Trodelvy
Sacituzumab Govitecan · Powder, For Solution · Intravenous
Uses
1 INDICATIONS AND USAGE TRODELVY 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. ( 1.1 , 14.1 ) Locally Advanced or Metastatic HR-Positive, HER2-Negative Breast Cancer For the treatment of adult patients with 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 who have received endocrine-based therapy and at least two additional systemic therapies in the metastatic setting. ( 1.1 , 14.2 ) 1.1 Locally Advanced or Metastatic Triple-Negative Breast Cancer First Line TRODELVY as a single agent is indicated 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. TRODELVY, in combination with pembrolizumab or pembrolizumab and berahyaluronidase alfa-pmph, is indicated for the first-line treatment of adult patients with unresectable locally advanced or metastatic TNBC whose tumors express PD-L1 [Combined Positive Score (CPS ≥ 10)] as determined by an FDA-authorized test [see Dosage and Administration (2.1) ] . Second Line or Later TRODELVY is indicated for the treatment of adult patients with unresectable locally advanced or metastatic TNBC who have received two or more prior systemic therapies, at least one of them for metastatic disease. 1.2 Locally Advanced or Metastatic HR-positive, HER2-negative Breast Cancer TRODELVY is indicated for the treatment of adult patients with 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 who have received endocrine-based therapy and at least two additional systemic therapies in the metastatic setting.
Dosage and administration
Do NOT substitute TRODELVY for or use with other drugs containing irinotecan or its active metabolite SN-38. ( 2 ) Premedication for prevention of infusion reactions and of chemotherapy-induced nausea and vomiting is recommended. ( 2.1 ) 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. ( 2.3 ) 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. ( 2.4 ) 2.1 Important Use Information and Premedication Do NOT substitute TRODELVY for or use with other drugs containing irinotecan or its active metabolite SN-38. Premedication Prior to each dose of TRODELVY, premedication for prevention of infusion reactions and of chemotherapy-induced nausea and vomiting (CINV) is recommended. Premedicate with antipyretics, H1 and H2 blockers prior to infusion, and corticosteroids may be used for patients who had prior infusion reactions. Premedicate with a 2 or 3 drug combination regimen (e.g., dexamethasone with either a 5-HT3 receptor antagonist or an NK 1 receptor antagonist, as well as other drugs as indicated). Prophylaxis for Neutropenia Primary prophylaxis with granulocyte colony-stimulating factor (G-CSF) is recommended starting in the first cycle for all patients at increased risk of febrile neutropenia [see Warnings and Precautions (5.1) ] . 2.2 Patient Selection for Combination Therapy Select patients for treatment of unresectable locally advanced or metastatic TNBC with TRODELVY in combination with pembrolizumab or pembrolizumab and berahyaluronidase alfa-pmph, based on the tumor expression of PD-L1 as confirmed by an FDA-authorized test [see Clinical Studies (14.1) ] . Information on FDA-authorized tests is available at http://www.fda.gov/companiondiagnostics . 2.3 Recommended Dosage The recommended dosage of TRODELVY as a single agent or in combination with pembrolizumab is 10 mg/kg administered as an intravenous infusion on Days 1 and 8 of each 21-day cycle. Continue TRODELVY until disease progression or unacceptable toxicity. Do not administer TRODELVY at doses greater than 10 mg/kg. When TRODELVY is administered in combination with pembrolizumab or pembrolizumab and berahyaluronidase alfa-pmph, discontinue pembrolizumab or pembrolizumab and berahyaluronidase alfa-pmph, after approximately 24 months. Refer to the Prescribing Information for pembrolizumab or pembrolizumab and berahyaluronidase alfa-pmph for the recommended dosing information. 