Sacituzumab Govitecan

What it is and how it works

Mechanism of Action Sacituzumab govitecan-hziy is a Trop-2-directed antibody-drug conjugate. Sacituzumab is a humanized antibody that recognizes Trop-2. The small molecule, SN-38, is a topoisomerase I inhibitor, which is covalently attached to the antibody by a linker. Pharmacology data suggest that sacituzumab govitecan-hziy binds to Trop-2-expressing cancer cells and is internalized with the subsequent release of SN-38 via hydrolysis of the linker. SN-38 interacts with topoisomerase I and prevents re-ligation of topoisomerase I-induced single strand breaks. The resulting DNA damage leads to apoptosis and cell death.

Indications

is a Trop-2-directed antibody and topoisomerase inhibitor conjugate indicated: Locally Advanced or Metastatic Triple-Negative Breast Cancer First Line As a single agent for the first-line treatment of adult patients with unresectable locally advanced or metastatic triple negative breast cancer (TNBC) who are not candidates for PD-1 or PD-L1 inhibitor-based therapy. ( 1.1 , 14.1 ) In combination with pembrolizumab or pembrolizumab and berahyaluronidase alfa-pmph for the first-line treatment of adult patients with unresectable locally advanced or metastatic TNBC whose tumors express PD-L1 (CPS ≥ 10) as determined by an FDA-authorized test. ( 1.1 , 14.1 ) Second Line or Later For the treatment of adult patients with unresectable locally advanced or mTNBC who have received two or more prior systemic therapies, at least one of them for metastatic disease.

Dosage and administration (summary)

Do NOT substitute TRODELVY for or use with other drugs containing irinotecan or its active metabolite SN-38. Premedication for prevention of infusion reactions and of chemotherapy-induced nausea and vomiting is recommended. The recommended dosage as a single agent or in combination with pembrolizumab is 10 mg/kg on Days 1 and 8 of 21-day cycles until disease progression or unacceptable toxicity. Monitor patients during the infusion and for at least 30 minutes after completion of infusion. Treatment interruption and/or dose reduction may be needed to manage adverse reactions. ( 2.4 , 2.5 ) See Full Prescribing Information for preparation and administration instructions.

Contraindications

is contraindicated in patients who have experienced a severe hypersensitivity reaction to TRODELVY . Severe hypersensitivity reaction to TRODELVY. ( 4 , 5.3 )

Warnings and precautions

Hypersensitivity and Infusion-Related Reactions : Hypersensitivity reactions including severe anaphylactic reactions have been observed. Monitor patients for infusion-related reactions. Permanently discontinue TRODELVY if severe or life-threatening reactions occur. Nausea/Vomiting : Use antiemetic preventive treatment and withhold TRODELVY for patients with Grade 3 nausea or Grade 3-4 vomiting at the time of scheduled treatment.

Pregnancy

Pregnancy Risk Summary Based on its mechanism of action, TRODELVY can cause teratogenicity and/or embryo-fetal lethality when administered to a pregnant woman. There are no available data in pregnant women to inform the drug-associated risk. TRODELVY contains a genotoxic component, SN-38, and is toxic to rapidly dividing cells .

Storage and supply

Store vials in a refrigerator at 2°C to 8°C (36°F to 46°F) in the original carton to protect from light until time of reconstitution. Do not freeze. TRODELVY is a hazardous drug. Follow applicable special handling and disposal procedures 1 .

Source: Sacituzumab Govitecan (Trodelvy) — US FDA prescribing information, 2026-06-24, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.