Recent advances in the management of epilepsy and obesity or obesity-related diseases have accounted for the carbonic anhydrase inhibitors becoming clinically used drugs. Although such diseases are not related to each other, they both share the human-expressed carbonic anhydrase (CA; EC 4.2.1.1) enzymes and some of their inhibitors, such as topiramate (TPM) and zonisamide (ZNS) as biologic targets and effective drugs, respectively. Herein we discuss the main features that have triggered appropriate medicinal chemistry-based experimental studies up to the validation of CAs for the management of such diseases. A combination therapy between TPM and phentermine (Qnexa/Qsymia) is currently marketed for the management of obesity and obesity-related diseases. Currently, the bupropion-ZNS slow-release compound, Empatic, is under FDA phase III clinical development for the same therapeutic application, confirming the great potential of CA as a drug target against obesity.
Carbonic anhydrase inhibitors for the treatment of epilepsy and obesity / Berrino, E.; Carta, F.. - (2019), pp. 311-329. [10.1016/B978-0-12-816476-1.00015-0].
Carbonic anhydrase inhibitors for the treatment of epilepsy and obesity
Berrino E.;
2019
Abstract
Recent advances in the management of epilepsy and obesity or obesity-related diseases have accounted for the carbonic anhydrase inhibitors becoming clinically used drugs. Although such diseases are not related to each other, they both share the human-expressed carbonic anhydrase (CA; EC 4.2.1.1) enzymes and some of their inhibitors, such as topiramate (TPM) and zonisamide (ZNS) as biologic targets and effective drugs, respectively. Herein we discuss the main features that have triggered appropriate medicinal chemistry-based experimental studies up to the validation of CAs for the management of such diseases. A combination therapy between TPM and phentermine (Qnexa/Qsymia) is currently marketed for the management of obesity and obesity-related diseases. Currently, the bupropion-ZNS slow-release compound, Empatic, is under FDA phase III clinical development for the same therapeutic application, confirming the great potential of CA as a drug target against obesity.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
