Version July 2025
Gilead Sciences is voluntarily withdrawing the US indication for Trodelvy (sacituzumab govitecan-hziy) for the treatment of adult patients with locally advanced or metastatic urothelial cancer who have previously received a platinum-containing chemotherapy and either programmed death receptor-1 (PD-1) or programmed death-ligand 1 (PD-L1) inhibitor. Sacituzumab govitecan was granted approval for this indication under the FDA’s accelerated approval program in 2021. This decision was made in consultation with the FDA. This decision does not affect the other approved sacituzumab govitecan indications within or outside of the United States.
Further information may be found at https://www.gilead.com/company/company-statements/2024/gilead-provides-update-on-us-indication-for-trodelvy-in-metastatic-urothelial-cancer.
Sacituzumab govitecan can cause severe, life-threatening, or fatal neutropenia. Withhold sacituzumab govitecan for ANC below 1,500/mm3 or neutropenic fever. Monitor blood cell counts periodically during treatment. Primary prophylaxis with G-CSF is recommended for all patients at increased risk of febrile neutropenia. Initiate anti-infective treatment in patients with febrile neutropenia without delay.
Sacituzumab govitecan can cause severe diarrhea. Monitor patients with diarrhea and give fluid and electrolytes as needed. At the onset of diarrhea, evaluate for infectious causes and, if negative, promptly initiate loperamide. If severe diarrhea occurs, withhold sacituzumab govitecan until resolved to ≤ Grade 1 and reduce subsequent doses.
Dosage guidance:
Safety : Premedicate with antipyretics and H1/H2 antagonists prior to sacituzumab govitecan infusion; corticosteroids may be used if prior infusion-related reactions occurred. Medications and emergency equipment for the treatment of hypersensitivity or infusion reactions should be available for immediate use during infusion. 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 (including patients of older age or patients with prior neutropenia, poor performance status, organ dysfunction, or multiple comorbidities). Withhold sacituzumab govitecan dose on day 1 of any cycle for ANC <1,500/mm3; withhold dose on day 8 of any cycle for ANC <1,000/mm3. Do not substitute sacituzumab govitecan for (or use with) other medications containing irinotecan or its active metabolite SN-38.
Dosing: Calculate the required dose based on the patient's current body weight.
Clinical considerations : Sacituzumab govitecan is associated with a moderate to high emetic potential; antiemetics (either a 2 or 3 drug combination regimen) are recommended to prevent nausea and vomiting. Patients should be provided take home medications with clear instructions for nausea and vomiting prevention and treatment.
Breast cancer, triple negative, locally advanced or metastatic (previously treated): IV: 10 mg/kg on days 1 and 8 of a 21-day treatment cycle (maximum: 10 mg/kg/dose); continue until disease progression or unacceptable toxicity (Ref).
Breast cancer, locally advanced or metastatic, hormone receptor positive, HER2 negative (previously treated): IV: 10 mg/kg on days 1 and 8 of a 21-day treatment cycle (maximum: 10 mg/kg/dose); continue until disease progression or unacceptable toxicity (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
CrCl ≥30 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling; however, renal elimination of SN-38 (small molecule moiety of sacituzumab govitecan) is minimal.
CrCl ≤29 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
End-stage kidney disease: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
Mild impairment (total bilirubin ≤ ULN with AST > ULN or bilirubin >1 to 1.5 times ULN with any AST): No initial dosage adjustment necessary.
Moderate to severe impairment (total bilirubin >1.5 times ULN, or AST and ALT >3 times ULN without liver metastases, or AST and ALT >5 times ULN with liver metastases): There are no dosage adjustments provided in the manufacturer's labeling (no initial dosage recommendation can be made).
American Society of Clinical Oncology guidelines for appropriate systemic therapy dosing in adults with cancer with a BMI ≥30 kg/m2: Utilize patient's actual body weight for calculation of BSA- or weight-based dosing; manage regimen-related toxicities in the same manner as for patients with a BMI <30 kg/m2 (Ref).
