Peringatan Keamanan

Toxicity information regarding sacituzumab govitecan is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as neutropenia, diarrhea, hypersensitivity, nausea/vomiting, and other systemic effects related to cytotoxic drugs. Symptomatic and supportive measures are recommended.L13002

Sacituzumab govitecan

DB12893

biotech approved investigational

Deskripsi

Metastatic triple-negative breast cancer (mTNBC) is an aggressive form of breast cancer with limited treatment options involving cytotoxic chemotherapy agents.A193653 Targeted chemotherapy through the application of antibody-conjugated agents (ADCs) is a recent advance in cancer treatment.A193671 One such ADC is sacituzumab govitecan, which combines a humanized anti-trophoblast cell-surface antigen 2 (TROP-2) antibody with the topoisomerase I inhibitor SN-38.L13002, A193674

Sacituzumab govitecan was granted FDA approval on April 22nd, 2020 and is marketed under the brand name Trodelvy™ by Immunomedics, Inc.; it is currently indicated under accelerated approval for the treatment of mTNBC patients who have undergone two or more prior therapies. As a targeted cytotoxic agent, it is hoped to provide similar efficacy with reduced adverse effects.A193653 In November 2021 and July 20 2023, sacituzumab govitecan was also approved by the European Commission and Health Canada respectively.L39372,L47601

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Sacituzumab govitecan has a mean half-life of 16 hours, while free SN-38 has a mean half-life of 18 hours.[L13002, A193731]
Volume Distribusi Sacituzumab govitecan has a mean volume of distribution of 0.045 L/kg.[L13002]
Klirens (Clearance) Sacituzumab govitecan has a clearance rate of 0.002 L/h/kg.[L13002]

Absorpsi

In patients receiving 10 mg/kg sacituzumab govitecan the Cmax of the conjugate was 243,000 ± 45,600 ng/mL while the Cmax of free SN-38 was 127 ± 60 ng/mL. Similarly, the AUC0-168 for the conjugate/free SN-38 was 5,210,000 ± 1,230,000 and 3,900 ± 1,830 ng\*h/mL, respectively.L13002

Metabolisme

The metabolism of sacituzumab govitecan has not been extensively studied. The SN-38 moiety is known to undergo O-glucuronidation by UGT1A1, presumably in the liver, and the SN-38 glucuronide metabolite SN-38G is found in the serum of patients undergoing treatment.L13002, A193665

Rute Eliminasi

No detailed information exists for sacituzumab govitecan elimination; renal elimination of SN-38 is known to be minimal, and it is expected that the fecal route will be the major contributor.L13002, A193665

Interaksi Obat

460 Data
Diethylstilbestrol Diethylstilbestrol may increase the thrombogenic activities of Sacituzumab govitecan.
Chlorotrianisene Chlorotrianisene may increase the thrombogenic activities of Sacituzumab govitecan.
Conjugated estrogens Conjugated estrogens may increase the thrombogenic activities of Sacituzumab govitecan.
Estrone Estrone may increase the thrombogenic activities of Sacituzumab govitecan.
Estradiol Estradiol may increase the thrombogenic activities of Sacituzumab govitecan.
Dienestrol Dienestrol may increase the thrombogenic activities of Sacituzumab govitecan.
Mestranol Mestranol may increase the thrombogenic activities of Sacituzumab govitecan.
Estriol Estriol may increase the thrombogenic activities of Sacituzumab govitecan.
Estrone sulfate Estrone sulfate may increase the thrombogenic activities of Sacituzumab govitecan.
Quinestrol Quinestrol may increase the thrombogenic activities of Sacituzumab govitecan.
Hexestrol Hexestrol may increase the thrombogenic activities of Sacituzumab govitecan.
Tibolone Tibolone may increase the thrombogenic activities of Sacituzumab govitecan.
Synthetic Conjugated Estrogens, A Synthetic Conjugated Estrogens, A may increase the thrombogenic activities of Sacituzumab govitecan.
Synthetic Conjugated Estrogens, B Synthetic Conjugated Estrogens, B may increase the thrombogenic activities of Sacituzumab govitecan.
Polyestradiol phosphate Polyestradiol phosphate may increase the thrombogenic activities of Sacituzumab govitecan.
Esterified estrogens Esterified estrogens may increase the thrombogenic activities of Sacituzumab govitecan.
Zeranol Zeranol may increase the thrombogenic activities of Sacituzumab govitecan.
Equol Equol may increase the thrombogenic activities of Sacituzumab govitecan.
Promestriene Promestriene may increase the thrombogenic activities of Sacituzumab govitecan.
Methallenestril Methallenestril may increase the thrombogenic activities of Sacituzumab govitecan.
Epimestrol Epimestrol may increase the thrombogenic activities of Sacituzumab govitecan.
Moxestrol Moxestrol may increase the thrombogenic activities of Sacituzumab govitecan.
Estradiol acetate Estradiol acetate may increase the thrombogenic activities of Sacituzumab govitecan.
Estradiol benzoate Estradiol benzoate may increase the thrombogenic activities of Sacituzumab govitecan.
Estradiol cypionate Estradiol cypionate may increase the thrombogenic activities of Sacituzumab govitecan.
Estradiol valerate Estradiol valerate may increase the thrombogenic activities of Sacituzumab govitecan.
Biochanin A Biochanin A may increase the thrombogenic activities of Sacituzumab govitecan.
Formononetin Formononetin may increase the thrombogenic activities of Sacituzumab govitecan.
Estetrol Estetrol may increase the thrombogenic activities of Sacituzumab govitecan.
Cetuximab The risk or severity of adverse effects can be increased when Cetuximab is combined with Sacituzumab govitecan.
Human immunoglobulin G The risk or severity of adverse effects can be increased when Human immunoglobulin G is combined with Sacituzumab govitecan.
Omalizumab The risk or severity of adverse effects can be increased when Omalizumab is combined with Sacituzumab govitecan.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Sacituzumab govitecan.
Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Sacituzumab govitecan.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Sacituzumab govitecan.
Indium In-111 satumomab pendetide The risk or severity of adverse effects can be increased when Indium In-111 satumomab pendetide is combined with Sacituzumab govitecan.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Sacituzumab govitecan.
Trastuzumab The risk or severity of adverse effects can be increased when Trastuzumab is combined with Sacituzumab govitecan.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Sacituzumab govitecan.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Sacituzumab govitecan.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Sacituzumab govitecan.
Digoxin Immune Fab (Ovine) The risk or severity of adverse effects can be increased when Digoxin Immune Fab (Ovine) is combined with Sacituzumab govitecan.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Sacituzumab govitecan.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Sacituzumab govitecan.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Sacituzumab govitecan.
Capromab pendetide The risk or severity of adverse effects can be increased when Capromab pendetide is combined with Sacituzumab govitecan.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Sacituzumab govitecan.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Sacituzumab govitecan.
Natalizumab The risk or severity of adverse effects can be increased when Natalizumab is combined with Sacituzumab govitecan.
Palivizumab The risk or severity of adverse effects can be increased when Palivizumab is combined with Sacituzumab govitecan.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Sacituzumab govitecan.
Bevacizumab The risk or severity of adverse effects can be increased when Bevacizumab is combined with Sacituzumab govitecan.
Technetium Tc-99m arcitumomab The risk or severity of adverse effects can be increased when Technetium Tc-99m arcitumomab is combined with Sacituzumab govitecan.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Sacituzumab govitecan.
Panitumumab The risk or severity of adverse effects can be increased when Panitumumab is combined with Sacituzumab govitecan.
