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Table 1 β1-integrin inhibitors currently in preclinical or clinical development for cancer therapy

From: β1-integrins signaling and mammary tumor progression in transgenic mouse models: implications for human breast cancer

Drug or treatment

Type of therapeutic agent

Stage

Target

Tumor model

Reference

Clone AIIB2

Rat IgG1 mAb

Preclinical

β1-subunit

MCF-7 human breast cancer xenograft

[64]

Clone AIIB2 + ionizing radiation

Rat IgG1 mAb + radiotherapy

Preclinical

β1-subunit

MCF-7 human breast cancer xenograft

[102]

Clone 339.1

Rat IgG1 mAb

Preclinical

α5β1

SVR murine angiosarcoma and A673 human rhabdomyosarcoma xenografts

[95]

Volociximab

Chimeric (82% human/18% murine) IgG4 mAb

Preclinical

α5β1

Rabbit VX2 carcinoma model

[97]

  

Phase I

α5β1

Patients with advanced solid malignancies

[105]

  

Phase II

α5β1

Patients with platinum-resistant advanced epithelial ovarian cancer or primary peritoneal cancer

[96]

ATN-161

Small peptide antagonist

Preclinical

α5β1

MDA-MB-231 human breast xenograft and skeletal metastasis

[99]

  

Preclinical

α5β1

Lewis lung adenocarcinoma model

[98]

  

Phase I

α5β1

Patients with advanced solid malignancies

[106]

ATN-161 + 5-fl uorouracil

Small peptide antagonist + chemotherapy

Preclinical

α5β1

CT26 murine colorectal liver metastasis

[100]

  1. mAb, monoclonal antibody.