|
Dose level |
Recommended sacituzumab govitecan dosage and schedulea |
|---|---|
|
a Do not re-escalate the sacituzumab govitecan dose after a dose reduction for adverse reactions. | |
|
Usual (initial) dose |
10 mg/kg on days 1 and 8 of a 21-day treatment cycle |
|
First dose reduction levela |
7.5 mg/kg on days 1 and 8 of a 21-day treatment cyclea |
|
Second dose reduction levela |
5 mg/kg on days 1 and 8 of a 21-day treatment cyclea |
|
Further dose reductions necessary |
Permanently discontinue sacituzumab govitecan |
|
Adverse reaction |
Severity |
Sacituzumab govitecan dose modificationa |
|---|---|---|
|
a Do not re-escalate the sacituzumab govitecan dose after a dose reduction for adverse reactions. | ||
|
b G-CSF = granulocyte-colony stimulating factor. | ||
|
Hematologic toxicity | ||
|
Neutropenia |
ANC <1,500/mm3 on day 1 of any cycle |
Withhold sacituzumab govitecan. |
|
ANC <1,000/mm3 on day 8 of any cycle |
Withhold sacituzumab govitecan. | |
|
Grade 3 or 4 neutropenia (ANC <1,000/mm3) |
Withhold sacituzumab govitecan until ANC ≥1,500/mm3 for day 1 dose or ≥1,000/mm3 for day 8 dose. Administer G-CSFb during treatment as clinically indicated. Reduce sacituzumab govitecan dose by one dose level for each occurrence, or discontinue according to the table for dosage reduction levels.a | |
|
Neutropenic fever |
Any |
Withhold sacituzumab govitecan until ANC ≥1,500/mm3 for day 1 dose or ≥1,000/mm3 for day 8 dose. Administer G-CSFb during treatment as clinically indicated. Reduce sacituzumab govitecan dose by one dose level for each occurrence, or discontinue according to the table for dosage reduction levels.a |
|
Nonhematologic toxicity | ||
|
GI toxicity: Diarrhea |
Any |
Evaluate for infectious causes at onset of diarrhea. If negative, initiate loperamide 4 mg initially, followed by 2 mg with every diarrhea episode up to a maximum of 16 mg/day (discontinue loperamide 12 hours after diarrhea resolves). Initiate additional supportive measures (fluids, electrolytes) as clinically indicated. If an excessive cholinergic response (eg, abdominal cramping, salivation) occurs, may consider appropriate anticholinergic (eg, atropine) premedication with subsequent infusions. |
|
Grade 3 or 4, not controlled with anti-diarrheal agents |
Withhold sacituzumab govitecan until resolved to ≤ grade 1. Reduce sacituzumab govitecan dose by one dose level with each occurrence, or discontinue according to the table for dosage reduction levels.a | |
|
GI toxicity: Nausea or vomiting |
Grade 3 or 4, not controlled with antiemetics |
Withhold sacituzumab govitecan until resolved to ≤ grade 1. Reduce sacituzumab govitecan dose by one dose level with each occurrence, or discontinue according to the table for dosage reduction levels.a Additional antiemetics and supportive measures may be used as clinically indicated. Provide take-home medications for prevention and treatment of nausea and vomiting. |
|
Hypersensitivity |
Any |
May require discontinuation. |
|
Infusion-related reaction |
Grades 1 to 3 |
Slow infusion rate or interrupt the infusion. |
|
Grade 4 |
Permanently discontinue sacituzumab govitecan. | |
|
Other toxicities |
Grade 3 or 4 of any duration despite optimal medical management |
Withhold sacituzumab govitecan until resolved to ≤ grade 1. Reduce sacituzumab govitecan dose by one dose level with each occurrence, or discontinue according to the table for dosage reduction levels.a |
Refer to adult dosing.
Sacituzumab govitecan may cause neutropenia, including grades 3 and 4 and febrile neutropenia. Anemia, leukopenia, lymphocytopenia, and thrombocytopenia have also been reported. Neutropenia was the most common adverse reaction leading to treatment interruption in clinical trials.
Mechanism: Exact mechanism is unknown; SN-38 is the active metabolite of the cytotoxic agent irinotecan, a topoisomerase I inhibitor.
Onset: May occur at any time during treatment, including during the first cycle (Ref). Median onset of 16 days has been reported for neutropenia.
Risk factors:
• Patients who are homozygous for the UGT1A1*28 allele; Note: Toxic effects of irinotecan (of which, SN-38 is the active metabolite) have been associated with UGT1A1*28 homozygosity. Clinical trials of sacituzumab govitecan showed a numerically increased incidence of neutropenia in patients with a UGT1A1*28 genotype compared to *1/*28 or *1/*1 (Ref). Additional validation is needed prior to use of genetic testing for clinical decision making related to use of sacituzumab govitecan (Ref).