Ranibizumab The risk or severity of adverse effects can be increased when Ranibizumab is combined with Sacituzumab govitecan.
Galiximab The risk or severity of adverse effects can be increased when Galiximab is combined with Sacituzumab govitecan.
Pexelizumab The risk or severity of adverse effects can be increased when Pexelizumab is combined with Sacituzumab govitecan.
Afelimomab The risk or severity of adverse effects can be increased when Afelimomab is combined with Sacituzumab govitecan.
Epratuzumab The risk or severity of adverse effects can be increased when Epratuzumab is combined with Sacituzumab govitecan.
Bectumomab The risk or severity of adverse effects can be increased when Bectumomab is combined with Sacituzumab govitecan.
Oregovomab The risk or severity of adverse effects can be increased when Oregovomab is combined with Sacituzumab govitecan.
IGN311 The risk or severity of adverse effects can be increased when IGN311 is combined with Sacituzumab govitecan.
Adecatumumab The risk or severity of adverse effects can be increased when Adecatumumab is combined with Sacituzumab govitecan.
Labetuzumab The risk or severity of adverse effects can be increased when Labetuzumab is combined with Sacituzumab govitecan.
Matuzumab The risk or severity of adverse effects can be increased when Matuzumab is combined with Sacituzumab govitecan.
Fontolizumab The risk or severity of adverse effects can be increased when Fontolizumab is combined with Sacituzumab govitecan.
Bavituximab The risk or severity of adverse effects can be increased when Bavituximab is combined with Sacituzumab govitecan.
CR002 The risk or severity of adverse effects can be increased when CR002 is combined with Sacituzumab govitecan.
Rozrolimupab The risk or severity of adverse effects can be increased when Rozrolimupab is combined with Sacituzumab govitecan.
Girentuximab The risk or severity of adverse effects can be increased when Girentuximab is combined with Sacituzumab govitecan.
Obiltoxaximab The risk or severity of adverse effects can be increased when Obiltoxaximab is combined with Sacituzumab govitecan.
XTL-001 The risk or severity of adverse effects can be increased when XTL-001 is combined with Sacituzumab govitecan.
NAV 1800 The risk or severity of adverse effects can be increased when NAV 1800 is combined with Sacituzumab govitecan.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Sacituzumab govitecan.
Otelixizumab The risk or severity of adverse effects can be increased when Otelixizumab is combined with Sacituzumab govitecan.
AMG 108 The risk or severity of adverse effects can be increased when AMG 108 is combined with Sacituzumab govitecan.
Iratumumab The risk or severity of adverse effects can be increased when Iratumumab is combined with Sacituzumab govitecan.
Enokizumab The risk or severity of adverse effects can be increased when Enokizumab is combined with Sacituzumab govitecan.
Ramucirumab The risk or severity of adverse effects can be increased when Ramucirumab is combined with Sacituzumab govitecan.
Farletuzumab The risk or severity of adverse effects can be increased when Farletuzumab is combined with Sacituzumab govitecan.
Veltuzumab The risk or severity of adverse effects can be increased when Veltuzumab is combined with Sacituzumab govitecan.
Ustekinumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Sacituzumab govitecan.
Trastuzumab emtansine The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Sacituzumab govitecan.
PRO-542 The risk or severity of adverse effects can be increased when PRO-542 is combined with Sacituzumab govitecan.
TNX-901 The risk or severity of adverse effects can be increased when TNX-901 is combined with Sacituzumab govitecan.
Inotuzumab ozogamicin The risk or severity of adverse effects can be increased when Inotuzumab ozogamicin is combined with Sacituzumab govitecan.
RI 624 The risk or severity of adverse effects can be increased when RI 624 is combined with Sacituzumab govitecan.
Stamulumab The risk or severity of adverse effects can be increased when MYO-029 is combined with Sacituzumab govitecan.
CT-011 The risk or severity of adverse effects can be increased when CT-011 is combined with Sacituzumab govitecan.
Leronlimab The risk or severity of adverse effects can be increased when Leronlimab is combined with Sacituzumab govitecan.
Glembatumumab vedotin The risk or severity of adverse effects can be increased when Glembatumumab vedotin is combined with Sacituzumab govitecan.
Olaratumab The risk or severity of adverse effects can be increased when Olaratumab is combined with Sacituzumab govitecan.
IPH 2101 The risk or severity of adverse effects can be increased when IPH 2101 is combined with Sacituzumab govitecan.
TB-402 The risk or severity of adverse effects can be increased when TB-402 is combined with Sacituzumab govitecan.
Caplacizumab The risk or severity of adverse effects can be increased when Caplacizumab is combined with Sacituzumab govitecan.
IMC-1C11 The risk or severity of adverse effects can be increased when IMC-1C11 is combined with Sacituzumab govitecan.
Eldelumab The risk or severity of adverse effects can be increased when Eldelumab is combined with Sacituzumab govitecan.
Lumiliximab The risk or severity of adverse effects can be increased when Lumiliximab is combined with Sacituzumab govitecan.
Canakinumab The risk or severity of adverse effects can be increased when Canakinumab is combined with Sacituzumab govitecan.

