An anti-CTLA4 (cytotoxic T lymphocyte associated antigen 4) and anti-PD-1 (programmed cell death 1) bifunctional antibody, a pharmaceutical composition thereof and use thereof. Particularly, the anti-CTLA4 and anti-PD-1 bifunctional antibody comprises a first protein functional domain that targets PD-I and a second protein functional domain that targets CTLA4. The bifunctional antibody can bind toCTLA4 and PD-1 specifically, relieve immunosuppression of CTLA4 and PD-1 on an organism specifically, activate T lymphocytes, and thus has good application prospects.