Sacituzumab govitecan may cause diarrhea, including grades 3 and 4 diarrhea; permanent discontinuation due to diarrhea occurred rarely in clinical trials. Colitis and neutropenic enterocolitis have also been reported. Other GI adverse reactions may include abdominal pain, dyspepsia, and stomatitis. Abdominal cramps and increased salivation have also been reported in patients who experience an excessive cholinergic response to treatment.
Sacituzumab govitecan is associated with moderate to high emetic potential and may cause nausea and vomiting (including grades 3 and 4); premedication and/or treatment interruption may be required.
Mechanism: Dose-related; related to the pharmacologic action. SN-38 is the active metabolite of the cytotoxic agent irinotecan, a topoisomerase I inhibitor. When compared to irinotecan, sacituzumab govitecan results in lower concentrations of the glucuronidated form of SN-38 which may explain the lower incidence of diarrhea (Ref).
Sacituzumab govitecan may cause hypersensitivity reactions, including severe and life-threatening reactions; anaphylaxis and angioedema have been reported.
Onset: Rapid; reported within 24 hours of administration in over one-third of patients.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported in adults.
>10%:
Dermatologic: Alopecia (47% to 48%), pruritus (10% to 12%), skin rash (12%)
Endocrine & metabolic: Decreased serum albumin (32%), decreased serum calcium (36%), decreased serum magnesium (18% to 33%), decreased serum phosphate (17% to 26%), decreased serum potassium (22% to 33%), decreased serum sodium (19% to 22%), increased lactate dehydrogenase (16% to 18%), increased serum albumin (32%), increased serum glucose (37% to 49%), increased serum phosphate (16%), increased serum potassium (14%)
Gastrointestinal: Abdominal pain (20% to 30%), constipation (34% to 37%), decreased appetite (21% to 28%), diarrhea (59% to 62%; grades 3/4: 10% to 11%) (table 1), dyspepsia (11%), nausea (57% to 59%; grades 3/4: 1% to 3%) (table 2), stomatitis (17%; grades 3/4: 2%), vomiting (23% to 33%; grades 3/4: 1% to 2%) (table 3)
|
Drug (Sacituzumab Govitecan) |
Comparator (Single Agent Chemotherapy) |
Indication |
Number of Patients (Sacituzumab Govitecan) |
Number of Patients (Comparator) |
|---|---|---|---|---|
|
All grades: 62% |
All grades: 23% |
Locally advanced or metastatic HR-positive, HER2-negative breast cancer |
268 |
249 |
|
Grades 3/4: 10% |
Grades 3/4: 1% |
Locally advanced or metastatic HR-positive, HER2-negative breast cancer |
268 |
249 |
|
All grades: 59% |
All grades: 17% |
Metastatic triple-negative breast cancer |
258 |
224 |
|
Grades 3/4: 11% |
Grades 3/4: 1% |
Metastatic triple-negative breast cancer |
258 |
224 |
|
Drug (Sacituzumab Govitecan) |
Comparator (Single agent chemotherapy) |
Indication |
Number of Patients (Sacituzumab Govitecan) |
Number of Patients (Comparator) |
|---|---|---|---|---|
|
59% |
35% |
Locally advanced or metastatic HR-positive, HER2-negative breast cancer |
268 |
249 |
|
All grades: 57% |
All grades: 26% |
Metastatic triple-negative breast cancer |
258 |
224 |
|
Grades 3/4: 3% |
Grades 3/4: 0.4% |
Metastatic triple-negative breast cancer |
258 |
224 |
|
Drug (Sacituzumab Govitecan) |
Comparator (Single agent chemotherapy) |
Indication |
Number of Patients (Sacituzumab Govitecan) |
Number of Patients (Comparator) |
|---|---|---|---|---|
|
23% |
16% |
Locally advanced or metastatic HR-positive, HER2-negative breast cancer |
268 |
249 |
|
All grades: 33% |
All grades: 16% |
Metastatic triple-negative breast cancer |
258 |
224 |
|
Grades 3/4: 2% |
Grades 3/4: 1% |
Metastatic triple-negative breast cancer |
258 |
224 |
Genitourinary: Urinary tract infection (13%)
Hematologic & oncologic: Decreased hemoglobin (73% to 94%; grades 3/4: 8% to 9%) (table 4), decreased neutrophils (78% to 83%; grades 3/4: 49% to 53%) (table 5), decreased platelet count (21% to 23%; grades 3/4: 1%), eosinophilia (13%), leukopenia (86% to 88%, grades 3/4: 38% to 41%) (table 6), lymphocytopenia (65% to 88%; grades 3/4: 21% to 31%)