Target Protein

Tumor-associated calcium signal transducer 2 TACSTD2
DNA topoisomerase 1 TOP1
Far upstream element-binding protein 1 FUBP1

Referensi & Sumber

Synthesis reference: Cardillo TM, Govindan SV, Sharkey RM, Trisal P, Goldenberg DM: Humanized anti-Trop-2 IgG-SN-38 conjugate for effective treatment of diverse epithelial cancers: preclinical studies in human cancer xenograft models and monkeys. Clin Cancer Res. 2011 May 15;17(10):3157-69. doi: 10.1158/1078-0432.CCR-10-2939. Epub 2011 Mar 3.
Artikel (PubMed)
  • PMID: 30507322
    Zangardi ML, Spring LM, Nagayama A, Bardia A: Sacituzumab for the treatment of triple-negative breast cancer: the poster child of future therapy? Expert Opin Investig Drugs. 2019 Feb;28(2):107-112. doi: 10.1080/13543784.2019.1555239. Epub 2018 Dec 17.
  • PMID: 8253531
    Stein R, Basu A, Chen S, Shih LB, Goldenberg DM: Specificity and properties of MAb RS7-3G11 and the antigen defined by this pancarcinoma monoclonal antibody. Int J Cancer. 1993 Dec 2;55(6):938-46. doi: 10.1002/ijc.2910550611.
  • PMID: 7493360
    Shih LB, Xuan H, Aninipot R, Stein R, Goldenberg DM: In vitro and in vivo reactivity of an internalizing antibody, RS7, with human breast cancer. Cancer Res. 1995 Dec 1;55(23 Suppl):5857s-5863s.
  • PMID: 29989029
    Goldenberg DM, Stein R, Sharkey RM: The emergence of trophoblast cell-surface antigen 2 (TROP-2) as a novel cancer target. Oncotarget. 2018 Jun 22;9(48):28989-29006. doi: 10.18632/oncotarget.25615. eCollection 2018 Jun 22.
  • PMID: 31415916
    Bailly C: Irinotecan: 25 years of cancer treatment. Pharmacol Res. 2019 Oct;148:104398. doi: 10.1016/j.phrs.2019.104398. Epub 2019 Aug 12.
  • PMID: 29031818
    Khageh Hosseini S, Kolterer S, Steiner M, von Manstein V, Gerlach K, Trojan J, Waidmann O, Zeuzem S, Schulze JO, Hahn S, Steinhilber D, Gatterdam V, Tampe R, Biondi RM, Proschak E, Zornig M: Camptothecin and its analog SN-38, the active metabolite of irinotecan, inhibit binding of the transcriptional regulator and oncoprotein FUBP1 to its DNA target sequence FUSE. Biochem Pharmacol. 2017 Dec 15;146:53-62. doi: 10.1016/j.bcp.2017.10.003. Epub 2017 Oct 13.
  • PMID: 30931493
    Ponde N, Aftimos P, Piccart M: Antibody-Drug Conjugates in Breast Cancer: a Comprehensive Review. Curr Treat Options Oncol. 2019 Apr 1;20(5):37. doi: 10.1007/s11864-019-0633-6.
  • PMID: 21372224
    Cardillo TM, Govindan SV, Sharkey RM, Trisal P, Goldenberg DM: Humanized anti-Trop-2 IgG-SN-38 conjugate for effective treatment of diverse epithelial cancers: preclinical studies in human cancer xenograft models and monkeys. Clin Cancer Res. 2011 May 15;17(10):3157-69. doi: 10.1158/1078-0432.CCR-10-2939. Epub 2011 Mar 3.
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Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Trodelvy
    Powder, for solution • 180 mg/1 • Intravenous • US • Approved
  • Trodelvy
    Injection, powder, for solution • 200 mg • Intravenous • EU • Approved
  • Trodelvy
    Powder, for solution • 180 mg / vial • Intravenous • Canada • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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