms; Carcinoma, Non-Small-Cell Lung | Head and Neck Cancer Squamous Cell | HER2+ breast cancer, HER2-low, gastric | Metastatic Colorectal Cancer; Liver Metastases |
Overview Phase | APPROVED | PHASE_3 | APPROVED | PHASE_3 |
Overview Status | APPROVED | RECRUITING | APPROVED | RECRUITING |
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 · Emerging | Development Signal · Established | Development Signal · Emerging |
Overview Approval status | FDA approved | Investigational | FDA approved | Investigational |
Positioning Key differentiator | — | novel strategies of biotherapeutics | High DAR (~8), bystander effect, HER2-low activity | novel safety signals were identified |
Positioning Known limitation | — | resistance to anti-EGFR therapy by transcriptional reprogramming in patient-derived colorectal cancer models | HER2 antigen loss/downregulation, payload efflux, and dose-limiting ILD/pneumonitis leading to discontinuation. | downregulation of p-Akt and Ki-67 |
Positioning Development positioning | — | — | Leading efficacy in HER2 ADC class | — |
Technology Payload | — | — | DXd (topo-I inhibitor) | — |
Technology Linker | — | — | Cleavable tetrapeptide | — |
MoA Mechanism | — | targeting the epidermal growth factor receptor | 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. | Binding of the PD-1 ligands, PD-L1 and PD-L2, to the PD-1 receptor found on T cells, inhibits T cell proliferation and cytokine production |
MoA Biomarker | — | EGFR SR could be established with high | HER2 expression (IHC/ISH per indication); higher systemic exposure associated with greater ILD incidence (FDA label §12.2). | PD-L1)-positive |
PK/PD Half-life | — | 5.2 h | ADC ~5.8 days; total antibody ~6.1 days; released DXd ~2.7 days (5.4 mg/kg q3w) | — |
PK/PD Species | — | Pig | Minipig, Pig, Human, Tumor response (ORR, PFS), ILD incidence rises with exposure | Rat |
PK/PD Animal (cat.) | — | In vitro | Human, In vitro | Rat, In vitro |
PK/PD Experiment | — | Pharmacokinetic | Pharmacokinetic | PD |
PK/PD Biodistribution | — | — | Systemic exposure with tumor-selective HER2-mediated uptake | — |
Toxicology Species | — | Pig | Cynomolgus monkey, NHP, Rat, Minipig, Pig, Hamster, Human | Rat |
Toxicology Animal (cat.) | — | In vitro | NHP | Rat, In vitro |
Toxicology Major finding | Pneumonitis: Severe, life-threatening, or fatal pneumonitis may occur | A Phase I Study Comparing the Pharmacokinetics, Safety, and Immunogenicity of A140 Injection and Cetuximab (Erbitux ® ) in Healthy Chinese Male Subjects.. This study aimed to compare the pharmacokinetic (PK) profiles, safety, and immunogenicity of the proposed A140 with those of cetuximab (Erbitux ® ) in healthy Chinese male subjects. We conducted a randomized, single-dose, double-b… | ILD-like lung findings at high exposure | Thrombocytopenia and Splenomegaly in Locally Advanced Rectal Cancer Patients Receiving Total Neo |
Toxicology CRS | — | — | Minimal | — |
Toxicology NOAEL | — | — | 10 mg/kg | — |
Clinical Safety signal | Pneumonitis: Severe, life-threatening, or fatal pneumonitis may occur | A Phase I Study Comparing the Pharmacokinetics, Safety, and Immunogenicity of A140 Injection and Cetuximab (Erbitux ® ) in Healthy Chinese Male Subjects.. This study aimed to compare the pharmacokinetic (PK) profiles, safety, and immunogenicity of the proposed A140 with those of cetuximab (Erbitux ® ) in healthy Chinese male subjects. We conducted a randomized, single-dose, double-b… | ILD-like lung findings at high exposure | Thrombocytopenia and Splenomegaly in Locally Advanced Rectal Cancer Patients Receiving Total Neo |
Clinical Selected reported efficacy | ORR 23.8% | ORR 52.2% | ORR 79.7% | ORR 75.5% |
Clinical Reported ORR | 23.8% | 52.2% | 79.7% | 75.5% |
Clinical Reported PFS | — | — | NA | 8.2 |
Clinical Reported OS | — | — | NA | 33.7 |
Clinical Result source | ClinicalTrials.gov NCT03438396 | ClinicalTrials.gov NCT00527111 | ClinicalTrials.gov NCT03529110 | ClinicalTrials.gov NCT03581786 |
Clinical Program phase | APPROVED | PHASE_3 | APPROVED | PHASE_3 |
Clinical Trial activity | No active/completed counts | No active/completed counts | No active/completed counts | No active/completed counts |
Clinical Trial ref | NCT03438396 | NCT00527111 | NCT03529110 | NCT03581786 |
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: 4개 · 임상 갱신 필요 2개
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 | Tisotumab Vedotin | Erbitux | Enhertu (trastuzumab deruxtecan) | Toripalimab |
Overview Company | Genmab / Pfizer | Eli Lilly / Merck KGaA | Daiichi Sankyo / AstraZeneca | Junshi Biosciences |
