Drug intelligence / Profile preview

INCB057643 + paclitaxel

Development stage
Discontinued
Lead developer
Incyte
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

INCB057643 + paclitaxel is a **combination therapy** consisting of INCB057643, a selective small molecule inhibitor of BET (bromodomain and extra-terminal) proteins, administered with paclitaxel, a standard chemotherapeutic agent. INCB057643 inhibits BET proteins, which regulate expression of oncogenic genes such as c-Myc, thereby suppressing tumor cell proliferation and survival. Paclitaxel is a microtubule stabilizer that disrupts mitosis, leading to cancer cell death. This combination is being investigated for safety, tolerability, pharmacokinetics, and preliminary efficacy in patients with advanced malignancies, specifically in solid tumors for which paclitaxel is relevant. INCB057643 is developed by Incyte and is under clinical study in dose-escalation and dose-expansion protocols for its tolerability and efficacy when combined with standard-of-care agents such as paclitaxel[1][3].

02

Targets

BRD2 (Bromodomain-containing protein 2)BRD4 (Bromodomain-containing protein 4)TUBB (Tubulin (alpha and beta subunits))

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