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DRUG:

Trodelvy (sacituzumab govitecan-hziy)

i
Other names: IMMU-132, IMMU132, IMMU 132, RS7-SN38, hMN14-SN38, TROP-2-SN-38, hRS7-SN38 antibody drug conjugate, hRS7-SN 38, anti-TROP-2-SN-38 conjugate, anti-TROP-2-SN-38, hRS7-CL2-SN-38, IMMU0132, GS-0132
Company:
Gilead
Drug class:
Topoisomerase I inhibitor, TROP-2-targeted antibody-drug conjugate
Related drugs:
1d
The Importance of 5-hmC Expression Loss in Diagnosis of Mesothelioma and the Relationship Between TROP2 Expression and Histomorphological Parameters in Mesotheliomas. (PubMed, Int J Surg Pathol)
No significant association was found between TROP2 expression and other histological parameters.ConclusionLoss of ≥50% nuclear 5-hmC is a sensitive and specific marker for distinguishing mesothelioma from RMH. High TROP2 expression in tumors with high mitotic figures and higher nuclear and tumor grade suggests these patients may benefit from sacituzumab govitecan therapy.
Journal
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TACSTD2 (Tumor Associated Calcium Signal Transducer 2)
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Trodelvy (sacituzumab govitecan-hziy)
4d
TROP2/claudin program mediates immune exclusion to impede checkpoint blockade in breast cancer. (PubMed, J Immunother Cancer)
This study defines a new mechanism of barrier-mediated immune exclusion in cancer controlled by TROP2-dependent tight junctions. This mechanism drives tumor progression but can be targeted via TROP2-directed therapy to activate antitumor immunity and enhance immunotherapy response.
Journal • Checkpoint inhibition • PD(L)-1 Biomarker • IO biomarker
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CD8 (cluster of differentiation 8) • CLDN7 (Claudin 7) • TACSTD2 (Tumor Associated Calcium Signal Transducer 2)
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Trodelvy (sacituzumab govitecan-hziy)
4d
Sequential Use of Trastuzumab Deruxtecan and Sacituzumab Govitecan in Patients with Breast Cancer: A Pharmacological Approach to Support the Clinical Rationale. (PubMed, Drugs)
By contrast, sacituzumab govitecan is a TROP-2-targeted ADC conjugated through a hydrolysable CL2A linker to SN-38, the active metabolite of irinotecan. Clinically, trastuzumab deruxtecan has shown substantial efficacy in both HER2-positive and HER2-low breast cancer, whereas sacituzumab govitecan has demonstrated efficacy across triple-negative and hormone receptor-positive/HER2-negative breast cancers. Collectively, these agents highlight how variations in target antigen, linker chemistry, and payload potency impact ADC activity, therapeutic index, and potential strategies for sequential treatment in advanced breast cancer.
Review • Journal
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HER-2 (Human epidermal growth factor receptor 2) • SLX4 (SLX4 Structure-Specific Endonuclease Subunit) • TACSTD2 (Tumor Associated Calcium Signal Transducer 2)
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HER-2 positive • HR positive • HER-2 negative • HR positive + HER-2 negative
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Enhertu (fam-trastuzumab deruxtecan-nxki) • irinotecan • Trodelvy (sacituzumab govitecan-hziy)
6d
New P1/2 trial
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor) • UGT1A1 (UDP glucuronosyltransferase family 1 member A1)
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Trodelvy (sacituzumab govitecan-hziy) • Neupogen (filgrastim)
6d
New P2 trial • Platinum sensitive
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BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • HRD (Homologous Recombination Deficiency)
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BRCA2 mutation • BRCA1 mutation • HRD
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Avastin (bevacizumab) • carboplatin • gemcitabine • pegylated liposomal doxorubicin • Trodelvy (sacituzumab govitecan-hziy) • Aybintio (bevacizumab biosimilar) • Vegzelma (bevacizumab-adcd) • Avzivi (bevacizumab-tnjn) • Myocet (non-pegylated liposomal doxorubicin) • Duomeisu (pegylated liposomal doxorubicin)
6d
Cost-Effectiveness Analysis of Sacituzumab Govitecan Versus Chemotherapy for the Treatment of Metastatic Triple-Negative Breast Cancer With Different Trophoblast Cell-Surface Antigen 2 Expression Levels in Chinese Mainland. (PubMed, Value Health Reg Issues)
In conclusion, although SG is clinically effective for mTNBC, its high cost makes it economically unfeasible in mainland China. A substantial price reduction is essential for it to become a viable option, enabling more patients to benefit from its therapeutic potential.