2.4 Dosage Modifications for Adverse Reactions Management of adverse reactions may require temporary interruption, dose reduction, or permanent discontinuation of TRODELVY as described in Tables 1 and 2. Do not re-escalate the TRODELVY dose after a dose reduction for adverse reactions has been made. Table 1: Dosage Reduction Levels Dose Reduction Permanently discontinue TRODELVY in patients unable to tolerate 5 mg/kg. Dosage and Schedule First Reduce to 7.5 mg/kg Second Reduce to 5 mg/kg The recommended dosage modifications for adverse reactions are provided in Table 2. Table 2: Dosage Modifications for Adverse Reactions Adverse reactions Severity Dose Modification Neutropenia [see Warnings and Precautions (5.1) ] Grade 3-4 neutropenia (Absolute Neutrophil Count [ANC] <1,000/mm 3 ) or febrile neutropenia Withhold TRODELVY until ANC ≥1500/mm 3 for Day 1 dose or ANC ≥1000/mm 3 for Day 8 Dose Administer G-CSF during treatment as clinically indicated. Reduce one dose level for each occurrence of febrile neutropenia or prolonged Grade 3-4 neutropenia, or permanently discontinue according to Table 1. Nausea/Vomiting/ Diarrhea [see Warnings and Precautions (5.2 , 5.4) ] Grade 3-4 nausea, vomiting or diarrhea that is not controlled with antiemetics or anti-diarrheal agents Withhold TRODELVY until resolved to ≤ Grade 1 Reduce one dose level with each occurrence, or permanently discontinue according to Table 1. Infusion-Related Reaction [see Warnings and Precautions (5.3) ] Grade 1-3 infusion-related reactions Slow infusion rate or interrupt the infusion Grade 4 infusion-related reactions Permanently discontinue TRODELVY. Other Toxicities Other Grade 3-4 toxicities of any duration despite optimal medical management Withhold TRODELVY until resolved to ≤ Grade 1 Reduce one dose level with each occurrence or permanently discontinue according to Table 1. Dosage Modifications for Adverse Reactions for TRODELVY in Combination with Pembrolizumab or Pembrolizumab and berahyaluronidase alfa-pmph Interrupt or discontinue one or both drugs of the combination or reduce the dose of TRODELVY to manage adverse reactions as appropriate. Refer to the prescribing information for pembrolizumab or pembrolizumab and berahyaluronidase alfa-pmph for recommendations on dosage interruption or discontinuation due to adverse reactions. For TRODELVY dosage modifications, refer to Table 1 and Table 2. 2.5 Preparation and Administration Reconstitution TRODELVY is a hazardous drug. Follow applicable special handling and disposal procedures 1 . Calculate the required dose (mg) of TRODELVY based on the patient's current body weight [see Dosage and Administration (2.2) ] . Using a sterile syringe, slowly inject 20 mL of 0.9% Sodium Chloride Injection, USP, into each 180 mg TRODELVY vial. Each vial contains overfill to compensate for liquid loss during preparation and after reconstitution, the total resulting volume delivers a concentration of 10 mg/mL . Gently swirl vials and allow to dissolve for up to 15 minutes. Do not shake . Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
Dosage forms and strengths
For injection: 180 mg off-white to yellowish lyophilized powder in a single-dose vial. For injection: 180 mg lyophilized powder in single-dose vials for reconstitution. ( 3 )
Contraindications
4 CONTRAINDICATIONS TRODELVY is contraindicated in patients who have experienced a severe hypersensitivity reaction to TRODELVY [see Warnings and Precautions (5.3) ] . 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. ( 5.3 ) 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. ( 5.4 ) Patients with Reduced UGT1A1 Activity : Individuals who are homozygous for the UGT1A1*28 allele are at increased risk for neutropenia, febrile neutropenia, and anemia following initiation of TRODELVY. ( 5.5 ) Embryo-Fetal Toxicity : TRODELVY can cause fetal harm. Advise patients of potential risk to a fetus and to use effective contraception. ( 5.6 , 8.1 , 8.3 ) 5.1 Neutropenia TRODELVY can cause severe, life-threatening, or fatal neutropenia as early as the first cycle of treatment. Neutropenia occurred in 64% of patients treated with TRODELVY. Grade 3-4 neutropenia occurred in 48% of patients. Febrile neutropenia occurred in 6% of patients. The median time to first onset of neutropenia (including febrile neutropenia) was 19 days (range: 1 to 1022 days). Neutropenia occurred earlier in patients with reduced UGT1A1 activity [see Warnings and Precautions (5.5) ] . Neutropenic colitis occurred in 1.4% of patients. Primary prophylaxis with G-CSF is recommended starting in the first cycle of treatment in all patients at increased risk of febrile neutropenia, including older patients, patients with previous neutropenia, poor performance status, organ dysfunction, or multiple comorbidities [see Dosage and Administration (2.1) ] . Monitor absolute neutrophil count (ANC) during treatment. Withheld TRODELVY for ANC below 1500/mm 3 on Day 1 of any cycle or below 1000/mm 3 on Day 8 of any cycle. Withhold TRODELVY for neutropenic fever. Dose modifications may be required due to neutropenia. Treat neutropenia with G-CSF and administer prophylaxis in subsequent cycles as clinically indicated or indicated in Table 2 [see Dosage and Administration (2.4) ] . 