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Gunstar Heroes is a side scrolling shooter. The player has four weapons to choose from, and they can be combined in various pairs to create a total of 14 unique weapons. In addition to the weapons, the player can engage enemies in close quarters combat. It is possible to grab and toss enemies, perform sliding and jumping attacks and a long-range skid.

Unlike most games in the genre, the player has a life total calculated in numbers. Therefore, death to a player requires multiple hits but just one death will issue the option to continue or to end the game.
The main highlight of the game are its boss encounters, which often feature large enemies made up of multiple sprites allowing for fluid movement.

The original game was released at the same time as the soundtrack, and also contained music from the Gameboy Advance version of the game (Gunstar Super Heroes).

On February 23, 2006, Gunstar Heroes was released as part of the Gunstar Heroes: Treasure Box Collection for the PlayStation 2. It is also available on the Nintendo Wii's Virtual Console and in 2009 it was released on June 10th for Xbox Live Arcade and June 11th for PlayStation Network.