1. Immunology/Inflammation
  2. CD20 CD3
  3. Glofitamab

Glofitamab  (Synonyms: RO7082859)

Cat. No.: HY-P99024

Glofitamab (RO7082859) is a T-cell-engaging bispecific antibody possessing a novel 2:1 structure with bivalency for CD20 on B cells and monovalency for CD3 on T cells. Glofitamab leads to T-cell activation, proliferation, and tumor cell killing upon binding to CD20 on malignant cells. Glofitamab induces durable complete remissions in relapsed or refractory B-Cell non-Hodgkin lymphoma (B-NHL).

For research use only. We do not sell to patients.

CAS No. : 2229047-91-8

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Description

Glofitamab (RO7082859) is a T-cell-engaging bispecific antibody possessing a novel 2:1 structure with bivalency for CD20 on B cells and monovalency for CD3 on T cells. Glofitamab leads to T-cell activation, proliferation, and tumor cell killing upon binding to CD20 on malignant cells. Glofitamab induces durable complete remissions in relapsed or refractory B-Cell non-Hodgkin lymphoma (B-NHL)[1][2][3][4].

Isotype

Human IgG1 kappa

Recommend Isotype Controls
Species

Humanized

In Vitro

Glofitamab (0.1 µg/mL, 48 h) stimulates the expression of 4-1BB (CD137) on CD8+ tumor-infiltrating lymphocyte (TILs) in the lymphoma tumor microenvironment (TMEs) and augmented diffuse large B cell lymphoma (DLBCL) cell death combined with either FAP-IL2v (HY-P99902) or FAP-4-1BBL[4].
Glofitamab (0.2-200 ng/mL, 16 h)-mediated DLBCL cell killing requires the formation of stable T effector cell-tumor cell synapses[5].
Glofitamab has no effect on the transient reduction in T-lymphocyte subsets, NK cells and monocytes by Obinutuzumab (HY-P9910) pretreatment (Gpt)[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Glofitamab (0.3-100 μg/kg, i.v., a single dose) induces a dose-dependent increase in cytokine levels (IL-1Ra, IL-2, IL-5, IL-6, IL-8, IL-10, G-CSF, IFN-γ and TNF-α) in Cynomolgus Monkeys[3].
Glofitamab (0.5 mg/kg, i.v., a single dose) induces early and lasting T cell engagement and activity in mice[5].

Pharmacokinetic parameters of Glofitamab (i.v., a single dose) in cynomolgus monkeys with or without Obinutuzumab (Gpt: 50 mg/kg) (MeSt: Mechanistic Study; MTD: Maximum Tolerated Dose)[3]

Study Gpt Dose (μg/kg) CL(mL/day/kg) Vc(mL/kg) T1/2 (days) Cmax (μg/mL) AUClast/dose(h·μg/mL/μg/kg)
MTD No 0.3 nd nd nd 0.00374/0.00663 nd
MTD No 1 nd 45.6/nd nd 0.0188/nd 0.0162/nd
MTD No 3 864/920 35.8/31.9 0.218/0.180 0.0704/0.0798 0.0218/0.0234
MTD No 10 735/656 26.7/24.6 0.143/0.159 0.318/0.354 0.0290/0.0339
MTD No 30 600/653 27.9/36.1 0.173/0.151 0.958/0.759 0.0397/0.0335
MTD No 100 190/290 34.9/41.6 0.203/0.113 2.74/2.29 0.126/0.0826
MeSt No 100 384±106 43.2±7.26 0.314±0.158 2.22±0.384 0.0679±0.0246
MeSt Yes 100 81.7±18.3 41.1±5.59 2.82±0.959 2.56±0.320 0.308±0.0773

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Cynomolgus Monkeys[3]
Dosage: 0.3-100 μg/kg
Administration: i.v., a single dose, collected samples for cytokine measurements predose, 4, 24, 96 and 168 h post-dosing
Result: Resulted in cytokine levels peaked at 4 h post dose, with levels returning to baseline after 96 h for most cytokines in Cynomolgus Monkeys.
Animal Model: NSG mice co-injected with WSU and DLCL2 tumor cells and HSC-NSG-derived T cells[5]
Dosage: 0.5 mg/kg
Administration: i.v., a single dose, imaged 24, 48 or 72 hours post treatment
Result: Resulted in a higher frequency and longer duration of T cell-tumor cell interactions in mice, not only at early, but also at late time points.
Clinical Trial
CAS No.
Appearance

Liquid

Color

Colorless to light yellow

SMILES

[Glofitamab]

Shipping

Shipping with dry ice.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Format
  • IgG1-kappa/lambda with domain crossover, trivalent
Biological Activity
  • Flow cytometry analysis of Jurkat cells labelling CD3 with Glofitamab at 200 nM (Red). Goat anti human IgG Fc (Alexa Fluor488) was used as the secondary antibody at 1/1000 dilution. Isotype control - human IgG (Blue). Unlabeled control - Unlabelled cells (Gray).
  • Flow cytometry analysis of Raji cells labelling CD20 with Glofitamab at 20 nM (Red). Goat anti human IgG Fc (Alexa Fluor488) was used as the secondary antibody at 1/1000 dilution. Isotype control - human IgG (Blue). Unlabeled control - Unlabelled cells (Gray).
Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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