Drug intelligence / Profile preview

CWP232291 + lenalidomide + dexamethasone

Development stage
Phase 1
Lead developer
JW Pharmaceutical
Modality
Molecular Glues → Targeted Protein Degraders (TPDs) → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Modified Peptides → Peptides
Administration
Intravenous, Oral
01

Overview

CWP232291 is a small-molecule prodrug that is converted in serum to its active form, CWP232204. It targets Src associated in mitosis of 68 kDa (Sam68 or KHDRBS1) and acts as an inhibitor of the Wnt/β-catenin signaling pathway. This leads to induction of endoplasmic reticulum stress and apoptosis in selective cancer cells by reducing β-catenin levels and modulating Wnt target gene expression. Developed primarily for hematologic malignancies such as acute myeloid leukemia (AML), it has also shown preclinical activity against solid tumors like prostate cancer[1][2][3][4][5]. Lenalidomide is an immunomodulatory thalidomide derivative with antineoplastic, anti-angiogenic, and anti-inflammatory properties. It works through multiple mechanisms including inhibition of cereblon (CRBN), tumor necrosis factor alpha (TNFα), angiogenesis factors, and cell adhesion molecules; it enhances immune response against malignant cells[6][8]. Dexamethasone is a synthetic glucocorticoid corticosteroid with potent anti-inflammatory and immunosuppressant effects commonly used in combination regimens for hematologic cancers.

Other names
lenalidomidedexamethasone
02

Targets

CRBN (Cereblon)HSPA5 (Heat shock protein family A member 5)GR (Glucocorticoid receptor)TCF7KHDRBS1TNFA (Tumor necrosis factor alpha (soluble))

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