Sacituzumab govitecan, marketed under the brand name Trodelvy, represents a significant advancement in the field of antibody–drug conjugates (ADCs) for oncology. By combining a targeted monoclonal antibody with a potent cytotoxic payload, this therapy has expanded treatment possibilities in certain hard-to-treat cancers. Over recent years, evolving clinical evidence has continued to refine its role in modern cancer care, offering new insights into patient selection, safety considerations, and optimal sequencing within treatment regimens.
This article will explore Trodelvy’s current and emerging uses in cancer, its safety profile, recommended dosages, and what healthcare professionals can expect in clinical practice moving forward.
Which company produced Sacituzumab govitecan?
Sacituzumab govitecan, marketed as Trodelvy, was originally developed by Immunomedics, Inc., a U.S.-based biotechnology company specializing in antibody–drug conjugates (ADCs) for cancer treatment. Immunomedics focused on pairing targeted monoclonal antibodies with potent cytotoxic agents to create therapies capable of delivering chemotherapy directly to cancer cells, and Trodelvy became its flagship product.
In October 2020, Gilead Sciences acquired Immunomedics in a landmark $21 billion deal, gaining full ownership of Trodelvy and the supporting ADC technology platform. This acquisition marked Gilead’s significant expansion into oncology, adding a high-impact therapy to its portfolio and enabling further development of the drug for multiple cancer indications. Before the acquisition, Immunomedics had entered a strategic partnership with Everest Medicines in 2019 to develop, register, and commercialize Trodelvy across Greater China, South Korea, and parts of Southeast Asia. In 2022, Gilead consolidated global control by acquiring the remaining regional rights from Everest Medicines.
Gilead has also pursued research collaborations to broaden Trodelvy’s potential. One notable example is its clinical trial partnership with Merck, evaluating Trodelvy in combination with the PD-1 inhibitor pembrolizumab (Keytruda®) for first-line treatment of metastatic triple-negative breast cancer. These collaborations, coupled with Gilead’s global infrastructure, have helped accelerate the drug’s availability and exploration in new therapeutic areas.
How does Sacituzumab govitecan work?
Sacituzumab govitecan is an antibody–drug conjugate (ADC) that combines targeted delivery with a potent cytotoxic payload, offering a more precise approach to chemotherapy. Its mechanism of action centers on the protein Trop-2 (trophoblast cell-surface antigen 2), which is overexpressed in many epithelial cancers and associated with aggressive tumor behavior.
The antibody component of sacituzumab govitecan is engineered to recognize and bind selectively to Trop-2 on the surface of cancer cells. Once bound, the drug–antigen complex is internalized into the cell, where an enzymatically cleavable linker releases SN-38, the active metabolite of irinotecan. SN-38 is a potent topoisomerase I inhibitor, disrupting DNA replication and repair processes, ultimately inducing apoptosis.
A notable feature of sacituzumab govitecan’s design is that its linker allows for release of SN-38 not only within the targeted cell but also into the surrounding tumor microenvironment. This generates a bystander effect, enabling the cytotoxic agent to kill neighboring tumor cells that may not express high levels of Trop-2, thereby broadening the drug’s therapeutic reach.
By directly delivering a high concentration of chemotherapy to Trop-2–expressing tumor cells while limiting systemic exposure, sacituzumab govitecan aims to enhance efficacy and improve tolerability compared with conventional chemotherapy regimens.
What cancers does Sacituzumab govitecan approved to treat?
Sacituzumab govitecan (Trodelvy) has gained FDA approvals that reflect its growing role in treating difficult cancers, particularly breast and urothelial cancers. Its targeted approach to Trop-2–expressing tumors has led to expanded indications over the past few years, offering new options for patients with limited treatments available.
Key FDA approvals include:
- Metastatic triple-negative breast cancer (TNBC):
Approved initially in April 2020 (accelerated) and fully approved in April 2021 for adults with unresectable locally advanced or metastatic TNBC after at least two prior therapies. - Locally advanced or metastatic urothelial carcinoma:
Received accelerated approval in April 2021 for patients who had prior platinum-based chemotherapy and PD-1/PD-L1 immunotherapy. - Hormone receptor–positive, HER2-negative (HR+/HER2–) breast cancer:
Approved in February 2023 for adults with unresectable locally advanced or metastatic disease who have received endocrine-based therapy plus two or more systemic treatments.
Learn more about Breast Cancer: Symptoms Causes, Stages, Diagnosis and Treatment on OncoDaily.
What research is behind the approval?
FDA approvals of sacituzumab govitecan (Trodelvy) are supported by pivotal clinical trials across multiple cancer types. In metastatic triple-negative breast cancer, the Phase 3 ASCENT trial demonstrated significant improvements in progression-free and overall survival among patients previously treated with chemotherapy. For metastatic urothelial carcinoma, the Phase II TROPHY-U-01 trial showed meaningful tumor responses with a manageable safety profile. In HR-positive, HER2-negative breast cancer, the Phase 3 TROPiCS-02 trial confirmed superior survival outcomes compared with standard chemotherapy. The following sections provide a detailed review of each indication.
Trodelvy for TNBC
The approval for sacituzumab govitecan (Trodelvy) in metastatic triple-negative breast cancer was based on the Phase 3 ASCENT trial, which demonstrated significant improvements in both progression-free survival and overall survival. This randomized study enrolled 529 patients with unresectable locally advanced or metastatic disease who had received at least two prior chemotherapies.
Patients treated with sacituzumab govitecan experienced a median progression-free survival of 4.8 months compared to 1.7 months for those receiving chemotherapy, and median overall survival was extended to 11.8 months versus 6.9 months. The treatment was generally well tolerated, with common side effects including nausea, neutropenia, diarrhea, fatigue, and alopecia. Sacituzumab govitecan is administered at 10 mg/kg intravenously on days 1 and 8 of a 21-day cycle until disease progression or unacceptable toxicity.
Find full information on FDA.
Trodelvy for urothelial carcinoma
The approval for sacituzumab govitecan (Trodelvy) in metastatic urothelial carcinoma (mUC) was based on the results of the Phase II TROPHY-U-01 trial, which were published in the Journal of Clinical Oncology in 2021. This open-label, multicohort study enrolled 113 patients with locally advanced or metastatic urothelial cancer who had progressed after prior platinum-based chemotherapy and checkpoint inhibitor therapy.
Patients received sacituzumab govitecan at 10 mg/kg on days 1 and 8 of 21-day cycles. The trial showed an objective response rate (ORR) of 27%, with 77% of patients experiencing a reduction in measurable tumor size. The median duration of response was 7.2 months, while median progression-free survival (PFS) and overall survival (OS) were 5.4 months and 10.9 months, respectively.
Key grade 3 or higher adverse events included neutropenia (35%), leukopenia (18%), anemia (14%), diarrhea (10%), and febrile neutropenia (10%). Treatment discontinuation due to adverse events was low at 6%. The study demonstrated sacituzumab govitecan’s meaningful activity and manageable safety profile in a heavily pretreated population, supporting its accelerated FDA approval in this setting.
Trodelvy for Hormone receptor–positive, HER2-negative breast cancer
For adults with unresectable locally advanced or metastatic HR-positive, HER2-negative breast cancer, FDA approval of sacituzumab govitecan-hziy (Trodelvy, Gilead Sciences) was based on the TROPiCS-02 trial. This study enrolled 543 patients whose disease had progressed after endocrine therapy, a CDK4/6 inhibitor, and a taxane. Participants received either sacituzumab govitecan-hziy at 10 mg/kg intravenously on Days 1 and 8 of a 21-day cycle or single-agent chemotherapy chosen by the investigator, continuing treatment until disease progression or unacceptable toxicity.
Sacituzumab govitecan-hziy significantly improved median progression-free survival to 5.5 months compared with 4 months for chemotherapy and extended overall survival to 14.4 months versus 11.2 months. The most common side effects included low blood counts, diarrhea, fatigue, nausea, hair loss, and elevated blood glucose.
The approved dose is 10 mg/kg IV on Days 1 and 8 of a 21-day cycle until disease progression or unacceptable toxicity. This approval was reviewed through the FDA’s Project Orbis in collaboration with international regulatory partners.
Read more about approval on FDA Official Website.
Sacituzumab govitecan side effects and its management
While Sacituzumab govitecan targets cancer cells more precisely, it still carries a notable side-effect profile due to its cytotoxic payload. The most prominent adverse effects involve myelosuppression (especially neutropenia), gastrointestinal issues (notably diarrhea), fatigue, and nausea. These can often be anticipated, monitored, and managed proactively with supportive interventions and dose modifications.
Common Side Effects
The most frequent adverse effects of sacituzumab govitecan involve the blood and gastrointestinal system. Neutropenia is among the most significant, with many patients developing low levels of white blood cells, increasing the risk of infection. Anemia is also observed and may cause fatigue, weakness, or dizziness. Infections of the respiratory or urinary tract can arise as a consequence of immune suppression.
Gastrointestinal complaints are also common. Many patients experience diarrhea, nausea, vomiting, or abdominal discomfort during treatment. These symptoms can significantly affect quality of life if not controlled promptly. Fatigue, rash, decreased appetite, and changes in blood chemistry such as low phosphate levels or electrolyte disturbances are also frequently reported. While these side effects are common, most can be effectively managed with proactive monitoring and supportive measures, allowing treatment to continue safely.
Less Common Side Effects
Less frequent but potentially serious side effects may occur in a subset of patients. Febrile neutropenia, which is neutropenia accompanied by fever, can lead to hospitalization and requires urgent medical attention. Some patients experience dehydration, low sodium, potassium, or magnesium levels, or elevated liver enzymes. Rarely, mucositis, headache, constipation, and pain in the extremities may develop.
Although these reactions occur less often than the common toxicities, they can be clinically significant. Monitoring laboratory values and patient symptoms throughout therapy is critical in order to identify complications early and intervene before they progress.
