Ficerafusp alfa  (Synonyms: BCA-101; FMAB2)

Ficerafusp alfa (BCA-101) is a bispecific antibody targeting EGFR and TGFβ, with a K_d of 2.58 nM against EGFR and a K_d of 61.3 nM against TGFβ1. Ficerafusp alfa binds to EGFR, inhibits EGFR phosphorylation, blocks EGF-dependent cell proliferation, and mediates antibody-dependent cellular cytotoxicity against EGFR-positive tumor cells. Ficerafusp alfa sequesters TGFβ via its TGFβRII ECD domain, neutralizes the activity of TGFβ and TGFβ1, and blocks TGFβ-dependent processes, including epithelial-mesenchymal transition, cell invasion, and differentiation of inducible regulatory T cells. Ficerafusp alfa is applicable to research related to head and neck squamous cell carcinoma, advanced solid tumors, squamous non-small cell lung cancer, anal squamous cell carcinoma, colorectal cancer, and pancreatic cancer^[1][2][3].

IgG1-kappa-[PROTEIN]2-in-VK

Human IgG1 kappa, Isotype Control

Human

ERBB1/EGFR/HER1

Ficerafusp alfa (BCA-101) (56 nM; 120 hours) inhibits and reverts TGFβ-induced epithelial-to-mesenchymal transition in A549 cells, as measured by reduced IL11 secretion^[1].
In ELISA, Ficerafusp alfa is captured by plate-bound EGFR and the ability of Ficerafusp alfa to bind TGFβ as measured by spiking TGFβ followed by detection by a biotinylated anti-TGFβ antibody. Ficerafusp alfa shows a dose-dependent binding with an EC₅₀ of 0.09 nM, indicating both the anti-EGFR and TGFβ trap arms are simultaneously functional^[1].
Ficerafusp alfa could neutralize SMAD-mediated luciferase expression induced by TGFβ1 (EC₅₀ of 1.49 nM) and TGFβ3 (EC₅₀ of 3.51 nM), and not neutralize TGFβ2 in HEK-SMAD reporter assay^[1].

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

Ficerafusp alfa (1-50 mg/kg; i.p.; twice a week) exhibits potent, sustained antitumor efficacy in squamous cell carcinoma xenografts^[1].
Ficerafusp alfa (10 mg/kg; i.p.; twice a week) induces durable tumor regression and delayed relapse in head and neck squamous cell carcinoma patient-derived xenograft models^[1].
Ficerafusp alfa (50 mg/kg; i.p.; twice a week) enhances the antitumor efficacy of anti-PD1 immunotherapy in a syngeneic human EGFR-expressing melanoma model, producing superior event-free survival compared with monotherapies^[1].
Ficerafusp alfa (10 mg/kg; i.p.; twice a week) synergizes with Pembrolizumab (HY-P9902) to produce enhanced antitumor efficacy in a humanized prostate cancer xenograft model, with a TGI of 78% on day 18^[1].
Ficerafusp alfa (5 mg/kg; i.v.; single dose) systemically neutralizes TGFβ1 in BALB/c mice, suppressing levels below detection for 4 days^[1].
Ficerafusp alfa (10 mg/kg; i.p.; thrice weekly; 27 days) delivers sustained tumor growth delay in head and neck squamous cell carcinoma PDX models in female NOG mice and neutralizes 90% of tumor TGFβ^[3].
Ficerafusp alfa (i.p.; six total doses) enhances the antitumor efficacy of PD-1 blockade (Pembrolizumab dosed at 10 mg/kg Q5Dx5) in PC-3 xenografts in humanized Hu-NOG-EXL mice^[3].

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

1956  [NCBI]

P00533

ELISA, FACS, Functional assay

Unconjugated

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

178.105 kDa

2764727-44-6

Liquid

Colorless to light yellow

[Ficerafusp alfa]

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.

• 
  IgG1-kappa-[PROTEIN]2-in-VK

• 
  Immobilized EGFR Protein, Human (621a.a, HEK293, His, HY-P70613) can bind Ficerafusp alfa. The EC₅₀ for this effect is 8.521 ng/mL.

• [1]. Boreddy SR, et al. BCA101 Is a Tumor-Targeted Bifunctional Fusion Antibody That Simultaneously Inhibits EGFR and TGFβ Signaling to Durably Suppress Tumor Growth. Cancer Res. 2023;83(11):1883-1904.  [Content Brief]

  [2]. Hernando-Calvo A, et al. Phase I Clinical Trial of the Bifunctional EGFR/TGF-β Fusion Protein Ficerafusp Alfa (BCA101) Alone and in Combination with Pembrolizumab for Advanced Solid Tumors. Clin Cancer Res. 2025;31(22):4623-4632.  [Content Brief]

  [3].
  Author affiliations, et al. 874 Development of BCA101, a bifunctional antibody capable of simultaneously disabling EGFR and TGFβ signaling, as novel single-agent immunotherapy.