Charlize Theron, the only child of Gerda (née Maritz) and Charles Theron, was born in Benoni, a city near Johannesburg in South Africa, on 7 August 1975 and grew up on her parents' farm outside the city area. Her father was from an Afrikaner family, a South African ethnic group, predominantly consisting of the Dutch settlers, along with some French Huguenot and German.

Danie Theron, an Afrikaner military leader of the Second Boer War, was her great-great-uncle. In her early days Charlize attended Putfontein Primary School, but suffered throughout her childhood due to jaundice and tooth problems, even her milk teeth had to be surgically removed and she did not have permanent teeth, until she was around ten. Nevertheless, at the tender age of 13, she was admitted to a boarding school and after that, began her studies at the National School of the Arts in Johannesburg. Unfortunately, although she grew up in South Africa as an only child , there was turmoil in her family. During a visit home, her mother retrieved her own handgun to shoot and kill her father on 21 June 1991, in self-defense, when he threatened both Charlize and her mother with his gun while drunk and then physically attacked her mother and fired at both of them. However, her mother faced no charges as the shooting was legally adjudged to have been self-defence.

Since her childhood, Charlize dreamt to be a dancer, but after she won a competition in Salerno, Italy, at the age 16, she moved to Milan, a global capital of fashion and design in Italy, with her mother and two years later, they moved to New York City, where she continued to work as a model and began attending the Joffrey Ballet School, aspiring to be a ballet dancer, until a knee injury ended her chances of a career in dance.

Eventually, with the intention to work in the film industry, she flew to Los Angeles in 1994, on an one-way ticket her mother bought for her; and initially lived in a motel for a few months with the $300 budget that her mother had given her. During those days, she often had to steal bread from a basket in a restaurant to survive and one day, while making a loud scene after a bank refused to cash a cheque from her mother because it was out-of-state and she was not an American citizen, she was discovered by John Crosby, a talent agent, who encashed the cheque for her and gave her his business card with a request to meet him.. Crosby introduced her to an acting school and she played her first non-speaking and uncredited film role with three seconds of screen time in the horror B-film Children of the Corn III: Urban Harvest (1995).

However, the next year, Charlize Theron got the opportunity to play the role of the hitwoman Helga Svelgen in 2 Days in the Valley (1996), followed by the role of Tina Powers in That Thing You Do! (1996), which helped to gain her favourable notice and paved the way for her first leading role in The Devil’s Advocate (1997), which is credited as her breakthrough film.

In the film, a courtroom drama with a Faustian horror story, she appeared as Mary Ann Lomax, the haunted wife of Kevin Lomax, an unusually successful lawyer, played by Keanu Reeves and proved her acting ability and versatility, which led to further substantial roles, which include the adventure film Mighty Joe Young (1998), in which portrayed the role of Jill Young, the friend and protector of a fifteen-feet tall giant mountain gorilla, named Joe. After that, she played the role of Candy Kendall, a woman seeking an abortion in World War II-era Maine, in The Cider House Rules (1999).

During the early 2000s, Charlize appeared as Ashley in the action thriller Reindeer Games (2000), the last film directed by John Frankenheimer, before his death in 2002; as Erica Soltz in the crime drama The Yards (2000); as Adele Invergordon, the beautiful girlfriend of Junuh in the sports film The Legend of Bagger Vance (2000), directed by Robert Redford; as Gwen Sunday in the drama film Men of Honor (2000): as Sara Deever in the romantic film Sweet November (2001); as Laura Kensington in the crime comedy film The Curse of the Jade Scorpion (2001); and the crime thriller Trapped (2002). Despite achieving only limited commercial success, those films helped Chaelize to be established as an actress.

The next year, Charlize appeared as Stella Bridger, a professional safe cracker in the box office successful film The Italian Job (2003), a remake of the 1969 British film of the same name, followed by her stunning performance in the crime drama Monster (2003), portraying serial killer Aileen Wuornos, a former prostitute who was executed in Florida in 2002 for killing six men and inflicting horrible violence on her victims before their death, in the late 1980s and early 1990s. Although she was almost unrecognisable in the film as she had to put on weight of around 14 kg, she was profusely acclaimed by the critics and commoners for her performance in the film, even the famous film critic Roger Ebert felt that she gave one of the greatest performances in the history of the cinema. For her portrayal of the character of the infamous serial killer in the film, she won the Academy Award for Best Actress as the first South African actor, along with the Golden Globe Award, as well as the Screen Actors Guild Award, Silver Bear in Berlin International Film Festival and a BAFTA nomination for Best Performance by an Actor in a Leading Role

After her glorious performance in Monster, Charlize appeared as Gilda Bessé, the young, rebellious and provocative heiress of a French champagne magnate, who storms into the quiet life of the timid Oxford undergraduate, in Head in the Clouds (2004), set in the backdrop of the ruinous Spanish Civil War and Adolf Hitler's rise to power, and also played the role of Brit Ekland, the Swedish actress and singer, in the HBO film The Life and Death of Peter Sellers (2004), for which she earned a nomination for the Golden Globe Award. In addition, she also earned nominations for the Academy, BAFTA and Golden Globe Awards, for portraying the role of Josey Aimes, a single mother and an iron mine worker experiencing sexual harassment, in the critically acclaimed drama North Country (2005).

Her subsequent films during the decade include the critically acclaimed crime drama In the Valley of Elah (2007), in which she appeared as a police detective, the role of the ex-wife of an alcoholic superhero, who faced a traumatic childhood in the superhero movie Hancock (2008), a reckless, slatternly mother in the drama film Sleepwalking (2008), a woman who faced a traumatic childhood in the drama The Burning Plain (2008) and the post-apocalyptic drama The Road (2009).

After a short break from the film industry, Charlize Theron returned to the spotlight in 2011 with the black comedy Young Adult (2011), and was nominated for a Golden Globe Award for her performance in the film as Mavis Gary, a thirty-seven-year-old, depressed divorced and alcoholic fiction writer, who returns to her hometown in pursuit of her high-school sweetheart. After that, she played the role of villain in two big-budget films for a change, and appeared as the evil mother of Snow White in Snow White and the Huntsman (2012) and as a crew member with a hidden agenda in the science fiction thriller Prometheus (2012). Her subsequent films during the decade include the western comedy film A Million Ways to Die in the West (2014), the crime drama Dark Places (2015), the little-seen romantic drama The Last Face (2016), the action thriller Atomic Blonde (2017), and the black comedy Tully (2018). For her performance as Megyn Kelly in Bombshell (2019) that revolves around the allegation of sexual harassment against Fox News CEO Roger Ailes, by former female employees, Charlize Theron won her third nomination for an Academy Award, along with nominations for a Golden Globe and BAFTA Award.

In her personal life Charlize Theron was in relationship was with actor Craig Bieko, whom she dated from 1995 to 1997 and after that, she was in a three-year relationship with singer Stephan until October 2001. In the same year, she began a relationship with Irish actor Stuart Townsend, whom she met on the set of Trapped and they lived together till they split up in 2009. Following the split in 2009, she began dating American actor Sean Penn in December 2013, but that relationship also ended in a split in June 2015. However, she has adopted a daughter in March 2012 and another daughter in July 2015.