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repotrectinib + trametinib
- Development stage
- Unknown
- Lead developer
- Bristol Myers Squibb
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Repotrectinib + trametinib is an investigational **oral combination therapy** studied for the treatment of patients with **locally advanced or metastatic KRASG12D-mutant solid tumors**, including non-small cell lung cancer. Repotrectinib is a tyrosine kinase inhibitor (TKI) that targets ROS1, TRK, and ALK fusion proteins, while trametinib (marketed as Mekinist) is a selective inhibitor of MEK1 and MEK2, which are part of the mitogen-activated protein kinase (MAPK) signaling pathway. The combination is being explored for its potential synergistic activity in overcoming KRAS-mediated resistance pathways in solid tumors[1].
02
Targets
ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)NTRK2 (Tropomyosin-related kinase receptor type B)JAK2 (Janus kinase 2)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)NTRK3 (Tropomyosin receptor kinase C)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)NTRK1 (Tropomyosin-related receptor kinase A)
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