|
Drug (Sacituzumab Govitecan) |
Comparator (Single agent chemotherapy) |
Indication |
Number of Patients (Sacituzumab Govitecan) |
Number of Patients (Comparator) |
|---|---|---|---|---|
|
All grades: 73% |
All grades: 59% |
Locally advanced or metastatic HR-positive, HER2-negative breast cancer |
268 |
249 |
|
Grades 3/4: 8% |
Grades 3/4: 5% |
Locally advanced or metastatic HR-positive, HER2-negative breast cancer |
268 |
249 |
|
All grades: 94% |
All grades: 57% |
Metastatic triple-negative breast cancer |
258 |
224 |
|
Grades 3/4: 9% |
Grades 3/4: 6% |
Metastatic triple-negative breast cancer |
258 |
224 |
|
Drug (Sacituzumab Govitecan) |
Comparator (Single agent chemotherapy) |
Indication |
Number of Patients (Sacituzumab Govitecan) |
Number of Patients (Comparator) |
|---|---|---|---|---|
|
All grades: 83% |
All grades: 67% |
Locally advanced or metastatic HR-positive, HER2-negative breast cancer |
268 |
249 |
|
Grades 3/4: 53% |
Grades 3/4: 40% |
Locally advanced or metastatic HR-positive, HER2-negative breast cancer |
268 |
249 |
|
All grades: 78% |
All grades: 48% |
Metastatic triple-negative breast cancer |
258 |
224 |
|
Grades 3/4: 49% |
Grades 3/4: 36% |
Metastatic triple-negative breast cancer |
258 |
224 |
|
Drug (Sacituzumab Govitecan) |
Comparator (Single agent chemotherapy) |
Indication |
Number of Patients (Sacituzumab Govitecan) |
Number of Patients (Comparator) |
|---|---|---|---|---|
|
All grades: 88% |
All grades: 73% |
Locally advanced or metastatic HR-positive, HER2-negative breast cancer |
268 |
249 |
|
Grades 3/4: 38% |
Grades 3/4: 26% |
Locally advanced or metastatic HR-positive, HER2-negative breast cancer |
268 |
249 |
|
All grades: 86% |
All grades: 53% |
Metastatic triple-negative breast cancer |
258 |
224 |
|
Grades 3/4: 41% |
Grades 3/4: 25% |
Metastatic triple-negative breast cancer |
258 |
224 |
Hepatic: Increased serum alanine aminotransferase (21% to 26%), increased serum alkaline phosphatase (23% to 26%), increased serum aspartate aminotransferase (15% to 27%)
Nervous system: Fatigue (60% to 65%; including asthenia), headache (16% to 18%), insomnia (11%)
Neuromuscular & skeletal: Arthralgia (12% to 15%), back pain (16%)
Renal: Decreased creatinine clearance (24%)
Respiratory: Cough (12% to 24%), dyspnea (20%), upper respiratory tract infection (12%)
Miscellaneous: Fever (15%)
1% to 10%:
Cardiovascular: Hypotension (5%)
Dermatologic: Skin hyperpigmentation (3%)
Endocrine & metabolic: Decreased serum glucose (10%), hypokalemia (10%)
Gastrointestinal: Colitis (including neutropenic enterocolitis: ≤2%)
Genitourinary: Proteinuria (1%)
Hematologic & oncologic: Febrile neutropenia (4%)
Nervous system: Dizziness (10%), pain (5%)
Respiratory: Nasal congestion (3%), pneumonia (2%), rhinorrhea (5%)
<1%: Gastrointestinal: Enteritis
Frequency not defined:
Hypersensitivity: Hypersensitivity reaction (including anaphylaxis, angioedema)
Immunologic: Antibody development (including neutralizing)
Postmarketing: Renal: Acute interstitial nephritis (Guarin 2024)
Severe hypersensitivity to sacituzumab govitecan or any component of the formulation.
Special populations:
• Older age: In studies, patients ≥65 years of age experienced an increased incidence of neutropenia (including fatal outcomes) and/or a higher discontinuation rate due to adverse reactions (compared to patients <65 years of age).
Dosage form specific issues:
• Polysorbate 80: Some dosage forms may contain polysorbate 80 (also known as Tweens). Hypersensitivity reactions, usually a delayed reaction, have been reported following exposure to pharmaceutical products containing polysorbate 80 in certain individuals (Isaksson 2002; Lucente 2000; Shelley 1995). Thrombocytopenia, ascites, pulmonary deterioration, and renal and hepatic failure have been reported in premature neonates after receiving parenteral products containing polysorbate 80 (Alade 1986; CDC 1984). See manufacturer's labeling.
