title: Unravelling exemestane: From biology to clinical prospects.
abstract: Aromatase inhibitors (AIs) are anti-tumor agents used in clinic to treat hormone-dependent breast cancer. AIs block estrogens biosynthesis by inhibiting the enzyme aromatase, preventing tumor progression. Exemestane, a third-generation steroidal AI, belongs to this class of drugs and is currently used in clinic to treat postmenopausal women, due to its high efficacy and good tolerability. Here, its pharmacological and biological aspects as well as its clinical applications and comparison to other endocrine therapeutic agents, are reviewed. It is also focused the benefits and risks of exemestane, drawbacks to be overcome and aspects to be explored.
authors.affiliation: Faculty of Science and Technology, University of Coimbra, Calçada Martim de Freitas 3000-456 Coimbra, Portugal; UCIBIO-REQUIMTE, Laboratory of Biochemistry, Department of Biological Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge Viterbo Ferreira, no 228, 4050-313 Porto, Portugal.
authors.forename: Ana Filipa
authors.initials: AF
authors.lastname: Sobral
authors.affiliation: UCIBIO-REQUIMTE, Laboratory of Biochemistry, Department of Biological Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge Viterbo Ferreira, no 228, 4050-313 Porto, Portugal. Electronic address: cristinamaralibd@gmail.com.
authors.forename: Cristina
authors.initials: C
authors.lastname: Amaral
authors.affiliation: UCIBIO-REQUIMTE, Laboratory of Biochemistry, Department of Biological Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge Viterbo Ferreira, no 228, 4050-313 Porto, Portugal.
authors.forename: Georgina
authors.initials: G
authors.lastname: Correia-da-Silva
authors.affiliation: UCIBIO-REQUIMTE, Laboratory of Biochemistry, Department of Biological Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge Viterbo Ferreira, no 228, 4050-313 Porto, Portugal. Electronic address: natercia@ff.up.pt.
authors.forename: Natércia
authors.initials: N
authors.lastname: Teixeira
mesh_terms: D000077384:Anastrozole; D000730:Androstadienes / Q000378:metabolism / Q000627:therapeutic use*; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D017209:Apoptosis / Q000187:drug effects; D047072:Aromatase Inhibitors / Q000627:therapeutic use*; D001343:Autophagy / Q000187:drug effects; D001711:Biotransformation; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D059447:Cell Cycle Checkpoints / Q000187:drug effects; D045744:Cell Line, Tumor; D002986:Clinical Trials as Topic; D019008:Drug Resistance, Neoplasm; D005260:Female; D006801:Humans; D009570:Nitriles / Q000627:therapeutic use; D013629:Tamoxifen / Q000627:therapeutic use; D014230:Triazoles / Q000627:therapeutic use
chemical_list: D000730:Androstadienes; D000970:Antineoplastic Agents; D047072:Aromatase Inhibitors; D009570:Nitriles; D014230:Triazoles; D013629:Tamoxifen; D000077384:Anastrozole; C056516:exemestane; C542923:17-dihydroexemestane
keywords: Aromatase inhibitors; Clinical trials; Endocrine resistance; Endocrine therapy; Exemestane; Hormone-dependent breast cancer