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항목
ADCCurated CoreFDAApproved
sacituzumab govitecan (Trodelvy, IMMU-132, sacituzumab-govitecan-hziy)
Gilead / Immunomedics·TROP2
242 trials·t½ ADC ~16 h; free SN-38 ~18 h
Overview
Program
Trodelvy (sacituzumab govitecan)
Overview
Company
Gilead / Immunomedics
Overview
Modality
ADC
Overview
Target
TROP2
Overview
Indication
Metastatic triple-negative breast cancer, pretreated HR+/HER2− breast cancer
Overview
Phase
APPROVED
Overview
Status
APPROVED
Overview
Content status
Curated Core
Overview
Data Confidence
Data Confidence · High
Overview
Development Signal
Development Signal · Established
Overview
Approval status
FDA approved
Positioning
Key differentiator
Very high DAR plus a deliberately unstable linker — extracellular SN-38 release gives bystander killing in TROP2-heterogeneous tumors.
Positioning
Known limitation
TROP2 downregulation, TOP1 mutation, and ABC-transporter payload efflux.
Positioning
Development positioning
TROP2 class leader by approval history; now facing Datroway and other TROP2 ADCs.
Technology
Payload
SN-38 (topoisomerase I inhibitor)
Technology
Linker
Hydrolyzable CL2A, DAR ~7.6
Technology
DAR
DAR 7.6
MoA
Mechanism
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
TROP2 is broadly expressed in epithelial tumors; no companion diagnostic is required in the label.
PK/PD
Half-life
ADC ~16 h; free SN-38 ~18 h
PK/PD
Species
Mouse, ORR and PFS, ctDNA dynamics exploratory
PK/PD
Animal (cat.)
Human, Mouse, In vitro
PK/PD
Experiment
pd
Toxicology
Species
Cynomolgus monkey, Mouse, Hamster
Toxicology
Major finding
Boxed warning for severe neutropenia and severe diarrhea. Nausea, alopecia, fatigue, and rare hypersensitivity are common.
Toxicology
CRS
N/A
Clinical
Safety signal
Boxed warning for severe neutropenia and severe diarrhea. Nausea, alopecia, fatigue, and rare hypersensitivity are common.
Clinical
Selected reported efficacy
ORR 44%
Clinical
Reported ORR
44.0%
Clinical
Result source
ClinicalTrials.gov NCT04916002
Clinical
Program phase
APPROVED
Clinical
Trial activity
No active/completed counts
Clinical
Trial ref
NCT04916002
Preclinical
Animal (cat.)
Mouse