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PLX2853 + abiraterone acetate + prednisone
- Development stage
- Unknown
- Lead developer
- Plexxikon
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
PLX2853 + abiraterone acetate + prednisone is an investigational combination therapy being studied primarily for metastatic castration-resistant prostate cancer. PLX2853 is a potent, orally active small molecule inhibitor of bromodomain and extraterminal (BET) proteins, which function as epigenetic readers involved in transcriptional regulation of oncogenes such as MYC. By inhibiting BET proteins such as BRD4, PLX2853 modulates transcriptional programs critical for the survival and progression of cancer cells. Abiraterone acetate is a small molecule inhibitor of CYP17A1, blocking androgen biosynthesis; prednisone is a synthetic glucocorticoid used to reduce inflammation and counteract some adverse effects of abiraterone acetate. This combination is under clinical evaluation for safety, pharmacokinetics, and preliminary efficacy in advanced cancers, with a particular focus on prostate cancer[1][2][3][5][7].
- Other names
- OPN-2853 + abiraterone acetate + prednisone
02
Targets
BRD3 (Bromodomain-containing protein 3)BRDT (Bromodomain testis-specific protein)GR (Glucocorticoid receptor)BRD2 (Bromodomain-containing protein 2)CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)BRD4 (Bromodomain-containing protein 4)
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