5.2 Diarrhea TRODELVY can cause severe diarrhea. Diarrhea occurred in 62% of all patients treated with TRODELVY. Grade 3-4 diarrhea occurred in 10% of all patients treated with TRODELVY. One patient had intestinal perforation following diarrhea. Diarrhea that led to dehydration and subsequent acute kidney injury occurred in 0.6% of all patients. Withhold TRODELVY for Grade 3-4 diarrhea at the time of scheduled treatment administration and resume when resolved to ≤ Grade 1 [see Dosage and Administration (2.4) ]. At the onset of diarrhea, evaluate for infectious causes and if negative, promptly initiate loperamide, 4 mg initially followed by 2 mg with every episode of diarrhea for a maximum of 16 mg daily. Discontinue loperamide 12 hours after diarrhea resolves. Additional supportive measures (e.g., fluid and electrolyte replacement) may also be employed as clinically indicated. Patients who exhibit an excessive cholinergic response to treatment with TRODELVY (e.g., abdominal cramping, diarrhea, salivation, etc.) can receive appropriate premedication (e.g., atropine) for subsequent treatments. 5.3 Hypersensitivity and Infusion-Related Reactions TRODELVY can cause serious hypersensitivity reactions including life-threatening anaphylactic reactions. Severe signs and symptoms included cardiac arrest, hypotension, wheezing, angioedema, swelling, and skin reactions [see Contraindications (4) ] . Hypersensitivity reactions occurred in 28% of patients treated with TRODELVY with 13% occurring within 24 hours of dosage. Grade 3-4 hypersensitivity occurred in 1.5% of patients treated with TRODELVY with 0.4% of these occurring within 24 hours of dosage. The incidence of hypersensitivity reactions leading to permanent discontinuation of TRODELVY was 0.4%. The incidence of anaphylactic reaction was <0.1%. Premedication for infusion reactions in patients receiving TRODELVY is recommended . Have medications and emergency equipment to treat infusion-related reactions, including anaphylaxis, available for immediate use when administering TRODELVY [see Dosage and Administration (2.1) ]. Closely monitor patients for hypersensitivity and infusion-related reactions during each TRODELVY infusion and for at least 30 minutes after completion of each infusion [see Dosage and Administration (2.3) ] . Permanently discontinue TRODELVY for Grade 4 infusion-related reactions [see Dosage and Administration (2.4) ] . 5.4 Nausea and Vomiting TRODELVY is emetogenic and can cause severe nausea and vomiting. Nausea occurred in 63% of all patients treated with TRODELVY. Grade 3-4 nausea occurred in 3% of patients. Vomiting occurred in 33% of all patients treated with TRODELVY. Grade 3-4 vomiting occurred in 2% of these patients. Premedicate with a two or three drug combination regimen (e.g., dexamethasone with either a 5-HT3 receptor antagonist or an NK 1 receptor antagonist as well as other drugs as indicated) for prevention of chemotherapy-induced nausea and vomiting (CINV) [ see Dosage and Administration (2.1) ]. Withhold TRODELVY doses for Grade 3 nausea or Grade 3-4 vomiting at the time of scheduled treatment administration and resume with additional supportive measures when resolved to ≤Grade 1 [see Dosage and Administration (2.4) ]. Additional antiemetics and other supportive measures may also be employed as clinically indicated. All patients should be given take-home medications with clear instructions for prevention and treatment of nausea and vomiting. 5.5 Increased Risk of Adverse Reactions in Patients with Reduced UGT1A1 Activity Patients homozygous for the uridine diphosphate-glucuronosyl transferase 1A1 (UGT1A1)*28 allele are at increased risk for neutropenia, febrile neutropenia, and anemia; and may be at increased risk for other adverse reactions when treated with TRODELVY.
