Home Blog of Signal Transduction DNA Damage/DNA Repair PARP Review of second-generation androgen receptor inhibitor therapies and their role in prostate cancer management

Category

Archives

Popular Post

ESKM, a novel therapeutic agent for sensitive and resistant PH+ leukemias

The mechanism of resistance to JAK2 inhibitor in myeloproliferative neoplasms patients

Effects of PARP inhibitors in BRCA gene-mutated ovarian cancer

DASATINIB; An inhibitor of Receptor Tyrosine Kinase

GP130/JAK/STAT3 signaling pathway induces multiple myeloma

Review of second-generation androgen receptor inhibitor therapies and their role in prostate cancer management

Purpose of review: We review the published literature on the indications of second-generation androgen receptor inhibitors, Poly(ADP-Ribose) Polymerase (PARP) inhibitors, combination therapies, and their evolution throughout the advanced prostate cancer continuum.

Recent findings: Enzalutamide trials have published data supporting its use in metastatic hormone-sensitive prostate cancer (mHSPC), nonmetastatic castration-resistant prostate cancer (nmCRPC), and metastatic castration-resistant prostate cancer (mCRPC). Apalutamide trials have supported its indication for mHSPC and nmCRPC. Darolutamide trials currently support its use for nmCRPC. Abiraterone trials have supported its use in mCRPC and mHSPC. Olaparib and rucaparib have shown clinical benefit in heavily pretreated patients with mCRPC and DNA repair mutation genes.

Summary: Phase 3 trials and peer-reviewed literature demonstrate that enzalutamide, apalutamide, and darolutamide prolong overall survival (OS) in men with nmCRPC. Abiraterone, enzalutamide, and apalutamide improve OS in men with mHSPC. Abiraterone and enzalutamide have data supporting improvement in OS in men with mCRPC.

Related Products

Cat.No. Product Name Information
S1098 Rucaparib phosphate Rucaparib phosphate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3.

Related Targets

PARP