Drug intelligence / Profile preview

docetaxel + selumetinib

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

Docetaxel + selumetinib is an investigational combination therapy consisting of the chemotherapeutic agent docetaxel and the MEK1/2 inhibitor selumetinib. Docetaxel is a taxane-class cytotoxic drug that inhibits microtubule depolymerization, leading to cell cycle arrest and apoptosis. Selumetinib (also known as AZD6244 or ARRY-142886) is a selective small molecule inhibitor of MEK1/2, key kinases in the MAPK/ERK signaling pathway downstream of KRAS. The combination has been studied primarily in patients with advanced or metastatic non-small cell lung cancer (NSCLC) harboring KRAS mutations, as well as in other solid tumors with RAS pathway alterations. While early-phase studies suggested improved progression-free survival and objective response rates compared to docetaxel alone, later phase III trials did not demonstrate significant improvement in overall survival or progression-free survival for this combination over standard chemotherapy[1][2][4][5]. The regimen has also been evaluated for safety and tolerability in different populations[6][7].

Brand names
TaxotereKoselugo
Other names
docetaxel + selumetinib
02

Targets

TUBB (Tubulin (alpha and beta subunits))MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)

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