Non-steroidal aromatase inhibitor

Dutasteride, however, is a so-called dual inhibitor with both 5α-R1 and 5α-R2 inhibition. IC50 for 5α-R1 is 7 nM but 6 nM for 5α-R2. As mentioned above, it reduces DHT > 90% overall, or precisely % and for intraprostatic DHT the reduction is 97-99%. Dutasteride has also been found to inhibit 5α-R3, in vitro, with IC50= nM. [18] The 2,5-difluorophenyl side chain on the D-ring of the compound shows significant lipophilic features and as increased lipophilicity enhances the potency of the compounds binding at pocket site, its potency is much greater than of finasteride. [25]

BRCA2 gene is located on chromosome 13q12 and also classified as a tumour suppressor gene; though shares no homology with the BRCA1 gene. However, it can bind with BRCA1 to participate in DNA damage response pathway. BRCA2 protein functions as a mediator of the core mechanism of homologous recombination. Its mutations are linked to breast carcinomas that are ER and PR positive.  Though rarely associated with basal-like phenotype but still linked to a higher grade (II or III) when compared to age-matched sporadic cases

Non-steroidal aromatase inhibitor

non-steroidal aromatase inhibitor


non-steroidal aromatase inhibitornon-steroidal aromatase inhibitornon-steroidal aromatase inhibitornon-steroidal aromatase inhibitornon-steroidal aromatase inhibitor