Bexatamig  (Synonyms: SAR-443579)

Bexatamig (SAR-443579) is a trifunctional natural killer cell engager targeting IL-3R α/CD123, NKp46/NCR1/CD335 and Fc gamma RIIIA/CD16a. Bexatamig forms a cytolytic synapse between natural killer cells and CD123-positive tumor cells. By activating natural killer cells to induce tumor cell death, Bexatamig effectively reduces the burden of CD123-positive acute myeloid leukemia (AML) blasts. Bexatamig has been granted FDA Fast Track designation, and is primarily investigated for relapsed or refractory acute myeloid leukemia, B-cell acute lymphoblastic leukemia, and high-risk myelodysplastic syndromes^[1][2].

VH-Vkappa-G1Fc-Fab

Human

Bexatamig exhibits strong in vitro antitumor activity against AML cell lines^[2].
Bexatamig reduces the number of CD123-positive AML blasts in ex vivo testing^[2].

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

Bexatamig exhibits super-dose proportional characteristics at low doses and linear characteristics at high doses; at a dose of up to 3000 mg/kg administered once weekly, the early immunogenicity incidence rate is 26%^[1].

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

3563  [NCBI] & 9437  [NCBI]

P26951 & O76036

ELISA, FACS, Functional assay

Unconjugated

The product can be reconstituted/diluted with sterile PBS or saline.

170.838 kDa

2871775-98-1

Liquid

Colorless to light yellow

[Bexatamig]

Shipping with dry ice.

Please refer to the lot-specific COA for specific buffer information.

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

• 
  VH-Vkappa-G1Fc-Fab

• 
  Immobilized IL-3R alpha/CD123 Protein, Human (HEK293, His, HY-P70468) can bind Bexatamig. The EC₅₀ for this effect is 37.04 ng/mL.
• 
  Immobilized NKp46/NCR1 Protein, Human (HEK293, His, HY-P77810) can bind Bexatamig. The EC₅₀ for this effect is 35.75 ng/mL.
• 
  Flow cytometric analysis of 1X10⁶ HepG2 cells labeling IL3RA with Bexatamig (HY-P990905, red). Cells were fixed with 4% paraformaldehyde. Then stained with the primary antibody at 1/200 for an hour at 4℃. AF488-conjugated Goat Anti-Human IgG H&L (AF488) (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG1 kappa Isotype Control (HY-P99001, blue) was used as the isotype control.

• [1]. Jongen-Lavrencic M, et al. 823O Preliminary pharmacokinetics (PK) and pharmacodynamic (PD) analysis of the CD123 NK cell engager (NKCE) SAR443579 in patients (pts) with relapsed or refractory acute myeloid leukemia (R/R AML), B cell acute lymphoblastic leukemia (B-ALL) or high risk-myelodysplasia (HR-MDS)[J]. Annals of Oncology, 2023, 34: S543-S544.

  [2]. Bajel A, et al. First-in-human study of the CD123 NK cell engager SAR443579 in relapsed or refractory acute myeloid leukemia, B-cell acute lymphoblastic leukemia or high risk-myelodysplasia: updated safety, efficacy, pharmacokinetics and pharmacodynamics[J]. Blood, 2023, 142: 3474.