Jiataile Sacituzumab Tirumotecan for Injection

1. Indications and Usage
Triple-Negative Breast Cancer (TNBC):
Indicated for the treatment of adult patients with unresectable locally advanced or metastatic triple-negative breast cancer who have received at least two prior systemic therapies, at least one of them for metastatic disease .
Non-Small Cell Lung Cancer (NSCLC):
Indicated for the treatment of adult patients with locally advanced or metastatic non-squamous non-small cell lung cancer with epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R substitution mutations, who have progressed after treatment with EGFR tyrosine kinase inhibitor (TKI) and platinum-based chemotherapy .
2. Dosage and Administration
Route of Administration:
For Intravenous Infusion ONLY. Must be administered under the guidance of a physician experienced in the use of antineoplastic agents.
Prohibition: Do not administer via intravenous push or rapid injection .
Recommended Dosage:
Dose: 5 mg/kg administered intravenously once every 2 weeks.
Duration: Continue until disease progression or unacceptable toxicity .
Administration Instructions:
Infusion Time: For the first 4 infusions, administer over 90 ± 15 minutes. If no infusion-related reactions (IRR) occur, the duration may be shortened to no less than 60 minutes from the 5th infusion onwards .
Premedication: Prophylactic medication (e.g., antipyretics, antihistamines) is required prior to each administration to prevent IRRs .
Preparation:
Reconstitute with Water for Injections. The reconstituted solution should be diluted promptly. Do not shake the vial .
3. Mechanism of Action
Antibody-Drug Conjugate (ADC):
Sacituzumab Tirumotecan consists of a humanized anti-TROP2 monoclonal antibody, a cleavable linker, and a cytotoxic payload (topoisomerase I inhibitor KL610023) .
Targeted Delivery:
The antibody specifically binds to TROP2, which is overexpressed on tumor cells. The ADC complex is internalized into the tumor cell .
Cytotoxicity:
Inside the cell, the linker is cleaved, releasing the active payload (KL610023). This payload inhibits topoisomerase I, causing DNA damage and inducing tumor cell apoptosis .
4. Safety and Warnings
Neutropenia:
Severe and prolonged neutropenia can occur. Monitor blood counts regularly. Dose delays or reductions may be necessary for Grade 3 or higher neutropenia .
Infusion-Related Reactions (IRR):
Hypersensitivity and IRRs (e.g., dyspnea, hypotension, flushing) may occur. Interrupt or slow the infusion if reactions occur. Permanent discontinuation is required for life-threatening reactions .
Gastrointestinal Toxicity:
Stomatitis, nausea, vomiting, and diarrhea are common. Prophylactic antiemetics are recommended .
Embryo-Fetal Toxicity:
Can cause fetal harm based on its mechanism of action. Women of reproductive potential should use effective contraception during treatment .
5. Adverse Reactions
Most Common (>30%):
Decreased hemoglobin, leukopenia, neutropenia, stomatitis, rash, thrombocytopenia, alopecia, and nausea .
Grade 3 or Higher (>5%):
Neutropenia, anemia, leukopenia, stomatitis, and thrombocytopenia .
6. Drug Interactions
CYP3A Substrate:
Sacituzumab Tirumotecan is a substrate of CYP3A. Concomitant use with strong CYP3A4 inhibitors may increase the drug exposure and toxicity. Avoid combining with strong CYP3A4 inhibitors whenever possible .
7. Pharmaceutical Information
Chemical Composition:
Active Ingredient: Sacituzumab Tirumotecan .
Excipients: Histidine, Histidine Hydrochloride, Sucrose, Polysorbate 20 .
Appearance: White to off-white lyophilized cake; clear to pale yellow solution after reconstitution .
Storage:
Store in a refrigerator at 2°C to 8°C (36°F to 46°F) in the original carton to protect from light. Do not freeze .