Other warnings/precautions:
• Reduced UGT1A1 activity: Patients who are homozygous or heterozygous for the UGT1A1*28 allele may be at increased risk for adverse reactions, including neutropenia, febrile neutropenia, and anemia (compared to wild-type). Early acute-onset or unusually severe adverse reactions may be indicative of reduced UGT1A1 enzyme activity.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution Reconstituted, Intravenous [preservative free]:
Trodelvy: Sacituzumab govitecan-hziy 180 mg (1 ea) [contains polysorbate 80]
No
Solution (reconstituted) (Trodelvy Intravenous)
180 mg (per each): $3,015.89
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution Reconstituted, Intravenous:
Trodelvy: 180 mg (1 ea) [contains polysorbate 80]
IV: Administer the initial sacituzumab govitecan infusion over 3 hours; may administer subsequent infusions over 1 to 2 hours if prior infusions were tolerated. Protect infusion bag from light during infusion; however, tubing does not need to be protected from light during infusion and light-protective tubing is not necessary during the infusion. After infusion is complete, flush infusion line with 20 mL NS. Observe patients during infusion and for at least 30 minutes after each infusion. Administer infusion within 8 hours (including infusion time) after refrigeration.
Prior to each dose, premedicate with antipyretics and H 1/H 2 antagonists; corticosteroids may be administered if an infusion-related reaction occurred with a prior dose. Slow or interrupt the infusion if an infusion-related reaction develops; permanently discontinue for life-threatening infusion-related reactions.
Sacituzumab govitecan is associated with a moderate to high emetic potential; antiemetics (either a 2 or 3 drug combination regimen) are recommended to prevent nausea and vomiting.
Do not administer as an IV push or bolus. Do not administer with other medications.
Hazardous agent (NIOSH 2024 [table 1]).
Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2023; NIOSH 2024; USP-NF 2020).
Breast cancer, locally advanced or metastatic:
Treatment (as a single agent) of unresectable locally advanced or metastatic triple-negative breast cancer in adults who have received 2 or more prior systemic therapies, at least one of which was for metastatic disease.
Treatment (as a single agent) of 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 in adults who have received endocrine-based therapy and at least 2 additional systemic therapies in the metastatic setting.
Sacituzumab govitecan may be confused with datopotamab deruxtecan, fam-trastuzumab deruxtecan, irinotecan (conventional), irinotecan (liposomal), sarilumab, secukinumab, topotecan.
The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drug classes (chemotherapeutic agent, parenteral and oral) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Acute Care, Community/Ambulatory Care, and Long-Term Care Settings).
Do not substitute sacituzumab govitecan for (or use with) other medications containing irinotecan or its active metabolite SN-38.
Substrate of UGT1A1;
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
5-Aminosalicylic Acid Derivatives: May increase myelosuppressive effects of Myelosuppressive Agents. Risk C: Monitor
Abrocitinib: May increase immunosuppressive effects of Immunosuppressants (Cytotoxic Chemotherapy). Risk X: Avoid
Antithymocyte Globulin (Equine): Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Antithymocyte Globulin (Equine). Specifically, these effects may be unmasked if the dose of cytotoxic chemotherapy is reduced. Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Antithymocyte Globulin (Equine). Specifically, infections may occur with greater severity and/or atypical presentations. Risk C: Monitor
Antithyroid Agents: Myelosuppressive Agents may increase neutropenic effects of Antithyroid Agents. Risk C: Monitor
Baricitinib: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Baricitinib. Risk X: Avoid
BCG Products: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of BCG Products. Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of BCG Products. Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid
Belumosudil: May increase serum concentration of UGT1A1 Substrates. Management: Avoid coadministration of belumosudil with substrates of UGT1A1 for which minimal concentration increases can cause serious adverse effects. If coadministration is required, dose reductions of the UGT1A1 substrate may be required. Risk D: Consider Therapy Modification
Brincidofovir: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Brincidofovir. Risk C: Monitor
Brivudine: May increase adverse/toxic effects of Immunosuppressants (Cytotoxic Chemotherapy). Risk X: Avoid
Chikungunya Vaccine (Live): Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Chikungunya Vaccine (Live). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Chikungunya Vaccine (Live). Risk X: Avoid
