Drug intelligence / Profile preview

SM08502 + docetaxel

Development stage
Unknown
Lead developer
Biosplice Therapeutics
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**SM08502 + docetaxel** is an investigational combination therapy consisting of the small molecule SM08502 (cirtuvivint) and the chemotherapeutic agent docetaxel. SM08502 is a potent, orally administered, pan-CDC-like kinase (CLK) and dual-specificity tyrosine-regulated kinase (DYRK) inhibitor, primarily targeting CLK2, CLK3, CLK1, CLK4, and DYRK. Its mechanism involves inhibition of mRNA splicing via suppression of serine/arginine-rich splicing factor (SRSF) phosphorylation, thereby modulating alternative splicing and resulting in reduced Wnt pathway gene expression. This impacts key oncogenic pathways involved in cancer, including Wnt/β-catenin signaling. The combination with docetaxel (a microtubule inhibitor) enhances antitumor effects, with increased alternative splicing and more robust inhibition of tumor growth in preclinical models. The combination is under investigation for the treatment of advanced solid tumors, especially various cancers such as endometrial cancer, colorectal cancer, and others[2][4][5][6].

Brand names
cirtuvivint
Other names
SM 08502SM08502SM-08502cirtuvivint
02

Targets

CLK1 (CDC-like kinase 1)DYRK1B (Dual specificity tyrosine-phosphorylation-regulated kinase 1B)CLK3 (CDC-like kinase 3)DYRK2 (Dual-specificity tyrosine-phosphorylation-regulated kinase 2)CLK4TUBB (Tubulin (alpha and beta subunits))CLK2 (CDC-like kinase 2)DYRK1A (Dual-specificity tyrosine-phosphorylation-regulated kinase 1A)

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