Antibody-drug conjugates (ADCs) are efficacious drug delivery tools for tackling breast cancer (BC) through targeted delivery of anti-cancer agents to the tumor cells. The relative selectivity of the therapeutic antibody that targets cell surface antigens with higher expression profile in tumor than normal cells will increase the therapeutic window. The potency of the warhead or the cytotoxic payload has to be high in order for the ADC to be successful as only a small amount of antibodies reach the interior of the tumor cells. The advancement in linker technology has revolutionized the safety profile in terms of less inadvertent release of the anti-cancer drug in the blood plasma, enhanced the efficacy, and vastly improved the tolerability. With improvement in the design of the novel ADCs, many viable therapeutic options for breast cancer will emerge including non-immunogenic and highly selective monoclonal antibodies, stable polar or apolar cross-linkers and anti-cancer drugs that target specific mutations, gene addictions, and other therapeutic vulnerabilities. This may be employed as a single agent or in combination with chemo- or radio- or immunotherapies. Many ADCs are in clinical trials and hopefully the data will be promising in the near future. This brief review focuses on basic and newer trends in concepts involving ADC engineering to treat intractable cases of breast cancer.