Overview Modality | ADC | ANTIBODY | ADC | ANTIBODY |
Overview Target | Solid Malignancies | Colorectal Cancer | HER2 | Gastric Cancer |
Overview Indication | Colorectal Neoplasms; Carcinoma, Non-Small-Cell Lung | Head and Neck Cancer Squamous Cell | HER2+ breast cancer, HER2-low, gastric | Metastatic Colorectal Cancer; Liver Metastases |
Overview Phase | APPROVED | PHASE_3 | APPROVED | PHASE_3 |
Overview Status | APPROVED | RECRUITING | APPROVED | RECRUITING |
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 · Emerging | Development Signal · Established | Development Signal · Emerging |
Overview Approval status | FDA approved | Investigational | FDA approved | Investigational |
Positioning Key differentiator | — | novel strategies of biotherapeutics | High DAR (~8), bystander effect, HER2-low activity | novel safety signals were identified |
Positioning Known limitation | — | resistance to anti-EGFR therapy by transcriptional reprogramming in patient-derived colorectal cancer models | HER2 antigen loss/downregulation, payload efflux, and dose-limiting ILD/pneumonitis leading to discontinuation. | downregulation of p-Akt and Ki-67 |
Positioning Development positioning | — | — | Leading efficacy in HER2 ADC class | — |
Technology Payload | — | — | DXd (topo-I inhibitor) | — |
Technology Linker | — | — | Cleavable tetrapeptide | — |
MoA Mechanism | — | targeting the epidermal growth factor receptor | 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. | Binding of the PD-1 ligands, PD-L1 and PD-L2, to the PD-1 receptor found on T cells, inhibits T cell proliferation and cytokine production |
MoA Biomarker | — | EGFR SR could be established with high | HER2 expression (IHC/ISH per indication); higher systemic exposure associated with greater ILD incidence (FDA label §12.2). | PD-L1)-positive |
PK/PD Half-life | — | 5.2 h | ADC ~5.8 days; total antibody ~6.1 days; released DXd ~2.7 days (5.4 mg/kg q3w) | — |
PK/PD Species | — | Pig | Minipig, Pig, Human, Tumor response (ORR, PFS), ILD incidence rises with exposure | Rat |
PK/PD Animal (cat.) | — | In vitro | Human, In vitro | Rat, In vitro |
PK/PD Experiment | — | Pharmacokinetic | Pharmacokinetic | PD |
PK/PD Biodistribution | — | — | Systemic exposure with tumor-selective HER2-mediated uptake | — |
Toxicology Species | — | Pig | Cynomolgus monkey, NHP, Rat, Minipig, Pig, Hamster, Human | Rat |
Toxicology Animal (cat.) | — | In vitro | NHP | Rat, In vitro |
Toxicology Major finding | Pneumonitis: Severe, life-threatening, or fatal pneumonitis may occur | A Phase I Study Comparing the Pharmacokinetics, Safety, and Immunogenicity of A140 Injection and Cetuximab (Erbitux ® ) in Healthy Chinese Male Subjects.. This study aimed to compare the pharmacokinetic (PK) profiles, safety, and immunogenicity of the proposed A140 with those of cetuximab (Erbitux ® ) in healthy Chinese male subjects. We conducted a randomized, single-dose, double-b… | ILD-like lung findings at high exposure | Thrombocytopenia and Splenomegaly in Locally Advanced Rectal Cancer Patients Receiving Total Neo |
Toxicology CRS | — | — | Minimal | — |
Toxicology NOAEL | — | — | 10 mg/kg | — |
Clinical Safety signal | Pneumonitis: Severe, life-threatening, or fatal pneumonitis may occur | A Phase I Study Comparing the Pharmacokinetics, Safety, and Immunogenicity of A140 Injection and Cetuximab (Erbitux ® ) in Healthy Chinese Male Subjects.. This study aimed to compare the pharmacokinetic (PK) profiles, safety, and immunogenicity of the proposed A140 with those of cetuximab (Erbitux ® ) in healthy Chinese male subjects. We conducted a randomized, single-dose, double-b… | ILD-like lung findings at high exposure | Thrombocytopenia and Splenomegaly in Locally Advanced Rectal Cancer Patients Receiving Total Neo |
Clinical Selected reported efficacy | ORR 23.8% | ORR 52.2% | ORR 79.7% | ORR 75.5% |
Clinical Reported ORR | 23.8% | 52.2% | 79.7% | 75.5% |
Clinical Reported PFS | — | — | NA | 8.2 |
Clinical Reported OS | — | — | NA | 33.7 |
Clinical Result source | ClinicalTrials.gov NCT03438396 | ClinicalTrials.gov NCT00527111 | ClinicalTrials.gov NCT03529110 | ClinicalTrials.gov NCT03581786 |
Clinical Program phase | APPROVED | PHASE_3 | APPROVED | PHASE_3 |
Clinical Trial activity | No active/completed counts | No active/completed counts | No active/completed counts | No active/completed counts |
Clinical Trial ref | NCT03438396 | NCT00527111 | NCT03529110 | NCT03581786 |
Preclinical Animal (cat.) | — | — | Human, Mouse, In vitro | — |
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