Drug intelligence / Profile preview

dasatinib + lenalidomide + dexamethasone

Development stage
Phase 1
Lead developer
Bristol Myers Squibb
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

A combination regimen of three small molecule drugs—dasatinib (a tyrosine kinase inhibitor), lenalidomide (an immunomodulatory agent), and dexamethasone (a synthetic glucocorticoid)—used primarily in the treatment of hematologic malignancies such as multiple myeloma. Dasatinib inhibits BCR-ABL and SRC family kinases to block cancer cell proliferation. Lenalidomide modulates immune responses by altering cytokine production and enhancing cytotoxic T-cell and NK cell activity; it also induces degradation of key transcription factors in malignant cells via cereblon binding. Dexamethasone acts as an anti-inflammatory and immunosuppressant by activating the glucocorticoid receptor. This combination is under investigation for synergistic effects in relapsed or refractory multiple myeloma and other blood cancers[1][3][7].

02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)CRBN (Cereblon)GR (Glucocorticoid receptor)SFK (SRC family kinases)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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