Drug intelligence / Profile preview

HMPL-453 + docetaxel

Development stage
Phase 2
Lead developer
HUTCHMED
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

HMPL-453 + docetaxel is a combination therapy under investigation for advanced solid tumors, comprising HMPL-453—a novel, highly selective, and potent small molecule inhibitor targeting fibroblast growth factor receptors FGFR1, FGFR2, and FGFR3—and docetaxel, a taxane-class chemotherapy. HMPL-453 inhibits the FGFR pathway, which is implicated in tumor growth, angiogenesis, and therapy resistance, while docetaxel disrupts microtubule dynamics, inhibiting cell division. This combination targets tumors with aberrant FGFR signaling and is being assessed for safety, tolerability, pharmacokinetics, and preliminary efficacy, particularly in patients with advanced solid tumors refractory to standard treatments[2][6].

Other names
HMPL-453HMPL453HMPL 453fanregratinib
02

Targets

FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)TUBB (Tubulin (alpha and beta subunits))

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