Loncastuximab Tesirine

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CAS:1879918-31-6
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Products Intro: Product Name:Loncastuximab tesirine (ADC)
CAS:1879918-31-6
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Loncastuximab Tesirine Basic information
Product Name:Loncastuximab Tesirine
Synonyms:Loncastuximab Tesirine;Loncastuximab tesirine (ADC)
CAS:1879918-31-6
MF:
MW:0
EINECS:
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Mol File:Mol File
Loncastuximab Tesirine Structure
Loncastuximab Tesirine Chemical Properties
form Liquid
color Colorless to light yellow
Safety Information
MSDS Information
Loncastuximab Tesirine Usage And Synthesis
DescriptionLoncastuximab Tesirine (Zynlonta) is an antibody-drug conjugate (ADC) for the treatment of patients with relapsed or refractory diffuse large B-cell lymphoma (DLBCL).
UsesLoncastuximab tesirine is a human cluster of differentiation 19 (CD19)-directed antibody-drug conjugate (ADC). Once bound to CD19 on the cell membrane, loncastuximab tesirine is rapidly internalised and triggers cell death. Loncastuximab tesirin induces cell apoptosis, it can be used for the research of diffuse large B-cell lymphoma[1][2].
Mechanism of actionThe drug is composed of a humanized anti-CD19 monoclonal antibody coupled to a pyrrolobenzodiazepine (PBD) dimer toxin SG3199 (called tesirene). Loncastuximab Tesirine specifically binds to CD19-positive B cells through its antibody portion, then enters the cell through endocytosis, releasing tesirene, which exerts a cytotoxic effect by cross-linking with DNA.
Side effects Side effects of loncastuximab tesirine may include eye inflammation, thrombocytopenia, anemia, nausea, fatigue, fever and low blood pressure.
in vivo

Loncastuximab tesirine (0.25 or 0.5 mg/kg; single dose) shows anti-tumor effects in WSU-DLCL2 xenograft models[1]. Loncastuximab tesirine (0.33, 0.66, and 1 mg/kg; i.v. single dose) shows dose-dependently antitumor activity in Ramos xenograft models[2]. Loncastuximab tesirine (0.1 and 0.3 mg/kg; i.v. single dose) shows dose-dependently antitumor activity in CD19-expressing Daudi xenograft models[2]. Loncastuximab tesirine (0.3 and 1 mg/kg; i.v. single dose) results in significant, dose-dependent extension of survival in WSU-DLCL2 xenograft mouse models[2].

References[1] Nikoleta Sachini, et al. Combination of Loncastuximab Tesirine and Polatuzumab Vedotin Shows Increased Anti-Tumor Activity in Pre-Clinical Models of Non-Hodgkin Lymphoma. Blood. 2021.
[2] Zammarchi F, et al. ADCT-402, a PBD dimer-containing antibody drug conjugate targeting CD19-expressing malignancies. Blood. 2018 Mar 8;131(10):1094-1105. DOI:10.1182/blood-2017-10-813493
Loncastuximab Tesirine Preparation Products And Raw materials
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