Instructions for Sacituzumab govitecan

1. Generic name: gosatuzumab

Product name: TRODELVY, TRODELVY

All names: Sacituzumab Govitecan for Injection, Sacituzumab Govitecan for Injection, Sacituzumab, Todavir

2. Indications:

1. Breast cancer:

(1)Locally advanced or metastatic triple-negative breast cancer (mTNBC): Sacituzumab govitecan is indicated for the treatment of adult patients with unresectable locally advanced or metastatic triple-negative cancer who have received two or more prior systemic therapies, at least one of which was for metastatic disease.

(2) Unresectable locally advanced or metastatic hormone receptor (HR) positive, human epidermal growth factor receptor 2 (HER2) negative (IHC 0, IHC 1+ or IHC 2+/ISH–) Breast Cancer: Gosatuzumab is indicated for the treatment of adult patients with unresectable locally advanced or metastatic hormone receptor-positive, human epidermal growth factor receptor 2-negative breast cancer who have received endocrine-based therapy and at least two additional systemic therapies in the metastatic setting.

2. Urothelial carcinoma (mUC): Gosatuzumab is indicated for the treatment of adult patients with locally advanced or metastatic urothelial cancer who have previously received platinum-containing chemotherapy and programmed death receptor-1 (PD-1) or programmed death ligand-1 (PD-L1) inhibitors.

3. Usage and dosage:

1. Preoperative medication: Before patients take gosatuzumab each time, it is recommended to take preoperative medication to prevent infusion reactions and chemotherapy-induced nausea and vomiting (CINV). Patients with past infusion reactions can be treated medically with antipyretics, H1 and H2 blockers, and corticosteroids before infusion. Pretreat with a two- or three-drug combination regimen (eg, dexamethasone with a 5-HT3 receptor antagonist or an NK1 receptor antagonist, and other drugs as indicated).

2. Recommended dose: The recommended dose of gosatuzumab is 10 mg/kg, administered once a week as an intravenous infusion on days 1 and 8 of a 21-day treatment cycle. Continue treatment until disease progression or unacceptable toxicity. Do not give gosatuzumab to patients in doses greater than 10 mg/kg.

The patient’s first infusion time should exceed Observe patients for signs or symptoms of infusion-related reactions for 3 hours during the infusion and for at least 30 minutes after the initial dose; if tolerated by the previous infusion, infuse gosatuzumab within 1 to 2 hours. Observe the patient during the infusion and for at least30 minutes after the infusion.

Gosatuzumab is available as an intravenous infusion only. Do not give this product as an intravenous push or bolus injection.

4. Adverse reactions:

Across the four studies of gosatuzumab, the most common (≥25%) adverse reactions (including laboratory abnormalities) included decreased white blood cell count, decreased neutrophil count, decreased hemoglobin, diarrhea, nausea, decreased lymphocyte count, fatigue, alopecia, constipation, increased glucose, decreased albumin, vomiting, decreased appetite, decreased creatinine clearance, increased alkaline phosphatase, decreased magnesium, decreased potassium, and decreased sodium.

5. Storage:

Gosatuzumab is an injectable drug that is packaged in single-dose vials, which are usually stored in their original cartons in a refrigerator at 2°C to 8°C (36°F to 46°F) to protect them from light until reconstituted. Do not freeze. If not for immediate use, the infusion bag containing the gosatuzumab solution can be stored refrigerated in the dark at 2°C to 8°C (36°F to 46°F) for up to 24 hours. After refrigeration, inject dilute solution within 8 hours (including time of infusion) at room temperature to 25°C (77°F) without freezing or shaking.

6. Taboo:

1. Gosatuzumab is contraindicated in patients with severe allergic reactions to Sacituzumab Govitecan.

2. Do not use gosatuzumab to replace or be used together with other drugs containing irinotecan or its active metabolite SN-38.

7. Mechanism of action:

Gosatuzumab is aTrop-2-directed antibody-drug conjugate and a humanized antibody that recognizesTrop-2. The small molecule SN-38 is a topoisomerase I inhibitor covalently linked to the antibody through a linker. Pharmacological data indicate that gosatuzumab binds to cancer cells expressing Trop-2 and is internalized via hydrolysis of the linker with subsequent release of SN-38. SN-38 interacts with topoisomerase I and prevents the religation of topoisomerase I-induced single-strand breaks. The resulting DNA damage leads to apoptosis and cell death. Gosatuzumab reduces tumor growth in a triple-negative mouse xenograft model of cancer.

8. Special groups:

1. Women: Pregnant women taking Gosatuzumab can cause harm to the fetus , so it is recommended that women should not breastfeed during drug treatment and 1 month after the last dose; It is recommended that women of childbearing potential use effective contraceptive measures during drug treatment and within 6 months after the last dose.

2. Men: Due to potential genotoxicity, it is recommended that male patients with a female partner of reproductive potential use effective contraceptive measures during drug treatment and for 3 months after the last dose.

Gosatuzumab The original drug has been launched in China, but it has not yet been included in the medical insurance. The price of a 100mg bottle may be around 10,000 yuan, which is relatively expensive. Gosatuzumab Original drug marketed overseas has three versions: European version, American version, and Singapore version. SpecificationsThe price of each 100 mg bottle may be around RMB 10,000-35,000 (the price may fluctuate due to exchange rates). The ingredients of gosatuzumab sold domestically and abroad are basically the same. There is currently no generic version of gosatuzumab available on the market. For specific prices and drug information, please consult your medical consultant.