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API CSV38행 · 3개 프로그램

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항목
AntibodyCurated CoreFDAApproved
zanidatamab (Ziihera, ZW25, zanidatamab-hrii)
Jazz Pharmaceuticals / Zymeworks·HER2 (biparatopic)
35 trials·t½ ~7 days
AntibodyCurated CoreFDAApproved
trastuzumab (Herceptin, Ogivri, Herzuma)
Roche / Genentech·HER2
1100 trials·t½ 4 h
ADCCurated CoreFDAApproved
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
Ziihera (zanidatamab)Herceptin (trastuzumab)Enhertu (trastuzumab deruxtecan)
Overview
Company
Jazz Pharmaceuticals / ZymeworksRoche / GenentechDaiichi Sankyo / AstraZeneca
Overview
Modality
ANTIBODYANTIBODYADC
Overview
Target
HER2 (biparatopic)HER2HER2
Overview
Indication
First-line HER2-positive gastric, GEJ, or esophageal adenocarcinoma; previously treated HER2-positive biliary tract cancerHER2+ breast cancer, HER2+ gastric/GEJ adenocarcinomaHER2+ breast cancer, HER2-low, gastric
Overview
Phase
APPROVEDAPPROVEDAPPROVED
Overview
Status
APPROVEDAPPROVEDAPPROVED
Overview
Content status
Curated CoreCurated CoreCurated Core
Overview
Data Confidence
Data Confidence · HighData Confidence · HighData Confidence · High
Overview
Development Signal
Development Signal · EstablishedDevelopment Signal · EstablishedDevelopment Signal · Established
Overview
Approval status
FDA approvedFDA approvedFDA approved
Positioning
Key differentiator
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).novel bifunctional chelator (2E-C-NETA) for applications in 177 Lu-based TRTHigh DAR (~8), bystander effect, HER2-low activity
Positioning
Known limitation
HER2 heterogeneity, PI3K pathway activation, and bypass RTK signaling.resistance to trastuzumab-based targeted therapy and limited intratumoral antibody penetration continue to restrict clinical outcomesHER2 antigen loss/downregulation, payload efflux, and dose-limiting ILD/pneumonitis leading to discontinuation.
Positioning
Development positioning
Challenges the ToGA trastuzumab-chemo backbone in 1L HER2+ GEA; still the only HER2 agent with a dedicated BTC indication.Leading efficacy in HER2 ADC class
Technology
Payload
DXd (topo-I inhibitor)
Technology
Linker
Cleavable tetrapeptide
MoA
Mechanism
Simultaneous binding of two non-overlapping HER2 epitopes crosslinks adjacent receptors, causing receptor clustering, internalization, and degradation alongside ADCC and complement activity.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
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+.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
~7 days4 hADC ~5.8 days; total antibody ~6.1 days; released DXd ~2.7 days (5.4 mg/kg q3w)
PK/PD
Species
Cynomolgus monkey, Human, OS and PFS in GEA, ORR and DOR in BTCMouse, OS in metastatic BCMinipig, Pig, Human, Tumor response (ORR, PFS), ILD incidence rises with exposure
PK/PD
Animal (cat.)
Human, NHP, In vitroMouse, In vitroHuman, In vitro
PK/PD
Experiment
pdPharmacokineticPharmacokinetic
PK/PD
Biodistribution
Systemic exposure with tumor-selective HER2-mediated uptake
Toxicology
Species
HumanMouse, RatCynomolgus monkey, NHP, Rat, Minipig, Pig, Hamster, Human
Toxicology
Animal (cat.)
NHP
Toxicology
Major finding
Embryo-fetal toxicity warning. Diarrhea, infusion-related reactions, and left ventricular dysfunction require monitoring, as with the HER2 antibody class.Cardiotoxicity (LVEF decline, CHF risk especially with anthracyclines); infusion reactions; myelosuppression in combos.ILD-like lung findings at high exposure
Toxicology
CRS
N/AN/AMinimal
Toxicology
NOAEL
10 mg/kg
Clinical
Safety signal
Embryo-fetal toxicity warning. Diarrhea, infusion-related reactions, and left ventricular dysfunction require monitoring, as with the HER2 antibody class.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 52%ORR 91.2%ORR 79.7%
Clinical
Reported ORR
52%91.2%79.7%
Clinical
Reported PFS
~5.5 moNA
Clinical
Reported OS
15.54NA
Clinical
Result source
HERIZON-BTC-01 (NCT04466891)ClinicalTrials.gov NCT02149524ClinicalTrials.gov NCT03529110
Clinical
Program phase
APPROVEDAPPROVEDAPPROVED
Clinical
Trial activity
No active/completed countsNo active/completed countsNo active/completed counts
Clinical
Trial ref
NCT04466891NCT02149524NCT03529110
Preclinical
Animal (cat.)
UnknownHuman, Mouse, In vitro