Drug intelligence / Profile preview

INCB057643 + abiraterone + prednisone

Development stage
Discontinued
Lead developer
Incyte
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

INCB057643 + abiraterone + prednisone is an investigational three-drug combination for the treatment of advanced malignancies. The combination consists of INCB057643, a small molecule inhibitor that targets bromodomain and extra-terminal (BET) proteins to modulate oncogene expression via epigenetic regulation; abiraterone, an androgen biosynthesis inhibitor that targets cytochrome P450 17A1 (CYP17A1) to suppress androgen production; and prednisone, a synthetic glucocorticoid with anti-inflammatory and immunosuppressive properties. The combination is being studied in clinical trials to assess safety, tolerability, pharmacokinetics, and preliminary efficacy in patients with advanced solid tumors and hematologic malignancies as part of dose-escalation/expansion protocols[1][2][3].

02

Targets

BET (BET family proteins)CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)GR (Glucocorticoid receptor)BRD (Bromodomain-containing protein family)

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