Drug intelligence / Profile preview

MK-5108 + docetaxel

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

Overview

MK-5108 + docetaxel is a combination therapy composed of MK-5108, a highly selective, adenosine triphosphate–competitive Aurora A kinase inhibitor, and docetaxel, a microtubule-stabilizing chemotherapy agent. MK-5108 inhibits Aurora A kinase, disrupting processes vital for mitotic progression and cellular division, leading to apoptosis in tumor cells[1][2]. Docetaxel interferes with microtubule dynamics, promoting cancer cell death by stabilizing microtubule formation and preventing their depolymerization. Preclinical and early clinical evidence indicates that MK-5108 enhances the antitumor efficacy of docetaxel by sensitizing tumor tissues and promoting synergistic apoptotic effects, without exacerbating docetaxel toxicity[1][2][7]. This combination was investigated in Phase I trials primarily for advanced and refractory solid tumors[1][8].

02

Targets

TUBB (Tubulin (alpha and beta subunits))AURKB (Aurora kinase B)NTRK1 (Tropomyosin-related receptor kinase A)AURKA (Aurora kinase A)AURKC (Aurora kinase C)

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