{"entity":{"id":"sacituzumab-tirumotecan","kind":"drug","name":"Sacituzumab tirumotecan","aka":[],"tldr":"Sacituzumab tirumotecan is Kelun-Biotech's TROP2 ADC, approved in China in 2024 for pretreated triple-negative breast cancer and then EGFR-mutant lung cancer. Merck holds rights outside Greater China and runs the TroFuse programme of more than ten phase 3 trials across breast, lung, endometrial and cervical cancer; in the US it holds a priority voucher but no approval yet.","summary":"Kelun-Biotech's sac-TMT was approved by China's NMPA in 2024 for pretreated TNBC (the first TROP2 ADC approval in China) and later for EGFR-mutant NSCLC. Merck holds ex-Greater-China rights and runs the TroFuse programme of >10 phase 3 trials, including first-line TNBC (positive on primary endpoint per 2026 reports), HR+ breast, NSCLC, endometrial, and cervical cancer, many combined with pembrolizumab. FDA Breakthrough Therapy designation (EGFR-mutant NSCLC, 2024) and a Commissioner's National Priority Voucher (July 2026).","status":"approved","asOf":"2026-09-04","links":[{"label":"Frontiers review (2026)","url":"https://www.frontiersin.org/journals/oncology-reviews/articles/10.3389/or.2026.1781533/full"}],"tags":[],"related":[],"cancers":["tnbc","nsclc","breast-hr-positive","endometrial","cervical"],"sections":[],"technologies":["adc","topoisomerase-inhibitors"],"targets":["trop2"],"drugs":[],"companies":["kelun-biotech","merck"],"institutions":[],"pathways":[],"terms":["t030","hydrophilic-next-gen"],"trials":["nct06670196","nct06305754","nct06448312","nct07216703","nct07318558","nct06824467","nct06356311","nct06170788","nct06459180","nct06422143","nct06711900","nct06312137","nct06952504","nct06132958","nct05870319","nct06074588","nct04152499","nct05351788","nct05816252","nct07329322","nct06428409","nct06483334","nct06393374","nct06469944","nct07252739","nct06312176","nct07419295","nct06966700","nct07286149","nct05319730","nct06637423","nct07324629","nct06780111","nct06445972","nct06788912","nct06841354"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"code":"sac-TMT, MK-2870, SKB264","modality":"ADC","payload":"T030 (belotecan-derived TOP1 inhibitor), DAR ~7.4","linker":"Sulfonyl pyrimidine (CL2A-like), pH-sensitive and enzyme-cleavable","mechanism":"Anti-TROP2 IgG1 with a stable, irreversibly-conjugated linker and a belotecan-derived TOP1 payload with reported lower efflux-pump susceptibility.","approvals":[{"region":"China","year":2024,"indication":"Pretreated advanced TNBC; later EGFR-mutant NSCLC after TKI"}],"mechanismSteps":["Antibody binds TROP2 on the tumour cell surface","Receptor-ADC complex is internalised by endocytosis","Trafficked to the lysosome; linker is cleaved or antibody degraded","T030 (belotecan-derived TOP1 inhibitor) is released inside the cell","Topoisomerase-I is trapped on DNA; replication forks collapse into double-strand breaks","Tumour cell dies by apoptosis","Membrane-permeable payload diffuses to kill neighbouring antigen-negative cells (bystander effect)"],"dosing":{"route":"IV infusion","schedule":"5 mg/kg every 2 weeks (China label, TNBC); phase 3 trials use 4 mg/kg every 2 weeks in combination regimens","monitoring":"Blood counts; stomatitis and ocular surface care","source":"https://www.frontiersin.org/journals/oncology-reviews/articles/10.3389/or.2026.1781533/full"},"toxicity":[{"event":"Neutropenia","note":"Most common grade ≥3 event in OptiTROP-Breast01; rates per publication"},{"event":"Anaemia"},{"event":"Stomatitis"},{"event":"Nausea"},{"event":"Alopecia"}],"access":[{"country":"CN","reimbursement":"NMPA approved 2024; National Reimbursement Drug List inclusion from 2025","asOf":"2026-09-06"},{"country":"US","reimbursement":"Investigational; not yet approved","asOf":"2026-09-06"}],"regulatoryEvents":[{"date":"2022-05","type":"filing","region":"China","note":"Merck licenses ex-Greater-China rights (deal expanded December 2022)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2024-11","type":"approval","region":"China","note":"NMPA approval, pretreated advanced TNBC (OptiTROP-Breast01); first TROP2 ADC approved in China","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2024-12-03","type":"designation","region":"US","note":"Breakthrough Therapy designation, EGFR-mutant NSCLC after TKI","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2025-03","type":"approval","region":"China","note":"EGFR-mutant NSCLC after TKI failure","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2026-07","type":"designation","region":"US","note":"Commissioner's National Priority Voucher (CNPV) awarded","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"}]},"route":"/drugs/sacituzumab-tirumotecan/","neighbours":{"cancer":[{"id":"advanced-recurrent-endometrial-cancer","kind":"cancer","name":"Advanced or recurrent endometrial cancer","route":"/cancers/advanced-recurrent-endometrial-cancer/"},{"id":"urothelial","kind":"cancer","name":"Bladder & urothelial cancer","route":"/cancers/urothelial/"},{"id":"cervical","kind":"cancer","name":"Cervical cancer","route":"/cancers/cervical/"},{"id":"endometrial","kind":"cancer","name":"Endometrial cancer","route":"/cancers/endometrial/"},{"id":"endometrial-nsmp","kind":"cancer","name":"Endometrial cancer with no specific molecular profile","route":"/cancers/endometrial-nsmp/"},{"id":"her2-low-metastatic-breast-cancer","kind":"cancer","name":"HER2-low and HER2-ultralow metastatic breast cancer","route":"/cancers/her2-low-metastatic-breast-cancer/"},{"id":"breast-hr-positive","kind":"cancer","name":"HR-positive / HER2-negative breast cancer","route":"/cancers/breast-hr-positive/"},{"id":"tnbc-metastatic","kind":"cancer","name":"Metastatic triple-negative breast cancer","route":"/cancers/tnbc-metastatic/"},{"id":"nsclc","kind":"cancer","name":"Non-small-cell lung cancer","route":"/cancers/nsclc/"},{"id":"endometrial-p53-abnormal","kind":"cancer","name":"p53-abnormal endometrial cancer, including uterine serous carcinoma","route":"/cancers/endometrial-p53-abnormal/"},{"id":"pdl1-high-nsclc","kind":"cancer","name":"PD-L1-high non-small-cell lung cancer without a driver mutation","route":"/cancers/pdl1-high-nsclc/"},{"id":"recurrent-metastatic-cervical-cancer","kind":"cancer","name":"Recurrent or metastatic cervical cancer","route":"/cancers/recurrent-metastatic-cervical-cancer/"},{"id":"tnbc","kind":"cancer","name":"Triple-negative breast cancer (TNBC)","route":"/cancers/tnbc/"}],"technology":[{"id":"adc","kind":"technology","name":"Antibody-drug conjugate (ADC)","route":"/technologies/adc/"},{"id":"topoisomerase-inhibitors","kind":"technology","name":"Topoisomerase-I inhibitors (and ADC payloads)","route":"/technologies/topoisomerase-inhibitors/"},{"id":"trop2-pet","kind":"technology","name":"TROP2 PET","route":"/technologies/trop2-pet/"}],"target":[{"id":"trop2","kind":"target","name":"TROP2","route":"/targets/trop2/"}],"company":[{"id":"merck","kind":"company","name":"Merck & Co. 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