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sacituzumab tirumotecan + lorlatinib
- Development stage
- Phase 2
- Lead developer
- Merck
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Sacituzumab tirumotecan + lorlatinib is an investigational combination regimen being evaluated for the treatment of ALK fusion-positive non-small cell lung cancer (NSCLC). The regimen consists of sacituzumab tirumotecan (also known as SKB264 or MK-2870), a TROP2-directed antibody-drug conjugate (ADC), and lorlatinib, a third-generation tyrosine kinase inhibitor (TKI). Sacituzumab tirumotecan, developed by Kelun-Biotech and co-developed with Merck (MSD), utilizes a proprietary pyrimidine-thiol linker to deliver a novel topoisomerase I inhibitor payload to cells expressing TROP2. Lorlatinib, developed by Pfizer, is a potent inhibitor of ALK and ROS1 kinases designed to overcome resistance mutations. This combination is currently being studied in a Phase II clinical trial sponsored by the Guangdong Association of Clinical Trials, where patient selection is guided by peripheral blood circulating tumor DNA (ctDNA) analysis to identify ALK fusion-positive status in locally advanced or metastatic NSCLC.
- Other names
- SKB264 plus lorlatinibSKB-264 plus lorlatinibSKB 264 plus lorlatinibMK-2870 plus lorlatinibMK2870 plus lorlatinibMK 2870 plus lorlatinib
02
Targets
TNK2 (Activated Cdc42-associated kinase 1)ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)FAK (Focal adhesion kinase)PTK2BFER (FER tyrosine kinase)FDPS (Farnesyl pyrophosphate synthase)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)NTRK1 (Tropomyosin-related receptor kinase A)NTRK2 (Tropomyosin-related kinase receptor type B)NTRK3 (Tropomyosin receptor kinase C)TACSTD2 (Tumor-associated calcium signal transducer 2)LTK (Leukocyte receptor tyrosine kinase)
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