Abstract: The present disclosure provides a method of treating cancer in a subject. The method including administering to the subject: a) a therapeutically effective amount of a monocarboxylate transporter (MCT) inhibitor alone; or in combination with b) a therapeutically effective amount of an immunotherapy agent, wherein the monocarboxylate transporter inhibitor is represent by Formula (I): or a pharmaceutically acceptable salt thereof, wherein subscript n, B, W, X, Y, Z, each A, each R1, and R2 are as provided herein. Also provided are a pharmaceutical composition thereof and a kit thereof for treating cancer in a subject.