Side effects
The following adverse reactions are discussed in greater detail in other sections of the label: Neutropenia [see Warnings and Precautions (5.1) ] Diarrhea [see Warnings and Precautions (5.2) ] Hypersensitivity and Infusion-Related Reactions [see Warnings and Precautions (5.3) ] Nausea and Vomiting [see Warnings and Precautions (5.4) ] The most common adverse reactions including laboratory abnormalities: TRODELVY as a single agent (incidence ≥ 25%) were decreased leukocyte count, decreased neutrophil count, decreased hemoglobin, nausea, diarrhea, decreased lymphocyte count, fatigue, alopecia, increased glucose, constipation, vomiting, decreased albumin, increased alkaline phosphatase, decreased appetite, abdominal pain, decreased creatinine clearance, decreased magnesium, and decreased potassium. ( 6.1 ) TRODELVY in combination with pembrolizumab (incidence ≥25%) were decreased neutrophil count, decreased hemoglobin, decreased leukocyte count, diarrhea, nausea, decreased lymphocyte count, fatigue, alopecia, increased alkaline phosphatase, increased glucose, increased alanine aminotransferase, constipation, increased aspartate aminotransferase, rash, decreased potassium, increased lactate dehydrogenase, vomiting, abdominal pain, headache, increased eosinophils, and decreased albumin. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Gilead Sciences, Inc. at 1-888-983-4668 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. The pooled safety population described in the Warnings and Precautions section reflect exposure to TRODELVY as a single agent in 1354 patients, which included 641 patients with mTNBC and 322 patients with hormone receptor-positive (HR+)/human epidermal growth factor receptor 2-negative (HER2-) breast cancer from ASCENT-03, IMMU-132-01, ASCENT, and TROPiCS-02; and 391 patients with other tumor types. TRODELVY was administered as an intravenous infusion once weekly on Days 1 and 8 of 21-day treatment cycles at doses of 10 mg/kg until disease progression or unacceptable toxicity. Among the 1354 patients treated with TRODELVY, the median duration of treatment was 4.9 months (range: 0 to 63 months). In this pooled safety population, the most common (> 25%) adverse reactions including laboratory abnormalities were decreased leukocyte count (83%), decreased neutrophil count (77%), decreased hemoglobin (71%), nausea (63%), diarrhea (62%), decreased lymphocyte count (60%), fatigue (59%), alopecia (47%), increased glucose (40%), constipation (37%), vomiting (33%), decreased albumin (32%), increased alkaline phosphatase (30%) decreased appetite (28%), abdominal pain (27%), decreased creatinine clearance (27%), decreased magnesium (26%), and decreased potassium (26%). The data described in the following section reflects exposure to TRODELVY in combination with intravenous pembrolizumab in 221 patients with PD-L1 positive TNBC from ASCENT-04. Among the 221 patients who received TRODELVY in combination with intravenous pembrolizumab, the most common (≥ 25%) adverse reactions including laboratory abnormalities were decreased neutrophil count and decreased hemoglobin (86% each), decreased leukocyte count (84%), diarrhea (72%), nausea (68%), decreased lymphocyte count (61%), fatigue (58%), alopecia (52%), increased alkaline phosphatase and increased glucose (50% each), increased alanine aminotransferase (47%), constipation (41%), increased aspartate aminotransferase (40%), rash (37%), decreased potassium (35%), increased lactate dehydrogenase (34%), vomiting (29%), abdominal pain, headache, increased eosinophils (26% each) and decreased albumin (25%). Locally Advanced or Metastatic Triple-Negative Breast Cancer (TNBC) Single-Agent in Previously Untreated Unresectable Locally Advanced or Metastatic TNBC (ASCENT-03) The safety of TRODELVY was evaluated in 275 patients with unresectable locally advanced or metastatic TNBC who had not received previous systemic therapy for advanced disease and who were not candidates for PD-1 or PD-L1 inhibitor therapy who had received at least one dose of TRODELVY 10 mg/kg in ASCENT-03. [see Clinical Studies (14.1) ] . The median duration of treatment was 8.3 months (range: 0 to 29 months). Serious adverse reactions occurred in 26% of patients receiving TRODELVY. Serious adverse reactions in > 2% of patients included diarrhea, febrile neutropenia, and neutropenia (3.6% each) and pneumonia (2.9%). Fatal adverse reactions occurred in 2.5% of patients who received TRODELVY including sepsis (1.1%) and acute respiratory failure , neutropenic colitis, pneumonia, and septic shock (0.4% each). Permanent discontinuation of TRODELVY due to adverse reactions occurred in 3.6% of patients, of which interstitial lung disease accounted for 1.1%. Dosage interruptions of TRODELVY occurred in 66% of patients. Adverse reactions which required dosage interruption in ≥ 5% of patients were decreased neutrophil count (43%), diarrhea (6%), decreased leukocyte count and COVID-19 (5% each). Dose reductions of TRODELVY due to an adverse reaction occurred in 37% of patients. Adverse reaction which required dose reductions in >2% of patients included decreased neutrophil count (18%), diarrhea (6%), fatigue (4.7%), febrile neutropenia (2.5%), and weight decreased (2.2%).
