Anti-LILRB1 Monoclonal Antibodies for Therapeutic and Diagnostic Use

LILRB1 expression on myeloid cells regulates both innate and adaptive immune responses. Researchers at UTHealth Houston and UTSW developed novel agonistic anti-LILRB1 monoclonal antibodies (mAbs) for autoimmune and inflammatory disease treatments, and novel antagonistic anti-LILRB1 mAbs for cancer immunotherapies.

Background

LILRB1, a member of the ITIM-containing LILR receptor family, plays critical roles in regulation of both innate and adaptive immunity. It is expressed on several types of immune cells, including NK cells, and acts as an immune checkpoint protein. LILRB1 expression in myeloid-derived suppressor cells (MDSCs) can promote tumor growth and result in a suppressive immune microenvironment for tumor progression and metastasis. Study shows that the percentage of LILRB1-expressing NK cells is significantly higher in patients with late-stage cancer or poor prognosis, and thus LILRB1 may be a molecular target for immunotherapy for these patients. On the other hand, activation of LILRB1 signaling using agonistic antibodies can reduce tissue inflammation and can be used for management of autoimmune diseases. Therefore, both agonistic and antagonistic human anti-LILRB1 mAbs have potentials to treatment different human diseases, including cancers and auto-immune diseases.

Significance and Impact

Researchers at UTHealth Houston and The University of Texas Southwestern Medical Center (UTSW) identified that the percentage of LILRB1-expressing NK cells is significantly higher in patients with late-stage cancer or poor prognosis, and thus LILRB1 may be a molecular target for immunotherapy for these patients.  They further developed both agonistic and antagonistic humanized anti-LILRB1 mAbs. They also demonstrated LILRB1 blockade via antagonistic anti-LILRB1 mAbs increased the tumoricidal activity of NK cells against several types of cancer cells, including multiple myeloma, leukemia, lymphoma and solid tumors, in vitro and in vivo.

Benefits/Technology Advantages

•LILRB1 is highly expressed on NK cells from the peripheral blood of patients with multiple myeloma and prostate cancer.
•LILRB1 blockade via antagonistic anti-LILRB1 mAbs stimulated cytotoxic activity of NK cells against multiple myeloma, leukemia, lymphoma and solid tumors.
•LILRB1 blockade and NKG2D activation synergistically stimulated IFN-γ secretion from NK cells.

Related Publications

Heyu Chen et al. J. Immunother. Cancer. 2020. doi: 10.1136/jitc-2019-000515.

Intellectual Property Status
Published PCT application: PCT/US2021/043128
Nationalized in US, CN, HK, and EP
Available for licensing.
About the Inventors
Vice President of Drug Discovery at UTHealth Houston
Professor at UTHealth Houston and Co-Director of the CPRIT Core for Advanced Cancer Antibody Drug Modalities
Professor in Oncology at UTSW
Patent Information: