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Future Oncol ; 15(32): 3675-3682, 2019 Nov.
Article in English | MEDLINE | ID: mdl-31513453

ABSTRACT

The aromatase inhibitor letrozole (Femar®/Femara®) and the aromatase inactivator exemestane (Aromasin®) differ in their biochemical effect on the aromatase enzyme. Letrozole is a competitive aromatase inhibitor while exemestane binds irreversibly to the aromatase enzyme. This pharmacological difference is of clinical interest since a lack of cross-resistance has been documented. It has been demonstrated in several clinical trials that exemestane may cause a disease regression following resistance to nonsteroidal aromatase inhibitors. The exact mechanism(s) behind this phenomenon is yet unknown. Here, we present the NEOLETEXE trial with the aim of exploring the individual mechanisms involved behind the observed lack of cross resistance. Clinical trial registration: The trial has been approved by the Regional Ethics Committee of South-East Norway (project number 2015/84).


Subject(s)
Antineoplastic Agents , Antineoplastic Combined Chemotherapy Protocols , Aromatase Inhibitors , Breast Neoplasms/drug therapy , Drug Resistance, Neoplasm/drug effects , Androstadienes/administration & dosage , Androstadienes/pharmacology , Androstadienes/therapeutic use , Antineoplastic Agents/pharmacology , Antineoplastic Agents/therapeutic use , Antineoplastic Combined Chemotherapy Protocols/pharmacology , Antineoplastic Combined Chemotherapy Protocols/therapeutic use , Aromatase Inhibitors/pharmacology , Aromatase Inhibitors/therapeutic use , Breast Neoplasms/pathology , Breast Neoplasms/surgery , Cross-Over Studies , Drug Administration Schedule , Estradiol/blood , Female , Humans , Letrozole/administration & dosage , Letrozole/pharmacology , Letrozole/therapeutic use , Neoadjuvant Therapy , Postmenopause , Receptor, ErbB-2/metabolism , Receptors, Estrogen/metabolism
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