Drug interactions
7 DRUG INTERACTIONS UGT1A1 Inhibitors or Inducers : Avoid concomitant use. ( 7 ) 7.1 Effect of Other Drugs on TRODELVY UGT1A1 Inhibitors Avoid administering UGT1A1 inhibitors with TRODELVY. SN-38 is a UGT1A1 substrate. Concomitant administration of TRODELVY with inhibitors of UGT1A1 may increase the incidence of adverse reactions due to potential increase in systemic exposure to SN-38 [see Warnings and Precaution (5.5) and Clinical Pharmacology (12.3 , 12.5) ] . UGT1A1 Inducers Avoid administering UGT1A1 inducers with TRODELVY. SN-38 is a UGT1A1 substrate. Concomitant administration of TRODELVY with inducers of UGT1A1may reduce exposure to SN-38 [see Warnings and Precaution (5.5) and Clinical Pharmacology (12.3 , 12.5) ] .
Use in specific populations
Lactation: Advise not to breastfeed. ( 8.2 ) 8.1 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 [see Clinical Pharmacology (12.1) and Nonclinical Toxicology (13.1) ] . Advise pregnant women and females of reproductive potential of the potential risk to a fetus. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 – 4% and 15 – 20%, respectively. Data Animal data There were no reproductive and developmental toxicology studies conducted with sacituzumab govitecan-hziy. 8.2 Lactation Risk Summary There is no information regarding the presence of sacituzumab govitecan-hziy or SN-38 in human milk, the effects on the breastfed child, or the effects on milk production. Because of the potential for serious adverse reactions in a breastfed child, advise women not to breastfeed during treatment and for 1 month after the last dose of TRODELVY. 8.3 Females and Males of Reproductive Potential Pregnancy Testing Verify the pregnancy status of females of reproductive potential prior to the initiation of TRODELVY. Contraception Females TRODELVY can cause fetal harm when administered to a pregnant woman [see Use in Specific Populations (8.1) ] . Advise females of reproductive potential to use effective contraception during treatment with TRODELVY and for 6 months after the last dose. Males Because of the potential for genotoxicity, advise male patients with female partners of reproductive potential to use effective contraception during treatment with TRODELVY and for 3 months after the last dose. Infertility Females Based on findings in animals, TRODELVY may impair fertility in females of reproductive potential [see Nonclinical Toxicology (13.1) ] . 8.4 Pediatric Use Safety and effectiveness of TRODELVY have not been established in pediatric patients. 8.5 Geriatric Use As a Single Agent Of the 641 patients with TNBC who were treated with TRODELVY in clinical studies, 20% of patients were 65 years and older and 5% were 75 years and older. No overall differences in effectiveness were observed between patients ≥ 65 years of age and younger adult patients. Patients 65 and older had an increased incidence of neutropenia with fatal outcomes. Of the 322 patients with HR+/HER2- breast cancer who were treated with TRODELVY, 26% of patients were 65 years and older and 6% were 75 years and older. No overall differences in effectiveness were observed between patients ≥ 65 years of age and younger patients. There was a higher discontinuation rate due to adverse reactions in patients aged 65 years or older (14%) compared with younger patients (3%). In Combination with Pembrolizumab Of the 221 patients with TNBC who were treated with TRODELVY in combination with pembrolizumab in ASCENT-04, 26% of patients were 65 years and older and 5% were 75 years and older. No overall differences in effectiveness were observed between patients ≥ 65 years of age and younger adult patients. There was a higher rate of serious adverse reactions in patients aged 65 years or older (31%) compared with younger adult patients (26%). 8.6 Hepatic Impairment The safety of TRODELVY in patients with moderate (total bilirubin > 1.5 to 3 × ULN) or severe (total bilirubin > 3 × ULN) hepatic impairment has not been established. TRODELVY has not been evaluated in patients with AST or ALT > 3 ULN without liver metastases, or AST or ALT > 5 ULN with liver metastases.
