Drug intelligence / Profile preview

butylidenephthalide + pembrolizumab + temozolomide

Development stage
Preclinical
Lead developer
Everfront Biotech
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination regimen consisting of three agents: butylidenephthalide, pembrolizumab, and temozolomide. Butylidenephthalide is a small molecule derived from plants such as Angelica sinensis and Ligusticum species, with reported antitumor activity in glioblastoma multiforme and other cancers. Its mechanisms include modulation of AXL receptor tyrosine kinase, immunomodulation, induction of apoptosis via the protein kinase C/JNK pathway, cell cycle arrest through upregulation of p16/p21 by downregulating Skp2, inhibition of telomerase activity via hTERT repression, and interference with TGF-β/Smad signaling pathways[4][5][9]. Pembrolizumab is a monoclonal antibody targeting programmed cell death protein 1 (PD-1), acting as an immune checkpoint inhibitor to enhance anti-tumor immune responses. Temozolomide is an oral alkylating agent that induces DNA damage leading to tumor cell death; it is widely used in the treatment of gliomas and melanomas. The combination aims to leverage the cytotoxic effects of temozolomide with the immunomodulatory properties of both pembrolizumab and butylidenephthalide for enhanced anti-tumor efficacy.

Other names
3-butylidenephthalideLigusticum lactonen-butylidenephthalide
02

Targets

AXL (AXL receptor tyrosine kinase)DNATERT (Telomerase)PDCD1 (Programmed cell death protein 1 receptor)

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