Chloramphenicol (Ophthalmic): May increase adverse/toxic effects of Myelosuppressive Agents. Risk C: Monitor
Chloramphenicol (Systemic): Myelosuppressive Agents may increase myelosuppressive effects of Chloramphenicol (Systemic). Risk X: Avoid
Cladribine: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Cladribine. Risk X: Avoid
CloZAPine: Myelosuppressive Agents may increase adverse/toxic effects of CloZAPine. Specifically, the risk for neutropenia may be increased. Risk C: Monitor
Coccidioides immitis Skin Test: Coadministration of Immunosuppressants (Cytotoxic Chemotherapy) and Coccidioides immitis Skin Test may alter diagnostic results. Management: Consider discontinuing cytotoxic chemotherapy several weeks prior to coccidioides immitis skin antigen testing to increase the likelihood of accurate diagnostic results. Risk D: Consider Therapy Modification
COVID-19 Vaccine (Inactivated Virus): Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of COVID-19 Vaccine (Inactivated Virus). Risk C: Monitor
COVID-19 Vaccine (mRNA): Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of COVID-19 Vaccine (mRNA). Management: Give a 3-dose primary series for all patients aged 6 months and older taking immunosuppressive medications or therapies. Booster doses are recommended for certain age groups. See CDC guidance for details. Risk D: Consider Therapy Modification
COVID-19 Vaccine (Subunit): Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of COVID-19 Vaccine (Subunit). Risk C: Monitor
Deferiprone: Myelosuppressive Agents may increase neutropenic effects of Deferiprone. Management: Avoid the concomitant use of deferiprone and myelosuppressive agents whenever possible. If this combination cannot be avoided, monitor the absolute neutrophil count more closely. Risk D: Consider Therapy Modification
Dengue Tetravalent Vaccine (Live): Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Dengue Tetravalent Vaccine (Live). Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Dengue Tetravalent Vaccine (Live). Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid
Denosumab: May increase immunosuppressive effects of Immunosuppressants (Cytotoxic Chemotherapy). Management: Consider the risk of serious infections versus the potential benefits of coadministration of denosumab and cytotoxic chemotherapy. If combined, monitor patients for signs/symptoms of serious infections. Risk D: Consider Therapy Modification
Deucravacitinib: May increase immunosuppressive effects of Immunosuppressants (Cytotoxic Chemotherapy). Risk X: Avoid
Efgartigimod Alfa: May decrease therapeutic effects of Fc Receptor-Binding Agents. Risk C: Monitor
Etrasimod: May increase immunosuppressive effects of Immunosuppressants (Cytotoxic Chemotherapy). Risk X: Avoid
Fexinidazole: Myelosuppressive Agents may increase myelosuppressive effects of Fexinidazole. Risk X: Avoid
Filgotinib: May increase immunosuppressive effects of Immunosuppressants (Cytotoxic Chemotherapy). Risk X: Avoid
Inebilizumab: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Inebilizumab. Risk C: Monitor
Influenza Virus Vaccines: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Influenza Virus Vaccines. Management: Administer influenza vaccines at least 2 weeks prior to initiating chemotherapy if possible. If vaccination occurs less than 2 weeks prior to or during chemotherapy, revaccinate at least 3 months after therapy discontinued if immune competence restored. Risk D: Consider Therapy Modification
Irinotecan Products: May increase adverse/toxic effects of Sacituzumab Govitecan. Risk X: Avoid
Leflunomide: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Leflunomide. Management: Increase the frequency of chronic monitoring of platelet, white blood cell count, and hemoglobin or hematocrit to monthly, instead of every 6 to 8 weeks, if leflunomide is coadministered with immunosuppressive agents, such as cytotoxic chemotherapy. Risk D: Consider Therapy Modification
Lenograstim: Antineoplastic Agents may decrease therapeutic effects of Lenograstim. Management: Avoid the use of lenograstim 24 hours before until 24 hours after the completion of myelosuppressive cytotoxic chemotherapy. Risk D: Consider Therapy Modification
Linezolid: May increase myelosuppressive effects of Myelosuppressive Agents. Risk C: Monitor
Lipegfilgrastim: Antineoplastic Agents may decrease therapeutic effects of Lipegfilgrastim. Management: Avoid concomitant use of lipegfilgrastim and myelosuppressive cytotoxic chemotherapy. Lipegfilgrastim should be administered at least 24 hours after the completion of myelosuppressive cytotoxic chemotherapy. Risk D: Consider Therapy Modification
Mitapivat: May decrease serum concentration of UGT1A1 Substrates. Risk C: Monitor
Mumps- Rubella- or Varicella-Containing Live Vaccines: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Mumps- Rubella- or Varicella-Containing Live Vaccines. Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Mumps- Rubella- or Varicella-Containing Live Vaccines. Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid
Nadofaragene Firadenovec: Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Nadofaragene Firadenovec. Specifically, the risk of disseminated adenovirus infection may be increased. Risk X: Avoid
Natalizumab: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Natalizumab. Risk X: Avoid
Nipocalimab: May decrease therapeutic effects of Fc Receptor-Binding Agents. Risk C: Monitor
Ocrelizumab: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Ocrelizumab. Risk C: Monitor
Ofatumumab: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Ofatumumab. Risk C: Monitor
Olaparib: Myelosuppressive Agents may increase myelosuppressive effects of Olaparib. Risk C: Monitor
Palifermin: May increase adverse/toxic effects of Antineoplastic Agents. Specifically, the duration and severity of oral mucositis may be increased. Management: Do not administer palifermin within 24 hours before, during infusion of, or within 24 hours after administration of myelotoxic chemotherapy. Risk D: Consider Therapy Modification
Pidotimod: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Pidotimod. Risk C: Monitor
Pimecrolimus: May increase immunosuppressive effects of Immunosuppressants (Cytotoxic Chemotherapy). Risk X: Avoid
Piperacillin: May increase hypokalemic effects of Antineoplastic Agents. Risk C: Monitor
Pneumococcal Vaccines: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Pneumococcal Vaccines. Risk C: Monitor
Poliovirus Vaccine (Live/Trivalent/Oral): Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Poliovirus Vaccine (Live/Trivalent/Oral). Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Poliovirus Vaccine (Live/Trivalent/Oral). Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid
Polymethylmethacrylate: Immunosuppressants (Cytotoxic Chemotherapy) may increase hypersensitivity effects of Polymethylmethacrylate. Management: Use caution when considering use of bovine collagen-containing implants such as the polymethylmethacrylate-based Bellafill brand implant in patients who are receiving immunosuppressants. Consider use of additional skin tests prior to administration. Risk D: Consider Therapy Modification
Promazine: May increase myelosuppressive effects of Myelosuppressive Agents. Risk C: Monitor
Rabies Vaccine: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Rabies Vaccine. Management: Complete rabies vaccination at least 2 weeks before initiation of immunosuppressant therapy if possible. If combined, check for rabies antibody titers, and if vaccination is for post exposure prophylaxis, administer a 5th dose of the vaccine. Risk D: Consider Therapy Modification
Ritlecitinib: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Ritlecitinib. Risk X: Avoid
Ropeginterferon Alfa-2b: Myelosuppressive Agents may increase myelosuppressive effects of Ropeginterferon Alfa-2b. Management: Avoid coadministration of ropeginterferon alfa-2b and other myelosuppressive agents. If this combination cannot be avoided, monitor patients for excessive myelosuppressive effects. Risk D: Consider Therapy Modification
Rozanolixizumab: May decrease therapeutic effects of Fc Receptor-Binding Agents. Risk C: Monitor
Ruxolitinib (Topical): Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Ruxolitinib (Topical). Risk X: Avoid
Sipuleucel-T: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Sipuleucel-T. Management: Consider reducing the dose or discontinuing the use of immunosuppressants, such as cytotoxic chemotherapy, prior to initiating sipuleucel-T therapy. Risk D: Consider Therapy Modification
Sphingosine 1-Phosphate (S1P) Receptor Modulators: May increase immunosuppressive effects of Immunosuppressants (Cytotoxic Chemotherapy). Risk C: Monitor
Tacrolimus (Topical): Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Tacrolimus (Topical). Risk X: Avoid
Talimogene Laherparepvec: Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Talimogene Laherparepvec. Specifically, the risk of infection from the live, attenuated herpes simplex virus contained in talimogene laherparepvec may be increased. Risk X: Avoid
Tertomotide: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Tertomotide. Risk X: Avoid
Tofacitinib: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Tofacitinib. Risk X: Avoid
Typhoid Vaccine: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Typhoid Vaccine. Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Typhoid Vaccine. Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid
Ublituximab: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Ublituximab. Risk C: Monitor
UGT1A1 Inducers: May decrease active metabolite exposure of Sacituzumab Govitecan. Specifically, concentrations of SN-38 may be decreased. Risk X: Avoid
UGT1A1 Inhibitors: May increase active metabolite exposure of Sacituzumab Govitecan. Specifically, concentrations of SN-38 may be increased. Risk X: Avoid
