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sacituzumab tirumotecan   Click here for help

GtoPdb Ligand ID: 13791

Synonyms: Jiataile® | MK-2870 | sac-TMT | SKB-264 | SKB264
Approved drug
sacituzumab tirumotecan is an approved drug
Compound class: Antibody
Comment: Sacituzumab tirumotecan (SKB264/MK-2870) is an antibody-drug conjugate (ADC) [1-2]. It is the same humanized anti-TROP-2 monoclonal antibody as the previously approved ADC sacituzumab govitecan, but carrying a different topoisomerase inhibitor payload (tirumotecan/KL610023) that is a belotecan-derivative. TROP-2 is a transmembrane glycoprotein, cell surface antigen which has oncogenic activity in cancers of epithelial origin [6], but expression is restricted in normal tissue. Directing the topoisomerase inhibitor selectively to cancer cells via TROP-2 binding is predicted to limit toxicity towards healthy tissue/cells.
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
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Summary of Clinical Use Click here for help
Sacituzumab tirumotecan (SKB264/MK-2870) was progressed as an oncology clinical candidate. The Chinese drug regulator (NMPA) approved sacituzumab tirumotecan (Jiataile®) in November 2024, to treat advanced triple-negative breast cancer. The FDA granted sacituzumab tirumotecan breakthrough designation in December 2024, making it available as an option for pretreated advanced or metastatic nonsquamous non-small cell lung cancer (NSCLC) harboring EGFR mutations.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT05347134 SKB264 Injection Vs Investigator Selected Regimens to Treat Locally Advanced, Recurrent or Metastatic Triple-negative Breast Cancer Phase 3 Interventional Sichuan Kelun Pharmaceutical Research Institute Co., Ltd. 7
NCT07179783 Sacituzumab Tirumotecan in Combination With Tagitanlimab in the Treatment of Aggressive Variant Prostate Cancer (AVPC) and Neuroendocrine Prostate Cancer (NEPC) Phase 2 Interventional Tianjin Medical University Second Hospital
NCT07193160 Sacituzumab Tirumotecan in Combination With Furmonertinib as Second-line Treatment for EGFR-mutant Advanced or Metastatic NSCLC After Failure of First-line Third-generation EGFR-TKI Therapy Phase 2 Interventional Fudan University
NCT07197008 Sacituzumab Tirumotecan (Sac-TMT) Plus Bevacizumab in 3rd Generation EGFR-TKI Treated Advanced EGFR-mutant Nonsquamous NSCLC With Brain Metastasis Phase 2 Interventional Sun Yat-sen University
NCT07216703 A Clinical Study of Sacituzumab Tirumotecan (MK-2870) in Combination With Pembrolizumab (MK-3475) as First-line Maintenance Treatment of Cervical Cancer (MK-2870-036/TroFuse-036/GOG-3123/ENGOT-cx22) Phase 3 Interventional Merck Sharp & Dohme LLC
NCT05351788 SKB264 Combinatiton Therapy in Patients With Advanced or Metastatic Non-small Cell Lung Cancer. Phase 2 Interventional Sichuan Kelun Pharmaceutical Research Institute Co., Ltd. 4
NCT05631262 SKB264 Monotherapy in Selected Subjects with Advanced Solid Tumors Phase 2 Interventional Sichuan Kelun Pharmaceutical Research Institute Co., Ltd. 3,7
NCT04152499 Phase I-II, FIH, TROP2 ADC, Advanced Unresectable/Metastatic Solid Tumors, Refractory to Standard Therapies (KL264-01) Phase 1/Phase 2 Interventional Klus Pharma Inc. 5