Basal cell carcinoma (BCC) is the most common non-melanoma skin cancer, and its incidence continues to rise. Current management options are numerous and focus on tumour eradication while maximising cosmetic and functional capacity. Although surgery continues to be considered the main treatment modality, new pharmacological agents, such as immunomodulators, topical chemotherapeutic agents and photodynamic therapy, have emerged and show promising results. Pharmacological agents offer the potential for lower morbidity and improved tissue preservation compared with surgery and radiotherapy. However, pharmacological treatments possess higher failure rates when compared with surgery, and most studies have investigated only low-risk lesions. Several prospective, randomised, double-blind, vehicle-controlled studies have established the efficacy of imiquimod for superficial BCC. This review summarises the evidence regarding the mechanism, efficacy and safety of pharmacological agents based on the literature from the past 10 years. Experimental treatments that have been successfully utilised in the treatment of BCC are also discussed. Treatment of BCC with other agents, such as tazarotene, glycoalkaloid (BEC-5) cream, cidofovir and calcium dobesilate have been reported, but further studies are needed to ascertain the efficacy and adverse-effect profiles of these treatments.