GI-101A (GI Innovation)

GI-101A is a bispecific Fc fusion protein developed by GI Innovation, Inc. for the treatment of advanced or metastatic solid tumors, including cervical cancer, urothelial carcinoma, clear cell renal cell carcinoma, and non-small cell lung cancer. It is an optimized formulation of its predecessor, GI-101, designed for improved manufacturing consistency. The molecule consists of a CD80 ectodomain and a modified interleukin-2 variant (IL-2v) linked via a human IgG4 Fc region. GI-101A functions through a triple-targeting mechanism: the CD80 component acts as a checkpoint inhibitor by binding to CTLA-4, while the IL-2v component selectively stimulates cytotoxic T cells and natural killer (NK) cells by binding to the IL-2 receptor beta subunit, while simultaneously suppressing regulatory T cells (Tregs). It is currently being evaluated in Phase 1/2 clinical trials as a monotherapy and in combination with pembrolizumab or lenvatinib.