Sacituzumab govitecan

Pronunciation: SAK-i-TOOZ-ue-mab-GOE-vi-TEE-kan
Generic name: sacituzumab govitecan hziy
Brand name: Trodelvy
Dosage form: injection for intravenous infusion
Drug class: Miscellaneous antineoplastics

Medically reviewed by Carmen Pope, BPharm. Last updated on Oct 30, 2024.

What is Sacituzumab govitecan?

Sacituzumab govitecan (Trodelvy) is a targeted anticancer treatment that may be used to treat adults with the following cancers that have spread (metastasized) or cannot be removed by surgery:

• triple-negative breast cancer (negative for estrogen and progesterone hormone receptors and HER2 [TNBC]) who have received at least 2 prior treatments, including at least one for metastatic disease.
• hormone receptor-positive and human epidermal growth factor receptor 2-negative (HR+/HER2-) breast cancer who have previously received endocrine therapy and at least 2 additional treatments for metastatic disease
• bladder cancer and cancers of the urinary tract who have received a platinum-containing chemotherapy medicine and an immunotherapy medicine.

Trodelvy approval for bladder cancer was granted as an accelerated approval based on Phase 2, single-arm TROPHY-U-01 study. Continued FDA approval for MUC depended on confirmatory clinical trials showing a benefit. However, the confirmatory TROPiCS-04 study did not meet the primary endpoint of overall survival (OS) in the intention-to-treat (ITT) population. Therefore, Gilead plans to voluntarily withdraw the accelerated approval for Trodelvy in metastatic urothelial cancer. This decision does not affect the other approved Trodelvy indications.

Sacituzumab govitecan is a targeted antibody-drug conjugate (ADC) designed to deliver anticancer medicine directly into cells with Trop-2 proteins. Research has found certain types of cancer cells contain more Trop-2 protein than noncancerous cells.

Sacituzumab govitecan (sacituzumab govitecan-hziy) contains 3 different substances:

• sacituzumab, an antibody that looks for Trop-2
• an anticancer molecule, SN-38, which is a topoisomerase I inhibitor and the active metabolite of irinotecan
• and a linker that joins sacituzumab to SN-38.

Sacituzumab govitecan works by binding to Trop-2-expressing cancer cells. It is then taken up by the cell and the linker is hydrolyzed (broken apart) releasing SN-38 directly into the cell. SN-38 interacts with the enzyme topoisomerase I, causing single-strand breaks and DNA damage, leading to cell death and decreased tumor growth.

For metastatic HR+/HER2- breast cancer in men and women who had previously received endocrine-based therapy and at least two additional systemic therapies in the metastatic setting, sacituzumab govitecan is now recommended by the National Comprehensive Cancer Network (NCCN) as Category 1 or preferred treatment.

• An overall survival benefit of 3.2 months was reported with sacituzumab govitecan compared with single-agent chemotherapy (median OS: 14.4 months vs. 11.2 months; hazard ratio [HR]=0.79; 95% CI: 0.65-0.96; p=0.02).
• There was a 34% reduced risk of disease progression or death median PFS: 5.5 versus 4.0 months; HR: 0.66; 95% CI: 0.53-0.83; p=0.0003).
• 21% of those treated with sacituzumab govitecan versus 7% treated with single-agent chemotherapy were progression-free at one year.

Sacituzumab govitecan was first FDA approved on April 22, 2020, as the brand Trodelvy under the accelerated approval designation for relapsed or refractory metastatic TNBC, and gained full approval for this indication on April 7, 2021. It was granted accelerated approval for metastatic urothelial cancer on April 13, 2021 (continued approval may be dependent on clinical trials showing a benefit) and full approval for metastatic HR+/HER2- breast cancer on February 3, 2023. There is no Trodelvy generic available.

Sacituzumab govitecan side effects

The most common side effects of sacituzumab govitecan affecting 25% or more patients include:

• decreased white blood cell (leukocyte and lymphocyte) and red blood cell count
• feeling tired or weak
• hair loss (alopecia)
• constipation
• increased sugar levels in the blood
• decreased protein levels (albumin) in the blood
• decreased appetite
• changes in kidney function test
• increased levels of an enzyme called alkaline phosphatase in the blood (test for liver or bone problems)
• decreased levels of magnesium, potassium, and sodium in the blood.

These are not all of the possible side effects of sacituzumab govitecan. Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Warnings

Sacituzumab govitecan can cause serious side effects, including low white blood cell counts, severe diarrhea, and allergic or infusion-related reactions.

• Sacituzumab govitecan carries a black box warning for severe or life-threatening neutropenia and diarrhea.
• Patients with reduced UGT1A1 activity are at increased risk of side effects of sacituzumab govitecan such as low blood cell counts such as neutropenia (low levels of neutrophils – a type of white blood cell), febrile neutropenia, and anemia (low levels red blood cells).

Low white blood cell count (neutropenia), which may be severe and lead to infections that can be life-threatening or cause death. Your healthcare provider will monitor your blood cell counts during treatment. Call your healthcare provider right away if you develop any of the following signs of infection during treatment with sacituzumab govitecan:

• fever
• chills
• cough
• shortness of breath
• burning or pain when you urinate.

