Actress Barbara Parkins, who starred in the motion picture, suggested that Warwick be considered to sing the film's theme song. The song was to be given to Judy Garland, who had been fired from the film. Warwick performed the song, and when the film became a success in the early weeks of 1968, her single of the film theme became a million-seller, peaking at #2 for four weeks on the Billboard Hot 100 in early 1968, #2 on the Cash Box Top 100 and #1 on the Record World chart. The song was the B-side of another million selling tune composed for Warwick by Burt Bacharach and Hal David, "I Say a Little Prayer," which hit the Billboard Hot 100 Top 5 in November 1967. The single would become one of the biggest double-sided hits of the rock era.
Warwick re-recorded a Pat Williams-arranged and Burt Bacharach-produced version of the theme at A&R Studios in New York because contractual restrictions from her home label, Scepter Records, would not allow her version from the film to be included in the 20th Century-Fox soundtrack album. The re-recorded version became a million-seller. The RIAA-certified Gold Scepter LP that contained the hit version of the song, Dionne Warwick in Valley of the Dolls, peaked at number six on the Billboard Top 10 Albums chart, and would remain on the chart for over a year.
In the UK "(Theme from) Valley of the Dolls" had a February 1968 release with "Zip-a-Dee-Doo-Dah" as the B-side, peaking at UK #28.