Upadacitinib: Immunosuppressants (Cytotoxic Chemotherapy) may increase immunosuppressive effects of Upadacitinib. Risk X: Avoid
Vaccines (Live): Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Vaccines (Live). Specifically, the risk of vaccine-associated infection may be increased. Vaccines (Live) may decrease therapeutic effects of Immunosuppressants (Cytotoxic Chemotherapy). Risk X: Avoid
Vaccines (Non-Live/Inactivated/Non-Replicating): Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Vaccines (Non-Live/Inactivated/Non-Replicating). Management: Give non-live/inactivated/non-replicating vaccines at least 2 weeks prior to starting chemotherapy when possible. Patients vaccinated less than 14 days before or during chemotherapy should be revaccinated at least 3 months after therapy is complete. Risk D: Consider Therapy Modification
Yellow Fever Vaccine: Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Yellow Fever Vaccine. Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Yellow Fever Vaccine. Specifically, the risk of vaccine-associated infection may be increased. Risk X: Avoid
Zoster Vaccine (Live/Attenuated): Immunosuppressants (Cytotoxic Chemotherapy) may increase adverse/toxic effects of Zoster Vaccine (Live/Attenuated). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Cytotoxic Chemotherapy) may decrease therapeutic effects of Zoster Vaccine (Live/Attenuated). Risk X: Avoid
Evaluate pregnancy status prior to use in patients who could become pregnant. Patients who could become pregnant should use effective contraception during therapy and for 6 months after the last sacituzumab govitecan dose. Patients with partners who could become pregnant should use effective contraception during therapy and for 3 months after the last dose of sacituzumab govitecan.
Based on the mechanism of action, in utero exposure to sacituzumab govitecan may cause fetal harm.
Sacituzumab govitecan is composed of sacituzumab linked to SN-38. Sacituzumab is a humanized monoclonal antibody (IgG1). Placental transfer of human IgG is dependent upon the IgG subclass, maternal serum concentrations, newborn birth weight, and gestational age, generally increasing as pregnancy progresses. The lowest fetal IgG exposure would be expected during the period of organogenesis (Palmeira 2012; Pentsuk 2009). SN-38 is the genotoxic component.
It is not known if sacituzumab govitecan or SN-38 are present in breast milk.
Due to the potential for serious adverse reactions in the breastfed infant, breastfeeding is not recommended by the manufacturer during therapy and for 1 month after the last sacituzumab govitecan dose.
Monitor CBC with differential prior to dose on days 1 and 8 of each cycle and periodically during treatment as clinically necessary (especially in patients known to be homozygous or heterozygous for UGT1A1*28). Evaluate pregnancy status prior to use in patients who could become pregnant. Monitor for neutropenic fever, hypersensitivity reactions, and infusion-related reactions (observe during and for at least 30 minutes after infusion). Monitor (including patient self-monitoring, after clear clinician instruction) for diarrhea, nausea, and vomiting, as well as a clinical indication for additional antiemetics, antidiarrheals, and/or supportive measures (eg, fluids, electrolytes). Closely monitor for adverse reactions in patients with known reduced UGT1A1 activity.
The American Society of Clinical Oncology hepatitis B virus (HBV) screening and management provisional clinical opinion (ASCO [Hwang 2020]) recommends HBV screening with hepatitis B surface antigen, hepatitis B core antibody, total Ig or IgG, and antibody to hepatitis B surface antigen prior to beginning (or at the beginning of) systemic anticancer therapy; do not delay treatment for screening/results. Detection of chronic or past HBV infection requires a risk assessment to determine antiviral prophylaxis requirements, monitoring, and follow-up.
Sacituzumab govitecan is an antibody drug conjugate that consists of a humanized antitrophoblast cell-surface antigen 2 (Trop-2) monoclonal antibody coupled to the topoisomerase 1 inhibitor SN-38 via a cleavable linker (Bardia 2019). Trop-2 is a transmembrane glycoprotein that is highly expressed in many epithelial cancer cell surfaces (Tagawa 2021). TROP-2 is associated with cancer cell growth and has been detected in breast cancer cells (including triple-negative breast cancer cells). Sacituzumab govitecan binds to Trop-2 and is internalized; SN-38 is released in tumors both intracellularly and in the tumor microenvironment, leading to DNA damage, apoptosis, and cell death (Bardia 2019).
Distribution: Vdss: Sacituzumab govitecan: 3.6 L.
Metabolism: SN-38 (small molecule moiety of sacituzumab govitecan) is metabolized via UGT1A1.
Half-life elimination: Median: Sacituzumab govitecan: 23.4 hours; free SN-38: 17.6 hours.
Excretion: Clearance: Sacituzumab govitecan: 0.13 L/hour.
