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trametinib + trifluridine + tipiracil hydrochloride
- Development stage
- Discontinued
- Lead developer
- GSK
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
This combination therapy consists of trametinib, a small molecule MEK1/2 inhibitor, and TAS-102, a cytotoxic chemotherapy comprising trifluridine (a nucleoside analog) and tipiracil (a thymidine phosphorylase inhibitor). It was investigated by the City of Hope Medical Center in a Phase I clinical trial (NCT03317119) for the treatment of chemotherapy-resistant, RAS-mutated, PIK3CA/PTEN-wild-type metastatic colorectal cancer. Trametinib targets the MAPK/ERK pathway to inhibit cell proliferation, while trifluridine incorporates into DNA to cause DNA damage, and tipiracil maintains trifluridine levels by inhibiting its metabolism by thymidine phosphorylase. The trial concluded that while the combination demonstrated a manageable safety profile, it did not achieve meaningful clinical benefit in this specific refractory patient population.
- Brand names
- MekinistLonsurf
- Other names
- trametinibtrifluridinetipiracil hydrochloridetrifluridine and tipiracil hydrochloride
02
Targets
MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)DNAMEK1 (Dual specificity mitogen-activated protein kinase kinase 1)TYMP (Thymidine phosphorylase)TS (Thymidylate synthase)
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