Cancer, a highly deadly disease, necessitates safe, cost-effective, and readily accessible treatments to mitigate its impact. Theabrownin (THBR), a polyphenolic pigment found in Pu-erh tea, has garnered attention for its potential benefits in memory, liver health, and inflammation control. By observing different biological activities of THBR, recently researchers have unveiled THBR's promising anticancer properties across various human cancer types. By examining existing studies, it is evident that THBR demonstrates substantial potential in inhibiting cell proliferation and reducing tumour size with minimal harm to normal cells. These effects are achieved through the modulation of key molecular markers such as Bcl-2, Bax, various Caspases, Poly (ADP-ribose) polymerase cleavage (Cl-PARP), and zinc finger E box binding homeobox 1 (ZEB 1). This review aims to provide in-depth insights into THBR's role in cancer research. This review also elucidates the underlying anticancer mechanisms of THBR, offering promise as a novel anticancer drug to alleviate the global cancer burden.