In 2005, Zyrus joined Little Big Star, a talent show in the Philippines loosely patterned after American Idol. Eliminated after the first performance, Zyrus was called back as a wildcard contender and eventually became one of the finalists. Although a consistent top scorer in the final rounds, Zyrus did not win the title in the finale, only placing third.
Having seen online videos, Ellen DeGeneres invited Zyrus to appear on her show. He flew to the United States for the first time and performed two songs on the December 19, 2007 episode: "I Will Always Love You" and "And I Am Telling You". Following this American debut, Zyrus made a second appearance on Star King on December 28 as the "Most Requested Foreign Act", performing Gloria Gaynor's "I Will Survive" and singing a duet with Lena Park. In January 2008, Zyrus was invited to Malacañan Palace to perform for President Gloria Macapagal-Arroyo.
A CD/DVD of this concert, including Zyrus' The Bodyguard medley, was released on November 11, 2008. The show was aired several times on PBS and other public television networks starting in December 2008 under the Great Performances banner. One of the Singers at the concert was Pempengco's idol, Andrea Bocelli. Bocelli subsequently expressed interest in performing a duet with Pempengco with an invitation to be a guest on his birthday concert "The Cinema Tribute" held on July 20 at the Teatro del Silenzio in his hometown of Lajatico, Tuscany, Italy. Aside from the solo performance, Zyrus sang a duet of "The Prayer" with the famous tenor in front of more than 8,000 people.
The first major concert for Zyrus was called Charice: The Journey Begins, presented to a sold-out crowd on June 27 at the SMX Convention Center, SM Mall of Asia in the Philippines. Guests included Christian Bautista, Kuh Ledesma and Little Big Star finalists. On June 28, 2009, in concert, Zyrus revealed a planned duet with legendary pop singer Michael Jackson, explaining that Jackson's Lawyer said that Michael had chosen Zyrus to be his special guest on his tour. Michael had seen videos of Zyrus dancing to his songs and said right away, "I want this kid". When announcing this, Jake said "Yesterday morning, we were all shocked by the very sad news, the legendary pop singer Michael Jackson has gone away. Only two more weeks I was supposed to be with him on stage. We were going to perform Billie Jean." Zyrus contributed to two Christmas albums in 2009, first as David Archuleta's duet partner for the song "Have Yourself a Merry Little Christmas" on his Christmas album, Christmas from the Heart, then contributing a rendition of "The Christmas Song" to the compilation album, A Very Special Christmas 7. Zyrus was one of the headlining acts on the David Foster and Friends 10-city North American Tour that ran during the fall of 2009, and made a cameo appearance in the feature film Alvin and the Chipmunks: The Squeakquel, released in North America on December 23. The official movie Soundtrack includes Zyrus' rendition of "No One" by Alicia Keys, accompanied by The Chipettes. Later in the month, Zyrus appeared on the grand finale of Singapore Idol as a guest, performing two signature songs, The Bodyguard medley and "Note to God".
Raised in the Iglesia ni Cristo faith, Zyrus and younger brother Carl were baptized and confirmed into their mother's Roman Catholic faith on May 22, 2010, 12 days after Zyrus's 18th birthday, at the Pasig Cathedral in Pasig, Metro Manila, Philippines. The more than 40 godparents included ABS-CBN network President Charo Santos-Concio, Producer Laurenti Dyogi, The Buzz hosts Boy Abunda and Kris Aquino, segment host and radio personality Jobert Sucaldito, TV Patrol news anchors Karen Davila and Julius Babao, and Star Records head Annabelle Regalado-Borja. Philippine Daily Inquirer columnists Emmie Velarde and Pocholo Concepcion were also included. Oprah Winfrey and David Foster, two principal sponsors who played a major role in Zyrus's ascent to international stardom, were unable to attend and instead sent their own representatives to the ceremony.
On October 2011, Zyrus' estranged Father, 40-year-old construction worker Ricky Pempengco, was stabbed to death in the Philippines, forcing the cancellation of a concert in Singapore. Ricky had been at a small grocery store in San Pedro, Laguna, a city south of Metro Manila, when he brushed against a drunk man who became angry and stabbed him with an ice pick in the chest and back, according to the Laguna province police chief. Zyrus responded to the stabbing on Twitter: "I want to thank my fans from around the world for their support and love at this very difficult time for my family and I." "We are all very sad about this terrible tragedy" and "I loved him and I will still love him"; "He's still my Dad after all."
On January 18, 2012, Zyrus launched a ten-city tour across Asia to promote the official release of the studio album, Infinity, due later in 2012; the tour began in March.
Zyrus' exploration on his gender identity was a subject of public interest. On March 2012, Zyrus faced harsh criticism from the Internet and the media after changing hairstyle and fashion into a self-described "edgy and rock" look, responding: "I know some people think that this is very rebellious but it's not. It's just me evolving." On April 16, 2013, questions were raised after pictures surfaced online of Zyrus in masculine dress. In an interview, mother Raquel Pempengco said that she would respect her child's decision about his own identity. On May 28, The Philippine Star newspaper ran a story about Zyrus's 21st birthday party which was described as a "coming out of sorts". On June 2, 2013, Zyrus said that he identified as lesbian at that time during an interview with Boy Abunda at The Buzz in the Philippines, mentioning past relationships with other women in the industry. Nine months later, in March 2014, Zyrus debuted a new "boyish" look with much shorter hair cut and more tattoos. In a 2014 interview with Oprah Winfrey, Zyrus mentioned being attracted to girls since childhood and said "basically, my soul is male", but denied plans to pursue gender transition at that time.
On February 2, 2014, it was announced that Zyrus would sing "Right Where I Belong" for the direct-to-DVD movie The Swan Princess: A Royal Family Tale. In interviews, Zyrus reported almost losing the role after publicly coming out as lesbian in 2013. Later in 2014, Zyrus appeared on the October 19 episode of Oprah: Where Are They Now?.
In April 2017, Zyrus broke up with Alyssa Quijano, after four years of living together. In June 2017, Zyrus announced the adopting of his current name and discontinued the use of Charice, a name he previously went by, on Twitter and Instagram. Subsequently, Zyrus disclosed that he had undergone removal of both breasts in March, and had begun testosterone shots in April. In an interview with Papermag, he said "I am always thankful for the life of Charice that I experienced and the music that I shared, but that obviously belongs to her, it's not for me. I'm letting her go and be free."