Diarrhea, which may be severe. Your healthcare provider should monitor you for diarrhea and give you medicine as needed to help control your diarrhea. If you lose too much body fluids (dehydration) your healthcare provider may need to give you fluids and electrolytes to replace body salts. Call your healthcare provider right away:

• the first time that you get diarrhea during treatment with sacituzumab govitecan
• if you have black or bloody stools
• if you have symptoms of losing too much body fluid (dehydration) and body salts, such as light-headedness, dizziness, or faintness
• if you are unable to take fluids by mouth due to nausea or vomiting
• if you are not able to get your diarrhea under control within 24 hours.

Allergic and infusion-related reactions, including anaphylaxis. Tell your healthcare provider or nurse right away if you get any of the following symptoms of an allergic or infusion-related reaction during your infusion or within 24 hours after you receive a dose of sacituzumab govitecan including:

• • swelling of your face, lips, tongue, or throat
  • hives
  • skin rash, itching, or flushing of your skin
  • fever
  • difficulty breathing or wheezing
  • lightheadedness, dizziness, feeling faint, or pass out
  • chills or shaking chills (rigors).

Nausea and vomiting which may be severe. Before each dose, you will receive medicines to help prevent nausea and vomiting. You should take them as instructed. Call your healthcare provider right away if you have nausea or vomiting that is not controlled by the medicines prescribed for you. 

Can cause fetal harm. Women of childbearing potential should use adequate contraception during treatment.

It is not known if sacituzumab govitecan is safe and effective in people with moderate or severe liver problems or in children.

Before taking

Do not receive sacituzumab govitecan if you have had a severe allergic reaction to sacituzumab govitecan, Trodelvy, or any inactive ingredients in the injection.

Before receiving sacituzumab govitecan, tell your healthcare provider about all of your medical conditions, including if you:

• have been told that you carry a gene for uridine diphosphate-glucuronosyl transferase 1A1 (UGT1A1)*28. People who carry this gene have an increased risk of getting side effects.
• have liver problems.
• are pregnant or plan to become pregnant
• are breastfeeding or plan to breastfeed.

Pregnancy

Sacituzumab govitecan can harm your unborn baby. Your healthcare provider should check to see if you are pregnant before you start receiving it. Females who can become pregnant should use effective birth control during treatment and for 6 months after their last dose. Talk to your healthcare provider about birth control choices that may be right for you during this time. Tell your healthcare provider right away if you become pregnant during treatment with sacituzumab govitecan.

Sacituzumab govitecan may cause fertility problems in females, which could affect your ability to have a baby. Talk to your healthcare provider if fertility is a concern for you.

Males with a female partner who can become pregnant should use effective birth control during treatment and for 3 months after their last dose of sacituzumab govitecan.

Tell your healthcare provider right away if you or your partner become pregnant during treatment with sacituzumab govitecan.

Breastfeeding

It is not known if sacituzumab govitecan passes into your breastmilk and can harm your baby. Do not breastfeed during treatment and for 1 month after your last dose.

How is sacituzumab govitecan administered?

Your healthcare provider will give you sacituzumab govitecan into your vein through an intravenous (IV) line, as an infusion initially over 3 hours. If you tolerate the first dose well, future doses may be given over 1 to 2 hours.

• Sacituzumab govitecan (Trodelvy) is given 1 time each week, on Day 1 and Day 8 of a 21-day treatment cycle.
• Before each dose, you will receive medicines to help prevent infusion reactions and nausea and vomiting.
• You will be monitored for side effects during and for at least 30 minutes after you receive each infusion of this medication.
• Your healthcare provider may slow down or temporarily stop your infusion if you have an infusion-related reaction, or permanently stop this medication if you have a life-threatening infusion-related reaction.

Your healthcare provider will decide how long you will continue to receive sacituzumab govitecan.

Dosing information

The recommended dose of sacituzumab govitecan is 10 mg/kg once weekly on Days 1 and 8 of continuous 21-day treatment cycles.

See the Full Prescribing information for further details about sacituzumab govitecan dosing.

Related/similar drugs

Verzenio, Arimidex, Femara, Xeloda, Ibrance, Herceptin

What happens if I miss a dose?

If you miss or forget an appointment for sacituzumab govitecan, call your doctor or infusion center immediately to reschedule your infusion. It is important not to miss a planned appointment. Do not skip an appointment.

What other drugs affect sacituzumab govitecan?

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Certain medicines may affect the way sacituzumab govitecan works.

• Concomitant administration of UGT1A1 inhibitors such as flunitrazepam or propofol may increase the incidence of side effects due to a potential increase in systemic exposure to SN-38. Avoid co-administration.
• Exposure to SN-38 may be reduced in patients concomitantly receiving UGT1A1 Inducers such as phenytoin and phenobarbital. Avoid co-administration.

See the prescribing information for a full list of interactions.

Storage

Store vials in a refrigerator at 2°C to 8°C (36°F to 46°F) in the original carton to protect them from light until the time of reconstitution. Do not freeze.

Sacituzumab govitecan is a hazardous drug. Follow applicable special handling and disposal procedures.

Trodelvy ingredients

Active ingredient: sacituzumab govitecan-hziy

Inactive ingredients: 2-(N-morpholino) ethane sulfonic acid (MES), polysorbate 80, and trehalose dihydrate

Manufacturer

Trodelvy: Gilead Sciences, Inc.

Sacituzumab govitecan Biosimilars

Biosimilar and interchangeable products are biological products that are highly similar to and have no clinically meaningful differences from the reference product.

Reference products

These are biological products that have already been approved by the FDA, against which biosimilar products are compared. There is 1 for sacituzumab govitecan.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Medical Disclaimer