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API CSV34행 · 5개 프로그램

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항목
ADCCurated CoreFDAstaleApproved
trastuzumab deruxtecan (Enhertu, T-DXd, DS-8201, TDxd)
Daiichi Sankyo / AstraZeneca·HER2
243 trials
ADCCurated CoreFDAstaleApproved
ado-trastuzumab emtansine (Kadcyla, T-DM1, Trastuzumab Emtansine)
Roche / Genentech·HER2
186 trials
ADCCurated CoreFDAstaleApproved
sacituzumab govitecan-hziy (Trodelvy, IMMU-132, sacituzumab-govitecan-hziy)
Gilead / Immunomedics·TROP2
242 trials
ADCCurated CoreFDAstaleApproved
datopotamab deruxtecan-dlnk (Datroway, DS-1062, Dato-DXd)
Daiichi Sankyo / AstraZeneca·TROP2
50 trials
ADCCurated CorestaleApproved
disitamab vedotin (Disitamab Vedotin, RC48)
RemeGen·HER2
159 trials
Overview
Program
Enhertu (fam-trastuzumab deruxtecan-nxki)Kadcyla (ado-trastuzumab emtansine)Trodelvy (sacituzumab govitecan-hziy)Datroway (datopotamab deruxtecan-dlnk)Disitamab Vedotin (RC48)
Overview
Company
Daiichi Sankyo / AstraZenecaRoche / GenentechGilead / ImmunomedicsDaiichi Sankyo / AstraZenecaRemeGen
Overview
Modality
ADCADCADCADCADC
Overview
Target
HER2HER2TROP2TROP2HER2
Overview
Indication
HER2-positive breast cancer (including regimen-specific first-line and early-stage indications); HER2-low/ultralow breast cancer, HER2-positive gastric cancer, HER2-mutant NSCLC and HER2-positive solid tumors: consult the current US labelHER2+ breast cancerTNBC: regimen-specific first-line and previously treated indications; HR-positive/HER2-negative breast cancer after specified prior therapies. Consult current US label.HR-positive/HER2-negative breast cancer after specified prior therapies; EGFR-mutated NSCLC after specified prior therapies; first-line TNBC unsuitable for PD-1/PD-L1 therapy. Consult current US label.HER2+ urothelial, gastric, breast
Overview
Phase
APPROVEDAPPROVEDAPPROVEDAPPROVEDAPPROVED
Overview
Status
APPROVEDAPPROVEDAPPROVEDAPPROVEDACTIVE
Overview
Content status
Curated CoreCurated CoreCurated CoreCurated CoreCurated Core
Overview
Data Confidence
Editorial scope · Curated CoreEditorial scope · Curated CoreEditorial scope · Curated CoreEditorial scope · Curated CoreEditorial scope · Curated Core
Overview
Development Signal
Development Signal · EstablishedDevelopment Signal · EstablishedDevelopment Signal · EstablishedDevelopment Signal · EstablishedDevelopment Signal · Established
Overview
Approval status
FDA approvedFDA approvedFDA approvedFDA approvedApproved (flag incomplete)
Positioning
Key differentiator
High DAR (~8), bystander effect, HER2-low activityStable linker, DAR ~3.5Very high DAR plus a deliberately unstable linker — extracellular SN-38 release gives bystander killing in TROP2-heterogeneous tumors.Same DXd chemistry that made Enhertu work, aimed at TROP2 — high plasma stability with a short-half-life payload to limit systemic exposure.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).TROP2 downregulation, TOP1 mutation, and ABC-transporter payload efflux.TROP2 loss, SLFN11 status, and topoisomerase I pathway adaptation.resistance mechanisms, optimize payload delivery, and minimize off-target toxicity
Positioning
Development positioning
Indication- and regimen-specific; includes 1L + pertuzumab in HER2-positive metastatic breast cancer2LRegimen-specific; includes 1L TNBC indications from June 2026Indication-specific; includes 1L TNBC unsuitable for PD-1/PD-L1 therapy2L+
Technology
Payload
DXd (topo-I inhibitor)DM1 (maytansine derivative)SN-38 (topoisomerase I inhibitor)DXd (exatecan derivative, topoisomerase I inhibitor)MMAE
Technology
Linker
Cleavable tetrapeptideNon-cleavable stable thioether MCCHydrolyzable CL2A, DAR ~7.6Tetrapeptide-based cleavable maleimide linker, DAR ~4Cleavable
Technology
DAR
——DAR 7.6DAR 4—
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.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.Anti-TROP2 antibody delivers DXd intracellularly after lysosomal linker cleavage; topoisomerase I inhibition drives DNA damage, with membrane-permeable payload producing a bystander effect.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).TROP2 is broadly expressed in epithelial tumors; no companion diagnostic is required in the label.TROP2 expression is not a required companion diagnostic; quantitative continuous scoring (QCS) is investigational.HER2 expression (IHC); activity in HER2+ urothelial and gastric cancers.
Toxicology
Species
Cynomolgus monkey, NHP, Rat, HamsterCynomolgus monkey, RatCynomolgus monkey, HamsterRat, HamsterCynomolgus monkey
Toxicology
Animal (cat.)
NHPNHP——NHP
Toxicology
Major finding
ILD-like lung findings at high exposureThrombocytopenia, hepatotoxicityBoxed warning for severe neutropenia and severe diarrhea. Nausea, alopecia, fatigue, and rare hypersensitivity are common.Stomatitis, dry eye and keratitis, nausea, and alopecia. Interstitial lung disease is a class warning for DXd conjugates and requires prompt steroid intervention.Hematologic toxicity and peripheral neuropathy class effects of MMAE; ILD reported at lower frequency than DXd ADCs in published datasets.
Toxicology
CRS
MinimalMinimalN/AN/AN/A
Toxicology
NOAEL
10 mg/kg————
Clinical
Safety signal
ILD-like lung findings at high exposureThrombocytopenia, hepatotoxicityBoxed warning for severe neutropenia and severe diarrhea. Nausea, alopecia, fatigue, and rare hypersensitivity are common.Stomatitis, dry eye and keratitis, nausea, and alopecia. Interstitial lung disease is a class warning for DXd conjugates and requires prompt steroid intervention.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 87%—ORR 50%ORR 64%—
Clinical
Reported ORR
87% vs 81% (THP)—50% vs 47% (chemotherapy)64% vs 30% (chemotherapy)—
Clinical
Reported PFS
40.7 months vs 26.9 months (THP)—9.7 months vs 6.9 months (chemotherapy)10.8 months vs 5.6 months (chemotherapy)—
Clinical
Reported OS
Immature at the reported PFS analysis—Immature in FDA approval analysis23.7 months vs 18.7 months (chemotherapy)—
Clinical
Result source
FDA label 2026, Table 28 — DESTINY-Breast09 (NCT04784715)—FDA approval report 2026-06-24 — ASCENT-03 (NCT05382299)FDA approval report 2026-05-22 — TROPION-Breast02 (NCT05374512)—
Clinical
Program phase
APPROVEDAPPROVEDAPPROVEDAPPROVEDAPPROVED
Clinical
Trial activity
No active/completed countsNo active/completed countsNo active/completed countsNo active/completed countsNo active/completed counts
Clinical
Trial ref
NCT04784715—NCT05382299NCT05374512—
Preclinical
Animal (cat.)
Human, Mouse, In vitroIn vitroMouseMouse, In vitro—