Sacituzumab govitecan
ADCs
Antibody-drug conjugates (ADCs)High alert
An error with this medicine can cause serious harm: double checks and protocols are used.Pregnancy: avoid
Avoid in pregnancy. Can harm the fetus; a pregnancy test is done and effective contraception is used during and after treatment, and breastfeeding is avoided.
Anti-TROP-2 antibody carrying SN-38, the active form of irinotecan; used in advanced breast cancer. Boxed risks: severe neutropenia and diarrhoea.
Quick facts
- Group
- Antibody-drug conjugates (ADCs)
- Target
- TROP-2 (TACSTD2), a surface protein of many epithelial cancers
- Used for
- Unresectable
- Key effects
- Nausea · Fatigue · Hair loss
- Monitor
- Complete blood count before each dose
- ATC
- L01FX17
No doses: the clinician sets them by the current guideline.
Mechanism of action
The crystal structure shows the TROP-2 extracellular region alone; the antibody and the SN-38 payload are not in it.
The humanised antibody binds TROP-2 on tumour cells and carries SN-38, the active metabolite of irinotecan, linked through hinge cysteines. Inside the tumour SN-38 is released and blocks topoisomerase I, so DNA breaks accumulate and the cell dies.
- The antibody binds TROP-2 on the tumour cell
- SN-38 is released in and around the tumour
- SN-38 blocks topoisomerase I: DNA damage
- Tumour cell death
Indications
- Unresectable or metastatic triple-negative breast cancer, and hormone receptor-positive, HER2-negative breast cancer, after several prior systemic therapies. Breast cancer →
Adverse effects
Common
- Nausea, vomiting, diarrhoea, constipation
- Fatigue
- Hair loss
- Anaemia
- Decreased appetite
Contraindications
- Severe allergy to the drug
Key interactions
- UGT1A1 inhibitors
- Raise SN-38 exposure and toxicity; avoided when possible.
- UGT1A1 inducers
- Lower SN-38 exposure.
- Irinotecan
- Shares the same active compound (SN-38): toxicities add up.
What is monitored
- Complete blood count before each dose
- Bowel habit and hydration
- Infusion reactions during and after each dose
- UGT1A1 genotype when available or when toxicity is unexpected
Administration and safety
- Intravenous infusion only, never as a push; the patient is observed during and after each infusion.
- Premedication against infusion reactions and nausea is given as ordered.
- Hazardous drug: prepared and handled with chemotherapy precautions.
Pregnancy and breastfeeding
Avoid in pregnancy. Can harm the fetus; a pregnancy test is done and effective contraception is used during and after treatment, and breastfeeding is avoided.
Nursing care
- Check the neutrophil count before each dose and do not give it if the threshold set by the protocol is not met.
- Ask about the number of stools; early diarrhoea is reported at once.
- Watch for fever, chills or breathing difficulty during and after the infusion.
- Teaching: report fever and diarrhoea immediately, keep drinking fluids, use effective contraception.
Pharmacokinetics
- Absorption
- Intravenous infusion on set days of each cycle.
- Metabolism
- SN-38 is inactivated by glucuronidation through UGT1A1.
Test yourself
Think of the answer, then tap the question to see it.
Which antigen does sacituzumab govitecan target?
TROP-2, a surface protein of many epithelial cancers.
Which well-known chemotherapy shares sacituzumab govitecan's payload?
Irinotecan, whose active metabolite is SN-38.
What are the two boxed warnings of sacituzumab govitecan?
Severe neutropenia and severe diarrhoea.
Why does UGT1A1 matter for sacituzumab govitecan?
UGT1A1 inactivates SN-38; reduced activity raises the risk of neutropenia and diarrhoea.
Connections
← Back to the class: Antibody-drug conjugates (ADCs)
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Sacituzumab govitecan-hziy Injection: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); Sacituzumab Govitecan-hziy - NCI (National Cancer Institute, 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.