Drug intelligence / Profile preview

varlitinib + docetaxel

Development stage
Unknown
Lead developer
ASLAN Pharmaceuticals
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**Varlitinib + docetaxel** is an experimental combination therapy under clinical investigation for solid tumors and breast cancer. - **Varlitinib** (ARRY-334543) is a potent, orally active, reversible, small molecule tyrosine kinase inhibitor that selectively targets both ErbB-2 (HER2/neu) and EGFR (ErbB-1). It acts as an ATP-competitive inhibitor and demonstrates nanomolar potency, aiming to inhibit tumor cell growth and survival pathways. Varlitinib also reverses multidrug resistance mediated by certain ABC transporters (notably ABCG2), potentially enhancing chemotherapeutic efficacy[1][4][5][8]. - **Docetaxel** is a well-established antimicrotubule chemotherapeutic agent, classified as a taxane, which inhibits cell division by stabilizing microtubules and is commonly used in various solid tumors (notably breast, lung, prostate cancers). The rationale for combining varlitinib with docetaxel is based on evidence for additive or synergistic anti-tumor effect, particularly in tumors overexpressing HER2 or EGFR, and to potentially overcome resistance mechanisms[5].

Other names
varlitinib + docetaxelARRY-334543 + docetaxel
02

Targets

ERBB4 (Erb-b2 receptor tyrosine kinase 4)ERBB3 (Erb-b2 receptor tyrosine kinase 3)ERBB2 (Erb-b2 receptor tyrosine kinase 2)TUBB (Tubulin (alpha and beta subunits))EGFR T790M (Epidermal growth factor receptor T790M mutant)

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