Drug intelligence / Profile preview

lenalidomide + procarbazine

Development stage
Unknown
Lead developer
Starton Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Lenalidomide + procarbazine is an experimental, orally administered combination of two small‑molecule antineoplastic agents used in oncology research rather than as a marketed fixed‑dose product. Lenalidomide is an immunomodulatory derivative of thalidomide that binds the cereblon subunit of the cullin‑4 E3 ubiquitin ligase complex, altering substrate specificity and promoting degradation of transcription factors such as Ikaros (IKZF1), Aiolos (IKZF3), and CK1α, which leads to direct antitumor effects and enhanced immune-mediated cytotoxicity through modulation of cytokines, T‑cell co‑stimulation, and NK‑cell activity. Procarbazine is an oral alkylating chemotherapeutic and weak monoamine oxidase inhibitor that undergoes metabolic activation to form reactive intermediates that methylate DNA, causing strand breaks and inhibition of DNA, RNA, and protein synthesis, and is classically used in combination regimens for Hodgkin lymphoma and primary brain tumors. The combination of lenalidomide and procarbazine has been explored conceptually as a way to pair immunomodulatory and cytotoxic mechanisms, but it is not an established, named regimen and no dedicated fixed‑dose combination product is marketed.

02

Targets

DNACK1α (Casein kinase I alpha)IKZF3 (Zinc finger protein Aiolos)CRBN (Cereblon)IKZF1 (Ikaros family zinc finger protein 1)

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