Pregnancy
8.1 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 [see Clinical Pharmacology (12.1) and Nonclinical Toxicology (13.1) ] . Advise pregnant women and females of reproductive potential of the potential risk to a fetus. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 – 4% and 15 – 20%, respectively. Data Animal data There were no reproductive and developmental toxicology studies conducted with sacituzumab govitecan-hziy.
Pediatric use
8.4 Pediatric Use Safety and effectiveness of TRODELVY have not been established in pediatric patients.
Geriatric use
8.5 Geriatric Use As a Single Agent Of the 641 patients with TNBC who were treated with TRODELVY in clinical studies, 20% of patients were 65 years and older and 5% were 75 years and older. No overall differences in effectiveness were observed between patients ≥ 65 years of age and younger adult patients. Patients 65 and older had an increased incidence of neutropenia with fatal outcomes. Of the 322 patients with HR+/HER2- breast cancer who were treated with TRODELVY, 26% of patients were 65 years and older and 6% were 75 years and older. No overall differences in effectiveness were observed between patients ≥ 65 years of age and younger patients. There was a higher discontinuation rate due to adverse reactions in patients aged 65 years or older (14%) compared with younger patients (3%). In Combination with Pembrolizumab Of the 221 patients with TNBC who were treated with TRODELVY in combination with pembrolizumab in ASCENT-04, 26% of patients were 65 years and older and 5% were 75 years and older. No overall differences in effectiveness were observed between patients ≥ 65 years of age and younger adult patients. There was a higher rate of serious adverse reactions in patients aged 65 years or older (31%) compared with younger adult patients (26%).
Overdosage
In a clinical trial, planned doses of up to 18 mg/kg (approximately 1.8 times the maximum recommended dose of 10 mg/kg) of TRODELVY were administered. In these patients, a higher incidence of severe neutropenia was observed.
Description
Sacituzumab govitecan-hziy is a Trop-2 directed antibody and topoisomerase inhibitor conjugate, composed of the following three components: the humanized monoclonal antibody, hRS7 IgG1κ (also called sacituzumab), which binds to Trop-2 (the trophoblast cell-surface antigen-2); the drug SN-38, a topoisomerase inhibitor; a hydrolysable linker (called CL2A), which links the humanized monoclonal antibody to SN-38. The recombinant monoclonal antibody is produced by mammalian (murine myeloma) cells, while the small molecule components SN-38 and CL2A are produced by chemical synthesis. Sacituzumab govitecan-hziy contains on average 7 to 8 molecules of SN-38 per antibody molecule. Sacituzumab govitecan-hziy has a molecular weight of approximately 160 kilodaltons. Sacituzumab govitecan-hziy has the following chemical structure. TRODELVY (sacituzumab govitecan-hziy) for injection is a sterile, preservative-free, off-white to yellowish lyophilized powder for intravenous use in a 50 mL clear glass single-dose vial, with a rubber stopper and crimp-sealed with an aluminum flip-off cap. Each single-dose vial of TRODELVY delivers 180 mg sacituzumab govitecan-hziy, 71.7 mg 2-(N-morpholino) ethane sulfonic acid (MES), 1.8 mg polysorbate 80 and 153.99 mg trehalose. Reconstitution with 20 mL of 0.9% Sodium Chloride Injection, USP, results in a concentration of 10 mg/mL with a pH of 6.5. Chemical Structure
Mechanism of action
12.1 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. Sacituzumab govitecan-hziy decreased tumor growth in mouse xenograft models of triple-negative breast cancer.
