ANTI-PD-1 ANTIBODIES AND METHODS OF USE

Smart overview of the Invention

The patent application introduces binding molecules specifically designed to target programmed cell death protein 1 (PD-1). These molecules effectively block interactions between PD-1 and its ligands, programmed death-ligand 1 and 2 (PD-L1 and PD-L2). This mechanism is crucial for enhancing immune responses against cancer cells, as tumor cells often exploit PD-L1/L2 to evade immune detection.

The application details the composition of these binding molecules, which include variable heavy and light chain complementarity-determining regions (CDRs). These CDRs are specified with precise amino acid sequences, allowing for variations with one to two amino acid substitutions. The sequences are organized according to the Kabat numbering system, ensuring clarity and consistency in the description of these molecular structures.

The binding molecules are described as monoclonal antibodies or fragments thereof, with some embodiments being fully human and comprising different IgG isotypes. The antibodies are engineered to bind specific regions of human PD-1, enhancing their specificity and effectiveness. This binding action not only blocks PD-1 interactions but also potentially activates the immune system, providing a robust therapeutic approach against cancer.

Additionally, the patent outlines the creation of polynucleotides encoding these binding molecules, vectors containing these polynucleotides, and pharmaceutical compositions incorporating these elements. These compositions are carefully formulated, with specified concentrations of active ingredients and excipients, such as L-histidine, mannitol, sucrose, and polysorbate-80, to ensure stability and efficacy.

The application emphasizes the therapeutic potential of these compositions in cancer treatment, offering methods for administration and combination with other therapeutic agents. The figures included illustrate the selection strategy for anti-PD-1 antibodies and demonstrate their binding efficacy, providing visual support for the described innovations.