Journal • HEOR • Cost-effectiveness
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TACSTD2 (Tumor Associated Calcium Signal Transducer 2)
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Trodelvy (sacituzumab govitecan-hziy)
6d
Effectiveness, safety, and biomarker analysis of sacituzumab govitecan in Chinese metastatic breast cancer: a multicenter real-world study. (PubMed, Ther Adv Med Oncol)
In conclusion, SG showed similar effectiveness with ASCENT and TROPiCS-02 study in heavily pretreated Chinese MBC patients. Given the compromised effectiveness in patients with prior PD-1/PD-L1 inhibitors or PIK3CA mutation, future investigations are warranted to explore SG-based combination regimens or novel therapeutic strategies in the above population.
Journal • Real-world evidence • PD(L)-1 Biomarker • IO biomarker
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HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
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HR positive • HER-2 negative • PIK3CA mutation
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Trodelvy (sacituzumab govitecan-hziy)
7d
Sacituzumab Govitecan in Recurrent Glioblastoma (clinicaltrials.gov)
P2, N=32, Recruiting, The University of Texas Health Science Center at San Antonio | Trial completion date: Aug 2026 --> Feb 2028 | Trial primary completion date: Feb 2026 --> Feb 2027
Trial completion date • Trial primary completion date
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MGMT (6-O-methylguanine-DNA methyltransferase) • TACSTD2 (Tumor Associated Calcium Signal Transducer 2)
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IDH wild-type
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Trodelvy (sacituzumab govitecan-hziy)
10d
SURE-01: Sacituzumab Govitecan, Preceding Radical Cystectomy, in Treating Patients With Muscle-invasive Bladder Cancer (clinicaltrials.gov)
P2, N=44, Completed, IRCCS San Raffaele | Trial completion date: Jun 2025 --> Sep 2025 | Trial primary completion date: Jun 2025 --> Sep 2025 | Recruiting --> Completed
Trial completion • Trial completion date • Trial primary completion date
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cisplatin • irinotecan • Trodelvy (sacituzumab govitecan-hziy)
11d
Sacituzumab govitecan in Japanese participants with HR+/HER2- metastatic breast cancer: primary results from the phase II ASCENT-J02 study. (PubMed, Jpn J Clin Oncol)
Although the primary endpoint (ORR by IRC) was not met (P > .025), overall efficacy results were generally similar to TROPiCS-02, supporting access to SG in Japanese patients with HR+/HER2- mBC. Safety was consistent with the known and manageable SG safety profile.
P2 data • Journal
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HER-2 (Human epidermal growth factor receptor 2)
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HR positive • HER-2 negative • EGFR positive
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Trodelvy (sacituzumab govitecan-hziy)
13d
New P2 trial • IO biomarker
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Trodelvy (sacituzumab govitecan-hziy) • Cotelet (tagitanlimab)
14d
A Phase I/II Study of Sacituzumab Govitecan Plus Berzosertib in Small Cell Lung Cancer, Extra-Pulmonary Small Cell Neuroendocrine Cancer and Homologous Recombination-Deficient Cancers Resistant to PARP Inhibitors (clinicaltrials.gov)
P1/2, N=120, Recruiting, National Cancer Institute (NCI) | Trial completion date: Mar 2027 --> Mar 2029 | Trial primary completion date: Mar 2026 --> Mar 2028
Trial completion date • Trial primary completion date
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BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • HRD (Homologous Recombination Deficiency) • CDK12 (Cyclin dependent kinase 12) • BRCA (Breast cancer early onset) • CHEK2 (Checkpoint kinase 2) • RAD51B (RAD51 Paralog B) • BRIP1 (BRCA1 Interacting Protein C-terminal Helicase 1) • RAD51C (RAD51 paralog C) • RAD51D (RAD51 paralog D) • CHEK1 (Checkpoint kinase 1) • BARD1 (BRCA1 Associated RING Domain 1) • RAD54L (DNA Repair And Recombination Protein RAD54) • FANCL (FA Complementation Group L) • PPP2R2A (Protein Phosphatase 2, Regulatory Subunit B, Alpha)
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BRCA1 mutation • ATM mutation • PALB2 mutation • CDK12 mutation • CHEK2 mutation • BRIP1 mutation • RAD51C mutation • RAD51D mutation • RAD51B mutation • BARD1 mutation • CHEK1 mutation • RAD54L mutation
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berzosertib (M6620) • Trodelvy (sacituzumab govitecan-hziy)