How supplied
(sacituzumab govitecan-hziy) for injection is a sterile, off-white to yellowish lyophilized powder in a single-dose vial. Each TRODELVY vial is individually boxed in a carton: NDC 55135-132-01 contains one 180 mg vial 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 .
Storage
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 .
Patient information
Advise the patient to read the FDA-approved patient labeling ( Patient Information ) Neutropenia Advise patients of the risk of neutropenia. Instruct patients to immediately contact their healthcare provider if they experience fever, chills, or other signs of infection [see Warnings and Precautions (5.1) ] . Diarrhea Advise patients of the risk of diarrhea. Instruct patients to immediately contact their healthcare provider if they experience diarrhea for the first time during treatment; black or bloody stools; symptoms of dehydration such as lightheadedness, dizziness, or faintness; inability to take fluids by mouth due to nausea or vomiting; or inability to get diarrhea under control within 24 hours [see Warnings and Precautions (5.2) ]. Hypersensitivity and Infusion-Related Reactions Inform patients of the risk of serious infusion reactions and anaphylaxis. Instruct patients to immediately contact their healthcare provider if they experience facial, lip, tongue, or throat swelling, urticaria, difficulty breathing, lightheadedness, dizziness, chills, rigors, wheezing, pruritus, flushing, rash, hypotension, or fever that occur during or at any time following the infusion [see Warnings and Precautions (5.3) ] . Nausea/Vomiting Advise patients of the risk of nausea and vomiting. Premedication according to established guidelines with a two or three drug regimen for prevention of chemotherapy-induced nausea and vomiting (CINV) is also recommended. Additional antiemetics, sedatives, and other supportive measures may also be employed as clinically indicated. All patients should receive take-home medications for preventing and treating delayed nausea and vomiting, with clear instructions. Instruct patients to immediately contact their healthcare provider if they experience uncontrolled nausea or vomiting [see Warnings and Precautions (5.4) ] . Embryo-Fetal Toxicity Advise female patients to contact their healthcare provider if they are pregnant or become pregnant. Inform female patients of the risk to a fetus and potential loss of the pregnancy [see Use in Specific Populations (8.1) ]. Contraception Advise female patients of reproductive potential to use effective contraception during treatment and for 6 months after the last dose of TRODELVY [see Use in Specific Populations (8.3) ] . Advise male patients with female partners of reproductive potential to use effective contraception during treatment and for 3 months after the last dose of TRODELVY [see Use in Specific Populations (8.3) ] . Lactation Advise women not to breastfeed during treatment and for 1 month after the last dose of TRODELVY [see Use in Specific Populations (8.2) ]. Infertility Advise females of reproductive potential that TRODELVY may impair fertility [see Use in Specific Populations (8.3) ].
Label text from the FDA structured product label by Gilead Sciences, Inc. (revised Jun 24, 2026). Long sections are shortened; the complete label is on DailyMed.
Active ingredients
- Sacituzumab Govitecan in 1 product
Trodelvy NDC products (1)
| NDC | Strength & form | Labeler | Type |
|---|---|---|---|
| 55135-132 | Sacituzumab Govitecan 180 mg/1 Powder, For Solution | Gilead Sciences, Inc. | BLA |
Frequently asked questions
What is Trodelvy used for?
1 INDICATIONS AND USAGE TRODELVY 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…
What are the side effects of Trodelvy?
The following adverse reactions are discussed in greater detail in other sections of the label: Neutropenia [see Warnings and Precautions (5.1) ] Diarrhea [see Warnings and Precautions (5.2) ] Hypersensitivity and Infusion-Related Reactions [see Warnings and Precautions (5.3) ] Nausea and Vomiting [see Warnings and Precautions (5.4) ] The most common adverse reactions including laboratory… See the full label for the complete list.
Who makes Trodelvy?
Trodelvy is listed by 1 labeler in the FDA NDC directory, including Gilead Sciences, Inc..