Jiataile Sacituzumab Tirumotecan for Injection

1. Indications and Usage
Triple-Negative Breast Cancer (TNBC):
Treatment of adult patients with unresectable locally advanced or metastatic TNBC who have received at least two prior systemic therapies (at least one in the metastatic setting).
Non-Small Cell Lung Cancer (NSCLC):
Treatment of adult patients with EGFR mutation-positive, locally advanced or metastatic non-squamous NSCLC who have progressed on or after an EGFR tyrosine kinase inhibitor (TKI) and platinum-based chemotherapy.
2. Dosage and Administration
Route of Administration:
For Intravenous (IV) Infusion ONLY.
Recommended Dosage:
Standard Dose: 5 mg/kg.
Frequency: Administered once every 2 weeks (Q2W) until disease progression or unacceptable toxicity.
Critical Administration Instructions:
Pre-medication: Pre-medication is required before every administration to prevent infusion-related reactions.
First 4 Infusions: Must include diphenhydramine, acetaminophen, dexamethasone (10 mg IV), and an H2 receptor blocker (e.g., famotidine).
5th Infusion Onwards: Diphenhydramine and acetaminophen are required; corticosteroids and H2 blockers are at the physician’s discretion.
Infusion Time: First 4 infusions must be administered over 90 ± 15 minutes (up to 105 minutes if needed). If no reactions occur, subsequent infusions may be shortened to no less than 60 minutes.
Preparation: Reconstitute and dilute under aseptic conditions. Do not shake.
3. Mechanism of Action
Antibody-Drug Conjugate (ADC):
Composed of a recombinant anti-TROP2 humanized monoclonal antibody linked to KL610023 (a topoisomerase I inhibitor) via a carbonate linker with a pyrimidine moiety.
Targeted Delivery:
Binds to TROP2 on tumor cells, is internalized, and releases the cytotoxic payload, which inhibits DNA replication and induces cell death. It also exhibits an antibody-dependent cellular cytotoxicity (ADCC) effect.
4. Safety and Warnings
Neutropenia and Febrile Neutropenia:
Severe neutropenia and febrile neutropenia are very common and potentially fatal. Monitor absolute neutrophil count (ANC) regularly. Hold treatment for Grade 3 or 4 neutropenia and resume at a reduced dose upon recovery.
Infusion-Related Reactions:
Serious and fatal infusion-related reactions have been reported. Monitor patients closely during and after infusion.
Severe Diarrhea and Colitis:
Diarrhea and colitis can be severe and fatal. Manage promptly with antidiarrheals and hold/discontinue treatment as necessary.
Embryo-Fetal Toxicity:
Can cause fetal death. Advise females of reproductive potential to use effective contraception.
5. Adverse Reactions and Clinical Research
Most Common Adverse Reactions:
Neutropenia, leukopenia, anemia, thrombocytopenia, stomatitis (oral mucositis), rash, nausea, vomiting, alopecia, and fatigue.
Clinical Research Highlights:
In Phase 1/2 studies, sacituzumab tirumotecan demonstrated promising antitumor activity and a manageable safety profile in patients with metastatic TNBC and other solid tumors.
6. Drug Interactions
CYP3A Substrate:
As sacituzumab tirumotecan is a substrate of CYP3A, concomitant use with strong CYP3A4 inhibitors may increase exposure and should be avoided.
7. Pharmaceutical Information
Chemical Composition:
Active Ingredient: Sacituzumab tirumotecan.
Appearance: White to off-white疏松体 (loose body) prior to reconstitution; colorless to pale yellow clear liquid after reconstitution.
Packaging: Single-use vial (200 mg).
Storage: Store in the original carton at 2°C to 8°C. Do not freeze.