Management of Side Effects
Blood counts are monitored regularly, and drugs like granulocyte–colony stimulating factors can be used to prevent or treat neutropenia. Diarrhea is managed quickly with anti-diarrheal agents and hydration, while nausea and vomiting are controlled with preventive antiemetics. Infusion reactions are treated by pausing the infusion and giving antihistamines or steroids. Electrolyte abnormalities are corrected with supplementation, and supportive measures such as wigs or cooling caps can help with hair loss.
Dose reductions or short treatment breaks are sometimes necessary to allow recovery, but most patients can continue therapy safely with these adjustments.
What is the Recommended Dosage of Sacituzumab govitecan?
Sacituzumab govitecan is supplied as a 180 mg vial of lyophilized powder for intravenous infusion after reconstitution.
For triple-negative breast cancer (mTNBC), it is approved in adults with unresectable locally advanced or metastatic disease who have already received at least two prior systemic therapies, including one for metastatic disease. Treatment is given at a dose of 10 mg/kg on days 1 and 8 of a 21-day cycle, continued until disease progression or unacceptable side effects.
Patients receive premedication with antipyretics, H1 and H2 blockers, and antiemetics, often in a two- or three-drug combination such as dexamethasone plus a serotonin or NK1 receptor antagonist. Corticosteroids may be added for those with a history of infusion reactions. Because neutropenia is a known risk, primary prophylaxis with G-CSF is recommended in high-risk patients beginning with the first cycle.
For hormone receptor–positive, HER2-negative breast cancer, the same dosing schedule and premedication regimen apply. The indication is for adults with unresectable locally advanced or metastatic disease who have received endocrine therapy and at least two additional systemic treatments.
Previously, sacituzumab govitecan carried an indication for urothelial cancer, but this was withdrawn by the FDA in November 2024 after the phase 3 TROPiCS-04 trial failed to show an overall survival benefit.
Learn more about Bladder Cancer: Symptoms ,Causes, Stages, Diagnosis and Treatment on OncoDaily.
How is Sacituzumab govitecan administered?
Sacituzumab govitecan is prepared and given as an intravenous infusion. It is compatible only with 0.9% sodium chloride and should not be mixed with other infusion solutions or drugs.
The drug is supplied as a cytotoxic powder that must be reconstituted with saline to a concentration of 10 mg/mL. The vial is gently swirled until dissolved, inspected to ensure the solution is clear and yellow, and then diluted in a saline infusion bag to achieve the required dose. Any unused portion must be discarded.
Infusion is given over three hours for the first dose and may be shortened to one to two hours in later cycles if well tolerated. It should never be administered as an IV push or bolus. The infusion bag is kept protected from light, and the line is flushed with saline after completion. Patients are monitored during treatment and for at least 30 minutes afterward for signs of infusion-related reactions.
Unopened vials should be refrigerated at 2–8°C and protected from light. Once diluted, the solution should ideally be used immediately but can be refrigerated for up to 24 hours and then administered within eight hours at room temperature. Freezing and shaking must be avoided at all stages of preparation and storage.
Sacituzumab govitecan effectiveness over time
In June 2025, ESMO Open published new real-world data on sacituzumab govitecan (SG) in patients with metastatic triple-negative breast cancer (mTNBC) in the United States. The study evaluated 381 patients who had received at least two prior therapies. Median overall survival reached 11.3 months, and the median time to next treatment or death was 5.6 months, outcomes closely aligned with the pivotal ASCENT trial and other real-world evidence.
Neutropenia was among the most common side effects, occurring as grade 2 in 25% of patients and grade 3/4 in 27%. Prophylactic use of granulocyte colony-stimulating factor (G-CSF) significantly reduced these events, confirming its role in supportive care.
These findings confirm the effectiveness of sacituzumab govitecan in clinical practice and underscore that neutropenia, a key safety concern, can be successfully managed with G-CSF.
Read more about New Paper Alert: Managing Key Adverse Events of Sacituzumab Govitecan in Breast Cancer on OncoDaily.
Complementing these data, a recent review in The Oncologist by Tolaney et al. highlighted that adverse events with SG—particularly neutropenia, diarrhea, fatigue, and alopecia—are common but predictable and manageable. Early monitoring, patient education, and proactive use of supportive measures help preserve both treatment continuity and quality of life.
Together, these results emphasize that with proper management, sacituzumab govitecan delivers sustained clinical benefit and remains a cornerstone therapy for patients with advanced TNBC and HR+/HER2– breast cancer.
Ongoing trials with Sacituzumab govitecan
Sacituzumab govitecan is being investigated for advanced esophageal squamous cell carcinoma (ESCC) in a Phase II clinical trial (NCT06329869) led by the National Taiwan University Hospital. The study aims to evaluate the safety and effectiveness of the drug in patients whose tumors overexpress Trop-2, a protein found at higher levels in ESCC compared with esophageal dysplasia. By targeting Trop-2, sacituzumab govitecan is hypothesized to provide meaningful clinical benefit in this patient population.
Sacituzumab govitecan (IMMU-132) is being studied in a Phase II trial (NCT06028932) at Yale University for patients with recurrent or persistent platinum-resistant ovarian, fallopian tube, or primary peritoneal cancers. This open-label study aims to evaluate the clinical activity of the drug in this difficult-to-treat population by targeting Trop-2 with its antibody–drug conjugate mechanism.